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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 2885. Отображено 100.
23-02-2012 дата публикации

Developers and method of coloring lithographic printing members

Номер: US20120045720A1
Автор: Eynat Matzner, Ilan Levi, Moshe Marom, Murray Figov, Ruizheng Wang
Принадлежит: Individual

A color contrast image in imaged lithographic printing precursors can be obtained by contacting the imaged precursor with a coloration solution containing a colorless form of a photochromic compound. Residual amounts of this compound attached to the oleophilic surface of the imaged precursor can be changed to its colored form when exposed to UV light. The coloration solution can be an alkaline or acidic developer or an alkaline or acidic solution used separately after development. The coloration solution can also be a gum solution.

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Номер записи: 1
17-05-2012 дата публикации

Libraries of n-substituted-n-phenylethylsulfonamides for drug discovery

Номер: US20120122920A1
Автор: David Enrique MIGUEL CENTENO, Josep Castells Boliart, Marta Pascual Gilabert
Принадлежит: Institut Universitari de Ciencia i Tecnologia

New compounds are continually being sought for the treatment and prevention of disorders. The invention relates to N-substituted-N-phenylethylsulfonamides libraries which can be used in the search for, and identification of, new lead compounds that could modulate the functional activity of a biological target.

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Номер записи: 2
17-05-2012 дата публикации

Process for the preparation of strontium ranelate

Номер: US20120123131A1
Автор: Kapil Ramesh Hire, Koilpillai Joseph Prabahar, Prashant Bhaskarrao Patil, Pravin Bhalchandra Kulkarni
Принадлежит: Individual

The present invention relates to an improved process for the synthesis of strontium ranelate or hydrates thereof. More particularly, the present invention relates to an effective process for the preparation of a compound of formula III, which is a useful intermediate in the synthesis of strontium ranelate. wherein R 1 and R 2 represents substituted or unsubstituted linear or branched C 1 -C 6 alkyl group or C 3 -C 12 cyclic group.

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Номер записи: 3
18-04-2013 дата публикации

COMPOUNDS AND METHODS FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS

Номер: US20130096106A1
Автор: Chan Chun Kong Laval, Das Sanjoy Kumar, Halab Liliane, Hamelin Bettina, Ming-Qiang Zhang, Nguyen-Ba Nghe, Oswy Pereira Z., Poisson Carl, Proulx Melanie, Reddy Thumkunta Jagadeeswar
Принадлежит: Vertex Pharmaceuticals (Canada) Incorporated

Compounds represented by formula: 3. A compound according to claim 1 , wherein Z is 6-7 membered heterocycle or 6-7 membered cycloalkyl.4. A compound according to claim 1 , wherein Z is cyclohexyl claim 1 , piperidinyl claim 1 , N—(Calkyl)-piperidinyl claim 1 , hexahydrothiopyranyl claim 1 , azepanyl claim 1 , methylazepanyl claim 1 , N—(Calkyl)-piperidinylmethyl claim 1 , tetrahydropyranyl claim 1 , piperidinylmethyl claim 1 , pyridinyl claim 1 , pyridinylmethyl claim 1 , tetrahydrothiopyranyl claim 1 , dioxolanylmethyl or dioxanylmethyl which in each case is unsubstituted or substituted by one or more substituent chosen from halogen claim 1 , nitro claim 1 , nitroso claim 1 , SORf claim 1 , SORf claim 1 , PORcRd claim 1 , CONRgRh claim 1 , Calkyl claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , Caralkyl claim 1 , Caryl claim 1 , Calkyloxy claim 1 , Calkenyloxy claim 1 , Calkynyloxy claim 1 , Caryloxy claim 1 , C(O)Calkyl claim 1 , C(O)Calkenyl claim 1 , C(O)Calkynyl claim 1 , C(O)Caryl claim 1 , C(O)Caralkyl claim 1 , C(O)NHRf claim 1 , Cheterocycle claim 1 , hydroxyl claim 1 , NRgRh claim 1 , C(O)ORf claim 1 , cyano claim 1 , azido claim 1 , amidino or guanido;{'sub': 1-6', '2-6', '2-6', '6-10', '3-10', '3-10', '6-10, 'wherein Rf, Rc, Rd, Rg and Rh in each case is H, Calkyl, Calkenyl, Calkynyl, Caryl, Cheterocycle, Cheteroaralkyl or Caralkyl;'}or Rc and Rd are taken together with the oxygens to form a 5 to 10 membered heterocycle;or Rg and Rh are taken together with the nitrogen to form a 3 to 10 membered heterocycle.5. A compound according to claim 1 , wherein Z is cyclohexyl unsubstituted or substituted by one or more substituent chosen from halogen claim 1 , SORf claim 1 , CONRgRh claim 1 , Calkyl claim 1 , Caralkyl claim 1 , Caryl claim 1 , Calkyloxy claim 1 , C(O)Calkyl claim 1 , Cheterocycle claim 1 , hydroxyl claim 1 , NRgRh claim 1 , C(O)Orf or cyano;{'sub': '1-6', 'wherein Rf, Rg and Rh in each case is H or Calkyl.'}6. A compound according to claim 1 , ...

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Номер записи: 4
20-06-2013 дата публикации

METHODS FOR TREATING OR PREVENTING CANCER AND NEURODEGENERATIVE DISEASES

Номер: US20130158017A1
Автор: Li Yueming, Zhu Lei
Принадлежит: Sloan-Kettering Institute for Cancer Research

Provided are methods of treating or preventing a neurodegenerative disease comprising administering to a subject having a neurodegenerative disease an effective amount of a compound of Formula I: 218-. (canceled)21. (canceled)23. The method of claim 20 , wherein each Ris H.24. (canceled)25. The method of claim 20 , wherein v is 1 and X is in the 5-position of the thiopheno group.26. The method of claim 20 , wherein p is 1 and Ris in the 4-position of the phenyl group.2830-. (canceled)34. The method of claim 31 , wherein each Ris H.35. The method of claim 31 , wherein Ris H or methyl.36. The method of claim 31 , wherein Ris methyl.37. The method of claim 31 , wherein q is 0.38. The method of claim 31 , wherein v is 1 and X is in the 5-position of the thiopheno group.41. The method of claim 31 , wherein the neurodegenerative disease is Alzheimer's disease claim 31 , Parkinson's disease claim 31 , ALS claim 31 , or MS.42. The method of claim 31 , wherein the neurodegenerative disease is Alzheimer's disease. This application claims priority to U.S. Provisional Patent Application Ser. No. 61/139,751, filed Dec. 22, 2008, the entire content of which is incorporated herein by reference.The invention relates to methods of treatment or prevention of cancer and neurodegenerative diseases comprising administering an effective amount of a Sulfonamide-Based Compound to a subject.Alzheimer's disease (AD) is the most prevalent form of dementia. It is a neurodegenerative disorder, clinically characterized by progressive loss of memory and general cognitive function, and pathologically characterized by the deposition of extracellular proteinaceous plaques in the cortical and associative brain regions of sufferers. These plaques mainly comprise fibrillar aggregates of beta-amyloid peptide (Aβ). Aβ is formed from amyloid precursor protein (APP). APP is a ubiquitous membrane-spanning (type 1) glycoprotein, of which three major isoforms (APP695, APP751, and APP770) are known, that ...

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Номер записи: 5
20-06-2013 дата публикации

TG2 INHIBITORS AND USES THEREOF

Номер: US20130158087A1
Автор: Fok Jansina, Kumar Anupam, Mehta Kapil, ZHANG Shuxing
Принадлежит: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM

Methods and compounds for treating cancer, dmg resistance and/or metastasis are described herein. These methods and compounds can inhibit the expression of aberrant TG2 expression and/or inhibit the binding of GTP to TG2, and thereby prevent the induction of epithelial to mesenchymal transition of cancer cells, and a stem cell-like phenotype. 76. Use of the compound of , , or for the manufacture of a medicament for treating cancer.83. The method of , , or , wherein the compound treats cancer. This patent application claims priority to U.S. Patent Application Ser. No. 61/356,961 filed on Jun. 21, 2010 which is incorporated by reference herein in its entiretyThis invention is related to modulation of aberrant expression of TG2 and/or inhibition of GTP binding to TG2 to treat cancer, metastasis, drug resistance and other oncogenic properties.None.None.This disclosure includes a sequence listing submitted as a text file pursuant to 37 C.F.R., §1.52(e)(v) named sequence listing.txt, created on Jun. 16, 2010, with a size of 22,111 bytes, which is incorporated herein by reference. The attached sequence descriptions and Sequence Listing comply with the rules governing nucleotide and/or amino acid sequence disclosures in patent applications as set forth in 37 C.F.R. §§1.821-1.825.Epithelial-to-mesenchymal transition (“EMT”) is a complex dynamic process that occurs during embryonic development for reprogramming of epithelial cells. Downregulation of E-cadherin, which occurs during EMT, results in the loss of homotypic adhesion. Reactivation of EMT during adult life has been associated with various pathological conditions. For example, EMT promotes the detachment of cancer cells from the primary tumor and facilitates migration through the acquisition of stem cell like properties, including loss of cellular polarity and adhesion. Metastasis and resistance to systemic therapies pose major clinical challenges to the treatment of breast and other cancers. Identification of tumor- ...

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Номер записи: 6
27-06-2013 дата публикации

SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS

Номер: US20130165460A1
Автор: Beard Richard L., Donello John E., Garst Michael E., Liu Xiaoxia, Viswanath Veena, Yuan Haiqing
Принадлежит: ALLERGAN, INC.

The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. 2. A compound according to claim 1 , wherein:{'sup': '5', 'Ris S.'}3. A compound according to claim 1 , wherein:{'sup': '5', 'Ris —S(O)—.'}4. A compound according to claim 1 , wherein:{'sup': '5', 'sub': '2', 'Ris —S(O)—.'}5. A compound according to claim 1 , wherein:{'sup': '2', 'Ris methyl, isopropyl, 2-hydroxyethyl, methylpropionate, 2-methylpyridine, 3-methylpyridine, ethylacetate, N,N-dimethylpropanamide, N-isopropylpropanamide, N-(propan-2-yl)propanamide, propanamide hydroxycyclopent-3-yl, ethyl, N,N-dimethylacetamide, N-methylacetamide, 2-aminoethyl, H-imidazol-2-ylmethyl, 1H-imidazol-4-ylmethyl or ethyl-acetamide.'}6. A compound according to claim 1 , wherein:{'sup': '17', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl or halogen;'}{'sup': '18', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl or halogen;'}{'sup': '7', 'sub': 1-6', '1-6', '3-8, 'Ris halogen, CN, —OCalkyl, substituted or unsubstituted Calkyl or substituted or unsubstituted Ccycloalkyl; and'}{'sup': '8', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl or halogen.'}7. A compound according to claim 1 , wherein:{'sup': '17', 'Ris H;'}{'sup': '18', 'Ris H;'}{'sup': '7', 'sub': '1-6', 'Ris halogen, CN or —OCalkyl; and'}{'sup': '8', 'Ris H.'}8. A compound according to claim 1 , wherein:{'sup': '2', 'Ris methyl, isopropyl, 2-hydroxyethyl, methylpropionate, 2-methylpyridine, 3-methylpyridine, ethylacetate, N,N-dimethylpropanamide, N-isopropylpropanamide, N-(propan-2-yl)propanamide, propanamide hydroxycyclopent-3-yl, ethyl, N,N-dimethylacetamide, N-methylacetamide, 2-aminoethyl, H-imidazol-2-ylmethyl, 1H-imidazol-4-ylmethyl or ethyl-acetamide;'}{'sup': '5', 'sub': '2', 'Ris —S—, —S(O)—, or —S(O)—;'}{'sup': '17', 'Ris H;'}{'sup': '18', 'Ris H;'}{'sup': '7', 'sub': '1-6', ' ...

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Номер записи: 7
27-06-2013 дата публикации

Antiviral Drugs for Treatment of Arenavirus Infection

Номер: US20130165493A1
Автор: Amberg Sean M., Bolken Tove C., Dai Dongcheng, Hruby Dennis E.
Принадлежит: Siga Technologies, Inc,

Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, and Pichinde), Filoviridae (Ebola and Marburg viruses), Flaviviridae (yellow fever, Omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever). 167-. (canceled)68. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or excipient and a pharmaceutically effective amount of a compound or a pharmaceutically-acceptable salt thereof , selected from the group consisting of2-Phenyl-cyclopropanecarboxylic acid [1-(4-amino-phenyl)-eth-(E)-ylidene]-hydrazide;Cyclopropanecarboxylic acid (4-[1-[(2-phenyl-cyclopropanecarbonyl)-hydrazono]-ethyl]-phenyl)-amide;2-Phenyl-cyclopropanecarboxylic acid [1-(2,4-dimethoxy-phenyl)-eth-(E)-ylidene]-hydrazide;2-Phenyl-cyclopropanecarboxylic acid [1-p-tolyl-eth-(E)-ylidene]-hydrazide;2-Phenyl-cyclopropanecarboxylic acid [1-biphenyl-4-yl-eth-(E)-ylidene]-hydrazide;2-Phenyl-cyclopropanecarboxylic acid [1-(3,4-dimethoxy-phenyl)-eth-(E)-ylidene]-hydrazide;Furan-2-carboxylic acid (4-[1-[(2-phenyl-cyclopropanecarbonyl)-hydrazono]-ethyl]-phenyl)-amide;2,4-Dichloro-N-(4-[1-[(2-Phenyl-cyclopropanecarbonyl)-hydrazono]-ethyl]-phenyl)-benzamide;2-Phenyl-cyclopropanecarboxylic acid [1-(2-hydroxy-phenyl)-eth-(E)-ylidene]-hydrazide;Thiophene-2-carboxylic acid (4-[1-[(2-phenyl-cyclopropanecarbonyl)-hydrazono]-ethyl]-phenyl)-amide;2-Phenyl-cyclopropanecarboxylic acid [1-(4-dimethylamino-phenyl)-eth-(E)-ylidene]-hydrazide;2-Phenyl-cyclopropanecarboxylic acid [1-(4-methoxy- ...

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Номер записи: 8
18-07-2013 дата публикации

COMPOUNDS THAT INHIBIT (BLOCK) BITTER TASTE IN COMPOSITION AND METHODS OF MAKING SAME

Номер: US20130183252A1
Автор: Arellano Melissa, Brady Thomas, Brust Paul, Ching Brett Weylan, Darmohusodo Vincent, Karanewsky Donald S., Li Qing, Li Xiaodong, Ling Jing, Patron Andrew, Priest Chad, Pronin Alexey, Selchau Victor, Servant Guy, Tachdjian Catherine, Xu Hong, Zhang Lan, Zhao Wen
Принадлежит: Senomyx, Inc.

The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals. 2. The compound of claim 1 , wherein X is selected from the group consisting of hydrogen claim 1 , heteroalkyl claim 1 , substituted heteroalkyl claim 1 , heteroaryl claim 1 , substituted heteroaryl claim 1 , heteroarylalkyl claim 1 , substituted heteroarylalkyl claim 1 , CN claim 1 , S(O)R claim 1 , CONRR claim 1 , —COR claim 1 , SONRR claim 1 , NRSOR claim 1 , NRSONRR claim 1 , B(OR)(OR) claim 1 , P(O)(OR)(OR) claim 1 , and P(O)(R)(OR).7. A composition comprising one or more compounds of claim 1 , or a salt claim 1 , hydrate claim 1 , solvate or N oxide thereof claim 1 , and one or more pharmaceutically acceptable carriers.8. The composition of claim 7 , which is a food claim 7 , beverage or medicament for human consumption.9. A coffee or coffee flavored food or beverage or medicament composition that comprises at least one compound of or a salt claim 1 , hydrate claim 1 , solvate or N oxide thereof.10. The composition of claim 9 , which is an instant coffee claim 9 , ground coffee claim 9 , or brewed coffee.11. The composition of claim 9 , which is an instant coffee.12. A food claim 1 , beverage claim 1 , or medicament composition having a bitter taste wherein said bitter taste is alleviated or eliminated by the addition of an effective amount of a compound of or a salt claim 1 , hydrate claim 1 , ...

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Номер записи: 9
08-08-2013 дата публикации

COMPOUNDS AND METHODS FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS

Номер: US20130203706A1
Автор: Green Jeremy
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

A compound is represented by Structural Formula (I): 2. The compound of claim 1 , wherein:{'sup': a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'E', 'E', 'F', 'F, 'sub': 2', '2', '2', '2', '3-8', '6-10, 'each Q independently is selected from the group consisting of halogen, cyano, nitro, —OR, —SR, —S(O)R, —SOR, —NRR, —C(O)R, —C(O)OR, —OC(O)R, —NRC(O)R, —C(O)NRR, —NRC(O)NRR, —NRC(O)OR, —NRC(═NR)NRR, —OCONRR, —C(O)NRC(O)OR, —C(═NR)R, —C(═NOR)R, —SONRR, —NRSOR, —NRSONRR, —OP(O)(OR)OR, Ccarbocycle optionally substituted with one or more instances of J, 4-8 membered heterocycle optionally substituted with one or more instances of J, Caryl group optionally substituted with one or more instances of J, and 5-10 membered heteroaryl group optionally substituted with one or more instances of J;'}{'sub': 3-6', '4-6', '2', '2, 'sup': '1', 'Y is optionally substituted Ccycloalkyl, optionally substituted Ccycloalkenyl, —(Caliphatic group)-R, optionally substituted phenyl, or optionally substituted 5-6 membered heteroaryl, and wherein said Caliphatic group is optionally substituted; and'}{'sup': Y', 'a', 'a', 'a', 'a, 'each Jis independently selected from the group consisting of halogen, —CN, nitro, R, —OR, —COR, and —NRR.'}312-. (canceled)13. The compound of claim 2 , wherein Y is —(Caliphatic group)-Ror phenyl optionally substituted with one or more instances of Jindependently selected from the group consisting of chloro claim 2 , fluoro claim 2 , —CN claim 2 , nitro claim 2 , methyl claim 2 , ethyl claim 2 , —CF claim 2 , —OH claim 2 , —OMe claim 2 , —NH claim 2 , and —C(O)Me claim 2 , and wherein said Caliphatic group is optionally substituted.14. (canceled)15. The compound of claim 13 , wherein Y is —CH—CH—R claim 13 , —CH═CH—R claim 13 , or —C≡CR.1722-. (canceled)23. The compound of claim 16 , wherein:{'sup': '3', 'sub': '1-6', 'each Rindependently is —H or optionally substituted Calkyl;'}{'sup': 4', '6, 'sub': '1 ...

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Номер записи: 10
08-08-2013 дата публикации

PROCESS FOR PRODUCING THIOPHENE COMPOUND AND INTERMEDIATE THEREOF

Номер: US20130204013A1
Автор: Miyaji Katsuaki, Umezawa Shingo, YANAGIHARA Kazufumi
Принадлежит: NISSAN CHEMICAL INDUSTRIES, LTD.

To provide a novel process for producing a 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound or an intermediate thereof useful as an intermediate for production of medicines and agricultural chemicals. 110-. (canceled)12. The dihydrothiophene compound according to claim 11 , wherein:{'sup': '1', 'sub': 6-10', '1-10', '1-10', '1-10', '1-10, 'Ris a Caryl group unsubstituted or substituted with one or more halogen atoms, one or more Calkyl groups or one or more Calkoxy groups, such that the Calkyl groups and the Calkoxy groups are unsubstituted or substituted with one or more halogen atoms;'}{'sup': '2', 'sub': '1-3', 'Ris a Calkyl group unsubstituted or substituted with one or more halogen atoms; and'}{'sup': '3', 'Ris a hydrogen atom or a methyl group.'}13. The dihydrothiophene compound according to claim 12 , wherein Ris a phenyl group unsubstituted or substituted with one or more halogen atoms claim 12 , one or more Calkyl groups or one or more Calkoxy groups claim 12 , such that the Calkyl groups and the Calkoxy groups are unsubstituted or substituted with one or more halogen atom. The present invention relates to a process for producing, from a 2-aryl acetate compound, a corresponding 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound or an intermediate thereof.2-Aryl-3-hydroxy-4-substituted carbonyl thiophene compounds are compounds useful, for example, as intermediates for synthesis of thrombopoietin receptor activators (e.g. Patent Document 1).As a process for producing a 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound, only a process of synthesizing a 2-aryl-3-hydroxy-4-ester thiophene compound by a known production process (e.g. Patent Document 2), and converting the ester group at the 4-position to an alkylcarbonyl group has been known (e.g. Patent Document 1). However, conversion of the ester group to an alkylcarbonyl group requires multiple steps, and thus a production process with a smaller number of steps has been desired.As ...

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Номер записи: 11
22-08-2013 дата публикации

ORGANIC AMINE SALTS OF AMINOBENZOIC ACID DERIVATIVES AND METHOD FOR PRODUCING SAME

Номер: US20130217894A1
Автор: ISHIDA Mariko, Iwamoto Shunsuke, Nakano Satoshi, TAKEUCHI Kazuya, Yamamoto Masao
Принадлежит: NISSAN CHEMICAL INDUSTRIES, LTD.

A novel organic amine salt or salt with quaternary ammonium ion of 3-{[((2E)-2-{1-[5-(4-t-butylphenyl)-4-hydroxy-3-thienyl]ethylidene}hydrazino)carbonothioyl]amino}benzoic acid having useful properties as a drug is provided. 1. An organic amine salt of , or a salt with quaternary ammonium ion of 3-{[((2E)-2-{1-[5-(4-t-butylphenyl)-4-hydroxy-3-thienyl]ethylidene}hydrazino)carbonothioyl]amino}benzoic acid.2. The salt according to claim 1 , wherein the organic amine claim 1 , or the quaternary ammonium salt claim 1 , comprises a hydroxy group.3. The salt according to claim 2 , wherein the organic amine claim 2 , or the quaternary ammonium salt claim 2 , comprising the hydroxy group is ethanolamine claim 2 , tromethamine or choline.4. An ethanolamine salt of 3-{[((2E)-2-{1-[5-(4-t-butylphenyl)-4-hydroxy-3-thienyl]ethylidene}hydrazino)carbonothioyl]amino}benzoic acid.5. A tromethamine salt of 3-{[((2E)-2-{1-[5-(4-t-butylphenyl)-4-hydroxy-3-thienyl]ethylidene}hydrazino)carbonothioyl]amino}benzoic acid.6. A choline salt of 3-{[((2E)-2-{1-[5-(4-t-butylphenyl)-4-hydroxy-3-thienyl]ethylidene}hydrazino)carbonothioyl]amino}benzoic acid.7. A medicine claim 1 , comprising the salt of as an active ingredient.8. The medicine according to claim 7 , which is a thrombopoietin receptor activator.9. The medicine according to claim 7 , which is a platelet increasing agent.10. A method for producing the salt of claim 1 , comprising reacting 3-{[((2E)-2-{1-[5-(4-t-butylphenyl)-4-hydroxy-3-thienyl]ethylidene}hydrazino)carbonothioyl]amino}benzoic acid with the organic amine claim 1 , or the quaternary ammonium salt claim 1 , in a solvent.11. The method according to claim 10 , wherein the reacting occurs at 0 to 70° C. claim 10 , and a resulting organic amine salt claim 10 , or salt with quaternary ammonium ion claim 10 , is crystallized.12. The method according to claim 10 , wherein the organic amine claim 10 , or the quaternary ammonium salt claim 10 , is ethanolamine claim 10 , ...

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Номер записи: 12
19-09-2013 дата публикации

HETEROCYCLIC COMPOUNDS AND EXPANSION AGENTS FOR HEMATOPOIETIC STEM CELLS

Номер: US20130245255A1
Автор: Iwamoto Shunsuke, Miyaji Katsuaki, Nishino Taito
Принадлежит: NISSAN CHEMICAL INDUSTRIES, LTD.

An expansion agent for hematopoietic stem cells and/or hematopoietic progenitor cells useful for improvement in the efficiency of gene transfer into hematopoietic stem cells for gene therapy useful for treatment of various disorders is provided. 1. A compound represented by the formula (I):{'sup': 1', '2', '3', '4, 'sub': 1-10', '1-10, 'wherein each of R, R, Rand Ris independently a hydrogen atom or a Calkyl group (the Calkyl group may be optionally substituted with one or more halogen atoms),'}{'sup': 5', '1', '1', '1', '8', '9', '1', '8', '9', '10', '10', '11', '12', '11', '12', '13', '14', '13', '14', '11', '12', '11', '12', '15', '9', '2', '2', '16', '17', '16', '17', '3', '3', '2', '18', '19', '2', '18', '19', '4', '4', '9, 'sub': 2-14', '2-14', '2', '1', '2', '1', '1-3', '1', '2', '2', '2', '1-3', '2', '3', '3', '1-6', '1-6', '2', '4', '4', '2', '5', '5', '1-3', '1-3', '1-3', '1', '2', '6', '6', '1-3', '1-3', '2', '7', '2', '7', '1-3', '2-9', '2-14, 'Ris a Caryl group (the Caryl group is substituted with —V(wherein —Vis —(CH)mMNRR(wherein Mis —(C═O)— or —(SO)—, mis an integer of 0, 1 or 2, Ris a hydrogen atom or a Calkyl group, and when m=0, Ris —(CH)mOR(wherein mis an integer of 1 or 2, and Ris a hydrogen atom, a Calkyl group or —(CH)mT (wherein mis an integer of 1 or 2, and T is a hydroxyl group, a Calkoxy group or a Calkyl group)), —(CH)mNRR(wherein mis an integer of 1 or 2, and each of Rand Ris independently a hydrogen atom or —(CH)mQ (wherein mis an integer of 1 or 2, and Q is a hydroxy group, a Calkoxy group, —NRR(wherein each of Rand Ris independently a hydrogen atom or a Calkyl group)), or Rand Rmean, together with each other as —NRR, a substituent represented by the formula (II) or the formula (III) (wherein Ris a hydrogen atom, a Calkyl group or an amino-protecting group)), and when m=1 or 2, Ris any of those mentioned above or a hydrogen atom)), —V(wherein —Vis —(CH)mNRR(wherein mis an integer of 1 or 2, and each of Rand Ris independently a hydrogen ...

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Номер записи: 13
14-11-2013 дата публикации

Ire1alpha endonuclease specific inhibitor with cytotoxic activity

Номер: US20130303599A1
Автор: Albert C. Koong, Ioanna Papandreou
Принадлежит: Leland Stanford Junior University

Activation of the adaptive Ire1-XBP1 pathway has been identified in many solid tumors and hematological malignancies, including multiple myeloma (MM). What is disclosed is STF-083010, a novel small molecule inhibitor of Ire1. STF-083010 inhibited Ire1 endonuclease activity, without affecting its kinase activity, after ER stress both in vitro and in vivo. Treatment with STF-083010 showed significant anti-myeloma activity in model human MM xenografts. Similarly, STF-083010 was preferentially toxic to freshly isolated human CD138(+) MM cells when compared to other similarly isolated cell populations. The identification of this novel Ire1 inhibitor supports the hypothesis that the Ire1-XBP1 axis is a promising target for anti-cancer therapy, especially in the context of multiple myeloma.

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Номер записи: 14
12-12-2013 дата публикации

COMPOUNDS AND METHODS FOR TREATING DISEASES MEDIATED BY PROTEASE ACTIVATED RECEPTORS

Номер: US20130331411A1
Автор: Dockendorff Chris, Flaumenhaft Robert, MacPherson Lawrence
Принадлежит:

The invention relates to the use of a compound of Formula I for the treatment of protease-activated receptor mediated diseases by the administration of a compound of Formula I or a prodrug or metabolite thereof. 12-. (canceled)46-. (canceled)821-. (canceled)26. The method of claim 22 , wherein the patient is in need of inhibition of platelet activation.27. The method of claim 22 , wherein the patient is in need of inhibition of thrombus formation.28. The method of claim 22 , wherein the PAR1 disease is particular proliferative diseases of endothelial cells claim 22 , fibroblasts claim 22 , nephrocytes claim 22 , osteosarcoma cells claim 22 , muscle cells claim 22 , cancer cells and/or glia cells.2930-. (canceled)31. The method of claim 22 , wherein said PAR1 mediated disease is selected from acute Myocardial Infarction claim 22 , stable angina claim 22 , unstable angina claim 22 , aortocoronary bypass surgery claim 22 , acute occlusion following coronary angioplasty and or stent placement claim 22 , transient Ischemic attacks claim 22 , cerebrovascular disease claim 22 , peripheral vascular disease claim 22 , placental insufficiency claim 22 , prosthetic heart valves claim 22 , atrial fibrillation claim 22 , anticoagulation of tubing.32. (canceled)33. The method of claim 22 , wherein said disease or disorder is selected from acute myocardial infarction claim 22 , stable angina claim 22 , unstable angina claim 22 , transient ischemic attack claim 22 , cerebrovascular disease claim 22 , peripheral vascular disease claim 22 , placental insufficiency claim 22 , thrombosis subsequent to or associated with a surgical procedure claim 22 , thrombosis associated with atrial fibrillation claim 22 , and inflammation.3436-. (canceled)37. The method of claim 22 , wherein Cyl and Gare aromatic groups and Gis an alkyl group.38. The method of claim 22 , wherein each Gand Gis a group containing at least two carbons independently selected from aliphatic claim 22 , substituted ...

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Номер записи: 15
26-12-2013 дата публикации

Carboxylation of poly-/oligothiophenes

Номер: US20130345440A1
Автор: Asier Eleta-Lopez, Björn HENNINGER, Christian Severins, Kilian Tellmann, Leslaw Mleczko, Sigurd Buchholz
Принадлежит: Bayer Intellectual Property GmbH

The present invention relates to a process for carboxylation of poly/oligothiophenes using CO 2 .

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Номер записи: 16
02-01-2014 дата публикации

Process for producing thiophene compound and intermediate thereof

Номер: US20140005413A2
Автор: Katsuaki Miyaji, Kazufumi Yanagihara, Shingo Umezawa
Принадлежит: Nissan Chemical Corp

To provide a novel process for producing a 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound or an intermediate thereof useful as an intermediate for production of medicines and agricultural chemicals. A 2-aryl acetate compound represented by the formula (1): wherein R 1 is an aryl group or the like, R 4 is a C 1-3 alkyl group or the like, and X is a leaving group, is reacted with a thioacetic acid compound to form a thioacetyl compound (3), the thioacetyl compound (3) is reacted with a vinyl ketone compound to form a γ-ketosulfide compound (5), which is cyclized under basic conditions to form a dihydrothiophene compound (6), and the dihydrothiophene compound (6) is oxidized by using an oxidizing agent to produce a 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound (7).

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Номер записи: 17
20-02-2014 дата публикации

Lipophilic Curcumin Analogs And Methods Of Inhibiting HIV-1, Treating Latent HIV In The Brain, And Preventing HIV-Mediated Cognitive Decline And HIV Dementia

Номер: US20140051742A1
Автор: Kulkarni Amol, Nwulia Evaristus A.
Принадлежит:

Compounds having formulas (I) to (VIII), salts thereof, or combinations thereof and pharmaceutical compositions comprising one or more these compounds are described herein for the treatment of HIV and neurodegenerative effects caused by HIV. Also provided herein are methods and a kit for inhibiting HIV-1, treating latent HIV in the brain, and preventing HIV-mediated cognitive decline and HIV dementia comprising administering the compounds having the formulas (I) to (VIII) and pharmaceutical compositions comprising the compounds having these formulas. The compounds having formulas I through VIII are curcumin analogs which are advantageously characterized as having anti-retroviral, neuroprotective, anti-glucosidase, and anti-HIV integrase properties. In one aspect, the pharmaceutical composition is delivered intranasally. 2. The method according to claim 1 , wherein the pharmaceutical composition is intranasally administered.3. The method according to claim 1 , wherein the pharmaceutical composition further comprises an antiviral agent other than at least one compound of formulas (I) to (VIII).4. The method according to claim 3 , wherein the antiviral agent is selected from the group consisting of nucleoside reverse transcriptase inhibitors claim 3 , nonnucleoside reverse transcriptase inhibitors claim 3 , protease inhibitors claim 3 , integrase inhibitors claim 3 , fusion inhibitors claim 3 , chemokine receptor antagonists claim 3 , and combinations thereof.5. The method according to claim 1 , wherein the analog is dispersed into a pharmaceutically acceptable oil.8. A compound having any of formulas (II) to (VIII) as defined in .9. A pharmaceutical composition comprising at least one compound having any of formulas (II) through (VIII) as defined in .10. The pharmaceutical composition according to claim 9 , further comprising a pharmaceutically acceptable excipient claim 9 , diluent claim 9 , and/or carrier.11. The pharmaceutical composition according to claim 9 , ...

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Номер записи: 18
20-02-2014 дата публикации

SYNTHESIS OF AN ANTIVIRAL COMPOUND

Номер: US20140051866A1
Автор: Liu Qi, Watkins William John
Принадлежит: Gilead Sciences, Inc.

The present disclosure provides a processes for the preparation of a compound of Formula I: 7. The process of claim 5 , wherein the N-arylation reaction conditions comprise a catalyst.8. The process of claim 7 , wherein the catalyst is a palladium claim 7 , platinum claim 7 , or copper based catalyst.9. The process of claim 8 , wherein the catalyst is selected from the group consisting of tris(dibenzylideneacetone)dipalladium(0) claim 8 , copper(I) chloride claim 8 , copper(II) chloride claim 8 , copper(I) bromide claim 8 , copper(II) bromide claim 8 , copper(I) acetate claim 8 , copper(II) acetate claim 8 , copper(II) acetylacetonate claim 8 , copper(I) trifluoromethanesulfonate claim 8 , copper(II) trifluoromethanesulfonate claim 8 , copper(I) thiophene-2-carboxylate claim 8 , and copper(I) iodide.10. The process of claim 7 , wherein the N-arylation reaction conditions further comprise a ligand.11. The process of claim 10 , wherein the ligand is selected from the group consisting of 5-(di-tert-butylphosphino)-1′ claim 10 ,3′ claim 10 ,5′-triphenyl-1′H-[1 claim 10 ,4′]bipyrazole claim 10 , 2-(di-tert-butyl-phosphino)-1-phenyl-1H-pyrrole claim 10 , 2-(di-tert-butylphosphino)-1-(2-methoxyphenyl)-1H-pyrrole claim 10 , acetylacetone claim 10 , acetylcyclohexanone claim 10 , isobutyrylcyclohexanone claim 10 , N claim 10 ,N-dimethylcyclohexane-1 claim 10 ,2-diamine claim 10 , L-proline claim 10 , BINAP claim 10 , and N claim 10 ,N-diethylsalicylamide.12. The process of claim 7 , wherein the N-arylation reaction conditions further comprise a base.13. The process of claim 12 , wherein the base is selected from the group consisting of potassium hydroxide claim 12 , sodium hydroxide claim 12 , sodium tert-amylate claim 12 , cesium carbonate claim 12 , cesium hydroxide claim 12 , potassium phosphate tribasic claim 12 , sodium tertbutoxide claim 12 , sodium methoxide claim 12 , and sodium ethoxide.14. The process of claim 4 , wherein the acylation reaction conditions comprise ...

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Номер записи: 19
27-02-2014 дата публикации

BIARYL DERIVATIVES AS SELECTIVE 17BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 2 INHIBITORS

Номер: US20140057953A1
Автор: Hartmann Rolf, Marchais-Oberwinkler Sandrine, Werth Ruth, Xu Kuiying
Принадлежит:

The invention relates to selective, non-steroidal 17beta-hydroxysteroid dehydrogenase type 2 (l7beta-HSD2) inhibitors of formula (I), their production and use, notably for the treatment and prophylaxis of sex steroid deficient diseases like osteoporosis in men and women. 5. The compound according to claim 1 , wherein the variables claim 1 , if present claim 1 , have the following meaning:{'sub': '2', 'R1 and R3 are independently selected from H, —OH, alkoxy, alkyl, —N(R8), halogen, haloalkyl and phenyl;'}{'sub': 2', '2', '2', '2', '2', '2', '2', '1-6', '1-6, 'R2, R4, R6 and R7 are independently selected from H, —OR8, —COR8, —COOR8, —CONHR8, —OCOR8, —SON(R8), —N(R8), —NHCOR8, —NHSOR8, halogen, —CHN(R8), —CHOR8, aryl optionally substituted with up to three R8, Calkyl optionally substituted with up to three R8 and halo Calkyl;'}R5 is lower alkyl;{'sub': 1-6', '1-6', '2, 'R8 is selected from H, Calkyl optionally substituted with up to three R9, halogen, halo Calkyl, —OH, lower alkoxy, —NH, and 5- or 6-membered aromatic or heteroaromatic ring optionally substituted with up to three R9;'}{'sub': 1-4', '2, 'R9 is selected from —OH, alkoxy, halogen, haloalkyl, Calkyl, —NHand phenyl;'}X, Y and P are independently selected from CH, N, N(H) and S; and/orn is 0 or 1.8. The compound according to claim 1 , which is selected from the group consisting of3′-methoxy-N-(3-methoxybenzyl)-N-methylbiphenyl-4-carboxamide (1),3′-hydroxy-N-(3-hydroxybenzyl)-N-methylbiphenyl-4-carboxamide (2),N-(3-methoxybenzyl)-N,3′-dimethylbiphenyl-4-carboxamide (3),N-(3-hydroxybenzyl)-N,3′-dimethylbiphenyl-4-carboxamide (4),4′-methoxy-N-(3-methoxybenzyl)-N-methylbiphenyl-3-carboxamide (5),4′-hydroxy-N-(3-hydroxybenzyl)-N-methylbiphenyl-3-carboxamide (6),3′-methoxy-N-(3-methoxybenzyl)-N-methylbiphenyl-3-carboxamide (7,3′-hydroxy-N-(3-hydroxybenzyl)-N-methylbiphenyl-3-carboxamide (8),4′-methoxy-N-(3-methoxyphenyl)-N-methylbiphenyl-3-carboxamide (9),4′-hydroxy-N-(3-hydroxyphenyl)-N-methylbiphenyl-3- ...

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Номер записи: 20
06-03-2014 дата публикации

Thiophene-2-carboximidamide Based Selective Neuronal Nitric Oxide Inhibitors

Номер: US20140066635A1
Автор: Huang He, Jing Qing, Silverman Richard B.
Принадлежит: Northwestern University

Selective neuronal nitric oxide synthase (nNOS) inhibitor compounds designed with one or more thiophene-2-carboximidamide substituents for improved bioavailability. 1. A compound of a formulawherein L is a divalent CHCHmoiety with a meta-relationship to each said thiophene-2-carboximidamide moiety of said compound; or a salt thereof. This application claims priority benefit from application Ser. No. 61/695,187 filed Aug. 30, 2012, application Ser. No. 61/698,249 filed Sep. 7, 2012 and application Ser. No. 61/774,926 filed Mar. 8, 2013—each of which is incorporated herein by reference in its entirety.This invention was made with government support under grant number GM049725 awarded by the National Institutes of Health. The government has certain rights in the invention.Neuronal nitric oxide synthase (nNOS) catalyzes the oxidation of L-arginine to L-citrulline in the central nervous system, generating nitric oxide (NO), a critical neurotransmitter. Significant research has implicated the overexpression of nNOS—and overproduction of NO—in various neurological diseases, including Parkinson's, Alzheimer's, and Huntington's diseases, as well as neuronal damage due to stroke, cerebral palsy and migraine headaches. Inhibiting endothelial nitric oxide synthase (eNOS) and inducible nitric oxide synthase (iNOS) is, however, undesirable, because these isozymes are responsible for maintaining crucial body function. Thus, selective inhibition of nNOS over its closely related isoforms, eNOS and iNOS, has provided a promising strategy in the development of therapeutics for the treatment of neurodegenerative diseases. However, while certain compounds have exhibited good potency and high selectivity, they often suffer from poor bioavailability. As a result, there remains an on-going search in the art for effective bioavailable NOS inhibitors to realize the therapeutic potential of such compounds.In light of the foregoing, it is an object of the present invention to provide compounds ...

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Номер записи: 21
03-04-2014 дата публикации

Sweetner Compositions and Methods of Making Them

Номер: US20140093630A1
Автор: Boriruck Kitisin, Carolyn Podgurski, James Robert Zeller, Jennifer Ward, Kevin Wirtz, Maria Suparno, Rhondi Shigemura, Thitiwan Lebien
Принадлежит: Senomyx Inc

The present invention provides compositions comprising sucralose and 4-amino-5,6-dimethylthieno[2,3-d]pyrimidine-2(1H)-one or salts, solvates, and/or esters thereof and methods of making the compositions by spray drying. The present invention also provides ingestible compositions comprising compositions of the present invention and methods of making such foods. The present invention also includes a process of preparing 2-amino-thiophene derivatives, which are key intermediates for preparing 4-amino-5,6-dimethylthieno[2,3-d]pyrimidine-2(1H)-one.

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Номер записи: 22
03-04-2014 дата публикации

HETEROCYCLIC CARBOXYLIC ACID ESTER DERIVATIVE

Номер: US20140094489A1
Автор: Koshiba Takahiro, Ohsumi Koji, Suzuki Tamotsu, Tokumasu Munetaka
Принадлежит: AJINOMOTO CO., INC.

The present invention provides a blood glucose elevation inhibitor having a serine protease inhibitory action, which is a novel therapeutic or prophylactic agent for obesity. A compound represented by the following formula (I) 2. A compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein D is a benzene ring or a naphthalene ring.3. A compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein D is a benzene ring.4. A compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein R1 is a hydrogen atom or a halogen atom.5. A compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein Het is a 5- to 10-membered aromatic ring containing 1 to 3 hetero atoms.8. A compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein X is a lower alkylene group optionally having one or more substituents selected from the group consisting of a halogen atom claim 1 , a hydroxyl group claim 1 , an amino group claim 1 , a lower alkoxyl group claim 1 , a lower acyl group claim 1 , and an oxo group.9. A compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein n is 0 claim 1 , or n is 1 or 2 claim 1 , and R2 is a lower alkyl group.10. A compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein R3 is a hydrogen atom claim 1 , a lower alkyl group optionally having substituent(s) claim 1 , a lower alkenyl group optionally having substituent(s) claim 1 , or a lower cycloalkyl group optionally having substituent(s) claim 1 , wherein said substituent(s) is selected from the group consisting of a carboxyl group and —CONH—CH—COH.11. A compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein R2 and R3 are bonded together to form tetrahydropyridine.12. A compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein Y is a single bond or —C(R4a)(R4b)- claim 1 , wherein R4a and R4b ...

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Номер записи: 23
05-01-2017 дата публикации

COMPOUND USEFUL FOR MANUFACTURING SALACINOL, METHOD FOR MANUFACTURING THE COMPOUND, METHOD FOR MANUFACTURING SALACINOL, METHODS FOR PROTECTING AND DEPROTECTING DIOL GROUP, AND PROTECTIVE AGENT FOR DIOL GROUP

Номер: US20170001974A1
Автор: FUJINO Yuuta, KATSUMATA Taiji, NAGASE Hisato, NAKAMURA Koki, WATANABE Katsuyuki
Принадлежит: FUJIFILM Corporation

An object of the present invention is to provide a novel compound useful for manufacturing salacinol, a method for manufacturing the compound, a method for manufacturing salacinol, methods for protecting and deprotecting a diol group, and a protective agent for a diol group. A compound represented by Formula (1) is a compound useful for manufacturing salacinol. 2. The compound according to claim 1 ,{'sup': 1a', '1b, 'wherein Rand Rare the same as or different from each other and each represent a carboxy protective group.'}3. The compound according to claim 1 ,{'sup': 2', '3, 'wherein each of Rand Ris a hydroxy group.'}6. The compound according to claim 1 ,{'sup': '5', 'wherein Ris a phenyl group which may be substituted.'}7. The compound according to that is a compound selected from dimethyl 2-((4aS claim 1 ,8aR)-6-phenyltetrahydro[1 claim 1 ,3]dioxino[5 claim 1 ,4-d][1 claim 1 ,3]dioxin-2-yl)malonate claim 1 , dimethyl 2-((4R claim 1 ,5S)-5-hydroxy-4-(hydroxymethyl)-1 claim 1 ,3-dioxan-2-yl)malonate claim 1 , dimethyl 2-((4aR claim 1 ,8aS)-2 claim 1 ,2-dioxidotetrahydro[1 claim 1 ,3]dioxin[5 claim 1 ,4-d][1 claim 1 ,3 claim 1 ,2]dioxathiin-6-yl)malonate claim 1 , (4S claim 1 ,5S)-4-(((2R claim 1 ,3 S claim 1 ,4S)-3 claim 1 ,4-dihydroxy-2-(hydroxymethyl)tetrahydro-1H-thiophen-1-ium-1-yl) methyl-2-(1 claim 1 ,3-dimethoxy-1 claim 1 ,3-dioxopropan-2-yl)-1 claim 1 ,3-dioxan-5-yl sulfate claim 1 , (4S claim 1 ,5 S)-4-(((1 S claim 1 ,2R claim 1 ,3 S claim 1 ,4S)-3 claim 1 ,4-bis(benzyloxy)-2-((benzyloxy)methyl)tetrahydro-1H-thiophen-1-ium-1-yl)methyl)-2-(1 claim 1 ,3-dimethoxy-1 claim 1 ,3-dioxopropan-2-yl)-1 claim 1 ,3-dioxan-5-yl sulfate claim 1 , (4S claim 1 ,5S)-4-(((1 S claim 1 ,2R claim 1 ,3 S claim 1 ,4S)-3 claim 1 ,4-bis((4-methoxybenzyl)oxy)-2-(((4-methoxybenzyl)oxy)methyl)tetrahydro-1H-thiophen-1-ium-1-yl)methyl)-2-(1 claim 1 ,3-dimethoxy-1 claim 1 ,3-dioxopropan-2-yl)-1 claim 1 ,3-dioxan-5-yl sulfate claim 1 , diethyl 2-((4aS claim 1 ,8aR)-6-phenyltetrahydro[1 ...

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Номер записи: 24
04-01-2018 дата публикации

Hypdh inhibitors and methods of use for the treatment of kidney stones

Номер: US20180002275A1
Автор: Daniel Yohannes, Ross P. Holmes, W. Todd Lowther
Принадлежит: UAB RESEARCH FOUNDATION, Wake Forest University Health Sciences

Provided herein are compounds of Formula (I), Formula (II), and Formula (III), and compositions comprising the same, as well as methods of use thereof for controlling or inhibiting the formation of calcium oxalate kidney stones, inhibiting the production of glyoxylate and/or oxalate, and/or inhibiting hydroxyproline dehydrogenase (HYPDH).

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Номер записи: 25
11-01-2018 дата публикации

COMPOUND USEFUL FOR MANUFACTURING SALACINOL, METHOD FOR MANUFACTURING THE COMPOUND, METHOD FOR MANUFACTURING SALACINOL, METHODS FOR PROTECTING AND DEPROTECTING DIOL GROUP, AND PROTECTIVE AGENT FOR DIOL GROUP

Номер: US20180009777A1
Автор: FUJINO Yuuta, KATSUMATA Taiji, NAGASE Hisato, NAKAMURA Koki, WATANABE Katsuyuki
Принадлежит: FUJIFILM Corporation

An object of the present invention is to provide a novel compound useful for manufacturing salacinol, a method for manufacturing the compound, a method for manufacturing salacinol, methods for protecting and deprotecting a diol group, and a protective agent for a diol group. A compound represented by Formula (1) is a compound useful for manufacturing salacinol. 2. The manufacturing method according to claim 1 ,{'sup': 1a', '1b', '4a', '4b', '4c, 'wherein each of Rand Ris a carboxy protective group, and each of R, R, and Ris a hydrogen atom.'}4. The manufacturing method according to claim 3 ,{'sup': '5', 'wherein Ris a phenyl group which may be substituted.'}5. The manufacturing method according to claim 3 ,{'sup': 1a', '1b', '4a', '4b', '4c, 'wherein each of Rand Ris a carboxy protective group, and each of R, R, and Ris a hydrogen atom.'} The present application is a Divisional of U.S. application Ser. No. 15/268,829, filed Sep. 19, 2016 which is a continuation of PCT/JP2015/58197 filed on Mar. 19, 2015 and claims priority under 35 U.S.C. § 119 of Japanese Patent Application No. 57961/2014 filed on Mar. 20, 2014, the disclosures of which are incorporated herein by referenceThe present invention relates to a compound useful for manufacturing salacinol and a method for manufacturing the compound. The present invention also relates to a method for manufacturing salacinol, methods for protecting and deprotecting a diol group, and a protective agent for a diol group.In traditional Indian medicine, Salacia reticulata which is a climbing tree of the genus Salacia is used for treating diabetes. Salacinol is a component contained in plants of the genus Salacia such as Salacia reticulata and has a strong α-glucosidase inhibitory activity (Tetrahedron Letters, Vol. 38, No. 48., pp. 8367-8370 (1997)). Salacinol is obtained from, for example, extracts of plants of the genus Salacia (JP3030008B). However, the supply of plants of the genus Salacia is small, and it is difficult to ...

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Номер записи: 26
14-01-2021 дата публикации

PROCESSES FOR PREPARING PLASMA KALLIKREIN INHIBITORS

Номер: US20210009526A1
Автор: BHAT Ganapati, CHILCOTE TAMIE, KRISHNAN Baburaj, MALIK Vineet, SINHA Sukanto
Принадлежит:

A process for preparing and purifying a compound of Formula I is provided: 2. The process of claim 1 , wherein the reducing conditions comprise Raney nickel and H.3. The process of claim 2 , wherein the reducing conditions comprise Raney nickel at about 10 to about 40 mol % claim 2 , and Hat about 2 to about 20 kg/cm.4. The process of claim 3 , wherein the reducing conditions comprise Raney nickel at about 20 mol % claim 3 , and Hat about 10 kg/cm.5. The process of claim 1 , wherein the reducing conditions further comprise acetic acid as a solvent claim 1 , and heating at a temperature of about 30° C. to about 70° C.68.-. (canceled)9. The process of claim 2 , further comprising:(b) forming a slurry of the crude product in water at a temperature of about 25° C. to about 70° C. to provide a nickel-depleted product.1011.-. (canceled)12. The process of claim 9 , further comprising:(c) heating the nickel-depleted product in a solvent to remove further nickel.13. The process of claim 12 , wherein the solvent comprises a mixture of ethanol and acetic acid.14. The process of claim 12 , wherein the solvent comprises a mixture of methanol claim 12 , dimethyl glyoxime claim 12 , and methyl-t-butyl ether.16. The process of claim 15 , wherein the basic conditions comprise triethylamine and ethanol.17. The process of claim 16 , wherein the basic conditions further comprise heating at a temperature of about 50° C. to about 75° C.1820.-. (canceled)21. The process of claim 15 , wherein about 3 equivalents of hydroxylamine and triethylamine are used per equivalent of compound of Formula III.23. The process of claim 22 , wherein the aprotic conditions comprise triethylamine in dichloromethane.24. The process of claim 22 , wherein the aprotic conditions further comprise 1-propanephosphonic anhydride in ethyl acetate (T3P®).25. The process of claim 24 , wherein the aprotic conditions comprise incubating the compound of Formula IV with 4-(aminomethyl)benzonitrile hydrochloride and 1- ...

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Номер записи: 27
08-01-2015 дата публикации

PROCESS FOR PREPARATION OF RIVAROXABAN AND INTERMEDIATES THEREOF

Номер: US20150011756A1
Автор: Bodake Mahendra Bhagirath, Ippar Sharad Subhash, Mali Anil Chaturlal, Mathad Vijayavitthal Thippannachar, Niphade Navnath Chintaman, Patil Nilesh Sudhir, Talla Rajesh
Принадлежит:

An improved process for the preparation of Rivaroxaban wherein the process substantially eliminates the potential impurities. process for preparation of Rivaroxaban which uses a novel intermediate. A process for preparing the novel intermediate which is used for the preparation of Rivaroxaban. 2. The process of claim 1 , wherein the first solvent used in step (a) and step (c) may be either same or different; wherein the said solvent is an organic solvent selected from the group consisting of aliphatic hydrocarbons claim 1 , aromatic hydrocarbons claim 1 , amides including but not limited to dialkylformamides and dialkylacetamides claim 1 , ethers claim 1 , cyclic ethers claim 1 , substituted cyclic ethers claim 1 , alcohols claim 1 , ketones claim 1 , dialkylsulfoxides claim 1 , nitriles claim 1 , ionic liquids claim 1 , halogenated aliphatic hydrocarbons claim 1 , water or mixtures thereof.3. The process of claim 1 , wherein the second solvent used in step (b) is an organic solvent selected from the group consisting of aliphatic hydrocarbons claim 1 , aromatic hydrocarbons claim 1 , amides including but not limited to dialkylformamides and dialkylacetamides claim 1 , ethers claim 1 , cyclic ethers claim 1 , substituted cyclic ethers claim 1 , ketones claim 1 , dialkylsulfoxides claim 1 , nitriles claim 1 , ionic liquids claim 1 , halogenated aliphatic hydrocarbons or mixtures thereof.4. The process of claim 1 , wherein the third solvent used in step (d) is an organic solvent selected from the group consisting of aliphatic hydrocarbons claim 1 , aromatic hydrocarbons claim 1 , amides including but not limited to dialkylformamides and dialkylacetamides claim 1 , ethers claim 1 , cyclic ethers claim 1 , substituted cyclic ethers claim 1 , ketones claim 1 , dialkylsulfoxides claim 1 , nitriles claim 1 , ionic liquids claim 1 , halogenated aliphatic hydrocarbons claim 1 , water or mixtures thereof.5. The process of claim 1 , wherein the base used in step (b) and step (d ...

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Номер записи: 28
03-02-2022 дата публикации

SUBSTITUTED THIOPHENECARBOXAMIDES AND ANALOGUES AS ANTIBACTERIALS AGENTS

Номер: US20220033374A1
Автор: Bernier David, BRUNET Stephane, DUFOUR Jérémy, KNOBLOCH Thomas, NICOLAS Lionel, TSUCHIYA Tomoki
Принадлежит: Bayer Aktiengesellschaft

The present disclosure relates to substituted thiophene carboxamides and analogues thereof of formula (I) that may be used for protecting plants from bacterial diseases, in particular from bacterial diseases caused by bacteria belonging to the genus . 2. The compound of formula (I) according to wherein Ris selected from the group consisting of hydrogen atom claim 1 , C-C-alkyl claim 1 , benzyl claim 1 , benzyl substituted by hydroxyl claim 1 , C-C-alkyl substituted by a C-C-alkylsulfanyl and Ris a hydrogen atom; or Rand Rform claim 1 , together with the carbon atom to which they are linked claim 1 , a cyclopropyl.3. The compound of formula (I) according to wherein Ris selected from the group consisting of hydrogen atom claim 1 , C-C-alkyl claim 1 , C-C-haloalkyl claim 1 , C-C-cyanoalkyl claim 1 , C-C-alkenyl claim 1 , C-C-alkynyl claim 1 , C-C-cycloalkyl claim 1 , phenyl claim 1 , benzyl claim 1 , 4- claim 1 , 5- or 6-membered heterocyclyl claim 1 , —C-C-alkyl-Si(C-C-alkyl)and —C-C-alkyl-cyclopropyl.4. The compound of formula (I) according to claim 1 , wherein Ris selected from the group consisting of hydrogen atom claim 1 , C-C-alkyl claim 1 , C-C-haloalkyl claim 1 , C-C-cyanoalkyl claim 1 , C-C-alkenyl claim 1 , C-C-alkynyl claim 1 , C-C-cycloalkyl claim 1 , phenyl claim 1 , benzyl claim 1 , oxetanyl claim 1 , thietanyl claim 1 , dioxothietanyl claim 1 , oxolanyl claim 1 , oxanyl claim 1 , —C-C-alkyl-Si(C-C-alkyl)and —C-C-alkyl-cyclopropyl.5. A composition comprising at least one compound of formula (I) according to and at least one agriculturally suitable auxiliary.6. A method for controlling bacterial diseases comprising the step of applying (i) at least one compound of formula (I) according to claim 1 , or (ii) a composition comprising at least one compound of formula (I) according to and at least one agriculturally suitable auxiliary to plants claim 1 , plant parts claim 1 , seeds claim 1 , fruits or to the soil in which the plants grow. This application is a ...

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Номер записи: 29
17-01-2019 дата публикации

NEMATOCIDAL HETEROCYCLIC AMIDES

Номер: US20190014779A1
Автор: CAMPBELL Matthew James, DEANGELIS Andrew Jon, Lahm George Philip
Принадлежит: E. I. DU PONT DE NEMOURS AND COMPANY

Disclosed are compounds of Formulae 1, 1a, 1b and 2, 4. The compound of any one of , and , wherein{'sup': '2', 'Ris H;'}{'sup': 3', '6a', '6b', '6c, 'Ris —CRRR;'}{'sup': '4', 'Ris Cl or Br;'}{'sup': '6a', 'sub': 1', '3', '2', '3', '3', '6, 'Ris H, C-Calkyl, C-Calkenyl or C-Ccycloalkyl;'}{'sup': '6b', 'sub': 1', '3, 'Ris C-Calkyl;'}{'sup': 6c', '7a', '7b', '7c, 'sub': 1', '3', '1', '3', '1', '3', '1', '3, 'Ris H, halogen, cyano, C-Calkoxy, C-Calkylthio, C-Calkylsulfinyl, C-Calkylsulfonyl or —CRRR;'}{'sup': '7a', 'sub': 1', '3', '1', '3', '1', '3', '1', '3', '1', '2, 'Ris H, halogen, cyano, C-Calkoxy, C-Calkylthio, C-Calkylsulfinyl, C-Calkylsulfonyl or C-Calkyl;'}{'sup': '7b', 'sub': 1', '2, 'Ris H, halogen, cyano or C-Calkyl; and'}{'sup': '7c', 'sub': 1', '2, 'Ris H, halogen, cyano or C-Calkyl.'}6. The composition of wherein the ratio of 1b to 1a is at least 65:35.7. The composition of wherein the ratio of 1b to 1a is at least 75:25.8. The composition of wherein the ratio of 1b to 1a is at least 85:15.9. The composition of wherein the ratio of 1b to 1a is at least 95:5.10. The composition of wherein the ratio of 1b to 1a is at least 97:3.11. The composition of wherein the ratio of 1b to 1a is at least 99:1.12. The composition of wherein the ratio of 1b to 1a is essentially 100:0.13. A composition comprising a compound of any one of through claim 5 , and at least one additional component selected from the group consisting of surfactants claim 5 , solid diluents and liquid diluents claim 5 , said composition optionally further comprising at least one additional biologically active compound or agent.14. The composition of any one of through wherein the compound of Formula 1b is present in a nematocidally effective amount.15Bacillus thuringiensis. The composition of wherein the at least one additional biologically active compound or agent is selected from the group consisting of abamectin claim 13 , acephate claim 13 , acequinocyl claim 13 , acetamiprid claim 13 , ...

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Номер записи: 30
15-01-2015 дата публикации

Compounds as ppar beta/delta inhibitors for treating ppar beta/delta-mediated diseases

Номер: US20150018411A1
Автор: Gerhard Klebe, Josefine Stockert, Kerstin Kaddatz, Philipp Manuel Toth, Rolf Müller, Simone Naruhn, Stefanie Dörr, Veronika Pape, Wibke Diederich
Принадлежит: Philipps Universitaet Marburg

The present invention concerns substances which act as selective ligands of nuclear receptors of the PPAR beta/delta subtype and which can be used for the treatment of PPAR beta/delta-mediated diseases. The substances of this invention act as inhibitors of PPAR beta/delta receptors.

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Номер записи: 31
16-01-2020 дата публикации

UREA DERIVATIVE

Номер: US20200017439A1
Автор: Fukunaga Taichi, Matsumoto Koji, NAKAMURA Yuji, Soneda Tsuyoshi, Tanaka Naomi
Принадлежит: Daiichi Sankyo Company, Limited

An object of the present invention is to find a novel pharmaceutical that has an excellent tryptophanase inhibitory effect, and suppresses worsening of renal function to preserve the kidney by reducing production of indoxyl sulfate in the blood. The present invention provides a pharmaceutical composition containing, as an active ingredient, a compound represented by the following formula, or a pharmacologically acceptable salt thereof: 6. The compound according to or , or a pharmacologically acceptable salt thereof , wherein Rrepresents an ethyl group.7. The compound according to or , or a pharmacologically acceptable salt thereof , wherein Rrepresents a hydrogen atom , a fluorine atom or a cyano group.8. The compound according to any one of to , or a pharmacologically acceptable salt thereof , wherein Rrepresents a fluorine atom , a chlorine atom , a bromine atom , an iodine atom , a 2 ,2 ,2-trifluoroethyl group , a difluoromethoxy group or a trifluoromethoxy group.11. The compound according to or , or a pharmacologically acceptable salt thereof , wherein Rrepresents a cyclopropyl group.12. The compound according to any one of to , or a pharmacologically acceptable salt thereof , wherein Rrepresents an ethyl group or a cyclopropyl group.13. The compound according to any one of to , or a pharmacologically acceptable salt thereof , wherein Rrepresents a hydrogen atom , and Rrepresents a fluorine atom , a cyano group , a cyanomethyl group , a 2 ,2 ,2-trifluoroethyl group , a difluoromethoxy group or a trifluoromethoxy group.14. The compound according to any one of to , or a pharmacologically acceptable salt thereof , wherein Rrepresents a cyano group , and Rrepresents a hydrogen atom.17. The compound according to or , or a pharmacologically acceptable salt thereof , wherein Rand Rare the same or different and represent an ethyl group , a propyl group or an isopropyl group.18. The compound according to or , or a pharmacologically acceptable salt thereof , wherein Rand ...

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Номер записи: 32
21-01-2021 дата публикации

Diphenyl Substituted Thiophene-2-Amide Derivatives and Pharmaceutical Compositions Thereof Useful as Antimicrobial

Номер: US20210017147A1
Автор: BARDEN Christopher J., Lu Erhu, Sun Shengguo, Wu Fan
Принадлежит: Denovamed Inc.

Compounds or pharmaceutical acceptable salts thereof of Formula (I), in which RM have the meaning described herein and pharmaceutical compositions thereof useful as antimicrobial and/or adjuvant: 2. The compound of in which Rand Rare each independently methyl claim 1 , ethyl claim 1 , or isopropyl.3. The compound of in which Rand Rare each both chloro.4. The compound of in which Rand R4 are both methyl.5. The compound of in which Rand Rare both isopropyl.6. The compound of in which R6 is —CH(CF)OH and the compound of Formula I is a racemate.7. The compound of in which Ris —CH(CF)OH and the compound of Formula I is the (R) enantiomer.8. The compound of in which Ris —CH(CF)OH and the compound of Formula I is the (S) enantiomer.9. The compound of in which the compound is selected from compounds exemplified herein.10. A method of treatment of a microbial infection comprising administering an effective amount of an antimicrobial compound of to a patient in need thereof.11. The method of treatment of in which the microbial infection is substantially caused by Gram-positive bacteria.12Staphylococcal. The method of treatment of in which the microbial infection comprises infection.13Enterococcal. The method of treatment of in which the microbial infection comprises infection.14Bacillus. The method of treatment of in which the microbial infection comprises infection.15Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis, Enterococcus faecium, Bacillus cereus,Streptococcus. The method of treatment of in which the microbial infection is substantially caused by a bacterial species selected from and sp.16. A method of treatment of a microbial infection comprising administering an effective amount of an antimicrobial adjuvant compound of and an effective amount of an antimicrobial compound to a patient in need thereof.17. The method of treatment of in which the microbial infection is substantially caused by Gram-negative bacteria.18. The method of treatment of ...

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Номер записи: 33
28-01-2016 дата публикации

SYNTHETIC INTERMEDIATE OF 1-(2-DEOXY-2-FLUORO-4-THIO-ß-D-ARABINOFURANOSYL) CYTOSINE, SYNTHETIC INTERMEDIATE OF THIONUCLEOSIDE, AND METHOD FOR PRODUCING THE SAME

Номер: US20160024132A1
Автор: FUJINO Yuuta, IMOTO Junichi, Ito Takayuki, Matsumoto Takuya, NAKAMURA Kouki, OKADA Hideki, SHIMAMURA Satoshi, Takahashi Makoto, TAKAHASHI Motomasa, WADA Kenji, WATANABE Katsuyuki, YAMANE Takehiro
Принадлежит: FUJIFILM Corporation

A compound represented by a formula [1D] as shown below (wherein R, R, R, R, Rand Rrepresent a hydrogen atom, an optionally substituted Calkyl group, and the like) is useful as an intermediate for producing a thionucleoside, and the production method of the present invention is useful as a method for producing a thionucleoside. 3. The production method according to claim 1 , wherein{'sup': 1A', '1B', '2A', '2B, 'sub': '1-6', 'claim-text': {'br': None, 'sup': '2a', '—OR\u2003\u2003[15]'}, 'Rand R, which are the same or different, each represent a hydrogen atom, an optionally protected carboxyl group, an optionally substituted Calkyl group or an optionally substituted aryl group; Rand R, which are the same or different, each represent a hydrogen atom, a group represented by the following formula [15]{'sup': 2a', '3A', '3B, 'claim-text': {'br': None, 'sup': '3a', '—OR\u2003\u2003[16]'}, '(wherein Rrepresents a hydroxyl-protecting group), or an optionally substituted aryl group; Rand R, which are the same or different, each represent a hydrogen atom, a halogen atom, an optionally protected amino group, a group represented by the following formula [16]{'sup': 3a', '2A', '3A, 'sub': 1-6', '1-6, 'claim-text': {'br': None, 'sup': '1', '—O—Y—O—\u2003\u2003[17]'}, '(wherein Rrepresents a hydroxyl-protecting group), an optionally substituted Calkyl group, an optionally substituted Calkylthio group, an optionally substituted aryloxy group, an optionally substituted arylthio group or an optionally substituted heterocyclic thio group; or Rand Rmay together form a group represented by the following formula [17]{'sup': 1', '2A', '2A', '2B', '3A', '3B, 'sub': '1-6', '(wherein Yrepresents an optionally substituted Calkylene group or an optionally substituted siloxane group; and the bond on the left side binds to a carbon atom binding to R), or a bond; or R, R, Rand Rmay form an optionally substituted benzene ring together with carbon atoms to which they bind.'}4. The production ...

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Номер записи: 34
26-01-2017 дата публикации

N-HYDROXYLSULFONAMIDE DERIVATIVES AS NEW PHYSIOLOGICALLY USEFUL NITROXYL DONORS

Номер: US20170022154A1
Автор: BROOKFIELD Frederick Arthur, Cohen Andrew D., COURTNEY Stephen Martin, FROST Lisa Marie, KALISH Vincent Jacob, Toscano John P.
Принадлежит:

The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives. 2. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein A and B form a benzofuran.3. The compound of or a pharmaceutically acceptable salt thereof claim 2 , wherein x and y are 0.4. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein each Rand Ris independently selected from Cl claim 1 , F claim 1 , I claim 1 , Br claim 1 , SOCH claim 1 , SONHOH claim 1 , CF claim 1 , CH claim 1 , NO claim 1 , phenyl claim 1 , CN claim 1 , OCH claim 1 , OCF claim 1 , t-Bu claim 1 , O-iPr claim 1 , 4-nitrophenyloxy claim 1 , SCH(CH) claim 1 , S(O)CH(CH) claim 1 , morpholino claim 1 , N-methyl-piperazino claim 1 , dimethylamino claim 1 , piperidino claim 1 , cyclohexyloxy claim 1 , cyclopentylsulfanyl claim 1 , phenyl sulfanyl claim 1 , and phenyl sulfinyl.5. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H claim 1 , benzyl claim 1 , or tetrahydropyran-2-yl.6. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H.7. The compound of or a pharmaceutically acceptable salt thereof of claim 4 , wherein Ris H.9. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the compound of or a pharmaceutically acceptable salt thereof; and'}a pharmaceutically acceptable carrier.10. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00007', 'claim 7'}, 'the compound of or a ...

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Номер записи: 35
24-04-2014 дата публикации

THIOLACTONE ANTIBIOTICS

Номер: US20140113941A1
Автор: Bommineni Gopal Reddy, Kapilashrami Kanishk, Machutta Carl, TONGE Peter
Принадлежит: The Research Foundation for The State University of New York

This invention provides a compound having the structure 20. A pharmaceutical composition comprising the compound of and a pharmaceutically acceptable carrier. This application claims priority of U.S. Provisional Application No. 61/467,761, filed Mar. 25, 2011, the contents of which are hereby incorporated by reference.The invention was made with government support under NIH Grant number 5R01A104463909 awarded by the National Institutes of Health. The government may have certain rights in the invention.Throughout this application, certain publications are referenced in parentheses. Full citations for these publications may be found immediately preceding the claims. The disclosures of these publications in their entireties are hereby incorporated by reference into this application in order to describe more fully the state of the art to which this invention relates.Thiolactomycin (TLM) is a natural product thiolactone first isolated from sp., a bacterial strain identified from a Japanese soil sample in 1981 (4). TLM is rapidly absorbed in rats when administered both orally and by intramuscular injection, and it provides protection from both urinary tract and oral infections in animals infected with and (14).The antibacterial activity of TLM is known to result from an inhibition of fatty acid biosynthesis. TLM is a selective and reversible inhibitor of the KAS enzymes in the FAS-II pathway (4, 6, 16), but does not inhibit the mammalian FAS-I enzymes (17). TLM resistant strains contain mutations in the fabB KAS gene (18) and overproduction of FabB confers TLM resistance in vivo (19) suggesting that FabB is the major cellular target. Based on kinetic and structural data, TLM is thought to be a competitive inhibitor of malonyl-ACP (5-6), and studies have shown that TLM binds preferentially to the covalently modified KAS acyl-enzyme intermediate with slow onset kinetics (15).Although slow onset kinetics are observed when TLM binds to acyl-KasA (15), the inhibitor only has a ...

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Номер записи: 36
29-01-2015 дата публикации

SPHINGOLIPID METABOLITE MIMETICS

Номер: US20150031892A1
Автор: Huang Zhizhen, Liu Feiyan, Liu Kebin, Wu Ping
Принадлежит:

Sphingolipid metabolite mimetics and methods of synthesizing them are provided. The sphingolipid metabolite mimetics are shown to be effective at inducing apoptosis in various types of tumor cells. Further, the sphingolipid metabolite mimetics are shown to be effective at sensitizing multiple types of tumor cells to TRAIL-induced apoptosis. Formulations containing one or more sphingolipid metabolite mimetics and, optionally, one or more cell death receptor agonists are provided. Methods of treating cancer in a subject in need thereof are provided using one or more sphingolipid metabolite mimetics. 1. (canceled)3. The compound of having a structure according to Formula I claim 2 , wherein{'sub': 1', '10', '20, 'Ris a C-Clinear alkyl, and'}{'sub': '2', 'Ris selected from the group consisting of phenyl, 2-furanyl, 2-thiophenyl, 1,3-pentadienyl, 2-phenylethenyl, isoquinoline, indole, methyl indole, benzofuranyl, naphthalene, hydroxynaphthalene, and cyclohex-4-ene-1,2,3-triol.'}4. The compound of having a structure according to Formula II claim 2 , whereinY is methyl,{'sub': 3', '10', '20, 'Ris a C-Clinear alkyl, and'}{'sub': '4', 'Ris selected from the group consisting of phenyl, 2-furanyl, 2-thiophenyl, 1,3-pentadienyl, 2-phenylethenyl, isoquinoline, indole, methyl indole, benzofuranyl, naphthalene, hydroxynaphthalene, and cyclohex-4-ene-1,2,3-triol.'}5. The compound of selected from the group consisting of (S)-2-Amino-3-hydroxy-N-dodecylpropanamide claim 2 , (S)-2-Amino-3-hydroxy-N-dodecylpropanamide claim 2 , (2S claim 2 ,3R)-2-Amino-3-hydroxy-N-octadecylbutanamide claim 2 , (2E claim 2 ,4E)-N-((2S claim 2 ,3R)-3-hydroxy-1-oxo-1-(dodecylamino)butan-2-yl)-2 claim 2 ,4-hexadienoic acid amide claim 2 , (2E claim 2 ,4E)-N-((2S claim 2 ,3R)-3-hydroxy-1-oxo-1-(dodecylamino)butan-2-yl)-2 claim 2 ,4-hexadienoic acid amide claim 2 , (2E claim 2 ,4E)-N-((2S claim 2 ,3R)-3-hydroxy-1-oxo-1-(octadecylamino)butan-2-yl)-2 claim 2 ,4-hexadienoic acid amide claim 2 , (2E claim 2 ,4E ...

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Номер записи: 37
30-01-2020 дата публикации

COMPOSITION COMPRISING A COMPOUND OF THIOLACTONE TYPE AND A PARTICULAR SOLVENT AND PROCESS FOR TREATING KERATIN MATERIALS WITH THE COMPOSITION

Номер: US20200031796A1
Автор: CHAUMONTET Manon, Daubresse Nicolas, VOISIN Sébastien
Принадлежит:

The present invention relates to a composition comprising: (a) at least one compound of thiolactone type, and (b) one or more solvents, which may be identical or different, chosen from polar (non-)protic organic solvents; the pH of said composition being less than or equal to 7. 125.-. (canceled)32. The composition according to claim 31 , wherein the at last one compound of formula (I) is chosen from the compounds of formulae (38) to (122) and (153) to (258).33. The composition according to claim 26 , wherein the at least one compound of formula (I) is present in an amount ranging from 0.01% to 50% by weight claim 26 , relative to the total weight of the composition.34. The composition according to claim 26 , wherein the at least one polar (non-)protic organic solvent is chosen from:{'sub': 1', '6, '(b1) monoalcohols comprising a hydroxyl group and a C-C(alkyl);'}{'sub': 2', '8, '(b2) polyols comprising from 2 to 30 hydroxyl groups and a (C-C)alkyl group;'}{'sub': a', 'p', 'a', 'a', 'a', '1', '6, '(b3) the compounds of formula R—S(O)—R′, wherein Rand R′, which may be identical or different, represent a (C-C)alkyl, and p is equal to 1 or 2.'}35. The composition according to claim 34 , wherein the composition comprises at least two solvents each chosen from a different category (b1) claim 34 , (b2) and (b3).36. The composition according to claim 34 , wherein the monoalcohols are chosen from ethanol claim 34 , propanol claim 34 , isopropanol claim 34 , butanol claim 34 , or a mixture of these compounds.37. The composition according to claim 34 , wherein the polyalcohols are chosen from polyols comprising at least three carbon atoms and ethylene glycol.38. The composition according to claim 34 , wherein the solvents are chosen from the compounds of formula R—S(O)—R′ (III) below [{'br': None, 'sub': a', 'p', 'a, 'R—S(O)—R′'}, {'sub': a', 'a, 'claim-text': [{'sub': 1', '6', '1', '4, 'a linear or branched (C-C)alkyl group, optionally substituted with one or more atoms or ...

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Номер записи: 38
03-03-2022 дата публикации

NOVEL WHITENING AGENTS FOR CELLULOSIC SUBSTRATES

Номер: US20220064576A1
Автор: "Morrall Donna DAngelo", Baker Keith Homer, Cummings Michael David, HONG Xiayong Michael, Kieken Laurent D., KOTT Kevin Lee, LOUGHNANE Brian Joseph, Moore Patrick D., SADLOWSKI Eugene Steven, SIVIK Mark Robert, STARKS Leonard J., Torres Eduardo, Valenti Dominick J., VALENTI Michael A.
Принадлежит:

This invention relates to novel whitening agents for cellulosic substrates. The whitening agents are comprised of at least two components: at least one chromophore component and at least one polymeric component. Suitable chromophore components generally fluoresce blue, red, violet, or purple color when exposed to ultraviolet light, or they may absorb light to reflect these same shades. The whitening agents are further characterized by having a dispersion component value of the Hansen Solubility Parameter of less than or equal to about 17 MPa. This invention also relates to laundry care compositions including but not limited to liquid and/or powder laundry detergent formulations and rinse added fabric softening (RAFS) compositions that comprise such whitening agents.

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Номер записи: 39
08-05-2014 дата публикации

HETEROCYCLIC INHIBITORS OF NECROPTOSIS

Номер: US20140128437A1
Автор: Cuny Gregory D., Degterrev Alexei, JR. John A., Proco, Teng Xin, Yuan Junying
Принадлежит:

The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-α) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I) and (Ia)-(Ie) and are shown to inhibit TNF-α induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring the compounds of the invention. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role. 2. The compound of claim 1 , wherein{'sup': '1', 'Ris selected from methyl, ethyl, propyl, and butyl;'}{'sup': '2', 'Ris selected from hydrogen, halogen and cyano; and'}{'sup': '3', 'Ris selected from hydrogen, (S)-methyl, (S)-ethyl, (S)-propyl, and (S)-butyl;'}or any pharmaceutically acceptable salt thereof, or stereoisomer thereof.3. The compound of claim 2 , wherein{'sup': '1', 'Ris selected from methyl and isopropyl;'}{'sup': '2', 'Ris selected from hydrogen, chlorine, bromine and cyano;'}{'sup': '3', 'Ris selected from hydrogen and (S)-methyl; and'}{'sup': 1', '2, 'each Xand Xis independently chlorine or fluorine;'}or any pharmaceutically acceptable salt thereof, or stereoisomer thereof.4. The compound of claim 3 , wherein Ris methyl claim 3 , Ris cyano claim 3 , Ris (S)-methyl claim 3 , Xis chlorine claim 3 , and Xis fluorine;or any pharmaceutically acceptable salt thereof, or stereoisomer thereof.8. The compound of claim 7 , wherein Ris F claim 7 , Ris H claim 7 , and Ris Cl claim 7 ,or any pharmaceutically acceptable salt thereof, or stereoisomer thereof.9. The compound of claim 7 , wherein Ris F claim 7 , Ris a halogen claim 7 , and Ris Cl claim 7 ,or any pharmaceutically acceptable salt thereof, or stereoisomer thereof.10. The compound of claim 7 , wherein Ris F claim 7 , Ris H claim 7 , and Ris F claim 7 ,or any pharmaceutically acceptable salt thereof, or stereoisomer thereof.11. The compound of claim 7 ...

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Номер записи: 40
23-02-2017 дата публикации

PEPTIDOMIMETICS POSSESSING PHOTO-CONTROLLED BIOLOGICAL ACTIVITY

Номер: US20170051017A1
Автор: Afonin Sergiy, Babii Oleg, Komarov Igor, Mykhailiuk Pavlo, Ulrich Anne
Принадлежит:

The present invention relates to pharmaceutically and/or diagnostically active compounds, in particular peptide analogues (peptidomimetics), which can be reversibly controlled between an active and an inactive state by irradiation with light of different wavelengths. The present invention further relates to an intermediate compound usable in the manufacture of such pharmaceutically and/or diagnostically active compounds, as well as a manufacturing method thereof. 119-. (canceled)21. The photo-switchable molecular system according to claim 20 , wherein Rand Rare H.22. The photo-switchable molecular system according to claim 20 , wherein Rand Rare methyl.23. The photo-switchable molecular system according to claim 20 , wherein X is —CHCHCH— or —CFCFCF—.24. The photo-switchable molecular system according to claim 20 , wherein Yand Yare S.25. The photo-switchable molecular system according to claim 20 , wherein Rand Rare independently selected from the group consisting of H and a C-Calkyl group claim 20 , Rand Rare independently selected from the group consisting of a methyl group and an ethyl group and X is —CHCHCH— or —CFCFCF—.26. The photo-switchable molecular system according to claim 20 , wherein each of Rand Ris H claim 20 , each of Rand Ris a methyl group claim 20 , X is —CHCHCH— or —CFCFCF— claim 20 , and each of Yand Yis S.28. The method according to further comprising applying visible light to the compound of formula IVb to form the compound of formula IVa.29. The method according to claim 27 , wherein Rand Rare H.30. The method according to claim 27 , wherein Rand Rare methyl.31. The method according to claim 27 , wherein X is —CHCHCH— or —CFCFCF—.32. The method according to claim 27 , wherein Yand Yare S.33. The method according to claim 27 , wherein Rand Rare independently selected from the group consisting of H and a C-Calkyl group claim 27 , Rand Rare independently selected from the group consisting of a methyl group and an ethyl group and X is —CHCHCH— ...

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Номер записи: 41
21-02-2019 дата публикации

PRODUCTION METHOD OF THIENOPYRIMIDINE DERIVATIVE

Номер: US20190055261A1
Автор: MIWA Kazuhiro
Принадлежит:

The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like. 18-. (canceled)10: The compound of claim 9 , wherein Ris a nitro group claim 9 , or a salt thereof.11: The compound of claim 9 , wherein Ris an amino group claim 9 , or a salt thereof. The present invention relates to a production method of a thienopyrimidine derivative having a gonadotropin releasing hormone (GnRH) antagonistic action.Secretion of anterior pituitary hormones undergoes feedback control by peripheral hormones secreted from target organs of the respective hormones and by secretion-regulating hormones from the hypothalamus, which is the upper central organ of the anterior lobe of the pituitary (hereinafter, these hormones are collectively called “hypothalamic hormones” in this specification). Presently, as hypothalamic hormones, the existence of nine kinds of hormones including, for example, thyrotropin releasing hormone (TRH), and gonadotropin releasing hormone [GnRH, sometimes called as LH-RH (luteinizing hormone releasing hormone)] has been confirmed. By preventing LH-RH from binding with the LH-RH receptor in the anterior pituitary gland and suppressing the secretion of luteinizing hormone (LH) and follicle stimulation hormone (FSH) from the anterior pituitary gland, an antagonist for gonadotropin releasing hormone controls the effect of LH and FSH on the ovary, reduces the level of estrogen in blood, which is known to be associated with the development of endometriosis and uterine fibroids, and is ...

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Номер записи: 42
02-03-2017 дата публикации

Substituted arylcyclopentenes as therapeutic agents

Номер: US20170057941A1
Автор: Jeremiah H. Nguyen, Yariv Donde
Принадлежит: Allergan Inc

Disclosed herein is a compound of the formula Therapeutic methods, compositions, and medicaments, related thereto are also disclosed.

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Номер записи: 43
10-03-2016 дата публикации

CCR9 INHIBITORS AND METHODS OF USE THEREOF

Номер: US20160068479A1
Автор: Chen B. Shaowu, FLEMING PAUL E., Harriman Geraldine C.B., Shi Zhan
Принадлежит:

The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods. 2. (canceled)3. (canceled)4. The compound of claim 1 , wherein Aris a substituted or unsubstituted group selected from phenyl claim 1 , naphthyl claim 1 , thienyl claim 1 , and thianaphthenyl.5. The compound of claim 1 , wherein Aris a substituted or unsubstituted group selected from phenyl and pyridyl.6. The compound of claim 1 , wherein Aris a substituted or unsubstituted group selected from phenyl and thienyl.7. The compound of claim 1 , wherein Aris unsubstituted or is substituted with one or more substituents selected from substituted aliphatic claim 1 , unsubstituted aliphatic claim 1 , aryl claim 1 , arylalkyl claim 1 , substituted alkoxy claim 1 , unsubstituted alkoxy claim 1 , aryloxy claim 1 , arylalkoxy claim 1 , alkylthio claim 1 , halo claim 1 , nitro claim 1 , cyano claim 1 , S(O)-(aliphatic) claim 1 , S(O)-(aliphatic) claim 1 , NRS(O)-(aliphatic) claim 1 , C(O)N(R) claim 1 , C(O)R claim 1 , N(R) claim 1 , NRC(O)R claim 1 , and NRC(O)R claim 1 , wherein Rfor each occurrence is independently H or an aliphatic group claim 1 , and Ris an aliphatic group.8. The compound of claim 1 , wherein Aris unsubstituted or is substituted with one or more substituents selected from aliphatic claim 1 , alkoxy claim 1 , and haloalkoxy.9. (canceled)10. (canceled)11. The compound of claim 1 ,{'sub': '4', 'sup': +', '−, 'wherein Xis N—O.'}12. (canceled)13. (canceled)14. (canceled)15. (canceled)16. (canceled)17. (canceled)18. The compound of claim 6 , wherein:{'sub': 3', '21', '21, 'Xis CR, wherein Ris halo, nitro, aliphatic carbonyl, or trihalomethyl.'}19. The compound of claim 18 , wherein Ris Cl claim 18 , Br ...

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Номер записи: 44
11-03-2021 дата публикации

COMMERCIALLY VIABLE SYNTHESIS OF CANTHARIDIN AND BIOACTIVE CANTHARIDIN DERIVATIVES

Номер: US20210070771A1
Автор: Davidson Matthew Gene, Schow Steven R.
Принадлежит: Verrica Pharmaceuticals, Inc.

The present disclosure provides methods for synthesizing cantharidin and cantharidin derivatives. 1. A method for generating a cantharidin formulation comprising cantharidin or a cantharidin derivative , the method comprising reacting a precursor of said cantharidin or cantharidin derivative to form said cantharidin formulation having said cantharidin or cantharidin derivative at an exo-to-endo ratio of at least 6:1.28-. (canceled)9. The method of claim 1 , wherein said reacting is conducted at a pressure less than about 100 atm.1012-. (canceled)14. A method for generating a cantharidin formulation comprising cantharidin or a cantharidin derivative claim 1 , the method comprising reacting a precursor of said cantharidin or cantharidin derivative to form said cantharidin formulation having said cantharidin or cantharidin derivative claim 1 , wherein said reacting is conducted (i) in the absence of diethyl ether claim 1 , (ii) in the absence of a lithium or magnesium salt claim 1 , and (iii) at a pressure less than about 980 atmospheres (atm).1521-. (canceled)22. The method of claim 14 , wherein said reacting is conducted with the aid of a catalyst.2324-. (canceled)25. The method of claim 22 , wherein said catalyst comprises bis(cyclopentadienyl)zirconium(IV) bis(trifluoromethanesulfonate)tetrahydrofuran complex.26. The method of claim 22 , wherein said catalyst comprises aluminum chloride.2729-. (canceled)30. A cantharidin formulation comprising (i) cantharidin or a cantharidin derivative claim 22 , (ii) less than 0.1% diethyl ether and (iii) less than 0.1% lithium salt claim 22 , wherein said cantharidin or cantharidin derivative is at an exo-to-endo ratio of at least 6:1.3136-. (canceled)37. A cantharidin formulation comprising (i) cantharidin or a cantharidin derivative and (ii) a Lewis catalyst comprising one or more Lewis metals selected from the group consisting of Li (I) claim 22 , Mg (II) claim 22 , B (III) claim 22 , Al (III) claim 22 , Ti (IV) claim 22 , Zr ...

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Номер записи: 45
23-03-2017 дата публикации

QUATERNARY AMMONIUM ALKYL ESTERS AS STABLE PRODRUGS

Номер: US20170081304A1
Автор: Burk Robert M., Graham Richard S., Im Wha Bin, Lee Mu-Lan, Old David W.
Принадлежит:

Disclosed herein are compounds according to Formulas 1-12, compositions comprising these compounds, and methods of lowering intraocular pressure (IOP) or causing hair growth, and methods of using the same. 3. The compound of claim 1 , wherein Y is unsubstituted morpholino.4. The compound of claim 1 , wherein Het is unsubstituted thienyl.5. The compound of claim 1 , wherein Ph' is unsubstituted phenylene.6. The compound of claim 1 , wherein m is 0.7. The compound of claim 1 , wherein m is 1.8. The compound of claim 1 , wherein x is 0.9. The compound of claim 1 , wherein x is 1.10. The compound of claim 1 , wherein x is 2.11. The compound of claim 1 , wherein x is 3.12. The compound of claim 1 , wherein x is 4.13. The compound of claim 1 , wherein Y is Calkylamino.14. The compound of claim 1 , wherein Y is Ctrialkylammonium.15. The compound of claim 1 , wherein Phis 3 claim 1 ,5-dichlorophenyl.16. The compound of claim 2 , wherein Rand are Cl.17. The compound of claim 1 , wherein claim 1 , if substituents are present claim 1 , each substituent of Ph claim 1 , Ph claim 1 , and Het has a molecular weight of 15 g/mol to 500 g/mol.18. An ophthalmic liquid comprising a compound according to .19. A solid dosage form comprising a compound according to .20. A method of reducing intraocular pressure comprising administering a compound of to a mammal in need thereof.21. A method of growing hair comprising administering a compound of to a mammal in need thereof. This application is a non-provisional application which claims the benefit of U.S. provisional application 61/991,921 entitled “Quaternary Ammonium Alkyl Esters as Stable Prodrugs” filed on May 12, 2014 with docket number 19242PROV (AP) which is incorporated herein by reference in its entirety and serves as the basis for a priority claim for the present application.Ocular hypotensive agents are useful in the treatment of a number of various ocular hypertensive conditions, such as post-surgical and post-laser ...

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Номер записи: 46
31-03-2022 дата публикации

MODULATORS OF TMEM16A FOR TREATING RESPIRATORY DISEASE

Номер: US20220098164A1
Автор: Collingwood Stephen, HARGRAVE Jonathan David, HAY Duncan Alexander, Walker Edward
Принадлежит:

Compounds of general formula (I): 126.-. (canceled)30. The compound according to claim 27 , wherein Y is —CH—.31. The compound according to claim 27 , wherein:{'sup': '4', 'claim-ref': {'@idref': 'CLM-00027', '#text': 'claim 27'}, '#text': 'Ris a 6- to 11-membered aryl group selected from phenyl, naphthyl, indanyl, 1,2,3,4-tetrahydronaphthyl and benzocycloheptanyl, any of which is unsubstituted or substituted as defined in ; or'}{'sup': '4', 'claim-ref': {'@idref': 'CLM-00027', '#text': 'claim 27'}, '#text': 'Ris a 5- to 10-membered heteroaryl group selected from pyridyl, quinolinyl, quinoxalinyl, indazolyl, indolyl, benzoxazolyl, dihydrobenzofuranyl, furyl and thienyl, any of which is unsubstituted or substituted as defined in ; or'}{'sup': '4', 'claim-ref': {'@idref': 'CLM-00027', '#text': 'claim 27'}, '#text': 'Ris a carbocyclyl group selected from cyclohexyl and adamantyl, any of which is unsubstituted or substituted as defined in .'}34. The compound according to claim 32 , wherein:{'sup': ['11a', '11b'], 'sub': ['1-4', '1-4'], '#text': 'the compound is a compound of formula (Iai), (Ibi), (Ici), (Idi), (Iei), (Ifi) or (Igi) and either Ris H, halo, Calkyl or C(O)O(Calkyl) and Ris H; or'}{'sup': ['11a', '11b'], '#text': 'both Rand Rare halo; or'}{'sup': '11a', '#text': 'the compound is a compound of formula (Iaii), (Ibii), (Icii), (Idii), (Ieii), (Ifii) or (Igii) and Ris H; and'}{'sup': '11b', 'sub': ['1-4', '1-4', '1-4'], '#text': 'Ris Calkyl, Calkyl substituted with OH or Chaloalkyl; and'}{'sup': '11c', '#text': 'Ris H, halo, methyl or ethyl.'}36. A pharmaceutical composition comprising a compound according to and a pharmaceutically acceptable excipient.37. A method for the treatment or prophylaxis of diseases and conditions affected by modulation of TMEM16A claim 27 , the method comprising administering to a patient in need of such treatment an effective amount of a compound according to .38. The method of claim 37 , wherein the diseases and conditions affected ...

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Номер записи: 47
12-03-2020 дата публикации

NOVEL WHITENING AGENTS FOR CELLULOSIC SUBSTRATES

Номер: US20200080030A1
Автор: "Morrall Donna DAngelo", Baker Keith Homer, Cummings Michael David, HONG Xiayong Michael, Keiken Laurent D., KOTT Kevin Lee, LOUGHNANE Brian Joseph, Moore Patrick D., SADLOWSKI Eugene Steven, SIVIK Mark Robert, STARKS Leonard J., Torres Eduardo, Valenti Dominick J., VALENTI Michael A.
Принадлежит:

This invention relates to novel whitening agents for cellulosic substrates. The whitening agents are comprised of at least two components: at least one chromophore component and at least one polymeric component. Suitable chromophore components generally fluoresce blue, red, violet, or purple color when exposed to ultraviolet light, or they may absorb light to reflect these same shades. The whitening agents are further characterized by having a dispersion component value of the Hansen Solubility Parameter of less than or equal to about 17 MPa. This invention also relates to laundry care compositions including but not limited to liquid and/or powder laundry detergent formulations and rinse added fabric softening (RAFS) compositions that comprise such whitening agents. 2. The laundry care composition of claim 1 , wherein the whitening agent comprises a polyoxyalkylene chain having from 2 to about 20 repeating units.3. The laundry care composition of claim 1 , wherein the whitening agent comprises at least two hydroxyl groups.4. The laundry care composition of claim 3 , wherein the hydroxyl groups are primary hydroxyl moieties.5. The laundry care composition of claim 1 , wherein the whitening agent comprises an alkoxylated thiophene polymeric colorant.6. The laundry care composition of claim 1 , wherein the whitening agent possesses a dispersion component value of the Hansen Solubility Parameter of less than or equal to about 17 MPa.7. The laundry care composition of claim 6 , wherein the whitening agent possesses a dispersion component value of the Hansen Solubility Parameter from about 12 to about 17 MPa.8. The laundry care composition of claim 1 , wherein the whitening agent's chromophore exhibits an absorbance spectrum in water of from about 520 nanometers to about 640 nanometers.9. The laundry care composition of claim 1 , wherein the whitening agent's chromophore exhibits an emission spectrum in water of from about 400 nanometers to about 480 nanometers.10. A ...

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Номер записи: 48
31-03-2016 дата публикации

RADIOMITIGATING PHARMACEUTICAL FORMULATIONS

Номер: US20160090369A1
Автор: McBride William, Micewicz Ewa
Принадлежит:

The present disclosure relates to compounds of Formula (I) and (II), compositions containing the compounds (alone or in combination with other agents), and their use to prevent, mitigate or treat a) damage induced by ionizing radiation, b) inflammation or c) cancer. 2. A compound of claim 1 , wherein the aryl or heteroaryl group bears at least one substituent including a nitro substitutent.3. The compound of claim 2 , wherein the nitro substituent is disposed at a position on Adistal to the sulfonyl.4. The compound of any preceding claim 1 , wherein Ais a heterocyclic amine.5. The compound of claim 1 , wherein Ais NRR claim 1 , wherein each of Rand R claim 1 , independently claim 1 , is H claim 1 , alkyl claim 1 , alkenyl claim 1 , alkynyl claim 1 , aryl claim 1 , heteroaryl claim 1 , aralkyl claim 1 , or heteroaralkyl claim 1 , provided that Rand Rare not both H.7. The compound of claim 6 , wherein Yand Yare each ethyl.8. The compound of claim 6 , wherein Yand Ytaken together with X form a piperazine ring.10. The compound of claim 9 , wherein G is N and Ris selected from phenyl claim 9 , 4-fluorophenyl and 3-chlorophenyl.11. The compound of claim 9 , wherein Z is absent.12. The compound of claim 9 , wherein Z is prop-2-en-1-yl and Ris phenyl.14. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable excipient or solvent.15. A method of mitigating an effect of ionizing radiation on a cell claim 1 , organ claim 1 , tissue claim 1 , or organism claim 1 , comprising contacting the cell claim 1 , organ claim 1 , tissue claim 1 , or organism with a compound of .16. The method of claim 15 , wherein the compound contacts the cell before claim 15 , during claim 15 , or after exposure to ionizing radiation.17. A method of treating inflammation in an organism claim 1 , comprising administering to the organism a compound of .18. A method of treating cancer in an organism claim 1 , comprising administering to the organism a compound of .19. The ...

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Номер записи: 49
05-05-2022 дата публикации

PRODUCTION METHOD OF THIENOPYRIMIDINE DERIVATIVE

Номер: US20220135585A1
Автор: MIWA Kazuhiro
Принадлежит:

The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.

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Номер записи: 50
19-03-2020 дата публикации

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

Номер: US20200087270A1
Автор: Franchi Luigi, Ghosh Shomir, GLICK Gary, Jr. Anthony William, Katz Jason, Opipari, ROUSH William, SEIDEL Hans Martin, Shen Dong-Ming, VENKATRAMAN SHANKAR, WINKLER David Guenther
Принадлежит:

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: 1122.-. (canceled)127. The compound of claim 123 , wherein the sulfur in the moiety S(═O)(NR)═N— has (R) stereochemistry.128. The compound of claim 123 , wherein the sulfur in the moiety S(═O)(NR)═N— has (S) stereochemistry.129. A pharmaceutical composition comprising a compound as claimed in and one or more pharmaceutically acceptable excipients.130. A method for antagonising NLRP3 activity claim 124 , the method comprising contacting NLRP3 with an effective amount of a compound as claimed in .131. The method of claim 130 , wherein the method comprises administering the compound to a subject having a disease in which NLRP3 signaling contributes to the pathology and/or symptoms and/or progression of the disease.132. The method of claim 131 , wherein the subject is a human.133. A method for antagonising NLRP3 activity claim 125 , the method comprising contacting NLRP3 with an effective amount of a compound as claimed in .134. The method of claim 133 , wherein the method comprises administering the compound to a subject having a disease in which NLRP3 signaling contributes to the pathology and/or symptoms and/or progression of the disease.135. The method of claim 134 , wherein the subject is a human.136. A method for antagonising NLRP3 activity claim 126 , the method comprising contacting NLRP3 with an effective amount of a compound as claimed in .137. The method of claim 136 , wherein the method comprises administering the compound to a subject having a disease in which NLRP3 signaling contributes to the pathology and/or symptoms and/or progression of the disease.138. The method of claim 137 , wherein the subject is a human.139. A method for antagonising NLRP3 activity claim 129 , the method comprising contacting NLRP3 with a pharmaceutical composition as claimed in .140. The method of claim 139 , wherein the method comprises administering the pharmaceutical ...

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Номер записи: 51
30-03-2017 дата публикации

COMPOUND FOR ORGANIC PHOTOELECTRIC DEVICE AND ORGANIC PHOTOELECTRIC DEVICE AND IMAGE SENSOR INCLUDING THE SAME

Номер: US20170092868A1
Автор: BULLIARD Xavier, CHOI Hyesung, Choi Yeong Suk, Han Moon Gyu, IMASE Tatsuya, Jin Yong Wan, LEE Gae Hwang, Lee Kwang Hee, Leem Dong-Seok, Lim Seon-Jeong, SAKURAI Rie, SHIBUYA Hiromasa, Yagi Tadao, Yun Sung Young
Принадлежит: SAMSUNG ELECTRONICS CO., LTD.

A compound for an organic photoelectric device is represented by Chemical Formula 1. An organic photoelectric device includes a first electrode and a second electrode facing each other, and an active layer including the compound represented by Chemical Formula 1 between the first electrode and the second electrode. 2. The compound of claim 1 , wherein at least one of Arand Aris one of a naphthyl group and an anthracenyl group.3. The compound of claim 1 , wherein the compound has a maximum absorption wavelength (λ) of about 500 nm to about 600 nm.4. The compound of claim 1 , wherein the compound has a maximum absorption wavelength (λ) of about 530 nm to about 570 nm.5. The compound of claim 1 , wherein the compound exhibits a light absorption curve having a full width at half maximum (FWHM) in a thin film state of about 50 nm to about 120 nm.6. The compound of claim 7 , wherein the compound exhibits a light absorption curve having a full width at half maximum (FWHM) in a thin film state of about 50 nm to about 110 nm.7. The compound of claim 1 , wherein the compound is a p-type semiconductor compound.9. The organic photoelectric device of claim 8 , wherein the active layer has an absorption coefficient of greater than or equal to about 6×10cmwhen including the compound and Cin a volume ratio of about 0.9:1 to about 1.1:1.10. The organic photoelectric device of claim 8 , wherein the active layer has an absorption coefficient of about 6×10cmto about 6.7×10cmwhen including the compound and Cin a volume ratio of about 0.9:1 to about 1.1:1.11. The organic photoelectric device of claim 8 , wherein the active layer has a maximum absorption wavelength (λ) of about 500 nm to about 600 nm.12. The organic photoelectric device of claim 8 , wherein the active layer has a maximum absorption wavelength (λ) of about 530 nm to about 570 nm.13. The organic photoelectric device of claim 8 , wherein the active layer exhibits a light absorption curve having a full width at half maximum ( ...

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Номер записи: 52
12-05-2022 дата публикации

UREA DERIVATIVE

Номер: US20220144765A1
Автор: Fukunaga Taichi, Matsumoto Koji, NAKAMURA Yuji, Soneda Tsuyoshi, Tanaka Naomi
Принадлежит: Daiichi Sankyo Company, Limited

An object of the present invention is to find a novel pharmaceutical that has an excellent tryptophanase inhibitory effect and suppresses worsening of renal function to preserve the kidney by reducing production of indoxyl sulfate in the blood. The present invention provides a pharmaceutical composition containing, as an active ingredient, a compound represented by the following formula, or a pharmacologically acceptable salt thereof: 5. The compound according to claim 3 , or a pharmacologically acceptable salt thereof claim 3 , wherein Rand Rare the same or different and represent an ethyl group claim 3 , a propyl group or an isopropyl group.6. The compound according to claim 3 , or a pharmacologically acceptable salt thereof claim 3 , wherein Rand Rrepresent a combination of an ethyl group and an ethyl group claim 3 , or an ethyl group and a propyl group.7. The compound according to claim 3 , or a pharmacologically acceptable salt thereof claim 3 , wherein Rand Rboth represent an ethyl group.8. The compound according to claim 4 , or a pharmacologically acceptable salt thereof claim 4 , wherein Rrepresents a hydrogen atom.9. The compound according to claim 4 , or a pharmacologically acceptable salt thereof claim 4 , wherein Rrepresents a trifluoromethyl group claim 4 , a monofluoromethoxy group claim 4 , a difluoromethoxy group claim 4 , a trifluoromethoxy group claim 4 , a trifluoromethylthio group claim 4 , a phenyl group or a 2-fluorophenyl group.10. A pharmaceutical composition comprising claim 3 , as an active ingredient claim 3 , the compound according to claim 3 , or a pharmacologically acceptable salt thereof.11. The pharmaceutical composition according to claim 1 , comprising claim 1 , as an active ingredient claim 1 , a compound selected from the group consisting of:2-ethyl-2-[(phenylcarbamoyl)amino]butanoic acid,2-{[3-(chlorophenyl)carbamoyl]amino}-2-ethylbutanoic acid,2-{[4-(chlorophenyl)carbamoyl]amino}-2-ethylbutanoic acid,2-ethyl-2-{[(4-fluorophenyl) ...

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Номер записи: 53
12-05-2022 дата публикации

2-[Thiophen-2-yl)formamido]-N-(phenyl)-2-methylpropanamide derivatives and the use therof as medicament

Номер: US20220144796A1
Автор: ALLERS Kelly, Klinder Klaus, MUELLER Stephan Georg, MUELLER-VIEIRA Ursula, PAUTSCH Alexander, PRIEPKE Henning
Принадлежит:

The present invention relates to novel 2-[thiophen-2-yl)formamido]-N-(phenyl)-2-methylpropanamides of formula A 8. A pharmaceutically acceptable salt of a compound according to .9. A method for treating and/or preventing a mood disorder or a mood affective disorder claim 1 , comprising administering to a patient in need thereof a therapeutically effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt therefore claim 1 , wherein the mood disorder or mood affective disorder is selected from the group consisting of bipolar disorder I depressed claim 1 , hypomanic claim 1 , manic and mixed form; bipolar disorder II; depressive disorders; major depressive disorder with or without concomitant anxious distress claim 1 , mixed features claim 1 , melancholic features claim 1 , atypical features claim 1 , mood-congruent psychotic features claim 1 , mood-incongruent psychotic features claim 1 , and catatonia.10. The method according to wherein the depressive disorder is selected from the group consisting of single depressive episode disorder claim 9 , recurrent major depressive disorder claim 9 , minor depressive disorder claim 9 , depressive disorder with postpartum onset claim 9 , and depressive disorders with psychotic symptoms.11. The method according to claim 9 , wherein the compound is administered in addition to treatment with another antidepressant drug.12. The method according to claim 9 , wherein the compound is administered in addition to behavioural therapy.13. A pharmaceutical composition comprising the compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , in admixture with a pharmaceutically acceptable adjuvant claim 1 , diluent and/or carrier. The present invention relates to novel 2-[thiophen-2-yl)formamido]-N-(phenyl)-2-methylpropanamides of formula Aprocesses for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment or ...

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Номер записи: 54
28-03-2019 дата публикации

DIHETERO AMINES IN ELECTRICALLY CONDUCTIVE POLYMER COMPOSITIONS

Номер: US20190097137A1
Автор: RADU NORA SABINA, Zoombelt Arjan
Принадлежит:

Disclosed are electrically conductive polymer compositions, and their use in organic electronic devices. The electrically conductive polymer compositions include an intrinsically electrically conductive polymer having Formula II: 110.-. (canceled)13. The compound of claim 11 , wherein y=z=0.15. The compound of claim 11 , wherein Q=S.18. The polymer of claim 16 , wherein the polymer is a homopolymer.19. The polymer of claim 16 , wherein o=10-2000.20. The polymer of claim 16 , wherein Q=S.22. The composition of claim 21 , further comprising a fluorinated acid polymer.23. The composition of claim 21 , wherein the dihetero amine polymer is a homopolymer.24. An aqueous dispersion of the composition of .26. The composition of claim 21 , wherein Q=S.27. An electronic device comprising at least one buffer layer comprising the polymer composition of .28. An electronic device comprising at least one buffer layer comprising the polymer composition of . This application claims the benefit of U.S. Provisional Application No. 62/342,383, filed May 27, 2016, which is incorporated in its entirety herein by reference.This disclosure relates in general to dihetero amine compounds, dihetero amine polymers, electrically conductive polymer compositions containing dihetero amine polymers, and the use of such materials in organic electronic devices.Organic electronic devices define a category of products that include an active layer. Such devices convert electrical energy into radiation, detect signals through electronic processes, convert radiation into electrical energy, or include one or more organic semiconductor layers.Organic light-emitting diodes (OLEDs) are an organic electronic device comprising an organic layer capable of electroluminescence. OLEDs containing electrically conducting polymers can have the following configuration:The anode is typically any material that is transparent and has the ability to inject holes into the EL material, such as, for example, indium/tin oxide ...

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Номер записи: 55
28-04-2016 дата публикации

SULPHAMOYLTHIOPHENAMIDE DERIVATIVES AND THE USE THEREOF AS MEDICAMENTS FOR THE TREATMENT OF HEPATITIS B

Номер: US20160115149A1
Автор: Haché Geerwin Yvonne Paul, Last Stefaan Julien, Raboisson Pierre Jean-Marie Bernard, Vandyck Koen, Verschueren Wim Gaston
Принадлежит: JANSSEN SCIENCES IRELAND UC

Inhibitors of HBV replication of formula (I) 2. A compound according to claim 1 , wherein Ris fluoro or methyl.4. A compound according to wherein at least two of R claim 1 , Rand Rare each halogen.5. A compound according to wherein Ris methyl and Ris fluoro.6. A compound according to wherein Ris a 3-7 membered saturated ring optionally containing one oxygen.7. A compound according to wherein Ris a 4 or 5 membered saturated ring containing one oxygen.8. A compound according to wherein Ris a branched C-Calkyl optionally substituted with one or more fluoro.9. A method of treating HBV infection comprising administering a therapeutically effective amount of at least one compound of .10. A pharmaceutical composition comprising a compound according to claim 1 , and a pharmaceutically acceptable carrier.11. A product containing (a) a compound of claim 1 , and (b) at least one HBV inhibitor claim 1 , as a combined preparation for simultaneous claim 1 , separate or sequential use in the treatment of HBV infections.12. A compound according to claim 1 , selected from the group consisting of:N-(4-fluoro-3-methyl-phenyl)-5-[[(3S)-tetrahydrofuran-3-yl]sulfamoyl]thiophene-3-carboxamide;2-bromo-N-(4-fluoro-3-methyl-phenyl)-5-[[(3S)-tetrahydrofuran-3-yl]sulfamoyl]thiophene-3-carboxamide;2-chloro-N-(4-fluoro-3-methyl-phenyl)-5-[[(1R)-2-hydroxy-1-methyl-ethyl]sulfamoyl]thiophene-3-carboxamide;2-chloro-N-(4-fluoro-3-methyl-phenyl)-5-[[(3S)-tetrahydrofuran-3-yl]sulfamoyl]thiophene-3-carboxamide;N-(4-fluoro-3-methyl-phenyl)-5-[[(3S)-tetrahydrofuran-3-yl]sulfamoyl]-2-(trifluoromethyl)thiophene-3-carboxamide;2-cyclopropyl-N-(4-fluoro-3-methyl-phenyl)-5-[[(3S)-tetrahydrofuran-3-yl]sulfamoyl]thiophene-3-carboxamide;N-(4-fluoro-3-methyl-phenyl)-2-methyl-5-[[(3S)-tetrahydrofuran-3-yl]sulfamoyl]thiophene-3-carboxamide;N-(4-fluoro-3-methyl-phenyl)-4-[[(3S)-tetrahydrofuran-3-yl]sulfamoyl]thiophene-2-carboxamide;N-(4-fluoro-3-methyl-phenyl)-5-methyl-4-[[(3S)-tetrahydrofuran-3-yl]sulfamoyl]thiophene ...

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Номер записи: 56
10-07-2014 дата публикации

N-HYDROXYLSULFONAMIDE DERIVATIVES AS NEW PHYSIOLOGICALLY USEFUL NITROXYL DONORS

Номер: US20140194416A1
Автор: BROOKFIELD Frederick Arthur, Cohen Andrew D., COURTNEY Stephen Martin, FROST Lisa Marie, KALISH Vincent Jacob, Toscano John P.
Принадлежит:

The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives. 2. The compound of claim 1 , wherein Ris H.3. The compound of claim 1 , wherein x and y are both 1.4. The compound of claim 1 , wherein the compound is of the formula (I).5. The compound of wherein the compound is of the formula (I) and at least one of Rand Ris other than H.6. The compound of claim 4 , wherein the compound is of the formula (I) and at least one of Rand Ris an electron withdrawing group.7. The compound of claim 4 , wherein the compound is of the formula (I) and at least one of R claim 4 , R claim 4 , R claim 4 , Rand Ris carboxyl claim 4 , —COO-alkyl claim 4 , —C(O)NH claim 4 , —C(O)NRRwhere Ris hydrogen and Ris alkyl claim 4 , —C(O)NRRwhere Rand Rare independently alkyl claim 4 , —C(O)NRRwhere Rand Rare taken together with the nitrogen to which they are attached to form a heterocyclic or substituted heterocyclic ring claim 4 , —SONH claim 4 , —SONR-alkyl where R is hydrogen claim 4 , —SONR-alkyl where R is alkyl claim 4 , —SONR claim 4 , where the two R groups are taken together with the nitrogen to which they are attached to form a heterocyclic or substituted heterocyclic ring.8. The compound of claim 1 , wherein the compound is of the formula (II).9. The compound of claim 1 , wherein the compound is of the formula (III).10. A method of modulating the in vivo nitroxyl levels in an individual in need thereof claim 1 , the method comprising administering to the individual an N-hydroxysulfonamide of or ...

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Номер записи: 57
30-04-2015 дата публикации

THERAPEUTIC CYCLOPENTANOLS, COMPOSITIONS THEREOF, AND METHODS FOR USE THEREOF

Номер: US20150119454A1
Автор: Burk Robert M., Gac Todd S.
Принадлежит:

Described herein are well-defined cyclopentanols useful for treating glaucoma and ocular hypertension. 2. The compound of wherein X is halogen.3. The compound of wherein X is Cl.4. The compound of wherein L is C-Calkylene.5. The compound of wherein L is Calkylene.6. The compound of wherein A is Cto Calkyl.7. The compound of wherein A is Calkyl.8. The compound of wherein R is Cto Calkyl bearing at least one hydroxyl substituent.9. The compound of wherein R is Cto Calkyl bearing multiple hydroxyl substituents.10. The compound of wherein R is H or Cto Calkyl.11. The compound of wherein R is H.12. The compound of wherein Ris H or Cto Calkyl.13. The compound of wherein Ris H.14. The compound of wherein R is —CHCHN(R).15. The compound of wherein R is ethlymorpholino.17. A composition comprising at least one compound according to claim 1 , wherein the composition is a liquid which is ophthalmically acceptable.18. A method of treating glaucoma or ocular hypertension comprising administering to a subject in need thereof a therapeutically effective amount of a compound according to .19. The method of wherein the subject is human.20. A kit comprising the composition of claim 17 , a container claim 17 , and instructions for administration of the composition to a subject in need thereof for the treatment of glaucoma or ocular hypertension. This application is a non-provisional application claiming the benefit of U.S. provisional application 61/896,970 filed on Oct. 29, 2013, and U.S. 61/896,979 filed on Oct. 29, 2013, each of which is incorporated by reference in their entirety and serve as the basis for a priority claim of the present application.The present invention relates generally to compounds and methods for treating ocular disorders. The invention relates specifically to the use of certain well-defined cyclopentanols for the treatment of ocular hypertension and glaucoma.Ocular hypotensive agents are useful in the treatment of a number of various ocular hypertensive ...

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Номер записи: 58
07-05-2015 дата публикации

IMPROVED PROCESS FOR PREPARING RIVAROXABAN USING NOVEL INTERMEDIATES

Номер: US20150126733A1
Автор: Buthukuri Venkat Reddy, Dodda Mohan Rao
Принадлежит: SYMED LABS LIMITED

The present inventors have surprisingly found that rivaroxaban of formula I can be prepared in a one-pot process, in high purity and with high yield, by reacting 5-chlorothiophene-2-carboxylic acid or a salt thereof with a sulfonylating agent to produce a sulfonyl ester intermediate, which is then condensed with 4-[4-[(SS)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl]morjJholine-3-one or an acid addition salt thereof to produce rivaroxaban. 2. The process of claim 1 , wherein the group ‘R’ in the compounds of formulae III claim 1 , Va and Vb is selected from the group consisting of methyl claim 1 , ethyl claim 1 , propyl claim 1 , isopropyl claim 1 , isobutyl claim 1 , chloromethyl claim 1 , fluoromethyl claim 1 , trifluoromethyl claim 1 , phenyl claim 1 , p-tolyl claim 1 , benzyl claim 1 , 4-nitrophenyl claim 1 , 4-chlorophenyl claim 1 , 3-nitrophenyl and 4-chlorobenzyl.3. The process of claim 2 , wherein the group ‘R’ in the compounds of formulae III claim 2 , Va and Vb is methyl or p-tolyl.4. The process of claim 1 , wherein the one-pot process is carried out in the presence of a solvent or a mixture of solvents.5. The process of claim 4 , wherein the solvent is selected from the group consisting of a chlorinated hydrocarbon claim 4 , an ester claim 4 , a cyclic ether claim 4 , an aliphatic ether claim 4 , a hydrocarbon claim 4 , a polar aprotic solvent claim 4 , a nitrile claim 4 , an alcohol claim 4 , and mixtures thereof.6. The process of claim 5 , wherein the solvent is selected from the group consisting of dichloromethane claim 5 , dichloroethane claim 5 , chloroform claim 5 , carbon tetrachloride claim 5 , ethyl acetate claim 5 , methyl acetate claim 5 , isopropyl acetate claim 5 , tert-butyl methyl acetate claim 5 , ethyl formate claim 5 , tetrahydrofuran claim 5 , 2-methyl tetrahydrofuran claim 5 , dioxane claim 5 , diethyl ether claim 5 , diisopropyl ether claim 5 , methyl tert-butyl ether claim 5 , monoglyme claim 5 , diglyme claim 5 , n-pentane ...

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Номер записи: 59
05-05-2016 дата публикации

COMPOUND FOR ORGANIC PHOTOELECTRIC DEVICE AND ORGANIC PHOTOELECTRIC DEVICE, IMAGE SENSOR, AND ELECTRONIC DEVICE INCLUDING THE SAME

Номер: US20160126470A1
Автор: Han Moon Gyu, HEO Chuljoon, Jin Yong Wan, LEE Gae Hwang, Leem Dong-Seok, Lim Seon-Jeong, Park Kyung Bae, RO Takkyun, TADAO Yagi, Yun Sung Young
Принадлежит:

A compound for an organic photoelectric device is represented by Chemical Formula 1. An organic photoelectric device includes a first electrode and a second electrode facing each other and an active layer between the first electrode and the second electrode, the active layer including the compound represented by Chemical Formula 1. 6. The compound of claim 1 , wherein the compound has a maximum absorption wavelength (λ) of about 530 nm to about 570 nm in a thin film state.7. The compound of claim 1 , wherein the compound shows a light absorption curve having a full width at half maximum (FWHM) of about 50 nm to about 100 nm in a thin film state.8. The compound of claim 1 , wherein the compound is a p-type semiconductor compound.10. The compound of claim 9 , wherein the compound shows a light absorption curve having a full width at half maximum (FWHM) of about 50 nm to about 100 nm in a thin film state.11. An organic photoelectric device comprisinga first electrode and a second electrode facing each other, and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'an active layer between the first electrode and the second electrode, the active layer including the compound of .'}12. The organic photoelectric device of claim 11 , wherein the active layer further comprises an n-type semiconductor compound.13. The organic photoelectric device of claim 12 , wherein the n-type semiconductor compound is one of sub-phthalocyanine claim 12 , fullerene or a fullerene derivative claim 12 , thiophene or a thiophene derivative claim 12 , and a combination thereof.14. The organic photoelectric device of claim 12 , wherein the active layer comprises an intrinsic layer including the compound represented by Chemical Formula 1.15. The organic photoelectric device of claim 14 , wherein the active layer further comprises at least one of a p-type layer on one side of the intrinsic layer and an n-type layer on the other side of the intrinsic layer.16. The organic photoelectric device of claim ...

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Номер записи: 60
25-04-2019 дата публикации

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

Номер: US20190119224A1
Автор: Ghosh Shomir, GLICK Gary, ROUSH William R.
Принадлежит:

In one aspect, compounds of Formulae (I) and (II), or pharmaceutically acceptable salts thereof, are featured; Formula (I), Formula (II) or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formulae (I) and (II) can be as defined anywhere herein. 4. The compound of claim 3 , wherein Xis CR.60. The compound of claim 5 , wherein R is 1-hydroxycyclopropyl and R is H.8. The compound of any one of or claim 5 , wherein R is H.10. The compound of any one of or - claim 5 , wherein R and R taken together with the carbons connecting them form a four-membered to seven-membered ring A claim 5 , and R and R taken together with the carbons connecting them form a four-membered to seven-membered ring B.11. The compound of any one of or - claim 5 , wherein R is CN.16. The compound of any one of or claim 5 , wherein R is C(R)OH.17. The compound of any one of claim 5 , claim 5 , or claim 5 , wherein R is H.19. The compound of any one of or claim 5 , wherein Ris C(R)OH.20. The compound of any one of or claim 5 , wherein Ris H.21. The compound of any one of or - claim 5 , wherein R is C-Calkyl substituted with hydroxy.22. The compound of any one of or - claim 5 , wherein R is 1-hydroxy-1-cyclopropyl.23. The compound of any one of or - claim 5 , wherein R is Cl.25. The compound of any one of or claim 5 , wherein R is C(R)OH.27. The compound of any one of or claim 5 , wherein R is C(R)OH and Ris H.29. The compound of any one of or claim 5 , wherein Ris H and R is C-Ccycloalkyl substituted with hydroxy.32. The compound of any one of or claim 5 , wherein Ris H and Ris C-Calkyl substituted with hydroxy.33. The compound of any one of or claim 5 , wherein Ris C(R)OH and Ris H.35. The compound of any one of claim 5 , claim 5 , or claim 5 , wherein Ris H and Ris C-Calkyl substituted with hydroxyl.36. The compound of any one of claim 5 , claim 5 , or claim 5 , wherein Ris H and Ris C-Calkyl substituted with hydroxyl.37. The compound of any one of - claim 5 , wherein Ris H ...

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Номер записи: 61
25-04-2019 дата публикации

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

Номер: US20190119241A1
Автор: Ghosh Shomir, GLICK Gary, ROUSH William R., Shen Dong-Ming
Принадлежит:

In one aspect, compounds of Formula A, or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein. 10. The compound of claim 9 , wherein Xis N; and Xis S.13. The compound of claim 12 , wherein Xis S; and Xis CH.32. The compound of any one of claim 12 , claim 12 , or claim 12 , wherein Xis CR.33. The compound of any one of claim 12 , claim 12 , claim 12 , claim 12 , claim 12 , claim 12 , or claim 12 , wherein Ris 2-hydroxy-2-propyl.34. The compound of any one of claim 12 , claim 12 , claim 12 , claim 12 , claim 12 , claim 12 , or claim 12 , wherein Ris 1-hydroxy-1-cyclopropyl.35. The compound of any one of claim 12 , claim 12 , claim 12 , claim 12 , claim 12 , claim 12 , or claim 12 , wherein Ris dimethylaminomethyl.36. The compound of any one of claim 12 , claim 12 , claim 12 , claim 12 , claim 12 , claim 12 , or claim 12 , wherein Ris S(O)CH.37. The compound of any one of claim 12 , claim 12 , or claim 12 , wherein Xis CR.38. The compound of any one of claim 12 , claim 12 , or claim 12 , claim 12 , claim 12 , claim 12 , or claim 12 , wherein Ris 2-hydroxy-2-propyl.39. The compound of any one of claim 12 , claim 12 , or claim 12 , claim 12 , claim 12 , claim 12 , or claim 12 , wherein Ris 1-hydroxy-1-cyclopropyl.40. The compound of any one of claim 12 , claim 12 , or claim 12 , claim 12 , claim 12 , claim 12 , or claim 12 , wherein Ris dimethylaminomethyl.41. The compound of any one of claim 12 , claim 12 , or claim 12 , claim 12 , claim 12 , claim 12 , or claim 12 , wherein Ris S(O)CH.42. The compound of any one of claim 12 , claim 12 , or claim 12 , wherein Xis NR.43. The compound of claim 42 , wherein Ris isopropyl.44. The compound of claim 42 , wherein Ris methyl.45. The compound of claim 42 , wherein Ris benzyl.46. The compound of claim 42 , wherein Ris phenyl.47. The compound of any one of claim 42 , claim 42 , or claim 42 , wherein Xis CR.48. The compound of any one of claim 42 , claim 42 , claim ...

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Номер записи: 62
01-09-2022 дата публикации

SUBSTITUTED THIOPHENE CARBOXAMIDES AND DERIVATIVES THEREOF AS MICROBICIDES

Номер: US20220274945A1
Автор: Bernier David, BRUNET Stephane, DUFOUR Jérémy, KNOBLOCH Thomas, NICOLAS Lionel, TSUCHIYA Tomoki
Принадлежит: Bayer Aktiengesellschaft

The present disclosure relates to substituted thiophene carboxamide derivatives of formula (I), their use for controlling phytopathogenic microorganisms and compositions comprising thereof. 2: The compound of claim 1 , wherein Rare chlorine atoms.3: The compound of claim 1 , wherein Rare bromine atoms.4: The compound of claim 1 , wherein Ris selected from the group consisting of fluorine atom claim 1 , chlorine atom and bromine atom.5: The compound of claim 1 , wherein Rare different from R.6: The compound of claim 1 , wherein Rare chlorine atoms and Ris a bromine atom.7: The compound of claim 1 , wherein Ris selected from the group consisting of hydrogen atom claim 1 , C-C-alkyl claim 1 , C-C-haloalkyl claim 1 , C-C-cyanoalkyl claim 1 , C-C-alkenyl claim 1 , C-C-alkynyl claim 1 , C-C-cycloalkyl claim 1 , aralkyl and —C-C-alkyl-cyclopropyl.9: The method of claim 8 , wherein R are chlorine atoms.10: The method of claim 8 , wherein Rare bromine atoms.11: The method of claim 8 , wherein Ris selected from the group consisting of fluorine atom claim 8 , chlorine atom and bromine atom.12: The method of claim 8 , wherein Rare different from R.13: The method of claim 8 , wherein Rare chlorine atoms and Ris selected from the group consisting of fluorine atom and chlorine atom.14: The method of claim 8 , wherein Rare chlorine atoms and Ris a bromine atom.15: The method of claim 8 , wherein Ris selected from the group consisting of hydrogen atom claim 8 , C-C-alkyl claim 8 , C-C-haloalkyl claim 8 , C-C-cyanoalkyl claim 8 , C-C-alkenyl claim 8 , C-C-alkynyl claim 8 , C-C-cycloalkyl claim 8 , aryl claim 8 , heteroaryl claim 8 , aralkyl claim 8 , —C-C-alkyl-heteroaryl claim 8 , 4- claim 8 , 5- or 6-membered heterocyclyl claim 8 , —C-C-alkyl-Si(C-C-alkyl)and —C-C-alkyl-cyclopropyl.20: A composition comprising at least one compound of formula (I) according to and at least one agriculturally suitable carrier.21: The compound of claim 1 , wherein Ris selected from the group ...

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Номер записи: 63
08-09-2022 дата публикации

"TRPswitch" - A STEP FUNCTION CHEMO-OPTOGENETIC LIGAND

Номер: US20220280644A1
Автор: FUCHTER Matthew J., Lam Pui Ying, Peterson Randall Theodore, Thawani Aditya Raymond
Принадлежит:

Described herein are photoswitchable compounds that can activate TRPA1 channels in neuronal and non-neuronal cells. The TRPswitch molecules allow for optical control of both the activation and deactivation of TRPA1 channels. Such compounds can be used as research tools or therapeutics. 3. The compound of claim 1 , wherein each X is independently O or S and{'sub': 1', '1', 'n, 'R is a mono- or bi-cyclic aryl ring or a 5-10 membered mono or bi-cyclic heteroaryl ring optionally substituted with one or more of Q-(R);'}{'sub': 1', '3', '2', '2', 'm', '1-6', '1-6', '1-6', '1-6', '1-6', '2', '3', '3', '4', '3', '4', '2', '3', '4', '3', '4', '2', '3', '3', '2', '4', '2', '3', '4', '3', '3', '3', '2', '4', '2', '2', '3', '4', '2', '3', '1-6', '2-6', '1-6, 'Qis a covalent bond, H, O, halogen, cyano, —NR—, —CONR—, —NRCO—, oxo, nitro, —S(O), —Chaloalkyl, —Calkoxy, —Chaloalkoxy, —Chydroxyalkyl, —Ccyanoalkyl, —CO—, —SOR, —NRR, —NRCOR, —NRCONRR, —CONRR, —COR, —NRCOR, —SONRR, —CONR, —C(O)R, —NRSOR, —NRSONRR, —SONR, optionally substituted —Calkylene, optionally substituted —Calkenylene, or optionally substituted —Calkyl;'}{'sub': 1', '1-6', '1-6', '1-6', '1-6', '2-6', '2-6', '1', '6', '2', '5', '6', '7', '2', '5', '6', '2', '5', '6', '2', '5', '2', '2', '5', '2', '5', '2', '5', '6', '2', '2', '5', '2', '2', '5', '6', '2', '5', '2', '6', '2', '5', '2', '6', '7, 'Ris halogen, oxo, cyano, nitro, optionally substituted —Chaloalkyl, optionally substituted —Calkoxy, optionally substituted —Chaloalkoxy, optionally substituted —Calkyl, optionally substituted —Calkenyl, optionally substituted —Calkynyl, C-Chydroxyalkyl, optionally substituted heterocyclyl, optionally substituted cycloalkyl, optionally substituted heteroaryl, optionally substituted aryl, -Q-NRCONRR, -Q-NRR, -Q-NRCOR, -Q-COR, -Q-SOR, -Q-CONR, -Q-CONRR, -Q-COR, -Q-SONRR, -Q-NRSOR, or -Q-NRSONRR;'}{'sub': 2', '1-6', '1-6', '2-6, 'Qis a covalent bond, —Calkyl, —Calkylene, or —Calkenylene;'}{'sub': 2', '3', '4', '1-6', '1-6, 'R, R ...

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Номер записи: 64
26-05-2016 дата публикации

DUAL SITE CATALYST FOR MILD, SELECTIVE NITRILE REDUCTION

Номер: US20160145193A1
Автор: LU ZHIYAO, Williams Travis J.
Принадлежит:

A ruthenium bis(pyrazolyl)borate scaffold that enables cooperative reduction reactivity in which boron and ruthenium centers work in concert to effect selective nitrile reduction is provided. The pre-catalyst compound [κ-(1-pz)HB(N═CHCH)]Ru(cymene) TfO (pz=pyrazolyl) was synthesized using readily-available materials through a straightforward route, thus making it an appealing catalyst for a number of reactions.

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Номер записи: 65
02-06-2016 дата публикации

Thiophene-2-carboximidamide Based Selective Neuronal Nitric Oxide Synthase Inhibitors

Номер: US20160152590A1
Автор: Huang He, Jing Qing, Silverman Richard B.
Принадлежит:

Selective neuronal nitric oxide synthase (nNOS) inhibitor compounds designed with one or more thiophene-2-carboximidamide substituents for improved bioavailability. 2. The compound of wherein said phenyl moiety is meta-substituted.8. The compound of wherein L is selected from said CHCHand CH(OH)CH(OH) moieties.11. The compound of wherein each said X is O.12. The compound of wherein each said n and n′ is 0.13. The compound of wherein each said R is a thiophene-2-carboximidamide-substituted phenyl moiety.14. The compound of wherein each said compound is a trans stereoisomer.15. The compound of wherein each said n and n′ is 1.16. The compound of wherein each said R is a thiophene-2-carboximidamide-substituted phenyl moiety.17. The compound of selected from cis and trans stereoisomers. This application is a divisional of and claims priority to and the benefit of application Ser. No. 14/285,927 filed May 23, 2014 and issued as U.S. Pat. No. 9,242,957 on Jan. 26, 2016, which was a continuation of and claimed priority to and the benefit of application Ser. No. 14/015,551 filed Aug. 30, 2013 and issued as U.S. Pat. No. 8,735,606 on May 27, 2014, which claimed priority to and the benefit of application Ser. No. 61/695,187 filed Aug. 30, 2012, Application Ser. No. 61/698,249 filed Sep. 7, 2012 and application Ser. No. 61/774,926 filed Mar. 8, 2013—each of which is incorporated herein by reference in its entirety.This invention was made with government support under GM049725 awarded by the National Institutes of Health. The government has certain rights in the invention.Neuronal nitric oxide synthase (nNOS) catalyzes the oxidation of L-arginine to L-citrulline in the central nervous system, generating nitric oxide (NO), a critical neurotransmitter. Significant research has implicated the overexpression of nNOS—and overproduction of NO—in various neurological diseases, including Parkinson's, Alzheimer's, and Huntington's diseases, as well as neuronal damage due to stroke, ...

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Номер записи: 66
21-08-2014 дата публикации

2-HYDROXYHIPPURIC ACID ANALOGS, AND METHODS FOR THEIR SYNTHESIS AND USE

Номер: US20140234365A1
Автор: BANASZCZYK Mariusz
Принадлежит: ALERE SAN DIEGO, INC.

The present invention relates to novel 2-hydroxyhippuric acid analogs, and methods for their synthesis and use. Such analogs are designed to provide a protected or functional moiety such as a free thiol (—SH) group or a protected thiol group, thereby providing a convenient linkage chemistry for coupling under mild conditions to a suitable group on a target protein, polypeptide, solid phase or detectable label. 3. A compound or salt thereof according to claim 2 , wherein R1 is a thiolactone claim 2 , disulfide or a thioester.4. A compound or salt thereof according to claim 2 , wherein R 1 is a thiolactone having 5 ring members.5. A compound or salt thereof according to claim 2 , wherein X is —C(O)— claim 2 , Y is N(H)—Calkyl and Z is a thiolactone.6. A compound or salt thereof according to claim 2 , wherein R1 has the structure —CHC(O)N(H)—Z.7. A compound or salt thereof according to claim 2 , wherein Z is an alkyl thiol.9. A dimeric compound comprising two compounds according to claim 2 , wherein the dimeric compound is formed by disulfide bonding of the thiol or protected thiol in two compounds.11. A conjugate comprising one or more compounds according to covalently bound to a protein claim 1 , polypeptide claim 1 , detectable label claim 1 , nucleic acid claim 1 , or solid phase.12. A conjugate according to claim 11 , wherein the functional moiety is a sulfhydryl-reactive moiety selected from the group consisting of a maleimide claim 11 , an alkyl halide claim 11 , an aryl halide claim 11 , an alpha-haloacyl claim 11 , and a pyridyl disulfide.14. A conjugate according to claim 12 , wherein said detectable label is selected from the group consisting of an enzyme claim 12 , a fluorophore claim 12 , biotin claim 12 , avidin claim 12 , streptavidin claim 12 , digoxigenin claim 12 , maltose claim 12 , oligohistidine claim 12 , 2 claim 12 ,4-dintrobenzene claim 12 , phenylarsenate claim 12 , and a fluorescent latex particle claim 12 , nanogold particle.15. A conjugate ...

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Номер записи: 67
21-08-2014 дата публикации

Compositions and Methods for the Treatment of Norovirus Infection

Номер: US20140235683A1
Автор: Beigelman Leo, Kao C. Cheng, Smith Dave, Subba-Reddy Ch. V.
Принадлежит:

Compositions and methods for the treatment of norovirus infection are disclosed. 1. A method for the treatment of norovirus infection associated with clinical pathology in a patient in need thereof comprising administration of an effective amount of VX-222 or a pharmaceutical salt or prodrug thereof , said VX-222 being effective to inhibit norovirus RNA polymerase activity.3. A norovirus RNA polymerase inhibitor as claimed in selected from the group of compounds shown in .4. A norovirus RNA polymerase inhibitor as claimed in claim 2 , wherein Ris selected from the group consisting of a carbonyl claim 2 , a carboxylic acid claim 2 , a carboxylate ester claim 2 , a carboxyl claim 2 , an amide claim 2 , and aldehyde group.5. A pharmaceutical composition comprising at least one of the compounds of or or a pharmaceutically acceptable salt or prodrug thereof and one or more pharmaceutically acceptable excipients.6. A method for treating a viral infection in a subject in need thereof comprising administering an effective amount of the compound of or or a pharmaceutically acceptable salt thereof to the subject claim 2 , wherein said viral infection is a norovirus infection.7. A method for identifying agents which modulate norovirus RNA polymerase activity associated with clinical pathology comprising:a) incubating cells expressing said viral RNA polymerase and at least one innate immune receptor and a reporter gene operably linked to an interferon beta promoter in the presence and absence of a test agent, wherein in synthesis of viral RNA from said RNA polymerase triggers a cellular defense response which is effective to activate expression of said reporter gene; andb) measuring reporter gene expression in the presence and absence of said agent, alterations of said reporter gene expression in the presence of said agent being indicative of RNA polymerase modulatory activity.8. The method of claim 7 , wherein said innate immune receptor is selected from the group consisting ...

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Номер записи: 68
21-08-2014 дата публикации

SMALL MOLECULE INHIBITORS OF MCL-1 AND THE USES OF THEREOF

Номер: US20140235702A1
Автор: Abulwerdi Fardokht, Liao Chenzhong, Mohammad Ramzi, Nikolovska-Coleska Zaneta, Showalter Hollis D.
Принадлежит:

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having sulfonamido-1-hydroxynaphthalene structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases. 132.-. (canceled)40. A method of treating claim 33 , ameliorating claim 33 , or preventing a hyperproliferative disease in a patient comprising administering to said patient a therapeutically effective amount of a pharmaceutical composition comprising a compound recited in .41. The method of claim 40 , wherein said cancer is multiple myeloma and/or pancreatic cancer.42. The method of claim 40 , further comprising administering to said patient one or more anticancer agents claim 40 , wherein said one or more anticancer agents are selected from the group consisting of a chemotherapeutic agent and radiation therapy.43. The method of claim 40 , wherein said compound is capable of binding with Mcl-1 protein.44. The method of claim 43 , wherein said compound binds the BH3 groove within Mcl-1.45. The method of claim 44 , wherein said binding results in inhibited Mcl-1 protein activity.47. A kit comprising a compound recited in and instructions for administering said compound to a patient having a hyperproliferative disease.48. The kit of wherein said hyperproliferative disease is cancer.49. The kit of claim 48 , wherein said cancer is pancreatic cancer.50. The kit of further comprising one or more anticancer agents.51. The kit of claim 50 , wherein said compound is to be administered together with one or more anticancer agents. The present application claims priority to pending U.S. Provisional Patent Application No. 61/544,133, filed Oct. 6, 2011, the contents of which are incorporated by reference in its entirety.This invention was made with government support under Grant Nos. CA149442 and CA158976 awarded by the National Institutes of Health. The government has certain ...

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Номер записи: 69
21-08-2014 дата публикации

THIOPHENE COMPOUNDS

Номер: US20140235704A1
Автор: Luisi Brian
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

A co-crystal of Compound (1) includes Compound (1) and a co-crystal former selected from the group consisting of urea, nicotinamide, and isonicotinamide, wherein Compound (1) is characterized by the following structural formula: 2. The co-crystal of claim 1 , wherein the co-crystal former is urea.3. The co-crystal of claim 2 , characterized as having an X-ray powder diffraction pattern with characteristic peaks expressed in 2-theta±0.2 at the following positions: 18.4 claim 2 , 12.1 claim 2 , 15.6 claim 2 , 20.1 claim 2 , 10.8 claim 2 , and 11.7 claim 2 , wherein the X-ray powder diffraction pattern is obtained at room temperature using Cu K alpha radiation.4. The co-crystal of claim 2 , wherein the X-ray powder diffraction pattern includes characteristic peaks expressed in 2-theta±0.2 at the following positions with relative intensities in parentheses: 18.4 (100.0%) claim 2 , 12.1 (69.1%) claim 2 , 15.6 (65.0%) claim 2 , 20.1 (52.6%) claim 2 , 10.8 (46.5%) claim 2 , and 11.7 (44.1%).5. The co-crystal of claim 2 , characterized as having an endothermic peak in differential scanning calorimetry (DSC) at 190±2° C.6. The co-crystal of claim 2 , characterized as having X-ray powder diffraction pattern substantially the same as that shown in .7. The co-crystal of claim 1 , wherein the co-crystal former is nicotinamide.8. The co-crystal of claim 7 , characterized as having an X-ray powder diffraction pattern with characteristic peaks expressed in 2-theta±0.2 at the following positions: 21.7 and 15.5 claim 7 , wherein the X-ray powder diffraction pattern is obtained at room temperature using Cu K alpha radiation.9. The co-crystal of claim 8 , characterized as having an X-ray powder diffraction pattern with characteristic peaks expressed in 2-theta±0.2 at the following positions: 21.7 claim 8 , 10.2 claim 8 , 18.9 claim 8 , 17.8 claim 8 , 22.9 claim 8 , and 15.5 claim 8 , wherein the X-ray powder diffraction pattern is obtained at room temperature using Cu K alpha radiation ...

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Номер записи: 70
08-06-2017 дата публикации

HALOGEN-SUBSTITUTED HETEROCYCLIC COMPOUND SALT

Номер: US20170158663A1
Автор: ITO Masaaki, Iwase Noriaki, Kimura Tomio, Kono Shigeyuki, MATOYAMA Masaaki, MATSUNAGA Hirofumi, Nishida Hiroshi, NISHIKAWA Kenji, Okanari Eiji, OKUDO Makoto, USHIYAMA Shigeru
Принадлежит: UBE INDUSTRIES, LTD.

The invention provides a novel α-halogen-substituted thiophene compound salt that has a potent LPA receptor antagonistic action and is useful as a medicament. The salt is represented by the general formula (I): 2. The salt according to claim 1 , wherein the alkali metal or the alkaline earth metal is sodium claim 1 , potassium or calcium.3. A salt of (R)-1-[4′-(5-chloro-3-{[(1-phenylethoxy)carbonyl]amino}thiophen-2-yl)-2′-methoxy[1 claim 1 ,1′-biphenyl]-4-yl]cyclopropanecarboxylic acid with an alkali metal or an alkaline earth metal.4. The salt according to claim 3 , wherein the alkali metal or the alkaline earth metal is sodium claim 3 , potassium or calcium.5. A salt of (R)-1-{4′-[5-chloro-3-({[1-(2 claim 3 ,5-difluorophenyl)ethoxy]carbonyl}amino)thiophen-2-yl]-2′-methoxy-[1 claim 3 ,1′-biphenyl]-4-yl}cyclopropanecarboxylic acid with an alkali metal or an alkaline earth metal.6. The salt according to claim 5 , wherein the alkali metal or the alkaline earth metal is sodium claim 5 , potassium or calcium.7. A salt of (R)-1-{4′-[3-({[1-(2-chlorophenyl)ethoxy]carbonyl}amino)-5-fluorothiophen-2-yl]-2′-methoxy-[1 claim 5 ,1′-biphenyl]-4-yl}cyclopropanecarboxylic acid with an alkali metal or an alkaline earth metal.8. The salt according to claim 7 , wherein the alkali metal or the alkaline earth metal is sodium claim 7 , potassium or calcium.9. A salt of (R)-1-{4′-[5-chloro-3-({[1-(thiophen-3-yl)ethoxy]carbonyl}amino)thiophen-2-yl]-[1 claim 7 ,1-biphenyl]-4-yl}cyclopropanecarboxylic acid with an alkali metal or an alkaline earth metal.10. The salt according to claim 9 , wherein the alkali metal or the alkaline earth metal is sodium claim 9 , potassium or calcium.11. A salt of (R)-1-{4′-[5-fluoro-3-({[1-(4-methylthiophen-3-yl)ethoxy]carbonyl}amino)thiophen-2-yl]-[1 claim 9 ,1′-biphenyl]-4-yl}cyclopropanecarboxylic acid with an alkali metal or an alkaline earth metal.12. The salt according to claim 11 , wherein the alkali metal or the alkaline earth metal is sodium claim ...

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Номер записи: 71
14-06-2018 дата публикации

PROCESSES FOR THE PREPARATION OF 2-THIOPHENECARBONYL CHLORIDE

Номер: US20180162830A1
Автор: Miller William H., Walker Daniel P.
Принадлежит: MONSANTO TECHNOLOGY LLC

Provided herein are processes for the preparation of 2-thiophenecarbonyl chloride, which is useful, for example, in the preparation of 3,5-disubstituted-1,2,4-oxadiazoles, such as tioxazafen (3-phenyl-5-(2-thienyl)-1,2,4-oxadiazole). 1. A process for preparing 2-thiophenecarbonyl chloride , the process comprising:reacting thiophene with chlorosulfonyl isocyanate in a reaction medium comprising an organic solvent, thereby producing (thiophene-2-carbonyl)sulfamoyl chloride,wherein the reaction is initiated by mixing the thiophene and the chlorosulfonyl isocyanate,and wherein the chlorosulfonyl isocyanate is present in molar excess relative to thiophene.2. The process of wherein the organic solvent comprises a compound selected from the group consisting of C-Calkane solvents claim 1 , C-Chalogenated alkane solvents claim 1 , C-Calkylbenzenes claim 1 , halogenated aromatic solvents claim 1 , and dialkyl ether solvents of the general formula R—O—R′ claim 1 , wherein R and R′ are each independently selected from C-Calkyl.3. The process of wherein the organic solvent comprises a compound of the formula R—O—R′ wherein R is selected from C-Ccycloalkyl and R′ is methyl.4. The process of wherein the organic solvent comprises a compound of the formula R—O—R′ wherein R and R′ are each C-Calkyl.5. A process for preparing 2-thiophenecarbonyl chloride claim 1 , the process comprising:reacting thiophene with chlorosulfonyl isocyanate in a reaction medium comprising an organic solvent, thereby producing (thiophene-2-carbonyl)sulfamoyl chloride,wherein the organic solvent comprises dibutyl ether.6. The process of any one of to wherein the reaction is initiated by adding the thiophene to the chlorosulfonyl isocyanate claim 1 ,and wherein the chlorosulfonyl isocyanate is present in molar excess relative to the thiophene.7. The process of any one of to wherein the reaction is initiated by adding the chlorosulfonyl isocyanate to the thiophene claim 1 ,and wherein the chlorosulfonyl ...

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Номер записи: 72
29-09-2022 дата публикации

MECHANOREDOX REACTION USING PIEZOELECTRIC MATERIAL, AND PRODUCTION METHOD USING SAID REACTION

Номер: US20220306654A1
Автор: Ito Hajime, Kubota Koji
Принадлежит:

Disclosed are a method for producing a highly reactive intermediate, which comprises: preparing an electron-accepting active compound (1), preparing a piezoelectric material (3), and applying mechanical strain to the piezoelectric material (3) in the presence of the electron-accepting active compound (1) and the piezoelectric material (3), and subjecting the compound (1) to one-electron reduction to generate a corresponding highly reactive intermediate; a redox reaction method using the method for producing the same; and a method for producing a redox reaction product. 1. A method for generating a highly reactive intermediate , which comprises:preparing an electron-accepting active compound (1);preparing a piezoelectric material (3); andapplying mechanical strain to the piezoelectric material (3) in the presence of the electron-accepting active compound (1) and the piezoelectric material (3), and subjecting the compound (1) to one-electron reduction to generate a corresponding highly reactive intermediate.3. The method for generating a highly reactive intermediate according to claim 2 , wherein the electron-accepting active compound (1) is selected from an aryl compound having a leaving group represented by the formula (I-1):wherein, in the general formula (I-1), the optionally substituted aryl group as for A1 comprises a phenyl group, a naphthyl group, an anthracenyl group, a phenanthrenyl group, a biphenyl group, a terphenyl group, a pyrenyl group, a perylenyl group and a triphenyleny group,the optionally substituted heteroaryl group as for Al comprises a sulfur-containing heteroaryl group, an oxygen-containing heteroaryl group, a nitrogen-containing heteroaryl group, and a heteroaryl group containing two or more heteroatoms, andthe leaving group X comprises iodine, bromine, chlorine and a diazonium salt.4. The method for generating a highly reactive intermediate according to claim 1 , wherein the piezoelectric material (3) comprises at least one selected from ...

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Номер записи: 73
11-09-2014 дата публикации

Thiophene-2-carboximidamide Based Selective Neuronal Nitric Oxide Inhibitors

Номер: US20140256958A1
Автор: Huang He, Jing Qing, Silverman Richard B.
Принадлежит:

Selective neuronal nitric oxide synthase (nNOS) inhibitor compounds designed with one or more thiophene-2-carboximidamide substituents for improved bioavailability.

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Номер записи: 74
23-06-2016 дата публикации

Compositions and Methods for the Treatment of Norovirus Infection

Номер: US20160176856A1
Автор: Beigelman Leo, Kao C. Cheng, Smith Dave, Subba-Reddy Ch. V.
Принадлежит:

Compositions and methods for the treatment of norovirus infection are disclosed. 1. (canceled)3. A norovirus RNA polymerase inhibitor as claimed in selected from the group of compounds shown in .4. A norovirus RNA polymerase inhibitor as claimed in claim 2 , wherein Ris selected from the group consisting of a carboxylic acid claim 2 , a carboxylate ester claim 2 , and an amide.5. A pharmaceutical composition comprising at least one of the compounds of or or a pharmaceutically acceptable salt or prodrug thereof and one or more pharmaceutically acceptable excipients.6. (canceled)7. A method for identifying agents which modulate norovirus RNA polymerase activity associated with clinical pathology comprising:a) incubating cells expressing said viral RNA polymerase and at least one innate immune receptor and a reporter gene operably linked to an interferon beta promoter in the presence and absence of a test agent, wherein in synthesis of viral RNA from said RNA polymerase triggers a cellular defense response which is effective to activate expression of said reporter gene; andb) measuring reporter gene expression in the presence and absence of said agent, alterations of said reporter gene expression in the presence of said agent being indicative of RNA polymerase modulatory activity.8. The method of claim 7 , wherein said innate immune receptor is selected from the group consisting of RIG-1 and MDA5.9. The method of claim 7 , wherein said reporter gene is luciferase.10. The method of claim 7 , wherein said cellular defense response comprises production of RIG-1 ligands.11. The method of comprising co-expression of norovirus VPg or a variant thereof.12. The method of claim 7 , wherein said cells are selected from the group consisting of 293T cells claim 7 , Huh7 and macrophage cells.13. The method of claim 7 , wherein said agent is a non-nucleoside inhibitor or a nucleoside analog.14. The method of comprising co-expression of additional norovirus proteins.15. The norovirus ...

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Номер записи: 75
21-06-2018 дата публикации

METHODS OF SYNTHESIZING A DIFLUOROLACTAM ANALOG

Номер: US20180170918A1
Автор: Barrett Stephen Douglas, Colombo Joseph Michael, Germain Bradlee David, Kornilov Andriy, Kramer James Bernard, Uzieblo Adam
Принадлежит:

The present invention relates to processes and intermediates for preparing compounds of formula (IA), wherein R, R, R, R, and Lare as defined herein. Compounds of formula (IA) have been found useful as EPreceptor agonists useful in the treatment of glaucoma, osteoporosis, neuropathic pain, and related disorders. 4. The method of wherein Ris methyl and Ris H.5. The method of wherein Ris H and Ris methyl.9. The method of wherein the oxidizing agent is Dess-Martin periodinane.11. The method of wherein PG is —Si(R) claim 10 , 1-ethoxyethyl claim 10 , or tetrahydro-2H-pyran-2-yl; and R claim 10 , at each occurrence claim 10 , is independently selected from C-Calkyl and phenyl.13. The method of wherein the base is lithium hydride claim 12 , sodium hydride claim 12 , or potassium hydride; PG is —Si(R) claim 12 , 1-ethoxyethyl claim 12 , or tetrahydro-2H-pyran-2-yl; and R claim 12 , at each occurrence claim 12 , is independently selected from C-Calkyl and phenyl.15. The method of wherein PG is —Si(R) claim 14 , 1-ethoxyethyl claim 14 , or tetrahydro-2H-pyran-2-yl; and R claim 14 , at each occurrence claim 14 , is independently selected from C-Calkyl and phenyl.18. The method of wherein:{'sup': 1', '2, 'sub': 2', '3, 'Lis —(CH)-G-;'}{'sup': 4', '5, 'Rand Rare each independently H or methyl;'}{'sup': 6', '3', '7, 'sub': 2', '1', '4, 'Ris —CH—C≡C—C-Calkyl or L-R;'}{'sup': '3', 'sub': 3', '6, 'Lis C-Calkylene; and'}{'sup': '7', 'Ris phenyl.'}20. The method of wherein the oxidizing agent is Dess-Martin periodinane.22. The method of wherein PG is —Si(R) claim 21 , 1-ethoxyethyl claim 21 , or tetrahydro-2H-pyran-2-yl; and R claim 21 , at each occurrence claim 21 , is independently selected from C-Calkyl and phenyl.24. The method of wherein the base is lithium hydride claim 23 , sodium hydride claim 23 , or potassium hydride; PG is —Si(R) claim 23 , 1-ethoxyethyl claim 23 , or tetrahydro-2H-pyran-2-yl; and R claim 23 , at each occurrence claim 23 , is independently selected from C- ...

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Номер записи: 76
08-07-2021 дата публикации

UREA DERIVATIVE

Номер: US20210206716A1
Автор: Fukunaga Taichi, Matsumoto Koji, NAKAMURA Yuji, Soneda Tsuyoshi, Tanaka Naomi
Принадлежит: Daiichi Sankyo Company, Limited

An object of the present invention is to find a novel pharmaceutical that has an excellent tryptophanase inhibitory effect and suppresses worsening of renal function to preserve the kidney by reducing production of indoxyl sulfate in the blood. The present invention provides a pharmaceutical composition containing, as an active ingredient, a compound represented by the following formula, or a pharmacologically acceptable salt thereof: 4. The compound according to claim 2 , or a pharmacologically acceptable salt thereof claim 2 , wherein Rrepresents an ethyl group.5. The compound according to claim 3 , or a pharmacologically acceptable salt thereof claim 3 , wherein Rrepresents a hydrogen atom claim 3 , a fluorine atom or a cyano group.6. The compound according to claim 3 , or a pharmacologically acceptable salt thereof claim 3 , wherein Rrepresents a fluorine atom claim 3 , a chlorine atom claim 3 , a 2 claim 3 ,2 claim 3 ,2-trifluoroethyl group claim 3 , a difluoromethoxy group or a trifluoromethoxy group.9. The compound according to claim 7 , or a pharmacologically acceptable salt thereof claim 7 , wherein Rand Rare the same or different and represent an ethyl group claim 7 , a propyl group or an isopropyl group.10. The compound according to claim 7 , or a pharmacologically acceptable salt thereof claim 7 , wherein Rand Rrepresent a combination of an ethyl group and an ethyl group claim 7 , or an ethyl group and a propyl group.11. The compound according to claim 7 , or a pharmacologically acceptable salt thereof claim 7 , wherein Rand Rboth represent an ethyl group.12. The compound according to claim 8 , or a pharmacologically acceptable salt thereof claim 8 , wherein Rrepresents a hydrogen atom.13. The compound according to claim 8 , or a pharmacologically acceptable salt thereof claim 8 , wherein Rrepresents a trifluoromethyl group claim 8 , a monofluoromethoxy group claim 8 , a difluoromethoxy group claim 8 , a trifluoromethoxy group claim 8 , a ...

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Номер записи: 77
06-07-2017 дата публикации

ACYLOXYALKYL CARBAMATE PRODRUGS, METHODS OF SYNTHESIS AND USE

Номер: US20170190657A1
Автор: Gallop Mark A., Ludwikow Maria J., Peng Ge, Phan Thu, Yao Fenmei
Принадлежит: XenoPort, Inc.

The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof. 152-. (canceled)54. The method of claim 53 , wherein Ris hydrogen.55. The method of wherein Ris selected from Calkyl claim 53 , substituted Calkyl claim 53 , Ccycloalkyl claim 53 , phenyl claim 53 , substituted phenyl claim 53 , Cphenylalkyl and pyridyl.56. The method of claim 53 , wherein Ris selected from methyl claim 53 , ethyl claim 53 , n-propyl claim 53 , isopropyl claim 53 , n-butyl claim 53 , isobutyl claim 53 , sec-butyl claim 53 , tert-butyl claim 53 , n-pentyl claim 53 , isopentyl claim 53 , sec-pentyl claim 53 , neopentyl claim 53 , 1 claim 53 ,1-dimethoxyethyl claim 53 , 1 claim 53 ,1-diethoxyethyl claim 53 , phenyl claim 53 , 4-methoxyphenyl claim 53 , benzyl claim 53 , phenethyl claim 53 , styryl claim 53 , cyclopropyl claim 53 , cyclobutyl claim 53 , cyclopentyl claim 53 , cyclohexyl claim 53 , 2-pyridyl claim 53 , 3-pyridyl and 4-pyridyl.57. The method of claim 53 , wherein Ris selected from methyl claim 53 , ethyl claim 53 , n-propyl claim 53 , isopropyl claim 53 , n-butyl claim 53 , isobutyl claim 53 , sec-butyl claim 53 , tert-butyl claim 53 , n-pentyl claim 53 , isopentyl claim 53 , sec-pentyl claim 53 , neopentyl claim 53 , 1 claim 53 ,1-diethoxyethyl claim 53 , phenyl claim 53 , cyclohexyl and 3-pyridyl.58. ...

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Номер записи: 78
20-07-2017 дата публикации

Chiral Diacylhydrazine Ligands for Modulating the Expression of Exogenous Genes via an Ecdysone Receptor Complex

Номер: US20170204079A1
Автор: HORMANN Robert Eugene, Li Bing
Принадлежит: Intrexon Corporation

The present invention provides diacylhydrazine ligands and chiral diacylhydrazine ligands for use with ecdysone receptor-based inducible gene expression systems. Thus, the present invention is useful for applications such as gene therapy, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable. An advantage of the present invention is that it provides a means to regulate gene expression and to tailor expression levels to suit the user's requirements. 125-. (canceled)27. The process of wherein B is 3 claim 26 ,5-di-methylphenyl.28. The process of wherein A is 2-ethyl-3-methoxyphenyl.29. The process of wherein Ris tert-butyl.30. (canceled)32. The method of claim 31 , wherein said ecdysone receptor complex is a chimeric ecdysone receptor complex and said DNA binding sequence further comprises a promoter.3335-. (canceled)36. The method of claim 31 , wherein the subject is a human.37. The method of claim 31 , wherein said cells are autologous cells.38. The method of claim 37 , wherein said autologous cells contain said ecdysone receptor complex and the DNA binding sequence for the ecdysone complex claim 37 , and said cells are implanted by injection into said subject to make it transgenic.39. (canceled)40. The method of claim 38 , wherein said injection is into a tumor.41. The method of claim 31 , wherein said ligand is administered to said transgenic subject as part of a pharmaceutical composition comprising a pharmaceutically acceptable carrier.42. The method of claim 41 , wherein said pharmaceutical composition is administered orally.43. The method of claim 41 , wherein said pharmaceutically acceptable carrier comprises a lipophilic solvent.45. (canceled)46. (canceled)47. The method of claim 31 , wherein said ecdysone receptor complex or ecdysone receptor ligand binding domain comprises a mutation ...

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Номер записи: 79
27-07-2017 дата публикации

PRODUCTION METHOD OF THIENOPYRIMIDINE DERIVATIVE

Номер: US20170210753A1
Автор: Fukuoka Koichiro, KOMURA Fumiya, MIWA Kazuhiro, Sasaki Tsuyoshi
Принадлежит:

The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like. 1. A method of producing ethyl (2 ,6-difluorobenzyl)-[4-dimethylaminomethyl-3-(6-methoxypyridazin-3-ylcarbamoyl)-5-(4-nitrophenyl)thiophen-2-yl]carbamate or a salt thereof , which comprises reacting 2-[(2 ,6-difluorobenzypethoxycarbonylamino]-4-dimethylaminomethyl-5-(4-nitrophenyl)thiophene-3-carboxylic acid or a salt thereof with 3-amino-6-methoxypyridazine or a salt thereof in the presence of propylphosphonic anhydride and a base.2. The method of claim 1 , wherein the base is selected from the group consisting of diisopropylethylamine and triethylamine.3. The method of claim 1 , wherein the reacting is carried out in the presence of a solvent selected from the group consisting of dimethylacetamide claim 1 , dimethylformamide claim 1 , dimethylsulfoxide claim 1 , tetrahydrofuran claim 1 , acetonitrile and ethyl acetate.4. The method of claim 1 , wherein the reacting is carried out at a temperature of 0° C. to 80° C. for a time of 1 to 24 hours.5. The method of claim 1 , wherein the reacting is carried out at a temperature of 50° C. to 60° C. for a time of 1 to 3 hours.6. The method of claim 1 , wherein the amount of the 3-amino-6-methoxypyridazine or the salt thereof used is 1.0 to 3.0 equivalents claim 1 , wherein the amount of the propylphosphonic anhydride used is 1.0 to 3.0 equivalents claim 1 , wherein the amount of the base used is 1 to 4 equivalents claim 1 , relative to the 2-[(2 claim 1 ,6- ...

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Номер записи: 80
09-10-2014 дата публикации

MODULATORS OF C3A RECEPTORS

Номер: US20140302069A1
Автор: Fairlie David, REID Robert C.
Принадлежит:

Heterocyclic compounds that modulate C3a receptors and their use in the treatment or prevention of inflammatory diseases, infectious diseases, cancers, metabolic disorders, obesity, type 2 diabetes, metabolic syndrome and associated cardiovascular diseases are described. The use of the compounds in stimulating or suppressing an immune response is also described together with pharmaceutical compositions comprising the compounds or their pharmaceutically acceptable salts. 8. A compound according to wherein Ris COH.9. A compound according to wherein Ris selected from hydrogen claim 1 , —Calkyl claim 1 , —Calkenyl claim 1 , —Ccycloalkyl claim 1 , cycloalkenyl claim 1 , aryl claim 1 , and 5 or 6 membered heterocyclyl and heteroaryl.10. A compound according to wherein Ris hydrogen.11. A compound according to wherein Ris selected from methyl claim 9 , ethyl claim 9 , propyl claim 9 , isopropyl claim 9 , cyclohexyl claim 9 , cyclohexenyl claim 9 , cyclohexadienyl and phenyl.12. A compound according to wherein Ris selected from hydrogen claim 1 , —CH claim 1 , cyclohexyl claim 1 , phenyl claim 1 , —(CH)NHC(═NH)NH claim 1 , —CH—CONH claim 1 , —CHCOH claim 1 , —CHSH claim 1 , —(CH)CONH claim 1 , —(CH)COH claim 1 , —CH(4-imidazolyl) claim 1 , —CH(CH)CHCH claim 1 , —CHCH(CH) claim 1 , —(CH)NH claim 1 , —(CH)SCH claim 1 , —CHPh claim 1 , —CHOH claim 1 , —CH(CH)OH claim 1 , —CH(3-indolyl) claim 1 , —CH(4-hydroxyphenyl) claim 1 , —CH(CH)and —(CH)cyclohexyl.13. A compound according to wherein Ris selected from —CHCH(CH)and —CH(CH)CHCH.14. A compound according to wherein Ris selected from —NHC(O)R claim 1 , —NHC(O)R claim 1 , —NHC(O)NHRand —NHSOR.15. A compound according to wherein Ris selected from Calkyl claim 14 , cycloalkyl claim 14 , cycloalkenyl claim 14 , aryl claim 14 , heterocyclyl claim 14 , heteroaryl claim 14 , —CHcycloalkyl claim 14 , —CHcycloalkenyl claim 14 , —CHaryl claim 14 , —CHheterocyclyl claim 14 , —CHheteroaryl and —CH(CH)aryl claim 14 , wherein each cycloalkyl ...

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Номер записи: 81
04-07-2019 дата публикации

METHODS OF SYNTHESIZING A DIFLUOROLACTAM ANALOG

Номер: US20190202816A1
Автор: Barrett Stephen Douglas, Colombo Joseph Michael, Germain Bradlee David, Kornilov Andriy, Kramer James Bernard, Uzieblo Adam
Принадлежит:

The present invention relates to processes and intermediates for preparing compounds of formula (IA), wherein R, R, R, R, and Lare as defined herein. Compounds of formula (IA) have been found useful as EPreceptor agonists useful in the treatment of glaucoma, osteoporosis, neuropathic pain, and related disorders. 4. The method of wherein Ris methyl and Ris H.5. The method of wherein Ris H and Ris methyl.9. The method of wherein the oxidizing agent is Dess-Martin periodinane.11. The method of wherein PG is —Si(R) claim 10 , 1-ethoxyethyl claim 10 , or tetrahydro-2H-pyran-2-yl; and R claim 10 , at each occurrence claim 10 , is independently selected from C-Calkyl and phenyl.13. The method of wherein the base is lithium hydride claim 12 , sodium hydride claim 12 , or potassium hydride; PG is —Si(R) claim 12 , 1-ethoxyethyl claim 12 , or tetrahydro-2H-pyran-2-yl; and R claim 12 , at each occurrence claim 12 , is independently selected from C-Calkyl and phenyl.15. The method of wherein PG is —Si(R) claim 14 , 1-ethoxyethyl claim 14 , or tetrahydro-2H-pyran-2-yl; and R claim 14 , at each occurrence claim 14 , is independently selected from C-Calkyl and phenyl.18. The method of wherein:{'sup': 1', '2, 'sub': 2', '3, 'Lis —(CH)-G-;'}{'sup': 4', '5, 'Rand Rare each independently H or methyl;'}{'sup': 6', '3', '7, 'sub': 2', '1', '4, 'Ris —CH—C≡C—C-Calkyl or L-R;'}{'sup': '3', 'sub': 3', '6, 'Lis C-Calkylene; and'}{'sup': '7', 'Ris phenyl.'}20. The method of wherein the oxidizing agent is Dess-Martin periodinane.22. The method of wherein PG is —Si(R) claim 21 , 1-ethoxyethyl claim 21 , or tetrahydro-2H-pyran-2-yl; and R claim 21 , at each occurrence claim 21 , is independently selected from C-Calkyl and phenyl.24. The method of wherein the base is lithium hydride claim 23 , sodium hydride claim 23 , or potassium hydride; PG is —Si(R) claim 23 , 1-ethoxyethyl claim 23 , or tetrahydro-2H-pyran-2-yl; and R claim 23 , at each occurrence claim 23 , is independently selected from C- ...

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Номер записи: 82
04-07-2019 дата публикации

METHOD FOR THE PREPARATION OF SUBSTITUTED THIOLACTONES, NEW SUBSTITUTED THIOLACTONES AND USES THEREOF

Номер: US20190202849A1
Автор: COUTELIER Olivier, Destarac Mathias, KULAI Ihor
Принадлежит:

The invention relates to a method for preparing substituted thiolactones of formula (I), new substituted thiolactones of formula (I′) that can be obtained by carrying out said method, and the use of substituted thiolactones of formula (I) or (I′) for synthesizing polymers or functionalizing surfaces or polymers. 2. Process according to claim 1 , wherein said process is carried out for the preparation of thiolactones of formula (I) in which:{'sup': 1', '7', '7′', '10', '11', '8', '9', '15′', '15', '15′', '16′', '16', '16′, 'sub': n', '2n+1', '2', 'p', '3-p, 'Zis a group chosen from the groups P(O)(OR)(OR); CF; B(OR); OR; SiR(OR); NR(C═O)R, in which R is a hydrogen atom and NR(C═O)OR, in which R is a hydrogen atom, and/or'}Y is a hydrogen atom or a group chosen from an alkyl radical.3. Process according to claim 1 , wherein said process is carried out for the preparation of substituted thiolactones of formula (I) in which:{'sup': 1', '10', '11', '8', '9', '15′', '15', '15′', '16′', '16', '16′, 'sub': n', '2n+1', '2', 'p', '3-p, 'Zis a group chosen from the groups dimethylphosphonate and diethylphosphonate; CF; B(OR), OR, SiR(OR), NR(C═O)R, in which R is a hydrogen atom and NR(C═O)OR, in which R is a hydrogen atom, and/or'}Y is a hydrogen atom or a methyl or hydroxymethyl group.4. Process according to claim 1 , wherein said process leads to the formation of a thiolactone of formula (I) claim 1 , chosen from:dimethyl 5-oxo-tetrahydrothiophen-2-ylphosphonate,diethyl (4-methyl-5-oxo-tetrahydrothiophen-2-yl)methylphosphonate,diethyl (5-oxo-tetrahydrothiophen-2-yl)methylphosphonate,3-methyl-5-pentyl-dihydrothiophen-2(3H)-one,5-pentyl-dihydrothiophen-2(3H)-one,3-methyl-5-(perfluorooctyl)dihydrothiophen-2(3H)-one,3-methyl-5-phenyldihydro-2H-thieno[2,3-c]pyrrole-2,4,6(3H, 5H)-trione,3-methyl-5-(perfluorobutyl)dihydrothiophen-2(3H)-one,(4-methyl-5-oxo-tetrahydrothiophen-2-yl)phosphonic acid,((4-methyl-5-oxo-tetrahydrothiophen-2-yl)methyl)phosphonic acid,(5-oxo- ...

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Номер записи: 83
04-08-2016 дата публикации

RADIOMITIGATING PHARMACEUTICAL FORMULATIONS

Номер: US20160221976A1
Автор: McBride William, Micewicz Ewa
Принадлежит:

The present disclosure relates to compounds of Formula (I) and (II), compositions containing the compounds (alone or in combination with other agents), and their use to prevent, mitigate or treat a) damage induced by ionizing radiation, b) inflammation or c) cancer. 2. A compound of claim 1 , wherein the aryl or heteroaryl group bears at least one substituent including a nitro substitutent.3. The compound of claim 2 , wherein the nitro substituent is disposed at a position on Adistal to the sulfonyl.4. The compound of claim 1 , wherein Ais a heterocyclic amine.5. The compound of claim 1 , wherein Ais NRR claim 1 , wherein each of Rand R claim 1 , independently claim 1 , is H claim 1 , alkyl claim 1 , alkenyl claim 1 , alkynyl claim 1 , aryl claim 1 , heteroaryl claim 1 , aralkyl claim 1 , or heteroaralkyl claim 1 , provided that Rand Rare not both H.7. The compound of claim 6 , wherein Yand Yare each ethyl.8. The compound of claim 6 , wherein Yand Ytaken together with X form a piperazine ring.10. The compound of claim 9 , wherein G is N and Ris selected from phenyl claim 9 , 4-fluorophenyl and 3-chlorophenyl.11. The compound of claim 9 , wherein Z is absent.12. The compound of claim 9 , wherein Z is prop-2-en-1-yl and Ris phenyl.14. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable excipient or solvent.15. A method of mitigating an effect of ionizing radiation on a cell claim 1 , organ claim 1 , tissue claim 1 , or organism claim 1 , comprising contacting the cell claim 1 , organ claim 1 , tissue claim 1 , or organism with a compound of .16. The method of claim 15 , wherein the compound contacts the cell before claim 15 , during claim 15 , or after exposure to ionizing radiation.17. A method of treating inflammation in an organism claim 1 , comprising administering to the organism a compound of .18. A method of treating cancer in an organism claim 1 , comprising administering to the organism a compound of .19. The method of ...

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Номер записи: 84
02-07-2020 дата публикации

ANTI-FUNGALS COMPOUNDS TARGETING THE SYNTHESIS OF FUNGAL SPHINGOLIPIDS

Номер: US20200207705A1
Автор: DEL POETA Maurizio, Haranahalli Krupanandan, Lazzarini Cristina, Ojima Iwao, Sun Yi
Принадлежит: The Research Foundation for The State University of New York

The present invention provides a compound having the structure: 2. The compound of claim 1 ,{'sub': 3', '5', '4', '6, 'wherein when Rand Rare each —H and Rand Rare each —Br, then A is other than para-bromophenyl, meta-bromophenyl, ortho-tolyl or 3-quinolinyl; and'}{'sub': 3', '5', '6', '4, 'when R, Rand Rare each —H and Ris —Br, then A is other than 3,5-dibromo-ortho-hydroxyphenyl, para-bromophenyl, meta-bromophenyl or ortho-tolyl.'}3. The compound of or claim 1 , wherein the aryl or heteroaryl is substituted with halogen claim 1 , C-Calkyl claim 1 , —OH claim 1 , —O—(C-Calkyl) claim 1 , —CHF claim 1 , —CF claim 1 , —OCHFor —OCF.4. The compound of or claim 1 , wherein the fused aryl or fused heteroaryl is substituted with halogen claim 1 , C-Calkyl claim 1 , —OH claim 1 , —O—(C-Calkyl) claim 1 , —CHF claim 1 , —CF claim 1 , —OCHFor —OCF.5. The compound of or claim 1 , wherein one of R-Ris other than —H.6. The compound of or claim 1 , wherein two of R-Ris other than —H.7. The compound of any one of - claim 1 , wherein A is monosubstituted.8. The compound of any one of - claim 1 , wherein A is disubstituted.9. The compound of any one of - claim 1 , wherein A is trisubstituted.10. The compound of or claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , and Rare each independently —H claim 1 , halogen claim 1 , C-Calkyl claim 1 , —OH claim 1 , —O—(C-Calkyl) claim 1 , —CHF claim 1 , —CF claim 1 , —OCHFor —OCF.11. The compound of claim 10 , wherein R claim 10 , R claim 10 , R claim 10 , and Rare each independently halogen claim 10 , —O—(C-Calkyl) claim 10 , —OCFor —CF.12. The compound of claim 11 , wherein R claim 11 , R claim 11 , R claim 11 , and Rare each independently halogen or —O—(C-Calkyl).13. The compound of claim 11 , wherein R claim 11 , R claim 11 , R claim 11 , and Rare each independently —Cl claim 11 , —Br claim 11 , —F claim 11 , —O—(C-Calkyl) claim 11 , —OCFor —CF.14. The compound of claim 12 , wherein R claim 12 , R claim 12 , R claim 12 , and Rare each ...

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Номер записи: 85
18-07-2019 дата публикации

NOVEL ANTAGONISTS OF THE GLUCAGON RECEPTOR

Номер: US20190218176A1
Автор: Boyer Serge Henri, Chen Mingwei, Craigo William, Dang Qun, Gomez-Galeno Jorge E., Grote Matthew P., Hecker Scott J., Lemus Robert Huerta, Li Haiqing, Mali Venkat Reddy, Nguyen Thanh Huu, Reddy Raja K., Sun Zhili, van Poelje Paul D.
Принадлежит:

The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof and pharmaceutical compositions comprising the same. 2. The method according to claim 1 , wherein{'sub': 1-6', '3', '1-6, 'D is a substituted group selected from phenyl or heteroaryl, wherein said group is substituted with L and, optionally, one or more additional substituents independently selected from C-alkyl, halogen, —CF, or C-haloalkyl;'}wherein said heteroaryl contains one or two heteroatoms independently selected from nitrogen, oxygen, or sulfur.3. The method according to claim 1 , wherein{'sup': 2', '2, 'sub': '1-3', 'Z is —C(O)N(R)—; wherein said Ris hydrogen or C-alkyl;'}{'sup': 27', '27, 'sub': '1-3', 'Y is a group selected from —O— or —CHR—; wherein Ris hydrogen or C-alkyl; and'}{'sup': '1', 'sub': '3', 'Ris a group selected from hydrogen, —F, or —CH.'}4. The method according to claim 1 , wherein{'sub': 3-8', '4-8', '3-8', '4-8', '1-6', '3', '3', '2', '3, 'E is a group selected from phenyl, C-cycloalkyl-substituted phenyl, C-cycloalkenyl-substituted phenyl, phenyl-substituted phenyl, benzyl, C-cycloalkyl-substituted benzyl, C-cycloalkenyl-substituted benzyl, or phenyl-benzyl, wherein each group is optionally substituted with one to three groups independently selected from halogen, —CN, —C-alkyl, halogen, —CF, —OCF, or —OCHCF.'}6. The method according to claim 1 ...

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Номер записи: 86
30-10-2014 дата публикации

NEW USE FOR A COMPOUND AS A MATRIX IN THE SPECIFIC DETECTION, IDENTIFICATION AND/OR QUANTIFICATION OF ALKALOIDS BY MALDI-TOF MASS SPECTROMETRY

Номер: US20140319331A1
Автор: Dias Marylène, Levillain Eric, RICHOMME Pascal, Schinkovitz Andreas, SERAPHIN Denis
Принадлежит:

There is provided (i) a method of analysing small molecules that may have a mass of <800 Da, in particular alkaloids, said method being generally referred to as MALDI-TOF-MS (or MALDI time-of-flight mass spectrometry), which is an acronym for a method of analysis by matrix-assisted laser desorption/ionisation time-of-flight mass spectrometry. Also provided is (ii) a molecule according to formula (I) and the use of the molecule as a matrix in the analysis method. 2. The use as claimed in claim 1 , wherein R2 is the —SCHgroup and/or n is 2 and/or Y is a —CN functional group and/or m is 1.3. The use as claimed in claim 1 , wherein:{'sub': 2', '2', '3, 'm=1, R1 is a —S(CH)CN group, and R2 is a —SCHgroup;'}{'sub': 2', '2', '2', '3', '3, 'm=1, R1 is a —S(CH)COCHgroup, and R2 is a —SCHgroup;'}{'sub': 2', '3', '3, 'm=1, R1 is a —S(CH)CN group, and R2 is a —SCHgroup;'}{'sub': 2', '2, 'm=1, R1 is a —S(CH)CN group, and R2 is hydrogen atom;'}{'sub': 2', '2', '2', '3, 'm=1, R1 is a —S(CH)COH group, and R2 is a —SCHgroup;'}{'sub': 2', '2', '2', '3, 'm=1, R1 is a —S(CH)—CHOH group, and R2 is a —SCHgroup;'}{'sub': 2', '2', '3', '3, 'm=1, R1 is a —S(CH)Ngroup, and R2 is a —SCHgroup; or'}{'sub': 2', '2', '3, 'm=1, R1 is a —S(CH)CCH group, and R2 is a —SCHgroup.'}4. The use as claimed in claim 1 , wherein the compound of formula (I) is 3-(5-(5-(methylthio)thiophen-2-yl)thiophen-2-ylthio)propanenitrile.5. The use as claimed in claim 1 , wherein said MALDI device is coupled to a time-of-flight analyzer.6. The use as claimed in claim 1 , for qualitative and quantitative analysis of a mixture of molecules or sample comprising at least one molecule of mass <800 Da.7. The use as claimed in claim 1 , wherein said molecule of mass <800 Da is selected from alkaloids.8. The use as claimed in claim 7 , wherein the alkaloids are selected from:the group of the Azolidines;the group of the Azines;the group of the Tropanes;the group of the Quinolines;the group of the Isoquinolines;the group of the ...

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Номер записи: 87
16-08-2018 дата публикации

Benzo Annulenes as Antiviral Agents

Номер: US20180230084A1
Автор: Ahmed Syed Kaleem, Augelli-Szafran Corinne E., Maddry Joseph A., Pathak Ashish Kumar
Принадлежит:

The present disclosure is concerned with benzo annulene compounds that are capable of inhibiting a viral infection and methods of treating viral infections such as, for example, chikungunya, Venezuelan equine encephalitis, dengue, influenza, and zika, using these compounds. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. 2. The compound of claim 1 , wherein Z is CH.3. The compound of claim 1 , wherein each of Rand Ris hydrogen.4. The compound of claim 1 , wherein Ris —OR.5. The compound of claim 1 , wherein Cyis selected from C5-C6 aryl and C4-C5 heteroaryl and substituted with 0 claim 1 , 1 claim 1 , or 2 groups independently selected from halogen claim 1 , —COH claim 1 , —CN claim 1 , —OH claim 1 , —NH claim 1 , C1-C8 alkyl claim 1 , C1-C8 haloalkyl claim 1 , C1-C8 alkylnitrile claim 1 , C1-C8 hydroxyalkyl claim 1 , C1-C8 alkoxy claim 1 , C1-C8 halohydroxyalkyl claim 1 , C1-C8 aminoalkyl claim 1 , C1-C8 alkylamino claim 1 , (C1-C8)(C1-C8) dialkylamino claim 1 , and Cy.6. The compound of claim 1 , wherein Cyis phenyl substituted with 0 claim 1 , 1 claim 1 , or 2 groups independently selected from halogen claim 1 , —COH claim 1 , —CN claim 1 , —OH claim 1 , —NH claim 1 , C1-C8 alkyl claim 1 , C1-C8 haloalkyl claim 1 , C1-C8 alkylnitrile claim 1 , C1-C8 hydroxyalkyl claim 1 , C1-C8 alkoxy claim 1 , C1-C8 halohydroxyalkyl claim 1 , C1-C8 aminoalkyl claim 1 , C1-C8 alkylamino claim 1 , (C1-C8)(C1-C8) dialkylamino and Cy.7. The compound of claim 1 , wherein Cyis phenyl substituted with a tert-butyl group.8. The compound of claim 1 , wherein Cyis C4-C5 heteroaryl substituted with 0 claim 1 , 1 claim 1 , or 2 groups independently selected from halogen claim 1 , —COH claim 1 , —CN claim 1 , —OH claim 1 , —NH claim 1 , C1-C8 alkyl claim 1 , C1-C8 haloalkyl claim 1 , C1-C8 alkylnitrile claim 1 , C1-C8 hydroxyalkyl claim 1 , C1-C8 alkoxy claim 1 , C1-C8 halohydroxyalkyl ...

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Номер записи: 88
17-09-2015 дата публикации

FLUORENE-TYPE COMPOUND, PHOTOPOLYMERIZATION INITIATOR COMPRISING SAID FLUORENE-TYPE COMPOUND, AND PHOTOSENSITIVE COMPOSITION CONTAINING SAID PHOTOPOLYMERIZATION INITIATOR

Номер: US20150259321A1
Автор: Harihara Makoto, Kuwamura Katsuji, YAMAZAKI Tomohiko
Принадлежит: DAITO CHEMIX CORPORATION

According to an embodiment of the present invention, there is provided a novel fluorene-based compound and a photopolymerization initiator using the fluorene-based compound. The fluorene-based compound according to an embodiment of the present invention is represented by the general formula (1). A photopolymerization initiator having additionally high sensitivity can be provided by using the fluorene-based compound. In addition, a photopolymerization initiator that can impart additionally excellent characteristics can be provided by appropriately selecting, for example, a substituent. 2. The fluorene-based compound according to claim 1 , wherein the Ror the R represents a methyl group.3. The fluorene-based compound according to claim 1 , wherein the Rrepresents a group represented by the formula (2) claim 1 , and the Rrepresents a linear claim 1 , branched claim 1 , or cyclic alkyl group having 1 to 7 carbon atoms claim 1 , a linear or branched halogenated alkyl group having 1 to 5 carbon atoms claim 1 , a linear or branched aminoalkyl group having 2 to 4 carbon atoms that may be substituted claim 1 , a phenyl group that may be substituted claim 1 , a phenylalkyl group having 7 to 11 carbon atoms that may be substituted claim 1 , a phenylalkyl group having 7 to 10 carbon atoms that is interrupted by one or more ether bonds or thioether bonds and may be substituted claim 1 , a condensed ring group that may be substituted claim 1 , or a heterocyclic group that may be substituted.4. The fluorene-based compound according to claim 1 , wherein the Rrepresents a group represented by the formula (3) claim 1 , and the Rrepresents a linear claim 1 , branched claim 1 , or cyclic alkyl group having 1 to 6 carbon atoms claim 1 , a linear or branched halogenated alkyl group having 1 to 4 carbon atoms claim 1 , a phenyl group that may be substituted claim 1 , a phenylalkyl group having 7 to 10 carbon atoms that may be substituted claim 1 , a phenylalkyl group having 7 to 9 carbon ...

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Номер записи: 89
20-11-2014 дата публикации

OLEANOLIC ACID AMIDATE DERIVATIVES, PREPARATION METHODS AND USES THEREOF

Номер: US20140343108A1
Автор: Lai Hongxi, Rong Frank, Xie Fuwen, Xu Rongzhen
Принадлежит:

The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel amidated derivatives of oleanolic acid according to formula (I) or a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments. 2. The amidated oleanolic acid derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein R is selected from the group consisting of aryl claim 1 , heteroaryl claim 1 , cycloalkyl claim 1 , heterocyclyl claim 1 , aryl-vinyl claim 1 , and heteroaryl-vinyl claim 1 , each of which is optionally substituted by halogen claim 1 , C-Calkyl or C-Calkoxy.3. The amidated oleanolic acid derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein the aryl is phenyl.4. The amidated oleanolic acid derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein the heteroaryl is furyl claim 1 , thienyl claim 1 , pyrrolyl claim 1 , or pyridyl.5. The amidated oleanolic acid derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein the cycloalkyl is cyclopropyl claim 1 , cyclopentyl or cyclohexyl.6. The amidated oleanolic acid derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein the heterocyclyl is tetrahydrofuryl claim 1 , tetrahydrothienyl claim 1 , piperidyl claim 1 , piperazinyl or morpholinyl.7. The amidated oleanolic acid derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein R is selected from optionally substituted heteroaryl-vinyl.10. A pharmaceutical composition claim 1 , comprising the amidated oleanolic acid derivative or a pharmaceutically acceptable salt thereof according to and optionally a pharmaceutically acceptable excipient.11. (canceled)12. A method for treating a subject suffering from tumor claim 1 , ...

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Номер записи: 90
27-11-2014 дата публикации

METHOD FOR REDUCING BLOOD PRESSURE USING INHIBITORS OF PLASMA KALLIKREIN

Номер: US20140348850A1
Автор: Clermont Allen, Feener Edward P.
Принадлежит:

The present invention relates to methods of reducing blood pressure in a subject by administering a plasma kallikrein inhibitor. 1. A method for reducing blood pressure in a subject in need thereof , said method comprising administering to said subject an effective amount of an inhibitor of plasma kallikrein.2. The method of claim 1 , wherein the subject is a human.3. The method of claim 2 , wherein the systolic blood pressure (SBP) of said subject is greater than 125 mm Hg.4. The method of claim 3 , wherein said SBP is greater than 139 mm Hg.5. The method of claim 4 , wherein the diastolic blood pressure of said subject is greater than 89 mm Hg.6. The method of claim 1 , wherein said subject is suffering from primary hypertension.7. The method of claim 1 , wherein said subject is suffering from secondary hypertension.8. The method of claim 1 , wherein said subject is prehypertensive.9. The method of claim 1 , wherein said subject has claim 1 , or is at increased risk of having claim 1 , angioedema.10. The method of claim 9 , wherein said subject has been previously treated with at least on angiotensin-converting enzyme (ACE inhibitor).11. The method of claim 1 , wherein the plasma kallikrein inhibitor is a selective plasma kallikrein inhibitor.12. The method of claim 1 , wherein the inhibitor is a naturally occurring compound.13. The method of claim 12 , wherein the inhibitor is the naturally occurring protein Cl-Inhibitor.14. The method of claim 1 , wherein the inhibitor is a non-naturally occurring compound.15. The method of claim 14 , wherein the inhibitor is ecallantide (DX-88).16. The method of claim 14 , wherein the inhibitor is a bicyclic peptide.17. The method of claim 16 , wherein said bicyclic peptide is selected from the group consisting of PK1-PK23.19. The method of claim 18 , wherein Ar is an aromatic ring selected from the group consisting of benzene claim 18 , pyridine claim 18 , and pyrimidine.20. The method of claim 18 , wherein Ar is a bond and m ...

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Номер записи: 91
13-09-2018 дата публикации

ACYLOXYALKYL CARBAMATE PRODRUGS, METHODS OF SYNTHESIS AND USE

Номер: US20180258032A1
Автор: Gallop Mark A., Ludwikow Maria J., Peng Ge, Phan Thu, Yao Fenmei
Принадлежит:

The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof. 152-. (canceled)54. The method of claim 53 , wherein Rand Rin the compound of Formula (XXIII) are different claim 53 , such that the carbon atom to which these substitutents are attached is a stereogenic center.55. The method of claim 53 , wherein Ris isopropyl claim 53 , Ris isopropyl claim 53 , Ris hydrogen claim 53 , the stereochemistry at the carbon to which Rand Rare attached is of the S-configuration and the compound of Formula (I) is substantially one diastereomer.56. The method of claim 53 , wherein Ris isopropyl claim 53 , Ris isopropyl claim 53 , Ris hydrogen claim 53 , the stereochemistry at the carbon to which Rand Rare attached is of the R-configuration and the compound of Formula (I) is substantially one diastereomer.55. The method of claim 53 , wherein Ris isopropyl claim 53 , Ris isopropyl claim 53 , Ris hydrogen claim 53 , Ris hydrogen claim 53 , Ris 4-chlorophenyl claim 53 , Ris hydrogen and Ris hydrogen.56. The method of claim 53 , wherein the method is carried out at a temperature between about −20° C. and about 40° C.57. The method of claim 53 , wherein the method is performed in the absence of a base.58. The method of claim 53 , wherein the method is performed in the presence of an inorganic base.59. The method ...

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Номер записи: 92
13-09-2018 дата публикации

NEAR INFRARED ABSORBING COMPOSITION, FILM, INFRARED CUT FILTER, SOLID IMAGE PICKUP ELEMENT, INFRARED ABSORBER, AND COMPOUND

Номер: US20180259849A1
Автор: Hirai Yuki, Jimbo Yoshihiro, SASAKI Daisuke
Принадлежит: FUJIFILM Corporation

A near infrared absorbing composition includes: a squarylium compound represented by the following Formula (1) and having an absorption maximum of 700 nm or longer; and a resin. In Formula (1), Arand Areach independently represent a divalent conjugated group which has a heteroaryl ring having a chalcogen atom, and Rto Reach independently represent a hydrogen atom or a substituent. The film and the infrared cut filter are formed of the near infrared absorbing composition. The solid image pickup element includes the infrared cut filter. 2. The near infrared absorbing composition according to claim 1 ,{'sup': 1', '2, 'wherein in the squarylium compound, a plane including Arand Arof Formula (1) includes a π-conjugated plane having 16 to 54 atoms.'}3. The near infrared absorbing composition according to claim 1 ,wherein the chalcogen atom is a sulfur atom.4. The near infrared absorbing composition according to claim 1 ,{'sup': 1', '2, 'wherein Arand Areach independently represent a thiophene ring, a thiazole ring, a fused ring including at least one of a thiophene ring or a thiazole ring, or a divalent conjugated group including a thiophene ring, a thiazole ring or a fused ring including at least one of a thiophene ring or a thiazole ring.'}5. The near infrared absorbing composition according to claim 1 ,{'sup': 1', '2, 'wherein Arand Areach independently include a thiophene ring or a thiazole ring, and'}{'sup': 1', '4, 'Rto Reach independently represent an aryl group or a heteroaryl group.'}6. The near infrared absorbing composition according to claim 5 ,{'sup': 1', '2', '3', '4, 'wherein at least one of R, R, R, or Rrepresents an aryl group or a heteroaryl group in which the number of atoms constituting a ring is 8 or more.'}7. The near infrared absorbing composition according to claim 5 ,{'sup': 1', '2', '3', '4, 'wherein at least one of R, R, R, or Rrepresents a naphthyl group.'}8. The near infrared absorbing composition according to claim 1 ,{'sup': 1', '2, 'wherein ...

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Номер записи: 93
04-12-2014 дата публикации

SUBSTITUTED CYCLOPENTENES AS THERAPEUTIC AGENTS

Номер: US20140357705A1
Автор: Donde Yariv, Nguyen Jeremiah H.
Принадлежит: ALLERGAN, INC.

Disclosed herein are compounds having a formula: 2. The compound of claim 1 , wherein L is C-Calkylene.3. The compound of claim 1 , wherein L is Calkylene.4. The compound of claim 1 , wherein A is phenylene claim 1 , thiophenylene claim 1 , furylene claim 1 , pyridinylene claim 1 , oxazolylene claim 1 , or thiazolylene.5. The compound of claim 4 , wherein A is thiophenylene.6. The compound of claim 1 , wherein B is substituted phenyl.7. The compound of claim 6 , wherein the substituent is 1-hydroxyhexyl.8. The compound of claim 1 , wherein Ris —H claim 1 , —CHOH claim 1 , or phenyl.9. The compound of claim 1 , wherein Ris —H.10. The compound of claim 1 , wherein Ris C-Calkyl.11. The compound of claim 1 , wherein Ris isopropyl.13. A composition comprising at least one compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and at least one pharmaceutically acceptable excipient.14. A method of treating glaucoma or ocular hypertension comprising administering to a subject in need thereof a compound according to or a pharmaceutically acceptable salt thereof.15. The method of wherein the subject is human.16. A kit comprising the composition of claim 13 , a container claim 13 , and instructions for administration of the composition to a subject in need thereof for the treatment of glaucoma or ocular hypertension. This application is a non-provisional application claiming the benefit of U.S. provisional application 61/829,892 filed on May 31, 2013, and U.S. provisional application 61/835,059 filed on Jun. 14, 2013, each of which is incorporated by reference in their entirety and serve as the basis for a priority claim of the present application.The present invention relates generally to compounds and methods for treating ocular disorders. The invention relates in particular to the use of certain well-defined substituted cyclopentenes for the treatment of ocular hypertension and glaucoma.Ocular hypotensive agents are useful in the treatment ...

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Номер записи: 94
11-11-2021 дата публикации

THIOPHENE CARBOXAMIDE DERIVATIVE AND PLANT DISEASE CONTROL AGENT COMPRISING SAME

Номер: US20210347755A1
Автор: JUN Kyung-Jin, KIM Do-hyoung, LEE Han-Young, Oh In Young, PARK Ki-Ju, Ryu Jae Wook, SHIN Myeong Su, SONG Min-Young, YEOM Hyun Suk
Принадлежит:

The present invention provides a thiophene carboxamide compound of the following General Formula (I), which is a novel fluorine-substituted biphenyl carboxamide-based compound, and provides a useful compound, as an agricultural and horticultural plant disease control agent, exhibiting an excellent control effect at a low dose. 2. The compound of claim 1 , wherein Y is a hydrogen atom and m is 0.3. The compound of claim 2 , wherein Y is a hydrogen atom; m is 0; R is (C1˜C6)alkyl claim 2 , (C2˜C6)alkenyl claim 2 , (C2˜C6)alkynyl claim 2 , (C1˜C6)alkyl which may be substituted by 1 to 5 halogen atoms claim 2 , (C1˜C3)alkyl which may be substituted with (C3˜C6)cycloalkyl claim 2 , (C1˜C3)alkyl which may be substituted with phenyl or pyridine claim 2 , phenyl(C1˜C3)alkyl (which may be substituted with a halogen atom) claim 2 , phenyl(C1˜C3)alkyl which may be substituted with (C1˜C4)alkyl claim 2 , or phenyl(C1˜C3)alkyl which may be substituted with (C1˜C4)alkoxy; R1 is (C1˜C4)alkyl or (C1˜C4)alkyl substituted with 1 to 3 halogen atoms; and R2 and R3 are a hydrogen atom.4. The compound of claim 3 , wherein Y is a hydrogen atom claim 3 , m is 0 claim 3 , R is (C1˜C6)alkyl or (C1˜C4)alkyl which may be substituted by 1 to 3 halogen atoms; R1 is methyl claim 3 , and R2 and R3 are a hydrogen atom.5. A plant disease control agent for agricultural and horticultural use claim 1 , comprising as an active ingredient the compound of the General Formula (I) according to claim 1 , a derivative thereof or a salt thereof.6. A method for controlling a plant disease claim 1 , comprising applying to a plant of interest or soil an effective amount of a compound of the General Formula (I) according to claim 1 , a derivative thereof or a salt thereof.7. (canceled) This application claims priority to Korean Application No. 10-2018-0119984 filed on Oct. 8, 2018, and all contents disclosed in the specification and drawings of the application are incorporated herein by reference.The present ...

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Номер записи: 95
05-09-2019 дата публикации

CYTOTOXIC AND ANTI-MITOTIC COMPOUNDS, AND METHODS OF USING THE SAME

Номер: US20190269785A1
Автор: BABCOOK John, Bourque Elyse Marie Josee, HEDBERG Bradley John, HSIEH Tom Han Hsiao, MANDEL Alexander Laurence, RICH James R., Winters Geoffrey C.
Принадлежит:

Compounds having cytotoxic and/or anti-mitotic activity are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having cytotoxic and/or anti-mitotic activity. 122.-. (canceled)23. A conjugate having the following structure:{'br': None, '(T)-(L)-(PT)\u2003\u2003 (VII)'}wherein (T) is a targeting moiety, (L) is a linker, and (PT) is a hemiasterlin analog, andwherein (PT) is covalently linked to (L) through the side chain of the N-terminal amino acid of (PT).2428.-. (canceled)31. The conjugate according to claim 30 , wherein Ris optionally substituted aryl or optionally substituted heteroaryl.32. The conjugate according to claim 30 , wherein Z is OH claim 30 , SH or NH.35. The conjugate according to claim 34 , wherein Ris optionally substituted aryl or optionally substituted heteroaryl.36. The conjugate according to claim 34 , wherein Ris optionally substituted aryl.38. The conjugate according to claim 37 , wherein Ris optionally substituted aryl or optionally substituted heteroaryl.39. The conjugate according to claim 37 , wherein Ris optionally substituted aryl.42. The conjugate according to claim 23 , wherein (L) is a cleavable linker.43. The conjugate according to claim 23 , wherein (L) is a cleavable linker comprising a self-immolative component.44. The conjugate according to claim 43 , wherein the self-immolative component comprises p-aminobenzylcarbamoyl (PABC).45. The conjugate according to claim 23 , wherein (L) comprises sulfosuccinimidyl 6-[3′(2-pyridyldithio)-propionamido]hexanoate (sulfo-LC-SPDP) claim 23 , succinimidyl 4-[N-maleimidomethyl]cyclohexane-1-carboxylate (SMCC) or maleimidocaproyl-valine-citrulline-PABC (MC-VC-PABC).47. The conjugate according to claim 23 , wherein (T) is an antibody or an ...

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Номер записи: 96
27-08-2020 дата публикации

SYNTHESIS OF CANTHARIDIN

Номер: US20200270269A1
Автор: Davidson Matthew Gene, Eklov Brian Matthew, Loertscher Brad Melvin, Schow Steven R., Wuts Peter
Принадлежит: Verrica Pharmaceuticals, Inc.

The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions). 2. The method of claim 1 , wherein the reaction is carried out in the absence of added acid.36-. (canceled)7. The method of claim 1 , wherein the reaction is carried out in the absence of a Brønsted acid.8. The method of claim 1 , wherein the reaction is carried out at a pressure of approximately 1 atm.9. The method of claim 1 , wherein the reaction is carried out in the absence of added acid and in the absence of increased pressure.10. The method of claim 1 , wherein the reaction is carried out in a solvent.1116-. (canceled)17. The method of claim 1 , wherein the reaction is carried out in the absence of solvent.1821-. (canceled)22. The method of claim 1 , wherein the reaction is carried out at a temperature below 100° C.23. The method of claim 22 , wherein the reaction is carried out at approximately room temperature.2429-. (canceled)30. The method of claim 1 , wherein furan is present in greater than 1 equivalent relative to the amount of Compound (2) in the reaction mixture.31. The method of claim 30 , wherein the ratio of Compound (2) to furan in the reaction mixture is from 1:4 to 1:5.32. (canceled)33. The method of claim 1 , wherein the Compound (1) is formed in exo/endo ratio of about 70:30 to 99:1.3436-. (canceled)37. The ...

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Номер записи: 97
20-10-2016 дата публикации

A PROCESS FOR THE SYNTHESIS OF ARYL SULFONES

Номер: US20160304447A1
Автор: Mhaske Santosh Baburao, Pandya Virat
Принадлежит:

The present patent discloses a novel, efficient and transition-metal-free room temperature single step process for synthesis of aryl sulfones and substituted aryl sulfones starting from aryl substrates. 2. The process according to claim 1 , wherein the fluoride ion source is selected from the group consisting of TBAF (Tetra-n-butylammonium fluoride) claim 1 , CsF (Cesium fluoride) claim 1 , NaF (Sodium Fluoride) claim 1 , RbF (Rubidium fluoride) or KF (Potassium fluoride).3. The process according to claim 1 , wherein the fluoride ion source is selected from TBAF or CsF.4. The process according to claim 1 , wherein the compound of formula I is selected from the group consisting of:1-Phenyl (sulfonyl)benzene (3);1,2-Difluoro-4-(phenylsulfonyl)benzene (5);1,2-Dimethyl-4-(phenylsulfonyl)benzene (7);1,4-Dimethyl-2-(phenylsulfonyl)benzene (9);1-Methoxy-3-(phenylsulfonyl)benzene (11);1,3-Dimethoxy-5-(phenylsulfonyl)benzene (13);1,2-Dimethoxy-4-(phenylsulfonyl)benzene (15);5-(Phenylsulfonyl)benzo[d][1,3]dioxole (17);(Methylsulfonyl)benzene (19);(Butylsulfonyl)benzene (21);1-Methyl-4-(phenylsulfonyl)benzene (23);1-(Tert-butyl)-4-(phenylsulfonyl)benzene (25);1-Methoxy-4-(phenylsulfonyl)benzene (27);1-(4-(phenylsulfonyl)phenyl)ethan-1-one (29);1-Nitro-4-(phenylsulfonyl)benzene (31);1-Fluoro-4-(phenylsulfonyl)benzene (33);2-bromo-5-(phenylsulfonyl)thiophene (35).5. The process according to claim 1 , wherein the compound of formula II is selected from the group consisting of:2-(trimethylsilyl)phenyl trifluoromethane-sulfonate (1)4,5-difluoro-2-(trimethylsilyl)phenyl trifluoromethane-sulfonate (4)4,5-dimethyl-2-(trimethylsilyl)phenyl trifluoromethane-sulfonate (6)3,6-dimethyl-2-(trimethylsilyl)phenyl trifluoromethane-sulfonate (8)3-methoxy-2-(trimethylsilyl)phenyl trifluoromethane-sulfonate (10)3,5-dimethoxy-2-(trimethylsilyl)phenyl trifluoromethane-sulfonate (12)4,5-dimethoxy-2-(trimethylsilyl)phenyl trifluoromethane-sulfonate (14)6-(trimethylsilyl)benzo[d][1,3]dioxol-5-yl ...

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Номер записи: 98
20-10-2016 дата публикации

SMALL MOLECULE INHIBITORS OF MCL-1 AND USES THEREOF

Номер: US20160304485A1
Автор: Mady Ahmed, Miao Lei, Nikolovska-Coleska Zaneta, STUCKEY Jeanne A.
Принадлежит:

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having benzoic acid structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases. 2. The compound of claim 1 , wherein R1 claim 1 , R2 claim 1 , R3 claim 1 , R4 claim 1 , X or Y claim 1 , independently include any chemical moiety that permits the resulting compound to bind the BH3 binding pocket of an Mcl-1 protein.3. The compound of claim 1 , wherein X-R1 is a substituted or non-substituted moiety comprising H claim 1 , C claim 1 , N claim 1 , O claim 1 , and/or S.6. The compound of claim 1 , wherein R2 is a substituted or non-substituted moiety comprising H claim 1 , C claim 1 , N claim 1 , O claim 1 , and/or S.11. The compound of claim 1 , wherein R4 is an acid moiety claim 1 , an ester moiety claim 1 , and/or a carboxylic bioisostere moiety.14. The compound of claim 1 , wherein the compound is comprised within a pharmaceutical composition.15. A method of treating claim 14 , ameliorating claim 14 , or preventing a hyperproliferative disease in a patient comprising administering to said patient a therapeutically effective amount of the pharmaceutical composition of claim 14 ,wherein said hyperproliferative disease is cancer, wherein said cancer is head and neck cancers, colon cancer, lung cancer, ovarian cancer, prostate cancer, multiple myeloma, acute myeloid leukemia, melanoma, breast cancer, and/or pancreatic cancer,wherein said patient is a human patient.16. The method of further comprising administering to said patient one or more anticancer agents claim 15 ,wherein said anticancer agent one or more of a chemotherapeutic agent, and radiation therapy.17. The method of claim 15 , wherein said compound is capable of one or more of binding with a Mcl-1 protein and/or binding the BH3 groove within Mcl-1 claim 15 ,wherein said binding results in inhibited Mcl-1 protein ...

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Номер записи: 99
29-10-2015 дата публикации

Water-soluble photochromic molecules

Номер: US20150307541A1
Автор: Hiroaki Tokiwa, Kiyoshi Ikeda, Masahiro Irie, Tadamune OTSUBO
Принадлежит: Rikkyo Educational Corp

A diarylethene compound having high water-solubility is provided, and the compound is a diarylethene compound of formula (I) wherein, Sg is a monovalent sugar-type residue consisting of a sugar-type compound (in which some of hydroxyl groups may be protected) selected from a group consisting of a six-membered ring sugar, a five-membered ring sugar, cyclitol and oligosaccharides containing a six-membered ring sugar, a five-membered ring sugar, or cyclitol and excluding an hydroxyl group; U is —(CH 2 )n-, —CH 2 —U′—, or —C(═O)— (wherein, n is an integer of 1 to 5, U′ is a C1-C10 alkyl group binding to Ar); and Ar is a group represented by formula (A1) or (A2); wherein, X is S, SO 2 , NR 3 (R 3 is a C1-C3 alkyl group) or O, R is C1-C4 alkyl group, R 1 and R 2 are independently a C1-C3 alkyl group, a is 0 or 1, b is an integer of 0-3, and * represents a bond with U); Y is a hydrogen atom or a halogen atom; m is an integer of 5-7.

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Номер записи: 100