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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 3954. Отображено 100.
02-02-2012 дата публикации

Heterocycle-amino acid derivatives for targeting cancer tissue and radioactive or non-radioactive labeled compounds thereof

Номер: US20120029177A1
Автор: Dinesh Shetty, Dong Soo Lee, Jae Min Jeong, June Key Chung, Myung Chul Lee
Принадлежит: SNU R&DB FOUNDATION

The present invention relates to novel amino acid derivatives containing heterocyclic chelating residues thereof; radioactive or nonradioactive metal complexes thereof; methods for preparation thereof; and apyrogenic and sterile preparative kits of the composition for targeting cancer cells. The compounds of the present invention can easily be taken up to cancer cells as they contain amino acid residues thereof; radioactive or nonradioactive metals can be labeled easily as they contain heterocyclic chelating residues thereof; cancer lesion can be imaged easily by targeting using the present invention.

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Номер записи: 1
24-05-2012 дата публикации

Dual-acting antihypertensive agents

Номер: US20120129900A1
Автор: Daniel Marquess, Keith Jendza, Paul R. Fatheree, Robert M. McKinnell, Ryan Hudson, Seok-Ki Choi, Sharath Hegde, Vivek Sasikumar
Принадлежит: Theravance Inc

The invention is directed to compounds of formula I: wherein Ar, r, R 3 , X, and R 5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula I have AT 1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.

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Номер записи: 2
20-12-2012 дата публикации

Process and intermediate compounds useful in the preparation of statins

Номер: US20120323011A1
Автор: David John Moody, Jonathan William Wiffen
Принадлежит: Redx Pharna PLC

There is provides a process for the preparation of a compound of formula (7): wherein R is an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group; provides that R is not a compound of Formula (a): wherein R a represents an alkyl group, such as a C 1-16 alkyl group, and preferably an isopropyl group; R b represents an aryl group, preferably a 4-fluorophenyl group; R c represents hydrogen, a protecting group or an alkyl group, such as a C 1-16 alkyl group, and preferably a methyl group; and Rd represents hydrogen, a protecting group or a SO 2 R e group where R e is an alkyl group, such as a C 1-16 alkyl group, and preferably a methyl group.

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Номер записи: 3
21-03-2013 дата публикации

Propynoic Acid Carbamoyl Methyl-Amides and Pharmaceutical Compositions and Methods Based Thereon

Номер: US20130071328A1
Автор: NEAMATI Nouri, PETASIS Nicos A., YAMADA Roppei
Принадлежит: UNIVERSITY OF SOUTHERN CALIFORNIA

This invention discloses a series of novel propynoic acid carbamoyl methyl-amides (PACMAs), methods for synthesizing the PACMAs and pharmaceutical compositions containing the PACMAs. These novel compounds and compositions show cytotoxicity in cancer cells and are useful as lead compounds for anti-cancer drugs or pharmaceutical agents. This invention also discloses treatment methods that uses the PACMAs and pharmaceutical compositions as well as methods for promoting the release and nuclear localization of the transcription factor Nrf2. 4. A compound according to claim 1 , wherein said compound further contains a substituent capable of being used in a biological or medical diagnostic imagining technique to quantify or identify associated biomarker proteins.5. A compound according to claim 3 , wherein said compound further contains a substituent capable of being used in a biological or medical diagnostic imagining technique to quantify or identify associated biomarker proteins.7. A pharmaceutical composition comprising any of the compounds of to and a pharmaceutically acceptable carrier.8. A method for treatment a cancer subject claim 3 , comprising the step of:{'claim-ref': {'@idref': 'CLM-00004', 'claim 4'}, 'administering to a person in need of said treatment method an effective amount of the pharmaceutical composition according to .'}9. A method of claim 8 , where the cancer is: breast cancer claim 8 , ovarian cancer claim 8 , prostate cancer claim 8 , colon cancer claim 8 , brain cancer claim 8 , pancreatic cancer claim 8 , skin cancer claim 8 , lung cancer claim 8 , and multiple myeloma.10. A method for promoting the release and nuclear localization of the transcription factor Nrf2 comprising the step of:{'claim-ref': {'@idref': 'CLM-00004', 'claim 4'}, 'administering an effective amount of the pharmaceutical compositions according to .'}10. A biological or medical diagnostic imaging technique claim 8 , comprising:{'claim-ref': [{'@idref': 'CLM-00004', 'claims 4 ...

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Номер записи: 4
18-04-2013 дата публикации

SUBSTITUTED AMINOPROPIONIC DERIVATIVES AS NEPRILYSIN INHIBITORS

Номер: US20130096127A1
Автор: Coppola Gary Mark, IWAKI Yuki, KARKI Rajeshri Ganesh, KAWANAMI Toshio, KSANDER Gary Michael, MOGI Muneto, Sun Robert
Принадлежит: NOVARTIS AG

The present invention provides a compound of formula I′; 3. The compound of wherein:{'sup': '1', 'sub': '1-7', 'Ris H or Calkyl;'}{'sup': 2', 'a', 'b', 'a', 'b, 'sub': 1-7', '3-7', '1-7', '1-7', '6-20', '1-7, 'Rfor each occurrence, is independently Calkyl, halo, Ccycloalkyl, hydroxy, Calkoxy, haloCalkyl, —NRR, Caryl, heteroaryl or heterocyclyl; wherein Rand Rfor each occurrence are independently H or Calkyl;'}{'sup': 3', '1', '1, 'Ris A-C(O)X;'}{'sup': '5', 'Ris H; and'}{'sup': 1', 'a', 'b, 'sub': '1-7', 'X and Xare independently OH, —O—Calkyl or NRR;'}{'sup': '1', 'Bis —C(O)NH— or —NHC(O)—;'}{'sup': '1', 'sub': 1-7', '3-7', '1-7', '3-7, 'Ais a linear or branched Calkylene; which is optionally substituted with one or more substituents independently selected from the group consisting of halo, Ccycloalkyl, Calkoxy, hydroxy and O-acetate; in which two geminal alkyl can optionally combine to form a Ccycloalkyl; or'}and wherein each heteroaryl is a monocyclic or bicyclic aromatic ring comprising 5-10 ring atoms selected from carbon atoms and 1 to 5 heteroatoms, and', 'each heterocyclyl is a monocyclic saturated or partially saturated but non-aromatic moiety comprising 4-7 ring atoms selected from carbon atoms and 1-5 heteroatoms, wherein each heteroatom of a heteroaryl or a heterocyclyl is independently selected from O, N and S, or a pharmaceutically acceptable salt thereof., 'n is 0, 1, 2, 3, 4 or 5;'}6. The compound of wherein Ais an optionally substituted linear or branched Calkylene claim 1 , or a pharmaceutically acceptable salt thereof.7. The compounds of wherein Ais CHCH claim 1 , or a pharmaceutically acceptable salt thereof.810-. (canceled)11. The compound of wherein Ris H claim 1 , Ris independently halo claim 1 , Calkoxy claim 1 , hydroxy claim 1 , Calkyl or halo-Calkyl claim 1 , n is 0 claim 1 , 1 or 2 and X and Xare independently OH or —O—Calkyl claim 1 , or a pharmaceutically acceptable salt thereof.12. The compounds of wherein n is 1 or 2; Ris meta-chloro ...

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Номер записи: 5
18-04-2013 дата публикации

Substituted carbamoylmethylamino acetic acid derivatives as novel NEP inhibitors

Номер: US20130096168A1
Автор: IWAKI Yuki, KAWANAMI Toshio, KSANDER Gary Michael, MOGI Muneto
Принадлежит: NOVARTIS AG

The present invention provides a compound of formula I; 119-. (canceled)22. The compound according to wherein s is 0; or a pharmaceutically acceptable salt thereof.23. The compounds according to wherein{'sup': '2', 'Xis Cl, or a pharmaceutically acceptable salt thereof.'}24. The compound according to selected from:(S)-2-[(S)-2-(3′-chloro-biphenyl-4-yl)-1-(1H-tetrazol-5-ylcarbamoyl)-ethylamino]-propionic acid ethyl ester;(S)-2-[(S)-2-(3′-chloro-biphenyl-4-yl)-1-(1H-tetrazol-5-ylcarbamoyl)-ethylamino]-propionic acid; and(S)-2-[(S)-2-(3′-Chloro-biphenyl-4-yl)-1-(3-hydroxy-isoxazol-5-ylcarbamoyl)-ethylamino]-propionic acid; or a pharmaceutically acceptable salt thereof.25. A pharmaceutical composition comprising a compound according to or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable carriers.26. A pharmaceutical composition comprising a compound according to or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable carriers.27. A combination comprising: a compound according to claim 20 , or a pharmaceutically acceptable salt thereof and one or more therapeutically active agents selected from HMG-Co-A reductase inhibitor claim 20 , an anigiotensin receptor blocker claim 20 , angiotensin converting enzyme Inhibitor claim 20 , a calcium channel blocker claim 20 , an endothelin antagonist claim 20 , a renin inhibitor claim 20 , a diuretic claim 20 , an ApoA-I mimic claim 20 , an anti-diabetic agent claim 20 , an obesity-reducing agent claim 20 , an aldosterone receptor blocker claim 20 , an endothelin receptor blocker claim 20 , an aldosterone synthase inhibitors claim 20 , a CETP inhibitor and a phophodiesterase type 5 (PDE5) inhibitor.28. A combination comprising: a compound according to or a pharmaceutically acceptable salt thereof and one or more therapeutically active agents selected from HMG-Co-A reductase inhibitor claim 24 , an anigiotensin receptor blocker claim 24 , angiotensin converting ...

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Номер записи: 6
02-05-2013 дата публикации

SPIRO COMPOUNDS AND PHARMACEUTICAL USE THEREOF

Номер: US20130109710A1
Автор: Aoyagi Kouichi, Katoh Susumu, Manabe Tomoyuki, Sasaki Shin-Ya, Shimada Takashi, Tsutsumi Kazuhiro, Ueno Hiroshi
Принадлежит: JAPAN TOBACCO INC.

The spiro compound represented by the following general formula [Ia], its pharmaceutically acceptable salt or a solvate thereof 3. The spiro compound claim 1 , the pharmaceutically acceptable salt thereof or the solvate thereof as claimed in claim 1 , wherein the number of the double bond in ring A of the spiro-ring AB is 0 or 1.4. The spiro compound claim 1 , the pharmaceutically acceptable salt thereof or the solvate thereof as claimed in claim 1 , wherein the number of the double bond in ring B of the spiro-ring AB is 0 or 1.5. The spiro compound claim 1 , the pharmaceutically acceptable salt thereof or the solvate thereof as claimed in claim 1 , wherein n3 is 1 or 2.6. The spiro compound claim 1 , the pharmaceutically acceptable salt thereof or the solvate thereof as claimed claim 1 , wherein the spiro-ring AB may be substituted by 1 to 3 same or different substituent(s).7. The spiro compound claim 1 , the pharmaceutically acceptable salt thereof or the solvate thereof as claimed in claim 1 ,{'sup': '1', 'wherein Ris'}(1) a hydrogen atom,{'sub': 1', '6, '(2) a C-Calkyl group,'}{'sub': 2', '6, '(3) a C-Calkenyl group,'}{'sub': 2', '6, '(4) a C-Calkynyl group,'}{'sub': 1', '6, '(5) a C-Calkoxy group,'}{'sub': 1', '6', '1', '6, '(6) a C-Calkoxy(C-C)alkyl group,'}{'sup': 11', '12', '11', '12, 'sub': 1', '6, '(7) —CONRRin which Rand Rare the same or different and each represents a hydrogen atom or a C-Calkyl group, or'}{'sub': 1', '6, '(8) a five-membered heteroaryl group which has at least one heteroatom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, and which may be substituted by a C-Calkyl group.'}8. The spiro compound claim 1 , the pharmaceutically acceptable salt thereof or the solvate thereof as claimed in claim 1 ,{'sup': '1', 'wherein Ris'}(1) a hydrogen atom,{'sub': 2', '6, '(2) a C-Calkenyl group,'}{'sub': 2', '6, '(3) a C-Calkynyl group,'}{'sub': 1', '6, '(4) a C-Calkoxy group or'}{'sub': 1', '6, '(5) a five- ...

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Номер записи: 7
30-05-2013 дата публикации

HIGHLY CRYSTALLINE VALSARTAN

Номер: US20130137737A1
Автор: Burgbacher Jens, Hahn Björn Thomas, Rampf Florian Andreas, Schneeberger Ricardo
Принадлежит: NOVARTIS AG

The present invention describes a highly crystalline form of valsartan, pharmaceutical compositions thereof and process for the preparation thereof. 1. A highly crystalline form of valsartan characterized by an XRPD pattern with a peak at about 31.0±0.2 degrees 2-theta and substantially lacking X-ray diffraction peaks between 0 and 8±0.2 degrees 2-theta.2. A highly crystalline form of valsartan having a peak melting point temperature of 140.8° C.±3° C.4. A process for the preparation of a highly crystalline form of valsartan comprising:(a) combining solid valsartan with a solvent that is an ester,(b) heating said combination to a temperature below complete dissolution of the solid valsartan;(c) stirring said mixture for a time effective to form a suspension with the solvents therein that form a mother liquor;(d) separating the solids in the suspension from the mother liquor; and(e) drying said solids to give a highly crystalline form of valsartan.5. A pharmaceutical composition comprising a pharmaceutically effective amount of the highly crystalline form of valsartan of in combination with a pharmaceutically acceptable carrier.6. A method for treating hypertension or elevated blood pressure in a patient comprising administering a pharmaceutical composition comprising a pharmaceutically effective amount of the highly crystalline form of valsartan of in combination with a pharmaceutically acceptable carrier to a patient in need thereof. Polymorphs of valsartan and/or salts thereof are described in China patent publication 200410067406.8, WO2004/083192; WO2007/017897; US Patent Publication 2008/0261959; WO2003/089417 A1; WO2006/076561 A1; WO2003/066606; WO2002/06253, U.S. Pat. No. 6,869,970. However, there remains a need to provide a form of valsartan that has a greater degree of crystallinity compared to known forms or polymorphs of valsartan.The present invention relates to a novel, highly crystalline form of valsartan, pharmaceutical compositions thereof and process ...

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Номер записи: 8
06-06-2013 дата публикации

PROCESS FOR THE PREPARATION OF VALSARTAN

Номер: US20130144067A1
Автор: Aminul Islam, Budidet Shankar Reddy, Chinta Raveendra Reddy, Meenakshisunderam Sivakumaran, Nangi Gangadhara Bhima Shankar, Nayini Mahendar Reddy, Yallapa Somappa Somannavar
Принадлежит:

The present invention relates to a process for the preparation of pure Valsartan (I) substantially free from impurities of formulae (Ia), (Ib), and (Ic), which comprises: (i) condensing 2-(4′-bromomethylphenyl)benzonitrile of formula (II) with L-valine methyl ester hydrochloride of formula (V) in the presence of a base in a solvent to produce N-[(2′-cyanobiphenyl-4-yl)methyl]-(L)-valine methyl ester of formula (VI); (ii) treating the compound VI of step (i) with acid followed by treating with base to produce pure compound VI substantially free from dimeric impurity of formula (Via); (iii) reacting the pure compound of formula (VI) with n-valeryl chloride in the presence of a base to produce pure N-valeryl-N-[(2′-cyanobiphenyl-4-yl)methyl]-(L)-valine methyl ester (VII) substantially free from alkene impurity of formula (Vila); (iv) reacting the compound of formula (VII) with trialkyltin chloride and a metal azide in a solvent at a reflux temperature to produce N-(1-oxopentyl)-N-[[2′-(2-tributyltinte-trazol-5-yl)-(1,1′-biphenyl)-4-yl]methyl]-(L)-valine methyl ester of formula (VHIb) free from thermal degradation impurity (Villa); (v) hydrolyzing the compound of formula (VHIb) in the presence of alkaline conditions to produce Valsartan (I). 2. The process according to claim 1 , wherein the above process is carried out without isolating the intermediate compounds N-[(2′-cyanobiphenyl-4-yl)methyl]-(L)-valine methyl ester (VI) claim 1 , N-valeryl-N-[(2′-cyanobiphenyl-4-yl)methyl]-(L)-valine methyl ester (VII) and N-(1-oxopentyl)-N-[[2′-(2-tributyltintetrazol-5-yl)-(1 claim 1 ,1′-biphenyl)-4-yl]methyl]-(L)-valine methyl ester (VIIIb).3. The process according to claim 1 , wherein the base used in step-(i) is selected from sodium carbonate claim 1 , sodium bicarbonate claim 1 , potassium carbonate claim 1 , and the solvent is selected from ethers claim 1 , esters claim 1 , chlorinated solvents or mixtures thereof.4. The process according to claim 1 , wherein the acid used in ...

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Номер записи: 9
20-06-2013 дата публикации

LIPOMACROCYCLES AND USES THEREOF

Номер: US20130156851A1
Автор: Cui Kunyuan, Liang Dong
Принадлежит:

What is described are macrocyclic compounds formed by reaction of a cyclic compound, which contains an amine, with an epoxide. The macrocyclic compound has the following structure: 2. The macrocyclic compound of claim 1 , comprising at least one amine.5. The macrocyclic compound of claim 4 , comprising a quaternary ammonium or a tertiary amine or both.6. The macrocyclic compound of claim 1 , wherein the cyclic compound is reacted with an amount of epoxide that is proportional to the number of amines in the cyclic compound.7. The macrocyclic compound of claim 1 , wherein the cyclic compound is reacted with an amount of epoxide that is less than the number of amines in the cyclic compound.8. The macrocyclic compound of claim 1 , wherein the cyclic compound is reacted with an amount of epoxide that is proportional to the amount of the cyclic compound.9. The macrocyclic compound of claim 4 , wherein R′ consists an molecular substituent selected from the group consisting of CH2—O—(CH2)9CH3 claim 4 , CH2—O—(CH2)11CH3 claim 4 , CH2—O—(CH2)13CH3 claim 4 , (CH2)9CH3 claim 4 , (CH2)11CH3 claim 4 , (CH2)11CH3 claim 4 , (CH2)13CH3 claim 4 , (CH2)15CH3 and CH2—O—CH(CH2CH3)((CH2)11CH3).10. (canceled)11. (canceled)12. (canceled)13. (canceled)14. (canceled)15. The macrocyclic compound according to any of claim 1 , wherein the macrocyclic compound is in a lipid-polynucleotide particle comprising a lipid and a polynucleotide.16. The macrocyclic compound according to any of claim 14 , wherein the polynucleotide is an RNA molecule.17. The macrocyclic compound of claim 16 , wherein the RNA molecule is an siRNA molecule.18. (canceled)19. The macrocyclic compound according to any of claim 1 , wherein the macrocyclic compound is a component of a liposome or a lipid particle.20. (canceled)21. (canceled)22. (canceled)23. (canceled)24. The macrocyclic compound according to any of claim 2 , wherein the macrocyclic compound is in a lipid-polynucleotide particle comprising a lipid and a ...

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Номер записи: 10
20-06-2013 дата публикации

INTERMEDIATES FOR THE PREPARATION OF HMG COA REDUCTASE INHIBITORS AND PROCESSES FOR THE PREPARATION THEREOF

Номер: US20130158263A1
Автор: DWIVEDI Shriprakash Dhar, PATEL Dhimant Jasubhai, Rupapara Mahesh Laljibhai
Принадлежит:

A compound of Formula (1), is disclosed 13. The process as claimed in step (a) of claim 12 , wherein the suitable organic solvent comprises one or more of toluene claim 12 , xylene claim 12 , ethylbenzene claim 12 , cyclohexane claim 12 , hexane claim 12 , heptane claim 12 , methylene dichloride claim 12 , ethylene dichloride claim 12 , and ethyl acetate.14. The process as claimed in step (a) of claim 12 , wherein the base comprises one or more inorganic bases selected from the group consisting of sodium hydroxide claim 12 , potassium hydroxide claim 12 , sodium bicarbonate claim 12 , potassium bicarbonate claim 12 , and sodium hydride claim 12 , or one or more organic bases selected from the group consisting of triethylamine claim 12 , diisopropylethylamine claim 12 , diisopropyl amine claim 12 , 1 claim 12 ,8-diazabicycloundec-7-ene (DBU) claim 12 , and pyridine.15. The process as claimed in step (c) of claim 12 , wherein the dialkylalkoxyborane is selected from group consisting of diethylmethoxyborane claim 12 , diethylethoxyborane claim 12 , and dimethylethoxyborane.16. The process as claimed in step (c) of claim 12 , wherein the base comprises one or more of alkali metal hydrides selected from the group consisting of sodium hydride claim 12 , potassium hydride claim 12 , lithium hydride claim 12 , sodium borohydride claim 12 , potassium borohydride claim 12 , and lithium aluminium hydride.17. The process as claimed in step (c) of claim 12 , further comprising purifying the compound of Formula (5′) in a suitable organic solvent selected from the group consisting of one or more of C-Calcohol claim 12 , water claim 12 , and aliphatic hydrocarbons.18. The process as claimed in step (d) of claim 12 , wherein the suitable reagent comprises one or more of 2 claim 12 ,2-dimethoxypropane claim 12 , 2 claim 12 ,2-dimethoxypentane claim 12 , 1 claim 12 ,1-dimethoxycyclohexane claim 12 , and 2 claim 12 ,2-dimethoxybutane.19. The process as claimed in step (d) of claim 12 , ...

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Номер записи: 11
25-07-2013 дата публикации

Hydrothiolation of Unactivated Alkenes

Номер: US20130190505A1
Автор: Jimmy Wu, Markku A. Savolainen
Принадлежит: Dartmouth College

The present invention is a method for promoting hydrothiolation of an unactivated alkenes with a thiol using gallium triflate.

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Номер записи: 12
15-08-2013 дата публикации

TETRAZOLIUM COMPOUND FOR DETECTING MICROORGANISMS, REAGENT FOR DETECTING MICROORGANISMS AND METHOD FOR DETECTING MICROORGANISMS

Номер: US20130210065A1
Автор: Onji Yuichi, Ushiyama Masashi
Принадлежит: JNC CORPORATION

The object of the present invention is to provide a compound used in a reagent for detecting microorganisms, by which microorganisms can be rapidly and reliably detected without requiring any special instrument, the reagent for detecting microorganisms, and a method for detecting microorganisms. The object can be achieved by a tetrazolium compound represented by general formula (I) below:

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Номер записи: 13
29-08-2013 дата публикации

METHOD AND DEVICE FOR THE DETECTION OF SULPHUR CONTAINING SPECIES

Номер: US20130224873A1
Автор: Fallis Ian, Morgan Ian
Принадлежит:

A method is provided for detecting sulphur-containing species (such as thiophosphorous esters, in particular phosphorylating agents), in which a suspected sulphur-containing species is brought into contact with a tetrazolium compound in the presence of base, typically at a pH of at least 8. A device, kit and tetrazolium compounds for use in such a method are also disclosed. 1. A method for the detection of sulphur containing species , the method comprising:bringing together a tetrazolium reagent, a suspected sulphur-containing species and one of:a base in aqueous alkaline conditions or a nucleophilic base in non-aqueous conditions.2. The method according to claim 1 , wherein the tetrazolium reagent claim 1 , the suspected sulphur-containing species claim 1 , and base are brought together in aqueous alkaline conditions claim 1 , wherein the pH is at least 10.3. The method according to claim 2 , wherein the pH is at least 12.4. (canceled)5. The method according to claim 1 , wherein the tetrazolium reagent is substantially stable to exposure to UV and visible light and substantially stable in the presence of base and substantially stable in the presence of base whilst exposed to UV or visible light.6. The method according to claim 1 , wherein the suspected sulphur-containing species is a species comprising a sulphur moiety bonded with a single bond to an adjacent moiety.7. (canceled)8. The method according to which comprises a method for detecting sulphur-containing phosphorylating agents claim 1 , the method comprising bringing together a tetrazolium reagent claim 1 , a species suspected of being a sulphur-containing phosphorylating agent and one of:a base in aqueous alkaline conditions or a nucleophilic base in non-aqueous conditions.9. method according to comprising sensing for the presence of colouration.10. (canceled)11. (canceled)12. The method according to comprising bringing together the suspected sulphur-containing species claim 1 , the base and tetrazolium ...

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Номер записи: 14
29-08-2013 дата публикации

USE OF AZIDES IN SYNTHESIS

Номер: US20130225819A1
Автор: Jamison Timothy F., Palde Prakash B.
Принадлежит: Massachusetts Institute of Technology

Described herein are inventive methods for synthesis of tetrazoles. In some embodiments, the method involves the use of a flow reactor. The methods provided herein are capable at being carried out in short reaction times, with high yields, with minimal side reactions, and/or with minimal chance of explosions caused by the presence of azides. 4. The method of claim 1 , wherein the reacting is carried out in the presence of a catalyst.5. The method of claim 4 , wherein the catalyst is ZrBr.6. The method of claim 4 , wherein the catalyst is provided in an amount of about 0.5 equiv claim 4 , about 0.75 equiv claim 4 , about 1 equiv claim 4 , about 1.5 equiv claim 4 , about 2 equiv claim 4 , about 3 equiv claim 4 , about 4 equiv claim 4 , or about 5 equiv. of the compound of formula (I).7. The method of claim 1 , wherein the reacting is carried out in a flow reactor.8. The method of claim 1 , wherein the azide source is NaN.9. The method of claim 1 , wherein the ratio of the azide source to a compound about formula (I) is about 1:1 claim 1 , about 1.05:1 claim 1 , about 1.1:1 claim 1 , about 1.2:1 claim 1 , about 1.3:1 claim 1 , about 1.4:1 claim 1 , about 1.5:1 claim 1 , about 2:1 claim 1 , about 3:1 claim 1 , or about 4:1.10. The method of claim 1 , wherein the conditions comprise reacting at a temperature of about 150° C. claim 1 , about 160° C. claim 1 , about 170° C. claim 1 , about 180° C. claim 1 , about 190° C. claim 1 , about 200° C. claim 1 , about 210° C. claim 1 , about 220° C. claim 1 , or about 230° C.11. The method of claim 1 , wherein the conditions comprise reacting at a temperature between about 150° C. and about 220° C.12. The method of claim 1 , wherein the conditions comprise reacting in a solution comprising water and a polar aprotic solvent.13. The method of claim 12 , wherein the ratio of water to polar aprotic solvent is between about 1:9 and about 9:1.14. The method of claim 1 , wherein the reaction is carried out under conditions suitable for ...

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Номер записи: 15
05-09-2013 дата публикации

MRI CONTRAST AGENT HAVING GADOLINIUM COMPLEX

Номер: US20130231475A1
Автор: Chang Yong Min, Gu Sung-Wook, Kim Hee-Kyung, Kim Tae-Jeong
Принадлежит: Kyungpook National University Industry-Academic Cooperation Foundation

The present invention relates to a magnetic resonance imaging (MRI) contrast agent including a gadolinium complex, more particularly to a DO3A-tranexamic acid or its ester compound, which is represented by the Chemical Formula 1. A DO3A-tranexamic acid or its ester compound may be prepared according to the present invention and a gadolinium complex may be prepared using the compound. An MRI contrast agent including the gadolinium complex prepared according to the present invention as an active ingredient has higher relaxivity as compared to the currently commercially available contrast agent. In addition, the MRI contrast agent according to the present invention has bifunctionality of liver-specific and blood-pool contrasting effect. Accordingly, since the MRI contrast agent including the gadolinium complex according to the present invention satisfies the key properties required for a contrast agent for MRI, it can be widely used as an MRI contrast agent and can provide enhanced contrasting effect as compared to the existing contrast agent. 2. A method of preparing the DO3A-tranexamic acid or its ester compound according to claim 1 , comprising:a) adding bromoacetyl bromide to trans-4(aminomethyl)cyclohexaneethylcarboxylate hydrochloride with stirring;{'sub': '3', 'b) adding DO3A-(′BuO)to the mixture with stiffing;'}c) adding TFA to the mixture to deprotect a tert-butyl group;d) conducting silica gel chromatography after removing all of solvent under low pressure and dissolving the mixture in methanol; ande) drying the product obtained from the chromatography under vacuum state to obtain a DO3A-tranexamic acid or its ester compound.3. The method according to claim 2 , wherein allyl-trans-4(aminomethyl)cyclohexaneethylcarboxylate hydrochloride is added instead of trans-4(aminomethyl)cyclohexaneethylcarboxylate hydrochloride in the step a).4. A composition for a ligand (L) of a complex claim 1 , which comprises the DO3A-tranexamic acid or its ester compound according ...

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Номер записи: 16
10-10-2013 дата публикации

TERPENOID ANALOGUES AND USES THEREOF FOR TREATING NEUROLOGICAL CONDITIONS

Номер: US20130267571A1
Автор: Lu Erhu, McLellan Alexander, Reed Mark A., Sun Shengguo, WEAVER Donald
Принадлежит: NeuroQuest Inc.

The present application provides a terpene analogue of Formula (I) or a pharmaceutically acceptable isomer, salt or ester thereof, and methods and uses thereof for treating neurological conditions such as pain in general and neuropathic pain. These terpene analogues can also be used to treat other electrical disorders in the central and peripheral nervous system. Also provided are methods of synthesizing the terpene analogues of Formula I. 2. The method of claim 1 , wherein Y is CH claim 1 , W is CH claim 1 , and X is O—CH claim 1 , O—CH-aryl claim 1 , NH claim 1 , N(H)—CH claim 1 , N—(CH) claim 1 , N(H)—C(═O)-aryl claim 1 , N(H)—C(═O)—CH claim 1 , N(H)—C(═O)-aryl(OH) claim 1 , SOMe claim 1 , or SOMe.3. The method of claim 1 , wherein Y is C═O and X is H claim 1 , OH claim 1 , NHN(H)—CH claim 1 , N—(CH) claim 1 , N(H)-aryl claim 1 , N(Me)OMe claim 1 , N(Me)OH claim 1 , or CF.5. The method of claim 1 , wherein:Y is absent;{'sub': 3', '3', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'X is —C(═O)H, —C(═O)CF—COOH, —CH(OH)CF, —C(OH)(CF), —C(═O)N(Me)OMe, C(═O)N(Me)OH, —CONHAryl, —CONH, —CONHAlkyl, —CON(Alkyl)—SOAryl, —SOalkyl, SOalkyl, —SONHAryl, —SON(Aryl), —SON(Alkyl), —SONHalkyl, or SONH; and'}{'sub': 1', '20, 'W is H, a substituted or unsubstituted Cto Calkyl, a substituted or unsubstituted aryl or a substituted or unsubstituted alkylaryl.'}6. The method of claim 1 , wherein the terpene analogue is selected from the group consisting of:(E)-1-methoxy-3,7-dimethylocta-2,6-diene,(E)-((3,7-dimethylocta-2,6-dienyloxy)methyl)benzene,3,7-dimethyloct-2,6-dienoic acid,N,3,7-trimethylocta-2,6-dienamide,(E)-3,7-dimethylocta-2,6-dien-1-amine,(E)-N-(3,7-dimethylocta-2,6-dienyl)benzamide,(E)-3,7-dimethylocta-2,6-dienal,(E)-3,7-dimethylocta-2,6-dienoic acid,(E)-N-(3,7-dimethylocta-2,6-dienyl)acetamide,(E)-3,7-dimethyl-N-phenylocta-2,6-dienamide,(E)-N-(3,7-dimethylocta-2,6-dienyl)-2-hydroxybenzamide,(E)-N,N,3,7-tetramethylocta-2,6-dienamide,(E)-N,N,3,7- ...

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Номер записи: 17
17-10-2013 дата публикации

(2-UREIDOACETAMIDO)ALKYL DERIVATIVES AS FORMYL PEPTIDE RECEPTOR 2 MODULATORS

Номер: US20130274230A1
Автор: Beard Richard L., Donello John E., Duong Tien, Garst Michael E., Viswanath Veena
Принадлежит: ALLERGAN, INC.

The present invention relates to (2-ureidoacetamido)alkyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor 2. 2. A compound according to claim 1 , wherein:{'sup': 3', '11', '16, 'sub': 1-8', '3', '2, 'Ris substituted or unsubstituted Calkyl, halogen, —SR, —CFor —S(O)R.'}4. A compound according to claim 1 , wherein:{'sup': 6', '19, 'sub': 1-8', '2, 'Ris substituted or unsubstituted Calkyl, or —CHR.'}5. A compound according to claim 1 , wherein:{'sup': '26', 'Ris hydrogen;'}{'sup': '27', 'Ris hydrogen;'}{'sup': '28', 'Ris hydrogen; and'}{'sup': '29', 'Ris hydrogen;'}8. A compound according to claim 1 , selected from:Diethyl({[(2S)-2-({[(4-bromophenyl)amino]carbonyl}amino)-4-methylpentanoyl]amino}methyl)phosphonate;(2S)-2-({[(4-Bromophenyl)amino]carbonyl}amino)-4-methyl-N-(1H-tetrazol-5-ylmethyl)pentanamide;(2S)-2-({[(4-Bromophenyl)amino]carbonyl}amino)-4-methyl-N-[2-(1H-tetrazol-5-yl)ethyl]pentanamide;(2S)-2-({[(4-Bromophenyl)amino]carbonyl}amino)-N-[(3-hydroxyisoxazol-5-yl)methyl]-4-methylpentanamide;Diethyl({[(2S)-2-({[(4-bromophenyl)amino]carbonyl}amino)-4-methylpentanoyl]amino}methyl)phosphonate;Diethyl({[(2S,3S)-2-({[(4-bromophenyl)amino]carbonyl}amino)-3-methylpentanoyl]amino}methyl)phosphonate;Diethyl({[(2S)-2-({[(4-bromophenyl)amino]carbonyl}amino)pentanoyl]amino}methyl)phosphonate;Diethyl({[(2S)-2-({[(4-bromophenyl)amino]carbonyl}amino)-3-phenylpropanoyl]amino}methyl)phosphonate;Diethyl(2-{[(2S)-2-({[(4-bromophenyl)amino]carbonyl}amino)-4-methylpentanoyl]amino}ethyl)phosphonate;Ethyl hydrogen ({[(2S)-2-({[(4-bromophenyl)amino]carbonyl}amino)-4-methyl pentanoyl]amino}methyl)phosphonate;Ethyl hydrogen ({[(2S,3S)-2-({[(4-bromophenyl)amino]carbonyl}amino)-3-methyl pentanoyl]amino}methyl)phosphonate;Ethyl hydrogen ({[(2S)-2-({[(4-bromophenyl)amino]carbonyl}amino)pentanoyl]amino}methyl)phosphonate;({[(2S)-4-Methyl-2-({[4-(trifluoromethyl)phenyl] ...

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Номер записи: 18
31-10-2013 дата публикации

HETEROARYLTHIO DERIVATIVES AND ANALOGUES

Номер: US20130289047A1
Автор: Fick David, Helton David
Принадлежит: EPIOMED THERAPEUTICS, INC.

Heteroarylthio compounds covalently linked to an arylpiperazine moiety for the treatment of neurological conditions. 7. The heteroarylthio compound of claim 1 , wherein m is selected from the group consisting of 2 claim 1 , 3 claim 1 , and 4.8. The heteroarylthio compound of claim 1 , wherein L is substituted with alkyl groups.14. The heteroarylthio compound of claim 1 , wherein the compound is selected from the group consisting of:1-{2-[(1-methyl-1H-imidazol-2-yl)thio]ethyl}-4-[3-(trifluoromethyl)phenyl]piperazine;1-[2-(5-pyridin-4-yl-[1,3,4]oxadiazol-2-ylsulfanyl)ethyl]-4-(3-trifluoromethylphenyl)piperazine;1-{3-[(1-methyl-1H-imidazol-2-yl)thio]propyl}-4-[3-chlorophenyl]piperazine;1-[3-(1-phenyl-1H-tetrazol-5-ylsulfanyl)propyl]-4-(3-chlorophenyl)piperazine; and1-[2-(5-pyridin-4-yl-[1,3,4]oxadiazol-2-ylsulfanyl)ethyl]-4-(3-trifluoromethylphenyl)piperazine.1518-. (canceled)19. The heteroarylthio compound of claim 1 , wherein the compound is selected from the group consisting of:4-{4-[3-(1-methyl-1H-imidazol-2-ylsulfanyl)propyl]piperazin-1-yl}furo[3,2-c]pyridine;4-{4-[3-(1-phenyl-1H-tetrazol-5-ylsulfanyl)propyl]piperazin-1-yl}furo[3,2-c]pyridine; and4-{4-[3-(5-pyridin-4-yl-[1,3,4]oxadiazol-2-sulfanyl)propyl]piperazin-1-yl}furo[3,2-c]pyridine.2021-. (canceled)22. A pharmaceutical composition comprising the heteroarylthio compound of and one or more pharmaceutically acceptable excipients.23. A method of treating a neurological condition claim 1 , comprising the step of administering the heteroarylthio compound of to a subject in need thereof.24. (canceled) This patent application claims the benefit of priority from U.S. Patent Application No. 61/393,349, filed on Oct. 14, 2010 and entitled HETEROARYLTHIO DERIVATIVES AND ANALOGUES. The disclosure of this application is hereby incorporated by reference herein in its entirety.The serotonin receptors, also known as 5-hydroxytryptamine receptors or 5-HT receptors, are a group of G protein-coupled receptors (GPCRs) and ...

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Номер записи: 19
31-10-2013 дата публикации

FUNGICIDE HYDROXIMOYL-TETRAZOLE DERIVATIVES

Номер: US20130289077A1
Автор: BENTING Juergen, Coqueron Pierre-Yves, Desbordes Philippe, Dubost Christophe, Portz Daniela, Rebstock Anne-Sophie, Wachendorff-Neumann Ulrike
Принадлежит:

The present invention relates to hydroximoyl-heterocycle derivatives of formula (I) 2. A compound according to wherein X represents a hydrogen atom claim 1 , a halogen atom claim 1 , substituted or non-substituted C-C-alkyl claim 1 , a substituted or non-substituted C-C-alkoxy claim 1 , a cyano group claim 1 , a methanesulfonyl group claim 1 , a nitro group claim 1 , a trifluoromethyl group or an aryl group.3. A compound according to wherein X represents a hydrogen atom claim 1 , a chlorine atom claim 1 , a fluorine atom claim 1 , a methyl group claim 1 , a tert-butyl group claim 1 , a methoxy group claim 1 , an ethoxy group claim 1 , a cyano group claim 1 , a methanesulfonyl group claim 1 , a nitro group claim 1 , a trifluoromethyl group or an aryl group.4. A compound according to wherein X represents a hydrogen atom.5. A compound according to wherein q represents 1.6. A compound according to wherein Y represents a substituted or non-substituted C-C-alkyl group.7. A compound according to wherein Y represents a methyl group or an ethyl group.8. A compound according to wherein R represents a hydrogen atom or a halogen atom.9. A compound according to wherein R represents a hydrogen atom or a chlorine atom10. A compound according to wherein Qrepresents a hydrogen atom claim 1 , substituted or non-substituted C-C-alkyl claim 1 , substituted or non-substituted C-C-cycloalkyl claim 1 , substituted or non-substituted C-C-alkenyl claim 1 , substituted or non-substituted C-C-alkynyl claim 1 , substituted or non-substituted aryl claim 1 , substituted or non-substituted claim 1 , saturated or unsaturated 4- claim 1 , 5- claim 1 , 6- claim 1 , 7- claim 1 , 8- claim 1 , 9- claim 1 , 10- claim 1 , or 11-membered heterocyclyl comprising up to 4 heteroatoms selected in the list consisting of N claim 1 , O claim 1 , S.11. A compound according to wherein Qrepresents a hydrogen atom claim 1 , or a substituted or non-substituted C-C-alkyl.12. A compound according to wherein Qrepresents ...

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Номер записи: 20
28-11-2013 дата публикации

ALTERNATIVE TO TETRAZENE

Номер: US20130317232A1
Автор: FRONABARGER JOHN W., Williams Michael D.
Принадлежит: PACIFIC SCIENTIFIC ENERGETIC MATERIALS COMPANY

Embodiments of materials suitable for use as a replacement for Tetrazene and methods of preparing such materials are described. In one embodiment, the material comprises MTX-1, as well as simple salts or complexes derived therefrom. The methods of preparing such materials include combining Tetrazene and an acid to form a suspension, where the acid is nitric acid, sulfuric acid, perchloric acid, or hydrochloric acid. A nitrite salt may be added to the suspension, where the nitrite salt is sodium nitrite, lithium nitrite, potassium nitrite, an aqueous solution of sodium nitrite, an aqueous solution of lithium nitrite, or an aqueous solution of potassium nitrite. In some embodiments, the suspension is stirred until the suspension has a white appearance. 13.-. (canceled)4. A composition comprising simple salts or complexes derived from MTX-1.57.-. (canceled)8. A compound comprising simple salts or complexes derived from MTX-1.911.-. (canceled)1323.-. (canceled)24. The composition of claim 4 , wherein the composition is used as a replacement for Tetrazene.25. The compound of claim 8 , wherein the compound is used as a replacement for Tetrazene.26. The compound of claim 12 , wherein the compound is used as a replacement for Tetrazene. This application claims the benefit of U.S. Provisional Patent Application Ser. No. 61/326,768, entitled “Alternatives to Tetrazene,” filed Apr. 22, 2010, and claims the benefit of U.S. Provisional Patent Application Ser. No. 61/370,563, entitled “Alternative to Tetrazene,” filed Aug. 4, 2010, the entire contents of each of which are incorporated herein by these references.This invention was made in part with U.S. government support under Contract No. N00014-09-M-0433 awarded by the United States of America for the Department of the Navy. The government has certain rights in this invention.This invention relates to explosives, and in particular to preparation of a primer sensitizer.1-amino-1(1H-tetrazol-5-yl)-azo-guanidine hydrate (“ ...

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Номер записи: 21
12-12-2013 дата публикации

TETRAZOLE COMPOUNDS AND METHODS OF MAKING AND USING SAME

Номер: US20130331420A1
Автор: Cramp Susan Mary, Dyke Hazel Joan, Pallin Thomas David
Принадлежит: Zafgen, Inc.

Described herein are tetrazole compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tetrazole compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2. 2. The compound of claim 1 , wherein A is phenyl.3. The compound of claim 1 , wherein B is a bond.4. The compound of claim 1 , wherein Ris selected from the group consisting of hydrogen claim 1 , halogen claim 1 , cyano claim 1 , hydroxyl claim 1 , Calkyl claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , Ccycloalkyl claim 1 , Calkoxy claim 1 , Calkenyloxy claim 1 , and Calkynyloxy claim 1 , wherein Calkenyl claim 1 , Calkynyl claim 1 , Calkenyloxy claim 1 , and Calkynyloxy are each independently optionally substituted by one or more substituents each independently selected from R claim 1 , wherein Calkyl and Calkoxy are each independently optionally substituted by one or more substituents each independently selected from R claim 1 , wherein Ccycloalkyl is optionally substituted by one or more substituents each independently selected from R.5. The compound of claim 1 , wherein Ris selected from the group consisting of H or Calkyl.6. The compound of claim 1 , wherein Ris H.7. The compound of claim 1 , wherein Ris selected from the group consisting of halogen claim 1 , cyano claim 1 , Calkyl claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , Ccycloalkyl claim 1 , Calkoxy claim 1 , Calkenyloxy claim 1 , Calkynyloxy claim 1 , Ccycloalkyloxy claim 1 , Calkyl-S(O)— claim 1 , Ccycloalkyl-Calkyl- claim 1 , and Ccycloalkyl-Calkoxy- claim 1 , wherein Calkyl claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , Calkoxy claim 1 , Calkenyloxy claim 1 , and Calkynyloxy are each independently optionally substituted by one or more substituents each independently selected from halogen claim 1 , hydroxyl claim 1 , RRN— claim 1 , or cyano claim 1 , wherein Ccycloalkyl and Ccycloalkoxy are each independently optionally ...

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Номер записи: 22
26-12-2013 дата публикации

PROCESS AND INTERMEDIATE COMPOUNDS USEFUL IN THE PREPARATION OF STATINS

Номер: US20130345429A1
Автор: Moody David John, Wiffen Jonathan William
Принадлежит:

There is provides a process for the preparation of a compound of formula (7): wherein R is an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group; provides that R is not a compound of Formula (a): wherein Rrepresents an alkyl group, such as a Calkyl group, and preferably an isopropyl group; Rrepresents an aryl group, preferably a 4-fluorophenyl group; Rrepresents hydrogen, a protecting group or an alkyl group, such as a Calkyl group, and preferably a methyl group; and Rd represents hydrogen, a protecting group or a SORgroup where Ris an alkyl group, such as a Calkyl group, and preferably a methyl group. 17-. (canceled)9. The process of wherein Y is Cl or Br.11. The process of claim 10 , wherein Ris an alkyl group and/or Ris an alkanoyl group.12. The process of claim 11 , wherein Ris a Calkyl group and/or Ris a Calkanoyl group.13. The process of claim 12 , wherein Ris a —C(O)CH(Me)CHCHor —C(O)C(Me)CHCHgroup14. The process of claim 10 , wherein Ris an alkanoyl group.15. The process of claim 14 , wherein Ris a Calkanoyl group16. The process of claim 14 , wherein Ris a —C(O)CH(Me)CHCHor a —C(O)C(Me)CHCHgroup.17. The process of claim 10 , wherein Ris a substituted or unsubstituted aryl group and/or Ris a substituted or unsubstituted alkyl group.18. The process of claim 17 , wherein Ris a 4-fluorophenyl group and/or Ris a cyclopropyl group.19. The process of claim 10 , wherein Ris a substituted or unsubstituted aryl group and/or Ris a substituted or unsubstituted alkyl group.20. The process of claim 19 , wherein Ris a 4-fluorophenyl group and/or Ris an isopropyl group.21. The process of claim 10 , wherein Ris a substituted or unsubstituted aryl or a substituted or unsubstituted aromatic heterocyclic group; Ris a substituted or unsubstituted aryl group; and/or Ris a substituted or unsubstituted aryl group.22. The process of claim 21 , wherein Ris a methyltetrazoyl group; Ris a 4-fluorophenyl group; and/or Ris a 4-fluorophenyl group.23. ...

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Номер записи: 23
02-01-2014 дата публикации

Compositions and Methods for Treating or Preventing Pneumovirus Infection and Associated Diseases

Номер: US20140005239A1
Автор: Cook Robert O., Reynolds Eugene R., Shekunov Boris, Zegar Siead I.
Принадлежит:

The present invention provides novel crystalline polymorphic forms of MDT-637, in particular, crystalline polymorphic forms with physicochemical properties specifically suited for drug production, amorphous formation, composite form, and methods of preparation thereof. The novel polymorphs described herein are useful for the treatment of respiratory disease, such as disease caused by respiratory syncytial virus. 1. A composition comprising a polymorph of MDT-637.2. The composition of claim 1 , wherein the polymorph of MDT-637 comprises a crystal form of P-3 dihydrate claim 1 , P-3 ethanolate claim 1 , P-3 monohydrate claim 1 , P-3 anyhydrous claim 1 , P-2 anhydrous claim 1 , P-4 claim 1 , P-6 claim 1 , P-7 or P-8.3. The composition of claim 1 , comprising an amorphous form of P-3 dihydrate claim 1 , P-3 ethanolate claim 1 , P-3 monohydrate claim 1 , P-3 anyhydrous claim 1 , P-2 anhydrous claim 1 , P-4 claim 1 , P-6 claim 1 , P-7 or P-8.4. The composition of claim 1 , optionally comprising one or more pharmaceutically acceptable carriers.5. The composition of claim 2 , wherein characteristic diffraction peaks of the hydrate crystal form of pattern P-2 are shown in .6. The composition of claim 2 , wherein characteristic diffraction peaks of the monohydrate crystal form of pattern P-3 are shown in .7. The composition of claim 2 , wherein characteristic diffraction peaks of the dihydrate crystal form of pattern P-3 are shown in .8. The composition of claim 2 , wherein characteristic diffraction peaks of the anhydrous crystal form of pattern P-2 are shown in .9. The composition of claim 2 , wherein characteristic diffraction peaks of the anhydrous crystal form of pattern P-3 are shown in .10. The composition of claim 2 , wherein characteristic diffraction peaks of the P-3 ethanolate crystal form are shown in .11. The composition of claim 2 , wherein characteristic diffraction peaks of the P-4 crystal form are shown in claim 2 , wherein characteristic diffraction peaks of ...

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Номер записи: 24
06-02-2014 дата публикации

C-substituted, 1h-azoles for amphoteric, solvent-less proton conductivity

Номер: US20140039132A1
Автор: Arthur W Snow, Brian L. Chaloux, Holly L. Ricks-Laskoski, Matthew Laskoski, Stephen M. Deese
Принадлежит: Individual

Disclosed herein are the compounds shown below. Also disclosed are methods of making the compounds. R 1 =—O—; R 2 =any alkyl chain; R 3 =—CH 3 , —CN, —COOCH 3 , -tetrazole, -imidazole, or -triazole; R 4 =—H or —R 5 ; R 5 =—H, -halogen, —C≡CH, or —C≡C—; n is a positive integer; and m is a positive integer.

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Номер записи: 25
13-02-2014 дата публикации

DUAL-ACTING ANTIHYPERTENSIVE AGENTS

Номер: US20140046075A1
Автор: Choi Seok-ki, Fatheree Paul R., Hudson Ryan, Jendza Keith, McKinnell Robert Murray, Sasikumar Vivek
Принадлежит: THERAVANCE, INC.

The invention is directed to compounds of formula I: 131-. (canceled)3354-. (canceled) This application claims the benefit of U.S. Provisional Application No. 60/899,264, filed on Feb. 2, 2007 and No. 60/901,531, filed on Feb. 15, 2007; the entire disclosures of which are incorporated herein by reference in their entirety.1. Field of the InventionThe present invention relates to novel compounds having angiotensin type 1 (AT) receptor antagonist activity and neprilysin-inhibition activity. The invention also relates to pharmaceutical compositions comprising such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat diseases such as hypertension.2. State of the ArtThe aim of antihypertensive therapy is to lower blood pressure and prevent hypertension-related complications such as myocardial infarction, stroke, and renal disease. For patients with uncomplicated hypertension (for example, no risk factors, target organ damage, or cardiovascular disease), it is hoped that reducing blood pressure will prevent development of cardiovascular and renal comorbidities, conditions that exist at the same time as the primary condition in the same patient. For those patients with existing risk factors or comorbidities, the therapeutic target is the slowing of comorbid disease progression and reduced mortality.Physicians generally prescribe pharmacological therapies for patients whose blood pressure cannot be adequately controlled by dietary and/or lifestyle modifications. Commonly used therapeutic classes act to promote diuresis, adrenergic inhibition, or vasodilation. A combination of drugs is often prescribed, depending upon what comorbidities are present.There are five common drug classes used to treat hypertension: diuretics, which include thiazide and thiazide-like diuretics such as hydrochlorothiazide, loop diuretics such as furosemide, and potassium-sparing diuretics such as triamterene; βadrenergic receptor blockers ...

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Номер записи: 26
06-03-2014 дата публикации

PROCESS FOR THE PREPARATION OF BIS-(1(2)H-TETRAZOL-5-YL)-AMINE MONOHYDRATE

Номер: US20140066630A1
Автор: BHIMIREDDY Nagi Reddy, IYENGAR Deevi Sarangapani, SAIKIA Anil
Принадлежит:

A process for the preparation of Bis-(1(2)H-tetrazol-5-yl)-amine monohydrate. 1. A process for the preparation of Bis-(1(2)H-tetrazol-5-yl)-amine monohydrate of the formula (I) , by the reaction of sodium dicynamide and sodium azide , by adding a 6 molar solution of hydrochloric acid in the presence of a catalytic amount of boric acid into the reaction mixture for a period of 2-8 hour at 55° to 58° C.2. A process for the preparation of Bis-(1(2)H-tetrazol-5-yl)-amine monohydrate of the formula (I) according to claim 1 , wherein the catalytic amount of boric acid is of 1% to 5% by weight.3. A process for the preparation of Bis-(1(2)H-tetrazol-5-yl)-amine monohydrate of the formula (I) according to claim 1 , wherein the reaction achieves a yield of 90% to 93%.4. A process for the preparation of Bis-(1(2)H-tetrazol-5-yl)-amine monohydrate of the formula (I) according to claim 1 , wherein the product is in fine crystalline nature. The present invention relates to an improved process for the preparation of Bis-(1(2)H-tetrazol-5-yl)-amine monohydrate of the formula (I) by the reaction of sodium dicynamide and sodium azide, by adding a 6 molar solution of hydrochloric acid in the presence or absence of a catalytic amount of boric acid (1% to 5% by weight) into the reaction mixture for a period of 2-8 hour at 55° to 58°Bis-(1(2)H-tetrazol-5-yl)-amine monohydrate of the formula also known as BTA having the structural formula (I), useful as a gas generant. According to the available literature, it is prepared by the reaction of sodium dicynamide with sodium azide in the presence of inorganic or organic acids.In the patent U.S. 2003/0060634, described this reaction in the presence of hydrochloric acid (HCl), sulphuric acid (H2SO4), phosphoric acid (H3PO4), nitric acid (HNO3), perchloric acid (HClO4) and the mixtures thereof. Also some organic acids like trifluoro acetic acid, trifluoromethane sulfonic acid and methane sulfonic acid. But this patent preferred hydrochloric acid ...

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Номер записи: 27
13-03-2014 дата публикации

COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATING OR PREVENTING PNEUMOVIRUS INFECTION AND ASSOCIATED DISEASES

Номер: US20140072532A1
Автор: Burns Christopher J., Gaboury Janet A., Laguerre Sylvie, Lessen Thomas A., Nitz Theodore J., Pevear Daniel C., Rys David J.
Принадлежит: MICRODOSE THERAPEUTX, INC.

Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infection. 4. A compound according to claim 1 , selected from the group consisting of:2,2′-[[3-(2,2,2-Trifluoroethyl)phenyl]methylene]bis[4-[[(5-methyl-1H-tetrazol-1-yl)imino]methyl]]phenol;3-[[Bis[[5-(5-methyl-1H-tetrazol-1-yl)imino]methyl]-2-hydroxyphenyl]methylene]benzeneethanol, acetate ester;3-[[Bis[[5-(5-methyl-1H-tetrazol-1-yl)imino]methyl]-2-hydroxyphenyl]methylene]benzeneethanol;2,2′-[[3-(4-Morpholinyl)phenyl]methylene]bis[4-[[(5-methyl-1H-tetrazol-1-yl)imino]methyl]]phenol;2,2′-[[3-(1-Piperidinyl)phenyl]methylene]bis[4-[[(5-methyl-1H-tetrazol-1-yl)imino]methyl]]phenol;3-[[Bis[[5-(5-methyl-1H-tetrazol-1-yl)imino]methyl]-2-hydroxyphenyl]methylene]-N,N-bis(methoxyethyl)benzenesulfonamide;3-[[Bis[[5-(5-methyl-1H-tetrazol-1-yl)imino]methyl]-2-hydroxyphenyl]methylene]-N-(hydroxyethyl)-N-methylbenzenesulfonamide;3-[[Bis[[5-(5-methyl-1H-tetrazol-1-yl)imino]methyl]-2-hydroxyphenyl]methylene]benzenepropanol;{'b': '3', '2,2′-[[-(4-Morpholinylsulfonyl)phenyl]methylene]bis[4-[[(5-methyl-1H-tetrazol-1-yl)imino]methyl]]phenol;'}2,2′-[[3-(Methoxyethoxy)phenyl]methylene]bis[4-[[5-methyl-1H-tetrazol-1-yl)imino]methyl]]phenol;2,2′-[[[3-Bis(phenylmethyl)amino]phenyl]methylene]bis[4-[[(5-methyl-1H-tetrazol-1-yl)imino]methyl]]phenol;3-[[Bis[[5-(5-methyl-1H-tetrazol-1-yl)imino]methyl]-2-hydroxyphenyl]methylene]phenoxyethanol, acetate ester;3-[[Bis[[5-(5-methyl-1H-tetrazol-1-yl)imino]methyl]-2-hydroxyphenyl]methylene]-N-(acetoxyethyl)-N-methylbenzenesulfonamide;3-[[Bis[[5-(5-methyl-1H-tetrazol-1-yl)imino]methyl]-2-hydroxyphenyl]methylene]phenoxyethanol;2-Hydroxy-N-[[3-[bis[[5-(5-methyl-1H-tetrazol-1-yl)imino]methyl]-2-hydroxylphenyl]methylene]phenyl]-N-(methylethyl)acetamide;2-(Acetyloxy)-N-[3-[[bis[[5-(5-methyl-1H-tetrazol-1-yl)imino]methyl]-2-hydroxyphenyl]methylene]phenyl]-N- ...

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Номер записи: 28
13-03-2014 дата публикации

Antibiotic Compositions for the Treatment of Gram Negative Infections

Номер: US20140073559A1
Автор: Bombardier Amy C.D., Curran William V., Hwang You Seok, Leese Richard A., Lippa Blaise S., Liu Christopher M., Zhang Yanzhi
Принадлежит:

Provided herein are novel compounds and novel protected compounds that can be derived from polymyxin, including, e.g., polymyxin A. The novel compounds have antibacterial properties against a diverse range of Gram negative bacteria and reduced toxicity compared to polymyxins such as polymyxin A. Also provided are antibacterial pharmaceutical compositions containing the novel compounds and novel protected compounds, as well as methods for preparing the antibacterial compounds and protected compounds. 2. The composition of claim 1 , further comprising a pharmaceutically acceptable carrier.3. The composition of claim 2 , wherein the composition is adapted for inhalation or intravenous administration.4. The composition of claim 1 , wherein the compound of Formula (Ia) is at least 94% enantiomerically pure.6. The method according to claim 5 , wherein the subject is a human claim 5 , an animal claim 5 , a cell culture claim 5 , or a plant.7. The method according to claim 5 , further comprising the step of determining the type of bacteria in the bacterial infection.8. The method of claim 5 , wherein the bacterial infection comprises claim 5 , consists essentially of or consists of Gram-negative bacteria.9. The method according to claim 5 , wherein the bacterial infection comprises a susceptible or multi-drug resistant bacteria.10Pseudomonas aeruginosa, AcinetobacterStenotrophomonas maltophilia, Escherichia coli, Klebsiella pneumoniae, CitrobacterEnterobacter. The method of claim 5 , wherein the bacterial infection comprises spp claim 5 , spp claim 5 , claim 5 , or a combination thereof.12Actinoplanes utahensis.. The process of claim 11 , wherein the deacylating agent is produced by13. The process of claim 11 , wherein the protecting group is 2-sulfo-9-fluorenylmethoxycarbonyl. This application is a continuation of U.S. application Ser. No. 13/167,495, filed Jun. 23, 2011, which claims the benefit of U.S. Provisional Application No. 61/382,270, filed on Sep. 13, 2010, and U ...

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Номер записи: 29
13-03-2014 дата публикации

VALSARTAN SALTS

Номер: US20140073677A1
Автор: Buehlmayer Peter, Marterer Wolfgang, Marti Erwin, Oswald Hans Rudolf
Принадлежит:

The invention relates to new salts of valsartan or crystalline, also partly crystalline and amorphous salts of valsartan, the respective production and usage, and pharmaceutical preparations containing such a salt. 1. A magnesium salt of valsartan.2. The salt according to in crystalline form.3. The salt according to in partially crystalline form.4. The salt according to in amorphous form.5. A magnesium hexahydrate salt of valsartan.6. The hexahydrate according to claim 5 , characterised by(i) an X-ray powder pattern taken with a Guinier camera comprising the following interlattice plane intervals: d in [A]: 19.7±0.3, 10.11±0.2, 9.8±0.2, 7.28±0.1, 5.81±0.05, 5.68±0.05, 5.03±0.05, 4.88±0.05, 4.18±0.05, 4.08±0.05, 3.46±0.05; or(ii) an ATR-IR spectrum having the following absorption bands expressed in reciprocal wave numbers (cm 1): 3378 (m); 3274 (m); 2956 (m); 1619 (st); 1557 (m); 1464 (m); 1419 (m); 1394 (st); 1374 (m); 1175 (m); 836 (m); 820 (s); 766 (st); 751 (m); 741 (st); 732 (st).7. A salt according in the form of a solvate.8. A salt according in the form of a hydrate.9. A pharmaceutical composition comprising the salt according to and a pharmaceutically acceptable excipient or additive.10. The pharmaceutical composition according to claim 9 , further comprising at least one of the following:(i) HMG-Co-A reductase inhibitor or a pharmaceutically acceptable salt thereof,(ii) angiotensin converting enzyme (ACE) Inhibitor or a pharmaceutical acceptable salt thereof,(iii) calcium channel blocker or a pharmaceutically acceptable salt thereof,(iv) aldosterone synthase inhibitor or a pharmaceutical acceptable salt thereof,(v) aldosterone antagonist or a pharmaceutically acceptable salt thereof,(vi) dual angiotensin converting enzyme/neutral endopeptidase (ACE/NEP) inhibitor or a pharmaceutical acceptable salt thereof,(vii) endothelin antagonist or a pharmaceutical acceptable salt thereof,(viii) renin inhibitor or a pharmaceutical acceptable salt thereof, or(ix) ...

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Номер записи: 30
27-03-2014 дата публикации

Substituted carbamoylmethylamino acetic acid derivatives as novel NEP inhibitors

Номер: US20140088165A1
Автор: IWAKI Yuki, KAWANAMI Toshio, KSANDER Gary Michael, Moji Muneto
Принадлежит: NOVARTIS AG

The present invention provides a compound of formula I; 7. The method of wherein{'sup': '1', 'sub': '2', 'Ais a bond or CH; or a pharmaceutically acceptable salt thereof.'}8. The method of wherein{'sup': 1', '5', '4, 'Ris methyl or ethyl, Rand Rare H; or a pharmaceutically acceptable salt thereof.'}10. The method of wherein{'sup': '3', 'Ris tetrazole; or a pharmaceutically acceptable salt thereof.'}11. The method of wherein{'sup': '2', 'Xis Cl, or a pharmaceutically acceptable salt thereof.'}1219-. (canceled) Endogenous atrial natriuretic peptides (ANP), also called atrial natriuretic factors (ANF) have diuretic, natriuretic and vasorelaxant functions in mammals. The natural ANF peptides is metabolically inactivated, in particular by a degrading enzyme which has been recognized to correspond to the enzyme neutral endopeptidase (NEP) EC 3.4.24.11, also responsible for e.g. the metabolic inactivation of enkephalins.Neutral endopeptidase (EC 3.4.24.11; enkephalinase; atriopeptidase; NEP) is a zinc-containing metalloprotease that cleaves a variety of peptide substrates on the amino side of hydrophobic residues [see , Vol. 45, p. 87 (1993)]. Substrates for this enzyme include, but are not limited to, atrial natriuretic peptide (ANP, also known as ANF), brain natriuretic peptide (BNP), met- and leu-enkephalin, bradykinin, neurokinin A, endothelin-1 and substance P. ANP is a potent vasorelaxant and natriuretic agent [see , Vol. 19, p. 1923 (2001)]. Infusion of ANP in normal subjects resulted in a reproducible, marked enhancement of natriuresis and diuresis, including increases in fractional excretion of sodium, urinary flow rate and glomerular filtration rate [see , Vol. 27, p. 927 (1987)]. However, ANP has a short half-life in circulation, and NEP in kidney cortex membranes has been shown to be the major enzyme responsible for degrading this peptide [see , Vol. 9, p. 173 (1988)]. Thus, inhibitors of NEP (neutral endopeptidase inhibitors, NEPi) should increase plasma ...

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Номер записи: 31
07-01-2016 дата публикации

CONJUGATED BIOLOGICAL MOLECULES AND THEIR PREPARATION

Номер: US20160000933A1
Автор: POLUKHTIN Andrei
Принадлежит:

Conjugation reagents of formula (1) that form a bridge between two cystein residues derived from the disulfide bond and a two-step process for the preparation of antibody conjugates are disclosed. 2. The compound of claim 1 , wherein L represents —SR claim 1 , —SOR claim 1 , —OSOR claim 1 , —NR claim 1 , —NHR claim 1 , —NHR claim 1 , halogen claim 1 , or —O◯ claim 1 , in which Rrepresents a hydrogen atom or an alkyl claim 1 , aryl claim 1 , or alkyl-aryl claim 1 , and ◯ represents a substituted aryl group containing at least one electron withdrawing substituent.3. The compound of claim 1 , wherein V represents —(CH)SOX claim 1 , in which n=1-6 claim 1 , and X represents H or counterion.4. The compound of claim 1 , wherein V represents a hydrophilic polymer.5. The compound of claim 1 , wherein X represents a drug claim 1 , a diagnostic moiety claim 1 , or a chelating agent.6. The compound of claim 1 , wherein X represents a detection moiety or hapten.7. The compound of claim 1 , wherein X represents a protein.8. A kit comprising the compound of .10. The conjugate of claim 9 , wherein X represents a drug claim 9 , a diagnostic moiety claim 9 , or a chelating agent.11. The conjugate of claim 9 , wherein V represents a hydrophilic polymer.12. The conjugate of claim 9 , wherein V represents a homo- or co-polymer selected from the group consisting of polyalkylene glycols claim 9 , polyvinylpyrrolidones claim 9 , polyacrylates claim 9 , polymethacrylates claim 9 , polyoxazolines claim 9 , polyvinylalcohols claim 9 , polyacrylamides claim 9 , polymethacrylamides claim 9 , HPMA copolymers claim 9 , polyesters claim 9 , polyacetals claim 9 , poly(ortho ester)s claim 9 , polycarbonates claim 9 , poly(imino carbonate)s claim 9 , polyamides claim 9 , copolymers of divinylether-maleic anhydride and styrene-maleic anhydride claim 9 , polysacoharides claim 9 , and polyglutamic acids.13. The conjugate of claim 9 , wherein V represents discrete or non-discrete claim 9 , branched or ...

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Номер записи: 32
03-01-2019 дата публикации

Compounds for the Detection, Capture and/or Separation of Polluting Gases

Номер: US20190001252A1
Автор: Jean-Manuel Raimundo, Julien Rodriguez, Olivier Yves Claude Siri, Philip Leslie Llewellyn, Vinicius Demétrio da Silva
Принадлежит: Aix Marseille Universite, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE CNRS

A subject of the present invention is the use of a compound having the general formula (I): (I) wherein V, W, X 4 , X 5 , X 6 , X 7 , X′ 4 , X′ 5 , X′ 6 , X′ 7 , Y, Y′, R 3 , R′ 3 , R 4 and R′ 4 are as defined in any one of claims 1 to 11 , for the detection, capture and/or separation of polluting gases, in particular those selected from the group comprising carbon dioxide, methane, sulfur dioxide, nitrogen oxides, carbon monoxide, linear hydrocarbons, linear mono-olefins and their mixtures, and preferably carbon dioxide. Another subject of the invention is a compound of formula (I) wherein V, W, X 4 , X 5 , X 6 , X 7 , X′ 4 , X′ 5 , X′ 6 , X′ 7 , Y, Y′, R 3 , R′ 3 , R 4 and R′ 4 are as defined in any one of claims 12 to 21 .

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Номер записи: 33
05-01-2017 дата публикации

AMINOTRIAZOLE- AND AMINOTETRAZOLE-BASED KDM1A INHIBITORS AS EPIGENETIC MODULATORS

Номер: US20170001968A1
Автор: KUTZ Craig J., Woster Patrick M.
Принадлежит: MUSC Foundation for Research Development

In some aspects, the present invention provides compounds of the formula (IV), wherein the variables are as defined herein, which may be used as inhibitors of histone demethylase or spermine oxidase. Also provided herein are pharmaceutical compositions of the compounds and methods using the compounds in the treatment of diseases such as cancer and cardiovascular disease. 3. The compound of either or , wherein Ris hydrogen.4. The compound of claim 3 , wherein Ris halo.5. The compound of claim 4 , wherein Ris —Br or —Cl.6. The compound of claim 5 , wherein Ris —Cl.7. The compound according to any one of - claim 5 , wherein Yis alkylaminodiyl.8. The compound of claim 7 , wherein Yis —CHNH— or —NHCH—.9. The compound according to any one of - claim 7 , wherein Xis —O— claim 7 , —S— claim 7 , or —NH—.10. The compound of claim 9 , wherein Xis —O—.11. The compound of claim 9 , wherein Xis —S—.12. The compound according to any one of - claim 9 , wherein Ris alkylor substituted alkyl.13. The compound of claim 12 , wherein Ris alkyl.14. The compound of claim 13 , wherein Ris methyl.15. The compound according to any one of - claim 13 , wherein Ris arylor substituted aryl.16. The compound of claim 15 , wherein Ris aryl.17. The compound of claim 16 , wherein Ris 1-napthyl claim 16 , 2-napthyl claim 16 , 4 claim 16 ,4′-diphenyl claim 16 , 4-methylphenyl claim 16 , 3 claim 16 ,5-dimethylphenyl claim 16 , 4-t-butylphenyl claim 16 , 2-isopropyl-4-methylphenyl claim 16 , 2-methylphenyl claim 16 , or 2 claim 16 ,3-dimethylphenyl.18. The compound of claim 15 , wherein Ris substituted aryl.20. The compound according to any one of - claim 15 , wherein Ris heteroarylor substituted heteroaryl.21. The compound of claim 20 , wherein Ris heteroaryl.22. The compound of claim 21 , wherein Ris indolyl.25. A pharmaceutical composition comprising a compound of - and an excipient.26. The pharmaceutical composition of claim 25 , wherein the pharmaceutical composition is formulated for oral claim 25 , ...

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Номер записи: 34
02-01-2020 дата публикации

HPPD VARIANTS AND METHODS OF USE

Номер: US20200002715A1
Автор: ARMSTRONG Roxanne, Dubald Manuel, Laber Bernd, Lange Gudrun, Poree Fabien
Принадлежит:

In the present invention, HPPD enzymes and plants containing them showing a full tolerance against several classes of HPPD-inhibitors are described. 1. A recombinant nucleic acid molecule encoding a 4-hydroxyphenylpyruvate dioxygenase (HPPD) protein comprising an amino acid sequence comprising a proline at the amino acid position corresponding to amino acid position 335 of SEQ ID NO: 1 and a tyrosine at the position corresponding to amino acid position 336 of SEQ ID NO: 1 , and wherein said HPPD protein is tolerant to an HPPD inhibitor herbicide.2. The recombinant nucleic acid molecule of claim 1 , wherein said HPPD amino acid sequence further comprises:i. an alanine, arginine, asparagine, aspartic acid, cysteine, glutamic acid, glutamine, glycine, histidine, isoleucine, leucine, lysine, methionine, phenylalanine, serine, threonine, tryptophan, tyrosine, or valine at the amino acid position corresponding to amino acid position 188 of SEQ ID NO:1;ii. an alanine, arginine, asparagine, aspartic acid, cysteine, glutamic acid, glutamine, glycine, histidine, leucine, lysine, methionine, phenylalanine, serine, threonine, tryptophan, tyrosine, or valine at the amino acid position corresponding to amino acid position 189 of SEQ ID NO:1;iii. an isoleucine, leucine, or methionine at the amino acid position corresponding to amino acid position 200 of SEQ ID NO: 1;iv. an alanine, leucine, proline, or asparagine at the amino acid position corresponding to amino acid position 215 of SEQ ID NO:1;v. a histidine or glutamine at the amino acid position corresponding to amino acid position 226 of SEQ ID NO:1;vi. a histidine, isoleucine, leucine, methionine, glutamine, arginine, alanine, lysine, serine, threonine, or valine at the amino acid position corresponding to amino acid position 339 of SEQ ID NO:1; orvii. an alanine, arginine, asparagine, aspartic acid, cysteine, glutamic acid, glutamine, glycine, histidine, isoleucine, leucine, lysine, methionine, phenylalanine, serine, ...

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Номер записи: 35
10-01-2019 дата публикации

LABELED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA), THEIR USE AS IMAGING AGENTS AND PHARMACEUTICAL AGENTS FOR THE TREATMENT OF PROSTATE CANCER

Номер: US20190008988A1
Автор: BAUDER-WÜST Ulrike, Benesova Martina, EDER Matthias, EISENHUT Michael, Haberkorn Uwe, KLIEM Hans-Christian, Kopka Klaus, KRATOCHWIL Clemens, Mier Walter, Schäfer Martin
Принадлежит:

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib). 114-. (canceled)16. The compound of claim 15 , wherein Chelator is a radical of:1,4,7,10-tetraazacyclododecane-N,N′,N″,N′″-tetraacetic acid (DOTA);N,N″-bis[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-N,N″-diacetic acid (HBED-CC);1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA);2-(4,7-bis(carboxymethyl)-1,4,7-triazonan-1-yl)pentanedioic acid (NODAGA);2-(4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl)pentanedioic acid (DOTAGA);1,4,7-triazacyclononane phosphinic acid (TRAP);1,4,7-triazacyclononane-1-[methyl(2-carboxyethyl)phosphinic acid]-4,7-bis[methyl(2-hydroxymethyl)phosphinic acid] (NOPO);3,6,9,15-tetraazabicyclo[9.3.1]pentadeca-1(15),11,13-triene-3,6,9-triacetic acid (PCTA);N′-{5-[Acetyl(hydroxy)amino]pentyl}-N-[5-({4-[(5-aminopentyl)(hydroxy)amino]-4-oxobutanoyl}amino)pentyl]-N-hydroxysuccinamide (DFO);diethylenetriaminepentaacetic acid (DTPA);trans-cyclohexyl-diethylenetriaminepentaacetic acid (CHX-DTPA);1-oxa-4,7,10-triazacyclododecane-4,7,10-triacetic acid (oxo-Do3A);p-isothiocyanatobenzyl-DTPA (SCN-Bz-DTPA);1-(p-isothiocyanatobenzyI)-3-methyl-DTPA (1B3M);2-(p-isothiocyanatobenzyI)-4-methyl-DTPA (1M3B); or1-(2)-methyl-4-isocyanatobenzyl-DTPA (MX-DTPA).18. A radiolabeled compound of .19. A radiolabeled compound of .20. A metal complex comprising a radionuclide and a compound of .21. The metal complex of claim 20 , wherein the radionuclide is selected from Zr claim 20 , Sc claim 20 , In claim 20 , Y claim 20 , Ga claim 20 , Lu claim 20 , Tc claim 20 , Cu claim 20 , Cu claim 20 , Gd claim 20 , Gd claim 20 , Gd claim 20 , Bi claim 20 , or Ac.22. A pharmaceutical composition comprising the compound of or a pharmaceutically acceptable ...

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Номер записи: 36
11-01-2018 дата публикации

PSMA TARGETED FLUORESCENT AGENTS FOR IMAGE GUIDED SURGERY

Номер: US20180009767A9
Автор: Chen Ying, Mease Ronnie C., Pomper Martin G., Ray Sangeeta, Sorger Jonathan
Принадлежит:

Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed. 3. The composition of claim 2 , wherein the composition is adapted for administration to a subject.4. The composition of claim 3 , wherein the composition comprises a unit dosage form of compound (3).5. The composition of claim 4 , wherein the unit dosage form delivers to the subject an amount of compound (3) between about 0.01 and about 8 mg/kg.6. The composition of claim 5 , wherein the unit dosage form delivers to the subject an amount of compound (3) of about 0.01 mg/kg claim 5 , about 0.05 mg/kg claim 5 , about 0.10 mg/kg claim 5 , about 0.20 mg/kg claim 5 , about 0.3 mg/kg claim 5 , about 0.35 mg/kg claim 5 , about 0.40 mg/kg claim 5 , about 0.45 mg/kg claim 5 , about 0.50 mg/kg claim 5 , about 0.55 mg/kg claim 5 , about 0.60 mg/kg claim 5 , about 0.65 mg/kg claim 5 , about 0.70 mg/kg claim 5 , about 0.75 mg/kg claim 5 , about 0.80 mg/kg claim 5 , about 0.90 mg/kg claim 5 , about 1 mg/kg claim 5 , about 2 claim 5 , mg/kg claim 5 , about 4 mg/kg claim 5 , about 6 mg/kg claim 5 , or about 8 mg/kg.7. The composition of claim 2 , wherein the composition is in a single dose form.8. The composition of claim 2 , wherein the composition is in dry form.9. The composition of claim 2 , wherein the composition is lyophilized in a sterile container.10. The composition of claim 2 , wherein the composition is contained within a sterile container.11. The composition of claim 10 , wherein the sterile container comprises a machine detectable identifier.12. The composition of claim 2 , further comprising one or more pharmaceutically acceptable excipients in an oral dosage form.13. The composition of claim 2 , further comprising one or more pharmaceutically acceptable carriers in an injectable dosage form.14. The composition of claim 2 , further ...

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Номер записи: 37
11-01-2018 дата публикации

TETRAZOLE BASED CORROSION INHIBITORS

Номер: US20180009768A1
Автор: Johnson Donald A., Reny Edouard Andre, Sawant Kailas B., Seetharaman Jothibasu, Sivaswamy Vaideeswaran
Принадлежит: ECOLAB USA INC.

Disclosed are corrosion inhibitor compounds and compositions useful for preventing or inhibiting corrosion of surfaces found in cooling water applications. In some embodiments, the surfaces may include mild steel, aluminum, brass, copper, galvanized steel, a copper alloy, admirality brass, or any combination thereof. Also disclosed are methods of using the compounds and compositions as corrosion inhibitors. In some embodiments, the corrosion inhibitor compounds and compositions are used in cooling water applications. 2. The composition of claim 1 , wherein{'sub': 6', '10', '2', '2', '1', '6', '1', '6', '1', '6', '2', '2', '1', '6, 'sup': 3', '4', '3', '4, 'L is C-C-alkylenyl substituted or unsubstituted with 1 to 3 substituents independently selected from the group consisting of —F, —Cl, —NO, —CN, —OH, —NH, C-Calkyl, C-Chaloalkyl, C-Calkoxy, —COR, and —CON(R), wherein Rand R, at each occurrence, are each independently selected from the group consisting of hydrogen and C-Calkyl.'}3. The composition of claim 1 , wherein L is unsubstituted C-C-alkylenyl.4. The composition of claim 1 , wherein L is C-C-alkylenyl substituted with one claim 1 , two claim 1 , or three tetrazolyl groups claim 1 , wherein said tetrazolyl groups are substituted or unsubstituted.5. The composition of claim 1 , wherein the compound of formula (II) is selected from the group consisting of:1,6-di(1H-tetrazol-5-yl)hexane (“HDTZ”);1,7-di(1H-tetrazol-5-yl)heptane (“HeDTZ”);1,8-di(1H-tetrazol-5-yl)octane (“ODTZ”); and5,5′,5″-(hexane-1,3,6-triyl)tris(1H-tetrazole) (“TCH-TZ”).6. The composition of claim 1 , further comprising one or more components claim 1 , each component independently selected from the group consisting of:a solvent;a tracer;a scale inhibitor;a dispersant;an acid; anda base.7. The composition of claim 1 , wherein the composition comprises about 40% by weight of one or more compounds of formula (II).8. The composition of claim 1 , wherein the composition is a stable water-based ...

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Номер записи: 38
08-01-2015 дата публикации

DUAL-ACTING ANTIHYPERTENSIVE AGENTS

Номер: US20150011597A1
Автор: Hegde Sharath, Marquess Daniel
Принадлежит: THERAVANCE BIOPHARMA R&D IP, LLC.

The invention is directed to compounds of formula I: 136-. (canceled)37. A method for treating hypertension , comprising administering to a patient a therapeutically effective amount of a compound having both ATreceptor-antagonizing activity and neprilysin enzyme-inhibiting activity.38. The method of claim 37 , wherein the compound has a pKvalue for binding to an ATreceptor greater than or equal to about 5.0 and a pICvalue for the inhibition of the neprilysin enzyme greater than or equal to about 5.0.39. The method of claim 38 , wherein the compound has a pKvalue greater than or equal to about 6.0.40. The method of claim 39 , wherein the compound has a pKvalue within the range of about 8.0-10.0.41. The method of claim 38 , wherein the compound has a pICvalue greater than or equal to about 6.0.42. The method of claim 41 , wherein the compound has a pICvalue within the range of about 7.0-10.0.43. (canceled)44. A method for treating heart failure claim 41 , comprising administering to a patient a therapeutically effective amount of a compound having both ATreceptor-antagonizing activity and NEP enzyme-inhibiting activity.45. The method of claim 44 , wherein the compound has a pKvalue for binding to an ATreceptor greater than or equal to about 5.0 and a pICvalue for the inhibition of the neprilysin enzyme greater than or equal to about 5.0.46. (canceled)47. A method of treating a patient suffering from a disease or disorder that is treated by antagonizing the ATreceptor and/or inhibiting the NEP enzyme claim 44 , comprising administering to a patient a therapeutically effective amount of a compound having both ATreceptor-antagonizing activity and NEP enzyme-inhibiting activity.48. The method of claim 47 , wherein the compound has a pKvalue for binding to an ATreceptor greater than or equal to about 5.0 and a pICvalue for the inhibition of the neprilysin enzyme greater than or equal to about 5.0.4954-. (canceled) This application claims the benefit of U.S. Provisional ...

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Номер записи: 39
14-01-2021 дата публикации

METHOD FOR PRODUCING THE CRYSTALLINE FORM OF MODIFICATION A OF CALCOBUTROL

Номер: US20210009534A1
Автор: PLATZEK Johannes, Trentmann Wilhelm
Принадлежит:

A method is described for production of a high purity compound of the formula (I) 2. The method of claim 1 , further comprising:{'sup': '3+', 'decomplexing a gadolinium complex of dihydroxy-hydroxy-methylpropyl-tetraazacyclododecane-triacetic acid (gadobutrol) to give a decomplexed solution comprising Gd ion and a dihydroxy-hydroxy-methylpropyl-tetraazacyclododecane-triacetic acid ligand; and'}precipitating a gadolinium salt from the decomplexed solution to provide the solution of the dihydroxy-hydroxy-methylpropyl-tetraazacyclododecane-triacetic acid ligand.3. The method of claim 2 , wherein decomplexing the gadolinium complex of dihydroxy-hydroxy-methylpropyl-tetraazacyclododecane-triacetic acid (gadobutrol) to give a decomplexed solution comprising Gd ion and a free dihydroxy-hydroxy-methylpropyl-tetraazacyclododecane-triacetic acid ligand comprises heating an aqueous solution of the gadolinium complex of dihydroxy-hydroxy-methylpropyl-tetraazacyclododecane-triacetic acid (gadobutrol) and oxalic acid to give a solution of gadolinium oxylate and the free dihydroxy-hydroxy-methylpropyl-tetraazacyclododecane-triacetic acid ligand.4. The method of claim 2 , wherein precipitating a gadolinium salt from the decomplexed solution to provide a solution of the dihydroxy-hydroxy-methylpropyl-tetraazacyclododecane-triacetic acid ligand comprises precipitating the gadolinium oxylate from the decomplexed solutions and filtering a precipitated gadolinium oxylate from the solution of dihydroxy-hydroxy-methylpropyl-tetraazacyclododecane-triacetic acid ligand.5. The method of claim 1 , wherein eluting the acidic ion exchange column having the bound dihydroxy-hydroxy-methylpropyl-tetraazacyclododecane-triacetic acid ligand with an aqueous basic solution comprises eluting the acidic ion exchange column having the bound hydroxy-hydroxy-methylpropyl-tetraazacyclododecane-triacetic acid ligand with an aqueous ammonia solution.6. The method of claim 1 , wherein crystallizing the calcium ...

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Номер записи: 40
19-01-2017 дата публикации

Pyrrole compounds as granzyme b inhibitors

Номер: US20170015705A1
Автор: Dale R. Cameron
Принадлежит: VIDA THERAPEUTICS Inc

Pyrrole compounds as Granzyme B inhibitors, compositions that include the compounds, and methods for using the compounds. Method for treating cutaneous scleroderma, epidermolysis bullosa, radiation dermatitis, alopecia areata, and discoid lupus erythematosus are provided.

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Номер записи: 41
19-01-2017 дата публикации

HPPD VARIANTS AND METHODS OF USE

Номер: US20170016018A1
Автор: ARMSTRONG Roxanne, Dubald Manuel, Laber Bernd, Lange Gudrun, Poree Fabien
Принадлежит: Bayer CropScience Aktiengesellschaft

In the present invention, HPPD enzymes and plants containing them showing a full tolerance against several classes of HPPD-inhibitors are described. 1. A recombinant nucleic acid molecule encoding a 4-hydroxyphenylpyruvate dioxygenase (HPPD) protein consisting of an amino acid sequence comprising a proline at the amino acid position corresponding to amino acid position 335 of SEQ ID NO:1 and a phenylalanine or a tyrosine at the position corresponding to amino acid position 336 of SEQ ID NO:1 , and wherein said HPPD protein is tolerant to an HPPD inhibitor herbicide.2. The recombinant nucleic acid molecule of claim 1 , wherein said encoded HPPD protein consists of an amino acid sequence further comprising:i. an alanine, arginine, asparagine, aspartic acid, cysteine, glutamic acid, glutamine, glycine, histidine, isoleucine, leucine, lysine, methionine, phenylalanine, serine, threonine, tryptophan, tyrosine, or valine at the amino acid position corresponding to amino acid position 188 of SEQ ID NO:1; andii. an alanine, arginine, asparagine, aspartic acid, cysteine, glutamic acid, glutamine, glycine, histidine, leucine, lysine, methionine, phenylalanine, serine, threonine, tryptophan, tyrosine, or valine at the amino acid position corresponding to amino acid position 189 of SEQ ID NO:1; andiii. an isoleucine, leucine, or methionine at the amino acid position corresponding to amino acid position 200 of SEQ ID NO:1; andiv. an alanine, leucine, proline, or asparagine at the amino acid position corresponding to amino acid position 215 of SEQ ID NO:1; andv. a histidine or glutamine at the amino acid position corresponding to amino acid position 226 of SEQ ID NO:1; andvi. a histidine, isoleucine, leucine, methionine, glutamine, arginine, alanine, lysine, serine, threonine, or valine at the amino acid position corresponding to amino acid position 339 of SEQ ID NO:1; andvii. an alanine, arginine, asparagine, aspartic acid, cysteine, glutamic acid, glutamine, glycine, histidine, ...

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Номер записи: 42
15-01-2015 дата публикации

HERBICIDAL 3- (SULFIN-/SULFONIMIDOYL) - BENZAMIDES

Номер: US20150018209A1
Автор: AHRENS HARTMUT, Braun Ralf, Dietrich Hansjoerg, Doerner-Rieping Simon, GATZWEILER ELMAR, KOEHN ARNIM, LEHR Stefan, ROSINGER CHRISTOPHER HUGH, SCHMUTZLER Dirk
Принадлежит:

The invention relates to sulfin- and sulfonimidoylbenzamides of general formula (S) used as herbicides. In said formula (I), R, R′, R″, X, W and Z represent radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogens. Q represents a tetrazolyl-, triazolyl or oxadiazolyl radicals. 4. A herbicidal composition which comprises a herbicidally active amount of at least one compound of formula (I) as claimed in and/or a salt thereof.5. The herbicidal composition as claimed in in a mixture with one or more formulation auxiliaries.6. The herbicidal composition as claimed in which comprises at least one further pesticidally active compound selected from the group consisting of insecticides claim 4 , acaricides claim 4 , herbicides claim 4 , fungicides claim 4 , safeners and growth regulators.7. The herbicidal composition as claimed in which comprises a safener.8. The herbicidal composition as claimed in which comprises cyprosulfamide claim 7 , cloquintocet-mexyl claim 7 , mefenpyr-diethyl or isoxadifen-ethyl.9. The herbicidal composition as claimed in which comprises a further herbicide.10. A method of controlling one or more unwanted plants claim 1 , which comprises applying an effective amount of at least one compound of formula (I) and/or a salt thereof as claimed in to the plants or to a location of unwanted plant growth.11. A compound of formula (I) and/or a salt thereof as claimed in capable of being used for controlling one or more unwanted plants.12. A compound as claimed in claim 11 , wherein the compound of the formula (I) and/or a salt thereof is employed for controlling one or more unwanted plants in one or more crops of useful plants.13. A compound as claimed in claim 12 , wherein the useful plants are transgenic useful plants. The invention relates to the technical field of the herbicides, in particular to that of the herbicides for the selective control of broad-leafed leaves and weed grasses in crops of useful plants.WO 2011/ ...

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Номер записи: 43
15-01-2015 дата публикации

HERBICIDALLY-EFFECTIVE SULFINYL AMINOBENZAMIDES

Номер: US20150018210A1
Автор: AHRENS HARTMUT, Braun Ralf, Dietrich Hansjoerg, GATZWEILER ELMAR, KOEHN ARNIM, LEHR Stefan, ROSINGER CHRISTOPHER HUGH, SCHMUTZLER Dirk
Принадлежит:

Sulfinylaminobenzamides of the general formula (I) as herbicides are described. 4. A herbicidal composition claim 1 , comprising a herbicidally active content of at least one compound of the formula (I) and/or salt as claimed in .5. The herbicidal composition as claimed in in a mixture with one or more formulation auxiliaries.6. The herbicidal composition as claimed in claim 4 , comprising at least one further pesticidally active substance selected from the group consisting of insecticides claim 4 , acaricides claim 4 , herbicides claim 4 , fungicides claim 4 , safeners and growth regulators.7. The herbicidal composition as claimed in claim 6 , comprising a safener.8. The herbicidal composition as claimed in claim 7 , comprising cyprosulfamide claim 7 , cloquintocet-mexyl claim 7 , mefenpyr-diethyl or isoxadifen-ethyl.9. The herbicidal composition as claimed in claim 6 , comprising a further herbicide.10. A method of controlling one or more unwanted plants claim 1 , comprising applying an effective amount of at least one compound of the formula (I) and/or salt as claimed in any of to the plants and/or to a site of unwanted vegetation.11. A compound of formula (I) and/or salt as claimed in capable of being used for controlling one or more unwanted plants.12. The compound and/or salt as claimed in claim 11 , wherein the compound of the formula (I) and/or salt is used for controlling one or more unwanted plants in one or more crops of useful plants.13. The compound and/or salt as claimed in claim 12 , wherein the useful plants are transgenic useful plants. The invention relates to the technical field of herbicides, especially that of herbicides for selective control of broad-leaved weeds and weed grasses in crops of useful plants.WO 2011035874 A1 discloses herbicidally active N-(1,2,5-oxadiazol-3-yl)benzamides. WO 2004052849 A1 discloses herbicidally active benzoyl derivatives bearing a sulfinylamino group in the 3 position of the phenyl ring. However, the herbicidal ...

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Номер записи: 44
16-01-2020 дата публикации

COMPOUNDS CONTAINING S-N-VALERYL-N-{[2'-(1H-TETRAZOLE-5-YL)-BIPHENYL-4-YL]-METHYL}-VALINE AND (2R,4S)-5-BIPHENYL-4-YL-4-(3-CARBOXY-PROPIONYLAMINO)-2-METHYL-PENTANOIC ACID ETHYL ESTER MOIETIES AND CATIONS

Номер: US20200016109A1
Автор: Blacklock Thomas J., Feng Lili, Girgis Michael J., GODTFREDSEN Sven Erik, Hu Bin, Karpinski Piotr Henryk, LIU Yugang, Prashad Mahavir, Sutton Paul Allen
Принадлежит:

A compound comprising of the angiotensin receptor antagonist (ARB) valsartan, the neutral endopeptidase inhibitor (NEPi) (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methylpentanoic acid ethyl ester and one or more monovalent cations such as Na useful for the treatment of hypertension and/or heart failure. 1. An amorphous solid form of a compound comprising anionic (S)—N-valeryl-N-{[2′-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-valine , anionic (2R ,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester , and sodium cations in a 1:1:3 molar ratio.2. A pharmaceutical composition comprising the amorphous solid form according to and at least one pharmaceutically acceptable excipient.3. A process for preparing the amorphous solid form according to claim 1 , the process comprising:dissolving (S)—N-valeryl-N-{[2′-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-valine or a pharmaceutically acceptable salt thereof, and (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester or a pharmaceutically acceptable salt thereof, in a first solvent to form a first solution;dissolving a sodium-containing compound in a second solvent to form a second solution;combining the first and second solutions to form a combined solution; anddrying the combined solution.4. The process according to claim 3 , wherein the first solvent is different from the second solvent.5. An amorphous solid form of a compound comprising anionic (S)—N-valeryl-N-{[2′-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-valine claim 3 , anionic (2R claim 3 ,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester claim 3 , and sodium cations in a 1:1:3 molar ratio claim 3 , and water.6. A pharmaceutical composition comprising the amorphous solid form according to and at least one pharmaceutically acceptable excipient.7. A process for preparing the amorphous solid form according to claim 5 , the process comprising:dissolving (S)—N- ...

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Номер записи: 45
16-01-2020 дата публикации

COMPOUNDS CONTAINING S-N-VALERYL-N-{[2'-(1H-TETRAZOLE-5-YL)-BIPHENYL-4-YL]-METHYL}-VALINE AND (2R,4S)-5-BIPHENYL-4-YL-4-(3-CARBOXY-PROPIONYLAMINO)-2-METHYL-PENTANOIC ACID ETHYL ESTER MOIETIES AND CATIONS

Номер: US20200016110A1
Автор: Blacklock Thomas J., Feng Lili, Girgis Michael J., GODTFREDSEN Sven Erik, Hu Bin, Karpinski Piotr Henryk, LIU Yugang, Prashad Mahavir, Sutton Paul Allen
Принадлежит:

A compound comprising of the angiotensin receptor antagonist (ARB) valsartan, the neutral endopeptidase inhibitor (NEPi) (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methylpentanoic acid ethyl ester and one or more monovalent cations such as Na+ useful for the treatment of hypertension and/or heart failure. 1. A glassy solid form of a compound comprising anionic (S)—N-valeryl-N-{[2′-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-valine , anionic (2R ,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester , and sodium cations in a 1:1:3 molar ratio.2. A pharmaceutical composition comprising the glassy solid form according to and at least one pharmaceutically acceptable excipient.3. A process for preparing the amorphous solid form according to claim 1 , the process comprising:dissolving (S)—N-valeryl-N-{[2′-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-valine or a pharmaceutically acceptable salt thereof, and (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester or a pharmaceutically acceptable salt thereof, in acetone to form a first solution;dissolving a NaOH in water to form a second solution;combining the first and second solutions and stirring them to form a combined solution; andevaporating the combined solution to obtain a glassy solid.4. A pharmaceutical composition comprising a compound comprising anionic (S)—N-valeryl-N-{[2′-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-valine claim 1 , anionic (2R claim 1 ,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester claim 1 , and sodium cations in a 1:1:3 molar ratio claim 1 , obtained by mixing the glassy solid form according to and at least one pharmaceutically acceptable excipient.5. A glassy solid form of a compound comprising anionic (S)—N-valeryl-N-{[2′-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-valine claim 1 , anionic (2R claim 1 ,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ...

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Номер записи: 46
16-01-2020 дата публикации

DIMERIC CONTRAST AGENTS

Номер: US20200017453A1
Автор: BOI Valeria, GIOVENZANA Giovanni Battista, Lattuada Luciano, NAPOLITANO Roberta
Принадлежит: BRACCO IMAGING S.P.A.

The present invention relates to new class of dimeric macrocycles capable of chelating paramagnetic metal ions, their chelated complexes with the paramagnetic metal ions and the use thereof as contrast agents, particularly suitable for Magnetic Resonance Imaging (MRI) analysis. 2. The compound according to in which Ris H.5. (canceled)7. The compound according to in which claim 6 , in the formula (III A)p is 2;r is from 2 to 5; and{'sup': '3', 'Ris H, or methyl.'}14. (canceled)16. The compound according to in which in the formula (I) n is 1 and Ris H.17. The compound according to in which in the formula (I) n is 1 and Ris methyl.18. A chelated complex of a compound according to with two paramagnetic metal ions selected from the group consisting of Fe claim 1 , Fe claim 1 , Cu claim 1 , Cr claim 1 , Gd claim 1 , Eu claim 1 , Dy claim 1 , La claim 1 , Yb and Mn claim 1 , or a physiologically acceptable salt thereof.19. The chelated complex according to claim 18 , wherein the paramagnetic metal ions are Gdions.20. The chelated complex according to with bivalent metal ion(s) claim 18 , wherein the physiologically acceptable salt is with a cation of (i) an inorganic base selected from an alkali metal and alkaline-earth metal claim 18 , (ii) an organic base selected from ethanolamine claim 18 , diethanolamine claim 18 , morpholine claim 18 , glucamine claim 18 , N-methylglucamine claim 18 , and N claim 18 ,N-dimethylglucamine or (iii) an amino acid selected from lysine claim 18 , arginine and ornithine.21. A method of MR imaging comprising:{'claim-ref': {'@idref': 'CLM-00018', 'claim 18'}, 'administering the chelated complex as defined in to a patient;'}submitting the patient to a radiation frequency selected to excite non-zero proton spin nuclei of the chelated complex; andrecording a MR signal from said nuclei.22. A pharmaceutical composition comprising a chelated complex of in combination with one or more pharmaceutically acceptable carriers claim 18 , diluents or ...

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Номер записи: 47
28-01-2016 дата публикации

PROCESS FOR PRODUCING 1,4,7,10-TETRAAZACYCLODODECANE-1,4,7,10-TETRAACETIC ACID AND COMPLEXES THEREOF

Номер: US20160024030A1
Автор: BOI Xavier, BUFFEL Diederik, BURT Jennifer, GANORKAR Rakesh
Принадлежит: AGFA HEALTHCARE

A process for producing 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) including salts and hydrates thereof of general formula (I) from the respective cyclen. 110-. (canceled)12. The process according to claim 11 , wherein step a) is performed at a pH≧13.13. The process according to claim 11 , wherein an amount of the halo-acetic acid in step a) is at least 4 equivalents with regard to an initial amount of cyclen and an amount of the base is at least two times a number of equivalents of the halo-acetic acid.14. The process according to claim 11 , wherein the halo-acetic acid is selected from the group consisting of iodoacetic acid claim 11 , bromoacetic acid claim 11 , and chloroacetic acid.15. The process according to claim 11 , wherein the base in step a) is an alkali metal hydroxide.16. The process according to claim 11 , wherein the acid added in step b) is selected from the group consisting of HCl claim 11 , HSO claim 11 , HNO claim 11 , HBr claim 11 , HI claim 11 , and HClO.17. The process according to claim 11 , wherein the heating and cooling steps in step b) occur claim 11 , respectively claim 11 , at a temperature in a range from 50 to 60° C. and a temperature in a range from 5 to 10° C.18. The process according to claim 11 , further comprising performing a washing step with a mixture of water and a water miscible low boiling organic solvent in a ratio from 1:1.5 to 1:3 (weight/weight) between step b) and step c).19. The process according to claim 11 , wherein claim 11 , in step e) claim 11 , the organic volatile acid used in the first stage is formic acid or acetic acid in an aqueous solution at a concentration between 0.01-0.1% or 0.1-0.3% respectively claim 11 , and the organic volatile acid used in the second stage is formic acid in an aqueous solution at a concentration in a range from 1 to 20%.20. A process for preparing gadoterate meglumine claim 11 , the process comprising the steps of:{'claim-ref': {'@idref': 'CLM-00011', 'claim ...

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Номер записи: 48
24-01-2019 дата публикации

SELECTIVE PHOTOACTIVATION OF AMINO ACIDS FOR SINGLE STEP PEPTIDE COUPLING

Номер: US20190023734A1
Автор: Jayaraman Vasanth
Принадлежит:

Disclosed herein are formulations, substrates, and arrays for amino acid and peptide synthesis on microarrays. In certain embodiments, methods for manufacturing and using the formulations, substrates, and arrays including one-step coupling, e.g., for synthesis of peptides in a C→N orientation are disclosed. In some embodiments, disclosed herein are formulations and methods for high efficiency coupling of biomolecules to a substrate. 113.-. (canceled)14. A method of attaching a coupling molecule to a substrate , comprising:obtaining a substrate comprising a plurality of amine groups for linking to a coupling molecule;contacting said substrate with a carboxylic acid activating formulation comprising: a carboxylic acid activating compound, wherein said compound is 1-(3-(diethylamino)-propyl)-4-(2-methoxyphenyl)-1,4-dihydro-5H-tetrazole-5-thione, a coupling molecule, and a solvent;selectively exposing said photoactive coupling formulation to light, thereby activating a carboxylic group of said coupling molecule at a selectively exposed area;coupling the activated carboxylic group of said coupling molecule to at least one of said plurality of amine groups at said selectively exposed area, wherein said coupling is performed multiple times at different selectively exposed areas on said substrate and wherein said coupling step has a coupling efficiency of at least 98.5%; andoptionally repeating said method to produce a desired polymer at said at least one carboxylic acid group.15. The method of claim 14 , wherein said coupling molecule is an amino acid.16. The method of claim 15 , wherein said amino acid has a protecting group attached to an amine group.17. The method of claim 16 , wherein said protecting group is Fmoc.18. A method of attaching a coupling molecule to a substrate claim 16 , comprising:obtaining a substrate comprising a plurality of amine groups for linking to a coupling molecule;contacting said substrate with a carboxylic acid activating formulation ...

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Номер записи: 49
28-01-2021 дата публикации

DIMERIC CONTRAST AGENTS

Номер: US20210024500A1
Автор: BOI Valeria, Lattuada Luciano, NAPOLITANO Roberta
Принадлежит: BRACCO IMAGING S.P.A.

The present invention relates to new class of dimeric macrocycles capable of chelating paramagnetic metal ions, their chelated complexes with metal ions and the use thereof as contrast agents, particularly suitable for Magnetic Resonance Imaging (MRI) analysis. 2. The compound according to in which Ris H.315.-. (canceled)18. The compound according to in which claim 1 , in the formula (IV) claim 1 , Ris a group of formula —(CH)CH(R)-G where s claim 1 , Rand G are as defined in .21. A chelated complex of a compound according to with two paramagnetic metal ions selected from the group consisting of Fe claim 1 , Fe claim 1 , Cu claim 1 , Cr claim 1 , Gd claim 1 , Eu claim 1 , Dy claim 1 , La claim 1 , Yb and Mn claim 1 , or a physiologically acceptable salt thereof.22. The chelated complex according to claim 21 , wherein the paramagnetic metal ions are Gd ions.23. The compound according to claim 1 , wherein the physiologically acceptable salt is with a cation of (i) an inorganic base selected from an alkali metal and alkaline-earth metal claim 1 , (ii) an organic base selected from ethanolamine claim 1 , diethanolamine claim 1 , morpholine claim 1 , glucamine claim 1 , N-methylglucamine claim 1 , and N claim 1 ,N-dimethylglucamine or (iii) an amino acid selected from lysine claim 1 , arginine and ornithine.24. The chelated complex according to claim 21 , wherein the physiologically acceptable salt is with a cation of (i) an inorganic base selected from an alkali metal and alkaline-earth metal claim 21 , (ii) an organic base selected from ethanolamine claim 21 , diethanolamine claim 21 , morpholine claim 21 , glucamine claim 21 , N-methylglucamine claim 21 , and N claim 21 ,N-dimethylglucamine or (iii) an amino acid selected from lysine claim 21 , arginine and ornithine.26. A pharmaceutical composition comprising a chelated complex of claim 21 , and at least one of a pharmaceutically acceptable carrier claim 21 , a diluent an excipient and combinations thereof.27. A ...

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Номер записи: 50
29-01-2015 дата публикации

ANTIMICROBIAL PEPTIDE COMPOSITIONS FOR PLANTS

Номер: US20150030566A1
Автор: De Beer Abré, Rautenbach Marina, Troskie Anscha Mari, Vosloo Johan Arnold
Принадлежит:

Compositions containing one or more tyrocidines, tryptocidines, phenycidines and/or gramicidin S, or derivatives and analogues thereof, are described for controlling antimicrobial growth on plants, plant material or plant growth media, and methods for controlling or preventing the growth of microbial pathogens, and in particular fungal pathogens, on plants, plant parts and plant material are described herein. The active agents used to control these pathogens are tyrocidines, tryptocidines, phenycidines and/or gramicidin S, or derivatives, analogues or modifications thereof. The tyrocidines, tryptocidines, phenycidines and/or gramicidin S are cyclic decapeptides having the general amino acid sequence cyclo(valine-Xrleucine-D-phenylalanine-proline-X-X-X-X-X) (SEQ ID NO: 1) or a derivative or analogue thereof, wherein Xis ornithine or lysine, Xis valine, leucine, isoleucine, phenylalanine, tryptophan or tyrosine; Xis the D-isomer of valine, leucine, isoleucine, phenylalanine, tryptophan, tyrosine, ornithine, or lysine; Xis asparagine, glutamine or leucine; Xis glutamine, the D-isomer of valine, leucine, or isoleucine; and X6 is tyrosine, phenylalanine, tryptophan or proline. 1. A plant antimicrobial composition for preventing or treating microbial growth on plants , plant parts or plant material , the composition comprising a cyclic decapeptide as an active agent which is a tyrocidine , tryptocidine , phenycidine or gramicidin S or an analogue thereof , the cyclic peptide comprising an amino acid sequence of cyclo(valine-X-leucine-D-phenylalanine-proline-X-X-X-X-X) (SEQ ID NO: 1) , wherein:{'sub': '1', 'Xis ornithine or lysine.'}2. The composition according to claim 1 , wherein:{'sub': '2', 'Xis valine, leucine, isoleucine, phenylalanine, tryptophan or tyrosine;'}{'sub': '3', 'Xis the D-isomer of valine, leucine, isoleucine, phenylalanine, tryptophan, tyrosine, ornithine, or lysine;'}{'sub': '4', 'Xis asparagine, glutamine or leucine;'}{'sub': '5', 'Xis glutamine, the ...

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Номер записи: 51
24-04-2014 дата публикации

EPOXYEICOSATRIENOIC ACID ANALOGS AND METHODS OF MAKING AND USING THE SAME

Номер: US20140113884A1
Автор: Campell William B., Falck John Russell, Imig John David
Принадлежит:

Compounds and compositions comprising epoxyeicosatrienoic acid (EET) analogs that act as EET agonists and are useful as medications in the treatment of drug-induced nephrotoxicity, hypertension and other related conditions. Methods of making and using the compounds and compositions are further described. 5. A composition comprising a compound of and a pharmaceutically acceptable carrier.6. A method of reducing hypertension in a subject claim 1 , comprising administering to a subject a therapeutically effective amount of a compound according to claim 1 , wherein hypertension in said subject is reduced.7. (canceled)8. (canceled)9. A method of reducing nephrotoxicity in a subject claim 1 , comprising administering to a subject a therapeutically effective amount of a compound according to claim 1 , wherein nephrotoxicity in said subject is reduced.10. The method of claim 9 , wherein the nephrotoxicity is drug-induced.11. The method of claim 10 , wherein the nephrotoxicity is cisplatin-induced.12. (canceled)13. (canceled)14. A method of reducing cisplatin nephrotoxicity in a subject claim 1 , comprising administering to a subject a therapeutically effective amount of a compound according to claim 1 , wherein cisplatin nephrotoxicity in said subject is reduced.15. (canceled)16. (canceled)17. A composition comprising a compound of and a pharmaceutically acceptable carrier.18. A method of reducing hypertension in a subject claim 4 , comprising administering to a subject a therapeutically effective amount of a compound according to claim 4 , wherein hypertension in said subject is reduced.19. A method of reducing nephrotoxicity in a subject claim 4 , comprising administering to a subject a therapeutically effective amount of a compound according to claim 4 , wherein nephrotoxicity in said subject is reduced.20. The method of claim 19 , wherein the nephrotoxicity is drug-induced.21. The method of claim 20 , wherein the nephrotoxicity is cisplatin-in-induced.22. A method of ...

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Номер записи: 52
02-02-2017 дата публикации

N-ALKOXYAMIDE CONJUGATES AS IMAGING AGENTS

Номер: US20170029386A9
Автор: Casebier David S., Cesati Richard R., Cheesman Edward H., Harris Thomas D., Looby Richard J., Robinson Simon P., Yalamanchili Padmaja
Принадлежит: Lantheus Medical Imaging, Inc.

The present disclosure is directed to compounds, diagnostic agents, and related methods. In some cases, methods for treating patients are provided. More specifically, the disclosure provides compounds, diagnostic agents, and kits for detecting and/or imaging and/or monitoring elastin rich tissues. In addition, the disclosure provides methods of detecting and/or imaging and/or monitoring the presence of coronary plaque, carotid plaque, iliac/femoral plaque, aortic plaque, renal artery plaque, plaque of any arterial vessel, aneurism, vasculitis, other diseases of the arterial wall, and/or damage or structural changes in ligaments, uterus, lungs or skin, as indicated by changes in total vessel wall area, internal lumen size, and exterior arterial perimeter. 150-. (canceled)52. The compound of claim 51 , wherein at least one Ris H.53. The compound of claim 51 , wherein X is N.54. The compound of claim 51 , wherein X is O claim 51 , S claim 51 , or P.55. The compound of claim 51 , wherein:X is N;{'sup': '1', 'Ris selected from the group consisting of hydrogen, alkyl, arylalkyl, and alkylarylalkyl;'}{'sup': 2', '3, 'Rand Rare each independently selected from the group consisting of hydrogen, alkyl, alkylaryl, aryl, arylalkyl, alkylarylalkyl, and heterocyclylalkyl;'}{'sup': '4', 'Ris selected from the group consisting of alkyl, alkylaryl, aryl, arylalkyl, and alkylarylalkyl,'}{'sup': 1', '2', '3', '4', '19', '20', '19', '20', '21', '22', '24', '24', '24', '24', '24', '24', '24', '24', '24', '24', '24', '24', '24', '24', '24', '24', '24', '24', '24', '24', '24', '24', '24', '24', '24', '24', '24, 'sub': 2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2, 'wherein each R, R, R, and Ris independently unsubstituted or substituted with one or more of the following: alkyl, alkenyl, cycloalkyl, alkylaryl, alkylcarbonyl, aryl, arylalkyl, alkylarylalkyl, alkoxy, alkoxyalkyl, alkoxycarbonyl, heteroalkyl, heterocyclyl, heterocyclylalkyl, —NRR, —SH, ...

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Номер записи: 53
31-01-2019 дата публикации

PHARMACEUTICAL COMPOSITION COMPRISING SACUBITRIL AND VALSARTAN

Номер: US20190030000A1
Автор: ALVAREZ FERNANDEZ Lisardo, DYMACEK Bohumil, Kumar Rohit, MITAS Petr, NOGUEIRAS NIETO Luis, VELADA CALZADA Jose, VIVANCOS MARTINEZ Marta
Принадлежит:

The present invention relates to a pharmaceutical composition comprising a physical mixture of sacubitril sodium and valsartan disodium, wherein the X-ray powder diffraction pattern of valsartan disodium comprises characteristic peaks at the following 2 theta (±0.2) angles: 4.70°, 9.29°, 22.34°, measured using a Cu Kα radiation. The invention further relates to the use of said pharmaceutical composition as medicament in the treatment of heart failure. 1. A pharmaceutical composition comprising a physical mixture of sacubitril sodium and valsartan disodium , wherein the X-ray powder diffraction pattern of valsartan disodium comprises characteristic peaks at the following 2 theta (±0.2) angles: 4.70° , 9.29° , 22.34° , measured using a Cu Kα radiation.2. The composition according to claim 1 , wherein the X-ray powder diffraction pattern of sacubitril sodium comprises characteristic peaks at the following 2 theta (±0.2) angles: 3.14° claim 1 , 6.25° claim 1 , 11.97° claim 1 , 12.73° claim 1 , 13.78° claim 1 , 16.50° claim 1 , 18.35° claim 1 , 19.93° claim 1 , 21.56° claim 1 , 23.75° claim 1 , 26.20° claim 1 , measured using a Cu Kα radiation.3. The composition according to containing one of the following combinations of amounts:(i) 25.6 mg sacubitril sodium and 28.3 mg valsartan disodium;(ii) 51.2 mg sacubitril sodium and 56.6 mg valsartan disodium; or(iii) 102.4 mg sacubitril sodium and 113.2 mg valsartan disodium.4. The composition according to claim 1 , wherein valsartan disodium has a particle size distribution Dequal to or less than 30 μm.5. The composition according to claim 1 , wherein sacubitril sodium has a particle size distribution Dequal to or less than 50 μm.6. The composition according to further comprising one or more diluents claim 1 , disintegrants claim 1 , glidants and lubricants; and wherein said composition is in the form of a tablet.7. The composition according to claim 6 , wherein the diluent is microcrystalline cellulose.8. The composition ...

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Номер записи: 54
31-01-2019 дата публикации

Pharmacokinetic enhancements of bifunctional chelates and uses thereof

Номер: US20190030194A1
Автор: Eric Steven BURAK, John Fitzmaurice Valliant, Ryan Wayne SIMMS, Stuart James MAHONEY
Принадлежит: Fusion Pharmaceuticals Inc

The present invention relates to conjugates including a chelating moiety of a metal complex thereof and a therapeutic or targeting moiety, methods for their production, and uses thereof.

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Номер записи: 55
30-01-2020 дата публикации

20-HETE RECEPTOR (GPR75) ANTAGONISTS AND METHODS OF USE

Номер: US20200030291A1
Автор: Falck John R., Garcia Victor, Schwartzman Miehal L.
Принадлежит:

The present invention concerns compounds and their use to treat cardiovascular disease, renal disease, thrombic disease, stroke, metabolic syndrome, cell proliferation, and ischemic cardiovascular disorders. Compounds of the present invention display significant potency as antagonists of 20-hydroxyeicosatetraenoic acid (20-HETE), and function as anti-hypertensive, anti-inflammatory, or anti-growth agents. 4. The compound of claim 2 , wherein R═C(O)R; R=glycine sodium salt; m=1; n=1; p=1; q=1; R═OH when R═H or R═H when R═OH; and R═CH.24. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.25. A method of treating cardiovascular disease claim 1 , renal disease claim 1 , diabetic retinopathy claim 1 , stroke claim 1 , obesity claim 1 , metabolic syndrome claim 1 , cancer claim 1 , or tumor growth in a subject comprising administering to said subject a therapeutically sufficient amount of a compound as shown in .26. The method of claim 25 , wherein the disease to be treated is diabetic nephropathy or diabetic retinopathy.27. The method of claim 25 , wherein administering comprises local claim 25 , regional claim 25 , systemic claim 25 , or continual administration.28. The method of claim 25 , further comprising providing to said subject a second therapy.29. The method of claim 28 , wherein said second therapy is provided prior to administering said compound.30. The method of claim 28 , wherein said second therapy is provided after administering said compound.31. The method of claim 28 , wherein said second therapy is provided at the same time as said compound.32. The method of claim 25 , wherein said subject is a human.33. A pharmaceutical composition comprising a compound as shown in claim 1 , dispersed in a pharmaceutically acceptable carrier claim 1 , buffer or diluent.34. A method of identifying a 20-HETE antagonist claim 1 , comprising the steps of:a) providing a polypeptide having a sequence of SEQ ID NO: 2;b) screening ...

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Номер записи: 56
24-02-2022 дата публикации

PHARMACOKINETIC ENHANCEMENTS OF BIFUNCTIONAL CHELATES AND USES THEREOF

Номер: US20220054664A1
Автор: Burak Eric Steven, Darwish Alla, Mahoney Stuart James, Simms Ryan Wayne, Valliant John Fitzmaurice
Принадлежит:

The present invention relates to conjugates including a chelating moiety of a metal complex thereof and a therapeutic or targeting moiety, methods for their production, and uses thereof. 2. The method of claim 1 , wherein said chelating moiety in Formula I is selected from the group consisting of DOTA (1 claim 1 ,4 claim 1 ,7 claim 1 ,10-tetraazacyclododecane-1 claim 1 ,4 claim 1 ,7 claim 1 ,10-tetraacetic acid) claim 1 , DOTMA (1R claim 1 ,4R claim 1 ,7R claim 1 ,10R)-α claim 1 , α′ claim 1 , α″ claim 1 , α′″-tetramethyl-1 claim 1 ,4 claim 1 ,7 claim 1 ,10-tetraazacyclododecane-1 claim 1 ,4 claim 1 ,7 claim 1 ,10-tetraacetic acid claim 1 , DOTAM (1 claim 1 ,4 claim 1 ,7 claim 1 ,10-tetrakis(carbamoylmethyl)-1 claim 1 ,4 claim 1 ,7 claim 1 ,10-tetraazacyclododecane) claim 1 , DOTPA (1 claim 1 ,4 claim 1 ,7 claim 1 ,10-tetraazacyclododecane-1 claim 1 ,4 claim 1 ,7 claim 1 ,10-tetra propionic acid) claim 1 , DO3AM-acetic acid (2-(4 claim 1 ,7 claim 1 ,10-tris(2-amino-2-oxoethyl)-1 claim 1 ,4 claim 1 ,7 claim 1 ,10-tetraazacyclododecan-1-yl)acetic acid) claim 1 , DOTA-GA anhydride (2 claim 1 ,2′ claim 1 ,2″-(10-(2 claim 1 ,6-dioxotetrahydro-2H-pyran-3-yl)-1 claim 1 ,4 claim 1 ,7 claim 1 ,10-tetraazacyclododecane-1 claim 1 ,4 claim 1 ,7-triyl)triacetic acid claim 1 , DOTP (1 claim 1 ,4 claim 1 ,7 claim 1 ,10-tetraazacyclododecane-1 claim 1 ,4 claim 1 ,7 claim 1 ,10-tetra(methylene phosphonic acid)) claim 1 , DOTMP (1 claim 1 ,4 claim 1 ,6 claim 1 ,10-tetraazacyclodecane-1 claim 1 ,4 claim 1 ,7 claim 1 ,10-tetramethylene phosphonic acid claim 1 , DOTA-4AMP (1 claim 1 ,4 claim 1 ,7 claim 1 ,10-tetraazacyclododecane-1 claim 1 ,4 claim 1 ,7 claim 1 ,10-tetrakis(acetamido-methylenephosphonic acid) claim 1 , CB-TE2A (1 claim 1 ,4 claim 1 ,8 claim 1 ,11-tetraazabicyclo[6.6.2]hexadecane-4 claim 1 ,11-diacetic acid) claim 1 , NOTA (1 claim 1 ,4 claim 1 ,7-triazacyclononane-1 claim 1 ,4 claim 1 ,7-triacetic acid) claim 1 , NOTP (1 claim 1 ,4 claim 1 ,7-triazacyclononane-1 claim 1 ...

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Номер записи: 57
07-02-2019 дата публикации

TETRAZOLE DERIVATIVES AS CYTOCHROME P450 INHIBITORS

Номер: US20190040020A1
Автор: Eriksson Leif, Sirsjö Allan, Strid Åke
Принадлежит:

According to the invention there is provided a compound of formula I, wherein Rand Rhave meanings given in the description, which compounds are useful in the treatment of skin disorders and other diseases. 2. The compound of Formula I according to claim 1 , wherein Ris a methyl group claim 1 , optionally substituted with one or more fluorine atoms.3. The compound of Formula I according to claim 1 , wherein Ris a carboxylic acid protecting group.4. The compound of Formula I according to claim 3 , wherein Ris said carboxylic acid protecting group and said carboxylic acid protecting group is selected from the group consisting of a Calkyl claim 3 , phenyl and benzyl.57.-. (canceled)10. The method of treatment according to claim 8 , wherein the condition is selected from a skin disorder; an undesirable growth or proliferation of cells; restenosis or thrombosis occurring upon the introduction of coronary stents; and inflammatory bowel disease.11. A pharmaceutical formulation comprising a compound of Formula I as defined in claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , in admixture with a pharmaceutically acceptable adjuvant claim 1 , diluent claim 1 , excipient or carrier.12. A pharmaceutical formulation according to claim 9 , wherein said compound of Formula I is present in an amount of from 0.01 to 90% by weight of the formulation.13. A pharmaceutical formulation according to claim 12 , wherein said compound of Formula I is present in an amount of from 0.05 to 50% by weight of the formulation.14. A pharmaceutical formulation according to claim 13 , wherein said compound of Formula I is present in an amount of from 1 to 20% by weight of the formulation.15. A pharmaceutical formulation according to claim 9 , wherein the amount of the compound of Formula I in the formulation is sufficient to achieve serum levels of between about 1 pM and about 1 mM in a patient.16. A pharmaceutical formulation according to claim 15 , wherein the amount of the compound ...

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Номер записи: 58
07-02-2019 дата публикации

FUNCTIONALIZED 1,2,4,5-TETRAZINE COMPOUNDS FOR USE IN BIOORTHOGONAL COUPLING REACTIONS

Номер: US20190040021A1
Автор: Devaraj Neal K., HILDERBRAND Scott A., Karver Mark R., Weissleder Ralph
Принадлежит:

The present application relates to functionalized 1,2,4,5-tetrazine compounds. The compounds are useful in compositions and methods using bioorthogonal inverse electron demand Diels-Alder cycloaddition reactions for the rapid and specific covalent delivery of a “payload” to a ligand bound to a biological target. 165-. (canceled)68. The peptide claim 66 , polypeptide or protein of claim 66 , wherein Ris hydrogen claim 66 , (C-C)alkyl claim 66 , or (C-C)haloalkyl.69. The peptide claim 68 , polypeptide or protein of claim 68 , wherein A is absent claim 68 , n2 is 0 and n1 is 1.71. The peptide claim 70 , polypeptide or protein of claim 70 , wherein n2 is 0.73. The peptide claim 72 , polypeptide or protein of claim 72 , wherein n1 is 3 claim 72 , 4 or 5 claim 72 , and n2 is 0 claim 72 , 1 claim 72 , or 2.75. The peptide claim 74 , polypeptide or protein of claim 74 , wherein n2 is other than 0 and n1 is 4.77. The peptide claim 76 , polypeptide or protein of claim 76 , wherein n1 is 1 or 2 and n2 is 5.79. The peptide claim 78 , polypeptide or protein of claim 78 , wherein n1 is 3 claim 78 , 4 or 5 and n2 is 0.81. The peptide claim 66 , polypeptide or protein of claim 66 , wherein the amino acid has (L) configuration.83. The method of claim 82 , wherein Ris hydrogen claim 82 , tert-butyloxycarbonyl or 9-fluorenylmethoxycarbonyl and Ris hydrogen or (C-C)alkyl.85. A peptide claim 82 , polypeptide or protein prepared by the process of . This application is a continuation of U.S. patent application Ser. No. 14/437,905, filed Apr. 23, 2015, which is pending, which is a U.S. National Phase Application under 35 U.S.C. § 371 of International Patent Application No. PCT/US2013/031524, filed internationally on Mar. 14, 2013, which claims the benefit of U.S. Provisional Application No. 61/718,008, filed Oct. 24, 2012. The entire disclosure of each of the aforementioned related applications is hereby incorporated by reference.This invention was made with Government support under Grant ...

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Номер записи: 59
18-02-2021 дата публикации

Stable amorphous form of sacubitril valsartan trisodium complex and processes for preparation thereof

Номер: US20210046050A1
Автор: Pavan Kumar Seethamraju, Ram Thaimattam, Ravindra Babu Bollu, Sivarami Reddy YASAM, Uma Maheswar Rao VASIREDDI, Venkateswar Rao Challagonda
Принадлежит: Laurus Labs Pvt Ltd

The present invention relates to stable amorphous form of sacubitril valsartan trisodium complex and its solid dispersion compounds, processes for their preparation and pharmaceutical composition comprising the same. The present invention also relates to an improved process for the preparation of sacubitril sodium and its use in the preparation of sacubitril valsartan trisodium complex.

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Номер записи: 60
06-02-2020 дата публикации

METHOD FOR PREPARATION OF INSENSITIVE HIGH EXPLOSIVE

Номер: US20200039895A1
Автор: Ho Chan-Yuan, Lin Tsair-Feng, Wang Yan-Lin
Принадлежит:

The present invention provides a method for the preparation of an insensitive high enthalpy explosive Dihydroxylammonium 5,5′-bistetrazole-1,1′-diolate (TKX-50) in the presence of N,N-dimethylformamide, N,N-dimethylacetamide, or N-Methyl-2-pyrrolidone as a solvent via a four-step, one-pot reaction route to obtain a final product after four reaction steps. The more dangerous intermediate diazidoglyoxime may be solved by the one-pot method without the need of isolation. Further, the cyclization reaction is carried out in the presence of dropwisely added concentrated sulfuric acid to replace hydrochloric gas so no hydrochloric gas generator is needed to greatly reduce the amount of waste acid so as to effectively reduce the cost by avoiding using hydrochloric gas steel cylinders which require much safety equipment. 1. A method for preparing an insensitive high enthalpy explosive via a four-step , one-pot reaction route , comprising:(A) performing a chlorination reaction: carrying out the chlorination reaction for 1˜4 hours when warming up to 25° C.˜50° C., after dissolving glyoxime in at least one of N,N-dimethylformamide, dimethylacetamide and N-methyl-2-pyrrolidone, then adding N-chlorosuccinimide to at least one of the N,N-dimethylformamide, the dimethylacetamide and the N-methyl-2-pyrrolidone with cooling to 0° C.˜10° C.;(B) performing an azidation reaction: adding sodium azide to at least one of the N,N-dimethylformamide, the dimethylacetamide and the N-methyl-2-pyrrolidone with cooling to −5° C.˜5° C. to carry out the azidation reaction for 3 hours at suitable temperature;{'sub': '2', '(C) performing a cyclization reaction: adding concentrated sulfuric acid to at least one of the N,N-dimethylformamide, the dimethylacetamide and the N-methyl-2-pyrrolidone to carry out the cyclization reaction for 14˜16 hours at suitable temperature before cooling and adding a 40% sodium hydroxide aqueous solution to adjust a pH value to obtain 1,1′-dihydroxy-5,5′-bistetrazole ...

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Номер записи: 61
12-02-2015 дата публикации

Compound, method for producing compound, and method for purifying compound

Номер: US20150045557A1
Автор: Kaoru Noda, Keiichiro Matsuda, Masayuki Matsushita, Satoshi Kajita
Принадлежит: Nippon Soda Co Ltd

The present invention provides a compound characterized by being represented by general formula (I): (wherein, A represents a halogen atom, alkyl group, haloalkyl group, alkoxy group, haloalkoxy group, alkylsulfonyl group, unsubstituted or substituted aryl group, cyano group or nitro group, n represents an integer of 0 to 5 (and A may be mutually the same or different when n is 2 or more), Y represents an alkyl group, M represents an alkaline metal or alkaline earth metal, and m represents an integer of 1 or 2).

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Номер записи: 62
01-05-2014 дата публикации

Cinnamic acid derivative, polymer thereof, and liquid crystal alignment layer comprising cured product thereof

Номер: US20140121345A1
Автор: Haruyoshi Takatsu, Isa Nishiyama, Martin Schadt, Masanao Hayashi, Masayuki Iwakubo, Sayaka Nose, Yutaka Nagashima
Принадлежит: DIC Corp

Provided is a liquid crystal alignment layer of which a constituent member is a compound represented by the general formula (I).

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Номер записи: 63
13-02-2020 дата публикации

EXTENDED ABSORBANCE SOLAR LEAF AND METHODS OF MAKING

Номер: US20200048094A1
Автор: King Scott B., Kobilka Brandon M., Kuczynski Joseph, Wertz Jason T.
Принадлежит:

In an embodiment is provided a method of making a photo-absorbing composition that includes forming a donor-acceptor small molecule (DASM) by bonding an electron donor portion to an electron acceptor portion; and bonding the DASM to a nanographene structure using a Stille coupling reaction, a Suzuki cross-coupling reaction, or a C—H activation cross-coupling reaction. In another embodiment is provided films that include a photo-absorbing composition. 2. The method of claim 1 , wherein bonding the DASM to the nanographene structure comprises:forming a Stille reagent from the DASM;brominating a polyphenylene-pyrene dione precursor of the nanographene structure; andreacting the Stille reagent with the brominated polyphenylene-pyrene dione precursor in a Stille coupling reaction.3. The method of claim 2 , wherein forming the DASM comprises cross-linking two or more portions of the DASM.4. The method of claim 2 , wherein the DASM has more than one electron donor portion or more than one electron acceptor portion.5. The method of claim 2 , wherein bonding the DASM to the nanographene structure comprises forming a network of the DASM and the nanographene structure.6. The method of claim 2 , wherein forming the Stille reagent comprises adding a thiophene group to the DASM.7. The method of claim 2 , wherein reacting the Stille reagent with the brominated polyphenylene-pyrene dione precursor forms a DASM-nanographene dione precursor claim 2 , and the method further comprises condensing the DASM-nanographene precursor and forming a DASM-nanographene complex.8. The method of claim 7 , wherein forming the DASM-nanographene complex comprises forming a DASM-nanographene dione precursor and reacting the DASM-nanographene dione precursor with a diamine selected from the group consisting of 1 claim 7 ,2-benzenediamine and 1 claim 7 ,10-phenanthroline diamine.11. The method of claim 10 , wherein bonding the DASM to the nanographene structure comprises:forming a Stille reagent from the ...

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Номер записи: 64
13-02-2020 дата публикации

PROCESS FOR THE PREPARATION OF A DUAL-ACTING ANGIOTENSIN RECEPTOR-NEPRILYSIN INHIBITOR COMPOUND

Номер: US20200048210A1
Автор: Parthasaradhi Reddy Bandi, Rathnakar Reddy Kura, Vamsi Krishna Bandi, VENKAT NARSIMHA REDDY Adullla
Принадлежит:

The present invention relates to a process for preparing amorphous form of Sacubitril/Valsartan sodium salt of Formula-II and pharmaceutical composition comprising thereof. 1. A pharmaceutical formulation comprising a therapeutically effective amount of amorphous Sacubitril/Valsartan trisodium salt of Formula-II. This application is a divisional application of U.S. application Ser. No. 16/208,696 filed Dec. 4, 2018, which is a divisional application of U.S. application Ser. No. 15/752,943 filed Feb. 15, 2018, which is a National Stage application of PCT/IB2016/055097 filed Aug. 26, 2016, which claims priority to IN 4528/CHE/2015 filed Aug. 28, 2015.The present invention relates to a process for preparing amorphous form of LCZ696 and pharmaceutical composition comprising thereof.LCZ696 is known as Sacubitril/Valsartan trisodium hemipetahydrate and chemically known as 3-[N-[1(S)-(biphenyl-4-ylmethyl)-4-ethoxy-3(R)-methyl-4-oxobutyl]carbamoyl]propionic acid and N-pentanoyl-N-[2′-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-L-valine trisodium hemipentahydrate and has the following structure, wherein designated as Formula-I.Sacubitril is a neprilysin inhibitor pro-drug (AHU-377) and has now been tested in hypertension. LCZ696 has been approved in US under the trade name Entresto® as a tablet having dosage strengths 24MG, 26MG; 49MG, 51MG and 97MG, 103MG for treating chronic heart failure.Pharmaceutical composition comprising Sacubitril or its pharmaceutically acceptable salt thereof and Valsartan or its pharmaceutically acceptable salt thereof is disclosed in U.S. Pat. No. 7,468,390 B2.Mixed crystal/Co-crystal form of Sacubitril/Valsartan trisodium hemipentahydrate has been disclosed in U.S. Pat. No. 8,877,938 B2 of Novartis Pharmaceuticals. US′938 discloses the synthesis of Co-crystal of Sacubitril/Valsartan trisodium hemipentahydrate, which is as shown in .US′938 also discloses the synthesis for Linked pro-drug of amorphous form of Sacubitril/Valsartan, which is as shown in ...

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Номер записи: 65
10-03-2022 дата публикации

OXYGEN SCAVENGERS, COMPOSITIONS COMPRISING THE SCAVENGERS, AND ARTICLES MADE FROM THE COMPOSITIONS

Номер: US20220073699A1
Автор: Dauzvardis Matthew J., Li Shenshen
Принадлежит:

The disclosure relates to oxygen scavenging molecules, compositions, methods of making the compositions, articles prepared from the compositions, and methods of making the articles. 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. 19-. (canceled)11. The compound of claim 10 , wherein the compound is a cyclic polymeric compound.1621-. (canceled)22. A method for producing a packaging material having a wall with oxygen barrier properties comprising:{'b': '0', 'claim-text': 'wherein said compound is present in an amount of about 0.10 to 10 weight present of said composition,', '#text': '(a) combining a base polymer with at least one compound according to claim to form a composition, the composition having at least one transition metal in a positive oxidation state, said metal being present in the composition in an amount of 10 to 400 ppm; and'}(b) forming the product of step (a) into a wall; and(c) forming a container which comprises said wall.23. A method for making an article comprising:{'claim-text': ['(i) a base polymer; and', {'b': '0', 'claim-text': 'wherein said compound is present in an amount of about 0.10 to 10 weight present of said composition;', '#text': '(ii) at least one compound according to claim , to form a composition, the composition having at least one transition metal in a positive oxidation state, said metal being present in the composition in an amount of 10 to 400 ppm;'}], '#text': '(a) forming a melt by combining in a melt processing zone:'}(b) forming an article from said melt.24. The method of claim 23 , wherein the article is a preform claim 23 , sheet claim 23 , bottle claim 23 , cup claim 23 , or jar.25. A composition comprising organic material normally susceptible to gradual degradation in the presence of oxygen during use over an extended period containing an antioxidant effective amount of a compound according to .26. (canceled)27. ...

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Номер записи: 66
21-02-2019 дата публикации

CATALYSTS

Номер: US20190055352A1
Автор: Chapman Andy, Chartoire Anthony, Hollis Emmalina, Kember Michael, Keyworth Colin, Williams Charlotte
Принадлежит:

The present invention relates to the field of polymerisation catalysts, and systems comprising these catalysts for polymerising carbon dioxide and an epoxide, a lactide and/or lactone, and/or an epoxide and an anhydride. The catalyst is of formula (I): 2. The catalyst of claim 1 , wherein at least one of Mor Mis Ni(II).3. The catalyst of claim 1 , wherein one of Mor Mis selected from Ni(II) and Ni(III)-X and the remaining occurrence of Mand Mis selected from Zn(II) claim 1 , Cr(III)-X claim 1 , Cr(II) claim 1 , Co(III)-X claim 1 , Co(II) claim 1 , Cu(II) claim 1 , Mn(III)-X claim 1 , Mn(II) claim 1 , Mg(II) claim 1 , Ni(II) claim 1 , Ni(III)-X claim 1 , Fe(II) claim 1 , Fe(III)-X claim 1 , Ti(II) claim 1 , Ti(III)-X claim 1 , V(II) claim 1 , V(III)-X claim 1 , Ge(IV)-(X)and Ti(IV)-(X).4. The catalyst of claim 3 , wherein the remaining occurrence of Mand Mis selected from Zn(II) claim 3 , Cr(III)-X claim 3 , Co(II) claim 3 , Cu(II) claim 3 , Mn(II) claim 3 , Mg(II) claim 3 , Ni(II) claim 3 , Ni(III)-X claim 3 , Fe(II) claim 3 , Fe(III)-X and V(II).5. The catalyst of claim 3 , wherein the remaining occurrence of Mand Mis selected from Zn(II) claim 3 , Cr(III)-X claim 3 , Co(II) claim 3 , Mn(II) claim 3 , Mg(II) claim 3 , Ni(II) claim 3 , Ni(III)-X claim 3 , Fe(II) claim 3 , and Fe(III)-X.6. The catalyst of claim 3 , wherein the remaining occurrence of Mand Mis selected from any of: Zn(II) claim 3 , Mg(II) claim 3 , Ni(II) claim 3 , Co(II) claim 3 , Co(III)-X and Ni(III)-X.7. The catalyst of claim 1 , wherein both Mand Mare Ni(II).8. The catalyst of claim 1 , wherein Ris selected from substituted or unsubstituted alkylene and substituted or unsubstituted arylene.9. The catalyst of claim 1 , wherein Ris selected from substituted or unsubstituted alkylene claim 1 , alkenylene claim 1 , alkynylene claim 1 , heteroalkylene claim 1 , heteroalkenylene claim 1 , heteroalkynylene claim 1 , arylene claim 1 , and cycloalkylene.10. The catalyst of claim 1 , wherein Ris selected ...

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Номер записи: 67
02-03-2017 дата публикации

METHOD FOR PRODUCING TETRAZOLINONE COMPOUND

Номер: US20170057935A1
Автор: SHIODA Takayuki, UJITA Satoru
Принадлежит: Sumitomo Chemical Company, Limited

A tetrazolinone compound represented by formula (1): 2. The method according to claim 1 , wherein Ris a methyl group claim 1 , and R claim 1 , Rand Rare a hydrogen atom.3. The method according to claim 1 , wherein R is an isopropyl group claim 1 , and X is a chlorine atom or a bromine atom.5. The method according to claim 4 , wherein Ris a methyl group claim 4 , and R claim 4 , Rand Rare a hydrogen atom.6. The method according to claim 4 , wherein R is an isopropyl group claim 4 , and X is a chlorine atom or a bromine atom. The present invention relates to a method for producing a tetrazolinone compound.WO2013/162072 describes that 1-(2-halogenomethylphenyl)-4-methyl-1,4-dihydrotetrazol-5-ones such as 1-(2-bromomethyl-3-methylphenyl)-4-methyl-1,4-dihydrotetrazol-5-one are useful as a production intermediate of pesticides. Further, as a method for producing 1-(2-bromomethyl-3-methylphenyl)-4-methyl-1,4-dihydrotetrazol-5-one, a production method comprising mixing 1-(2-methoxymethyl-3-methylphenyl)-4-methyl-1,4-dihydrotetrazol-5-one obtained by mixing 1-(2-methoxymethyl-3-bromophenyl)-4-methyl-1,4-dihydrotetrazol-5-one, methylboronic acid and palladium, with hydrogen bromide and acetic acid is described.The present invention provides a method for industrially advantageously producing a 1-(2-halogenomethylphenyl)-4-methyl-1,4-dihydrotetrazol-5-one.The present invention is as described below.[1] A method for producing a compound represented by formula (1):[wherein Rrepresents an alkyl group having 1 to 6 carbon atoms or a cycloalkyl group having 3 to 6 carbon atoms, R, Rand Reach independently represent a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or a cycloalkyl group having 3 to 6 carbon atoms, and Rrepresents a hydrogen atom, an alkyl group having 1 to 12 carbon atoms, a cycloalkyl group having 3 to 6 carbon atoms, an alkenyl group having 2 to 6 carbon atoms or a phenyl group] comprising steps of reacting a compound represented by formula (2):[wherein ...

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Номер записи: 68
04-03-2021 дата публикации

COMPOUNDS FOR TREATING EYE DISEASES AND METHODS THEREOF

Номер: US20210061800A1
Автор: KANNAN Srinivasaraghavan, LAM Kong Peng, LIM Hong Hwa, NG Shi Qin Vanessa, UTTAM Surana, VENKATACHALAM Gireedhar, VERMA Chandra
Принадлежит:

A compound of formula (I) or a salt, solvate or prodrug thereof: 2. The compound according to claim 1 , wherein at least one of Ror Ris C-Calkyl.5. The pharmaceutical composition according to claim 4 , further comprising an effective amount of a second therapeutic agent.711-. (canceled)12. The method according to claim 6 , wherein the compound of formula (I) or a pharmaceutically acceptable salt claim 6 , solvate claim 6 , or prodrug thereof is injected directly to the eye.13. The method according to claim 6 , wherein the compound of formula (I) or a pharmaceutically acceptable salt claim 6 , solvate claim 6 , or prodrug thereof is provided on the surface of the eye.14. The method according to claim 6 , wherein the compound of formula (I) or a pharmaceutically acceptable salt claim 6 , solvate claim 6 , or prodrug thereof is orally administerable.15. The compound according to claim 1 , wherein Ris an optionally substituted heteroaryl claim 1 , and wherein the optionally substituted group is selected from hydroxyl claim 1 , acyl claim 1 , alkyl claim 1 , alkoxy claim 1 , alkenyl claim 1 , alkenyloxy claim 1 , alkynyl claim 1 , alkynyloxy claim 1 , amino claim 1 , aminoacyl claim 1 , carboxyl claim 1 , acylamino claim 1 , cyano claim 1 , halogen claim 1 , 3 nitro claim 1 , phosphono claim 1 , sulfo claim 1 , phosphorylamino claim 1 , phosphinyl claim 1 , oxyacyl claim 1 , oxime claim 1 , oxime ether claim 1 , hydrazone claim 1 , oxyacylamino claim 1 , oxysulfonylamino claim 1 , aminoacyloxy claim 1 , trihalomethyl claim 1 , trialkylsilyl claim 1 , pentafluoroethyl claim 1 , trifluoromethoxy claim 1 , difluoromethoxy claim 1 , trifluoromethanethio claim 1 , trifluoroethenyl claim 1 , mono- and di-alkylamino claim 1 , mono- and di-(substituted alkyl)amino claim 1 , mono- and di-arylamino claim 1 , mono- and di-heteroarylamino claim 1 , mono- and di-heterocyclyl amino claim 1 , and unsymmetric di-substituted amines having different substituents.16. The pharmaceutical ...

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Номер записи: 69
20-02-2020 дата публикации

4-DIFLUOROMETHYL BENZOYL AMIDES WITH HERBICIDAL ACTION

Номер: US20200055829A1
Автор: AHRENS HARTMUT, Dietrich Hansjoerg, GATZWEILER ELMAR, MACHETTIRA Anu Bheemaiah, ROSINGER CHRISTOPHER HUGH, Tiebes Joerg, WALDRAFF CHRISTIAN
Принадлежит:

Benzoylamides of the general formula (I) are described as herbicides. 6. A herbicidal composition comprising at least one compound as claimed in mixed with one or more formulation auxiliaries.7. The herbicidal composition as claimed in claim 6 , comprising at least one further pesticidally active substance selected from the group consisting of insecticides claim 6 , acaricides claim 6 , herbicides claim 6 , fungicides claim 6 , safeners claim 6 , and growth regulators.8. A method for controlling one or more unwanted plants claim 1 , comprising applying an effective amount of at least one compound of the formula (I) as claimed in or of herbicidal compositions thereof to the plants or a site of unwanted vegetation.9. A product comprising a compound as claimed in or of herbicidal compositions thereof for controlling one or more unwanted plants.10. The product as claimed in claim 9 , wherein the compound is used for controlling unwanted plants in one or more crops of useful plants.11. The product as claimed in claim 10 , wherein the useful plants are transgenic useful plants.13. The compound as claimed in claim 12 , in whichX represents cyclopropyl, fluorine, chlorine, bromine or iodine,R represents methyl, ethyl, cyclopropylmethyl or methoxyethyl,n represents 0, 1 or 2.15. The compound as claimed in claim 14 , in whichX represents methyl, ethyl, cyclopropyl, fluorine, chlorine, bromine or iodine,R represents methyl, ethyl, cyclopropylmethyl or methoxyethyl,n represents 0, 1 or 2. The invention relates to the technical field of the herbicides, especially that of the herbicides for selective control of weeds and weed grasses in crops of useful plants.WO 2011/035874 A1, WO 2012/126932 A1, WO 2012/028579 A1 and WO 2016/146561 A1 describe herbicidally active benzoylamides which differ from one another essentially by the nature of the heterocyclic substituent. These benzoylamides may be substituted in the 2-, 3- and 4-positions of the phenyl ring by a large number of ...

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Номер записи: 70
28-02-2019 дата публикации

LABELED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA), THEIR USE AS IMAGING AGENTS AND PHARMACEUTICAL AGENTS FOR THE TREATMENT OF PROSTATE CANCER

Номер: US20190060491A1
Автор: BAUDER-WÜST Ulrike, Benesova Martina, EDER Matthias, EISENHUT Michael, Haberkorn Uwe, Kopka Klaus, Mier Walter, Schäfer Martin
Принадлежит:

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib). 114-. (canceled)16. The compound of claim 15 , wherein the compound is lyophilized.17. The compound of claim 15 , further comprising a pharmaceutically acceptable carrier claim 15 , wherein the compound and the pharmaceutically acceptable carrier are lyophilized.18. The compound of claim 17 , wherein the pharmaceutically acceptable carrier is selected from mannitol claim 17 , lactose claim 17 , glucose claim 17 , and albumin.21. The compound of claim 20 , wherein the radionuclide is chosen from Zr claim 20 , Sc claim 20 , In claim 20 , Y claim 20 , Ga claim 20 , Lu claim 20 , Tc claim 20 , Cu claim 20 , Cu claim 20 , Gd claim 20 , Gd claim 20 , Gd claim 20 , Bi claim 20 , or Ac.22. The compound of claim 20 , wherein the radionuclide is chosen from Cu claim 20 , Cu claim 20 , Ga claim 20 , Lu claim 20 , or Ac.23. The compound of claim 20 , wherein the radionuclide is Ga.24. The compound of claim 20 , wherein the radionuclide is Lu.25. The compound of claim 20 , wherein the radionuclide is Ac.26. The compound of claim 20 , wherein the radionuclide is chosen from Cu or Cu.27. The compound of claim 21 , wherein the radionuclide is chosen from Cu claim 21 , Cu claim 21 , Ga claim 21 , Lu claim 21 , or Ac.28. The compound of claim 21 , wherein the radionuclide is Ga.29. The compound of claim 21 , wherein the radionuclide is Lu.30. The compound of claim 21 , wherein the radionuclide is Ac.31. The compound of claim 21 , wherein the radionuclide is chosen from Cu or Cu.33. The composition of claim 32 , wherein the radionuclide is chosen from Zr claim 32 , Sc claim 32 , In claim 32 , Y claim 32 , Ga claim 32 , Lu claim 32 , Tc claim 32 , Cu claim 32 , Cu claim 32 , Gd ...

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Номер записи: 71
12-03-2015 дата публикации

LANTHANOID COMPLEX CAPSULE AND PARTICLE CONTRAST AGENTS, METHODS OF MAKING AND USING THEREOF

Номер: US20150071863A1
Автор: WALTERS Marc Anton
Принадлежит:

The invention relates to compositions of DOTA derivative compounds, lanthanoid-DOTA derivative molecular complex, and lanthanoid-complex encapsulated solid lipid particles or capsules, and methods of making and using the compositions. The solid lipid particles or capsules contain micelle cores stabilized by a hyperbranched polymer shell based from a crosslinked DOTA derivative compound or crosslinked lanthanoid-DOTA derivative complex. These solid lipid particles or capsules can be used in various applications, such as contrast agents or drug delivery vehicles. 114-. (canceled)1618-. (canceled)21. The hyperbranched polymeric nanoparticle or nanocapsule of claim 20 , wherein X is S.22. The hyperbranched polymeric nanoparticle or nanocapsule of claim 20 , wherein X is O claim 20 , and the crosslinking agent is divinyl sulfone (DVS) claim 20 , dicarboxylic acid claim 20 , diepoxybutane claim 20 , diepoxyoctane claim 20 , epichlorohydrin claim 20 , butanediol-diglycidyl ether (BDDE) claim 20 , ethylene glycol diglycidyl ether claim 20 , polyglycerol polyglycidyl ether claim 20 , ethylene sulfide claim 20 , glutaraldehyde claim 20 , bromoacetic anhydride claim 20 , acrylic anhydride claim 20 , 3-mercaptopropanoate claim 20 , thioacetic acid claim 20 , or combinations thereof.23. A hyperbranched polymer shell comprising the crosslinked hyperbranched polymeric nanoparticles or nanocapsules of .24. A mixed micelle comprisingan emulsifying wax as the micelle core; and{'claim-ref': {'@idref': 'CLM-00020', 'claim 20'}, 'at least one cationic surfactant associated to the surface of the micelle core, wherein the anionic portion of the cationic surfactant is the hyperbranched polymeric nanoparticle of .'}25. The mixed micelle of claim 24 , further comprising at least one neutral surfactant claim 24 , wherein the neutral surfactant molecular chains intersperse the individual molecules of cationic surfactant.26. The mixed micelle of claim 25 , wherein the cationic portion of the ...

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Номер записи: 72
15-03-2018 дата публикации

Fumarate Analogs and Uses Thereof

Номер: US20180071271A1
Автор: Bhamidipati Somasekhar, Darwish Ihab, Duncton Matthew, Singh Rajinder, Yu Jiaxin
Принадлежит:

Aspects of the present disclosure include compounds that find use for the treatment of a variety of autoimmune and inflammatory diseases and disorders. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes. 128.-. (canceled)30. The method of claim 29 , wherein the disease or disorder is psoriasis or multiple sclerosis.32. The method of claim 29 , wherein Xis a substituted heterocyclyl or a substituted heteroaryl claim 29 , wherein the substituent on Xis X claim 29 , wherein Xis Calkyl or a progroup.34. The method of claim 33 , wherein Ris aryl claim 33 , substituted aryl claim 33 , heteroaryl claim 33 , or substituted heteroaryl.35. The method of claim 33 , wherein Ris hydrogen claim 33 , alkyl claim 33 , substituted alkyl claim 33 , cycloalkyl claim 33 , substituted cycloalkyl.36. The method of claim 35 , wherein Ris hydrogen claim 35 , methyl claim 35 , ethyl claim 35 , isopropyl claim 35 , cyclopentyl claim 35 , 4-tetrahydropyranyl claim 35 , —CHCHOCH claim 35 , —CHOCH claim 35 , —CHC(O)OCH claim 35 , or —CHCH(CH)OH.37. The method of claim 32 , wherein Xis Calkyl.38. The method of claim 36 , wherein Xis methyl or tert-butyl.42. The method of claim 41 , wherein Rand Rare each independently selected from hydrogen and Calkyl.43. The method of claim 42 , wherein Rand Rare each hydrogen.44. The method of claim 42 , wherein Ris hydrogen and Ris Calkyl.45. The method of claim 41 , wherein R claim 41 , R claim 41 , Rand Rare each independently selected from hydrogen and Calkyl.46. The method of claim 45 , wherein R claim 45 , R claim 45 , Rand Rare each hydrogen.47. The method of claim 45 , wherein one of R claim 45 , R claim 45 , Rand Ris methyl and the remaining are hydrogen.48. The method of claim 45 , wherein two of R claim 45 , R claim 45 , ...

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Номер записи: 73
15-03-2018 дата публикации

TRANS-CYCLOHEPTENES AND HETERO-TRANS-CYCLOHEPTENES FOR BIOORTHOGONAL COUPLING

Номер: US20180072761A1
Автор: FANG Yinzhi, Fox Joseph, Zhang Han
Принадлежит: University of Delaware

A substituted trans-cycloheptene according to formula (I); wherein: a) Z and L are each selected from the group consisting of SiR, CH, CHOH, and CHR; Ris phenyl or CH; Ris phenyl, CH, (CH)CN, or (CH)OH, wherein n is an integer from 1 to 5; Rand Rare each individually selected from the group consisting of H, OH, and CH; and Z and L are not both SiRR; or b) Z is BocN, L is CH, Ris H, and Ris H; or c) Z is C=0, L is CH, Ris H, and Ris H. 2. The substituted trans-cycloheptene according to claim 1 , wherein Z claim 1 , L claim 1 , R claim 1 , and Rare according to any one of combinations a) through l):{'sub': '2', 'sup': a', 'b, 'a) Z is CHOH, L is CH, Ris H, and Ris H;'}{'sub': 2', '2, 'sup': a', 'b, 'b) Z is CHCHOH, L is CH, Ris H, and Ris H;'}{'sub': 2', '2, 'sup': a', 'b, 'c) Z is CH, L is CH, and Ris OH, and Ris H;'}{'sub': '2', 'sup': a', 'b, 'd) Z is CH, L, is CHOH, Ris OH, and Ris H;'}{'sub': '2', 'sup': a', 'b, 'e) Z is BocN, L, is CH, Ris H, and Ris H;'}{'sub': '2', 'sup': a', 'b, 'f) Z is C═O, L is CH, Ris H, and Ris H;'}{'sup': 1', '2', 'a', 'b', '1', '2, 'sub': 2', '3', '2', '3', '2', '4, 'g) Z is SiRR, L is CH, Ris H, Ris H, Ris CH, and Ris either (CH)CN or (CH)OH;'}{'sub': 3', '2', '3', '2', '3', '3, 'sup': a', 'b, 'h) Z is SiCH(CH)OH, L is CH, Ris CH, and Ris CH;'}{'sub': 2', '2, 'sup': a', 'b, 'i) Z is SiPh, L is CH, Ris H, and Ris H;'}{'sub': 3', '2', '2, 'sup': a', 'b, 'j) Z is Si(CH), L is CH, Ris OH, and Ris H;'}{'sub': 2', '2, 'sup': a', 'b, 'k) is CH, L is SiPh, Ris H, and Ris H;'}{'sub': 2', '3', '2', '4, 'sup': a', 'b, 'l) Z is CH, L is SiCH(CH)OH, Ris H, and Ris H.'}3. An adduct of the substituted trans-cycloheptene according to with a molecule selected from the group consisting of tetrazines claim 1 , ketenes claim 1 , conjugated dienes claim 1 , and 1 claim 1 ,3-dipoles.4. The adduct according to claim 3 , wherein the molecule is a tetrazine.5. The adduct according to claim 3 , wherein the molecule is a ketene.6. The adduct according to claim ...

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Номер записи: 74
16-03-2017 дата публикации

HETEROCYCLIC COMPOUNDS AS PESTICIDES

Номер: US20170073318A1
Автор: DEMBSKI Hardwin, Goergens Ulrich, Greul Joerg, Heilmann Eike Kevin, ILG Kerstin, Portz Daniela, Trautwein Axel, WROBLOWSKY Heinz-Juergen
Принадлежит: Bayer CropScience Aktiengesellschaft

The present application relates to novel heterocyclic compounds, to the use thereof for controlling animal pests including arthropods, insects and nematodes, and to processes and intermediates for preparation of the novel compounds. 6. Composition claim 1 , comprising a content of at least one compound of formula (I) according to .7. Method for controlling pests claim 1 , comprising allowing a compound of formula (I) according to or a composition thereof to act o none or more pests and/or their habitat.9. Compound of formula (IIa-1-a) according to claim 8 , in which R3 is hydrogen.11. Compound of formula (1-9) according to claim 10 , in which R3 is hydrogen. The present application relates to novel heterocyclic compounds, to the use thereof for controlling animal pests including arthropods, insects and nematodes, and to processes and intermediates for preparation of the novel compounds.Derivatives of 1-aryl-3-aroylamino-1,2,4-triazoles are known from WO 2012/006473.The compounds described therein have activity as phosphatase inhibitors.Moreover, the following compounds are known in Scifinder as “Commercial Source” (CAS No. of the 2-Cl compound=321434-03-1, that of the 4-Cl compound=303144-57-2), without description of any use:Crop protection agents, which also include pesticides, have to meet many demands, for example in relation to efficacy, persistence, and spectrum of action and possible use. Questions of toxicity and of combinability with other active ingredients or formulation auxiliaries play a role, as does the question of the expense that the synthesis of an active ingredient entails. In addition, resistances can occur. For all these reasons, the search for novel crop protection compositions cannot be considered to be complete, and there is a constant need for novel compounds having properties which, compared to the known compounds, are improved at least in relation to individual aspects.It was an object of the present invention to provide compounds which ...

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Номер записи: 75
19-03-2015 дата публикации

N-alkoxyamide conjugates as imaging agents

Номер: US20150078997A1
Автор: David S. Casebier, Edward H. Cheesman, Padmaja Yalamanchili, Richard J. Looby, Richard R. Cesati, Simon P. Robinson, Thomas D. Harris
Принадлежит: Lantheus Medical Imaging Inc

The present disclosure is directed to compounds, diagnostic agents, and related methods. In some cases, methods for treating patients are provided. More specifically, the disclosure provides compounds, diagnostic agents, and kits for detecting and/or imaging and/or monitoring elastin rich tissues. In addition, the disclosure provides methods of detecting and/or imaging and/or monitoring the presence of coronary plaque, carotid plaque, iliac/femoral plaque, aortic plaque, renal artery plaque, plaque of any arterial vessel, aneurism, vasculitis, other diseases of the arterial wall, and/or damage or structural changes in ligaments, uterus, lungs or skin, as indicated by changes in total vessel wall area, internal lumen size, and exterior arterial perimeter.

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Номер записи: 76
19-03-2015 дата публикации

RADIOLABELED PROSTATE SPECIFIC MEMBRANE ANTIGEN INHIBITORS

Номер: US20150078998A1
Автор: Babich John W., JOYAL John L., Lu Genliang, Zimmerman Craig
Принадлежит: Molecular Insight Pharmaceuticals

Compounds according to Formula I and Formula II are potent inhibitors of PSMA activity: 2. The compound of claim 1 , wherein X is (CHR) claim 1 , Y is C(O) claim 1 , W is hydrogen and k is 5.3. The compound of claim 1 , wherein L is —C(O)CH— and T is hydrogen.4. The compound of claim 1 , wherein Ris hydrogen and m is 2.5. The compound of claim 1 , wherein L is —C(O)—[(CH)—V]—(CH)—C(O)—U or —C(O)—(C-C)alkylene.6. The compound of claim 5 , wherein L is —C(O)methylene.7. The compound of claim 5 , wherein L is —C(O)—[(CH)—V]—(CH)—C(O)—U and T is hydrogen.8. The compound of claim 7 , wherein V is NR claim 7 , n is 2 and q is 1.9. The compound of claim 7 , wherein U is NRR.10. The compound of claim 9 , wherein Ris hydrogen and Ris —(CH)—NH—C(O)—(CH)—.11. The compound of claim 1 , wherein L is OR-benzylene and T is —(C-C)heteroaryl-(C-C)alkylene.12. The compound of claim 11 , wherein the heteroaryl is an imidazole claim 11 , further substituted with the group —(C-C)alkylene-C(O)—U.16. The compound of claim 4 , wherein W is —(CH)—COOH claim 4 , k is 1 claim 4 , L is —[C(O)—(CH(Z))—NH]—NRRand T is hydrogen.17. The compound of claim 16 , wherein Ris hydrogen claim 16 , Ris —C(O)CH— and j is 4.18. The compound of claim 4 , wherein W and T are hydrogen claim 4 , k is 5 claim 4 , and L is [C(O)—CH(Z)—NH]—C(O)—(CHR)—(CH)—U.19. The compound of claim 18 , wherein Z is —(CH)—NRRand U is —NRR.20. The compound of claim 18 , wherein m and t are 1 claim 18 , p is 4 and Ris —NH.21. The compound of claim 19 , wherein Ris hydrogen and Ris C(O)methylene.22. The compound of claim 19 , wherein Rand Rare each independently —(CH)—(C-C)heteroaryl.23. The compound of claim 18 , wherein p is 1 and the heteroaryl is an imidazole claim 18 , further substituted with the group —(C-C)alkylene-C(O)—U.25. A metal complex comprising a radionuclide and the compound of .26. The metal complex of claim 25 , wherein the radionuclide is selected from the group consisting of In claim 25 , Y claim 25 , Ga claim ...

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Номер записи: 77
19-03-2015 дата публикации

Method to Produce and Scale-Up Cocrystals and Salts Via Resonant Acoustic Mixing

Номер: US20150080567A1
Автор: am ENDE David J., ANDERSON Stephen R., SALAN Jerry
Принадлежит: Nalas Engineering Services Inc.

A method to produce and manufacture cocrystals and salts is disclosed wherein crystalline solids and other components were combined in the desired proportions into a mixing chamber and mixed at high intensity to afford a cocrystalline product. No grinding media were required. The mixing system consists of a resonant acoustic vibratory system capable of supplying a large amount of energy to the mixture and is tunable to a desired resonance frequency and amplitude. The use of resonant acoustic mixing to assist cocrystallization is novel. This discovery enables the manufacture of cocrystals and salt forms, simplifying their manufacture and scale-up, and avoiding the use of grinding methods or grinding media. The present invention affords the manufacture of cocrystals and salts on kilogram to multi-ton scale and is adaptable to continuous manufacturing through the use of resonant mixing methods. 1. A process for making a cocrystal from two or more compounds by combining compounds in a suitable vessel and subjecting the vessel and mixture to resonant acoustic mixing.2. The process according to wherein at least one of the compounds is a coformer.3. The process according to wherein a resonant frequency of mixing is from about 10 Hz to about 2000 Hz and acceleration energies for mixing in the range of 2 and 200 g-forces.4. The process according to wherein a solvent or mixture of solvents is added.5. The process according to claim 2 , wherein a solvent is added in which one or more coformers is slightly soluble to mediate the solid-solid interactions between the coformers.6. The process according to wherein a solvent or mixture of solvents is added or the presence of water vapor leads to the formation of a cocrystal hydrate or cocrystal solvate.7. A process for making a crystalline salt form by combining two compounds in a suitable vessel and subjecting the vessel and mixture to resonant acoustic mixing.8. The process according to wherein a resonant frequency of mixing is ...

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Номер записи: 78
18-03-2021 дата публикации

Nrf2 Activating Compounds and Uses Thereof

Номер: US20210078969A1
Автор: Duncton Matthew, Singh Rajinder
Принадлежит:

Aspects of the present disclosure include compounds that activate Nrf2. Such compounds find use in the treatment of autoimmune and inflammatory diseases and disorders, such as for example psoriasis and multiple sclerosis. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes. 120.-. (canceled)22. The method of claim 21 , wherein the disease or disorder is cardiac insufficiency.23. The method of claim 22 , wherein the cardiac insufficiency is selected from the group consisting of left ventricular insufficiency claim 22 , myocardial infarction claim 22 , and angina pectoris.24. The method of claim 21 , wherein the disease or disorder is asthma.25. The method of claim 21 , wherein the disease or disorder is arthritis.26. The method of claim 25 , wherein the arthritis is selected from the group consisting of inflammatory arthritis claim 25 , rheumatoid arthritis claim 25 , juvenile rheumatoid arthritis (juvenile idiopathic arthritis) claim 25 , psoriatic arthritis claim 25 , and ankylosing spondylitis.27. The method of claim 21 , wherein the disease or disorder is an inflammatory bowel disease.28. The method of claim 27 , wherein the inflammatory bowel disease is selected from the group consisting of Crohn's disease and ulcerative colitis.29. The method of claim 27 , wherein the inflammatory bowel disease is Crohn's disease.30. The method of claim 21 , wherein the disease or disorder is a chronic obstructive pulmonary disease.31. The method of claim 30 , wherein the chronic obstructive pulmonary disease is selected from the group consisting of bronchitis and emphysema.33. The method of claim 21 , wherein the sulfonyl is selected from alkyl-SO— claim 21 , substituted alkyl-SO— claim 21 , alkenyl-SO— claim 21 , substituted alkenyl-SO— claim 21 , ...

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Номер записи: 79
14-03-2019 дата публикации

PROCESS FOR THE PREPARATION OF TRISODIUM (4-{[1S,3R)-1-([1,1'-BIPHENYL]-4-YLMETHYL)-4-ETHOXY-3-METHYL-4-OXOBUTYL]AMINO}-4-OXOBUTANOATE)-(N-PETANOYL-N-{[2'-(1H-TETRAZOL-1-1D-5-YL)[1,1'-BIPHENYL]-4-YL]METHYL}- L-VALINATE) AND ITS POLYMORPHS THEREOF

Номер: US20190077775A1
Автор: AMBATI Srinivasa Rao, Boge Rajesham, NANDIGAMA Chkradhar, SAGYAM Rajeshwar Reddy, SAJJA Eswaraiah, SRINIVASAN Thirumalai Rajan
Принадлежит:

The present invention relates to a process for the preparation of Trisodium (4-{[(1S.3R)-1-([1,1′-biphenyl]-4-yl-methyl)-4-ethoxy-3-methyl-4-oxobutyl]amino}-4-oxo butanoate)-(N-pentanoyl-N-{[2′-(1H-tetrazol-1-id-5-yl)[1,1′-biphenyl]-4-yl]methyl}-L-valinate) represented by the following structural formula-1: 1. A process for the preparation of Trisodium (4-{[(1S ,3R)-1-([1 ,1′-biphenyl]-4-ylmethyl)-4-ethoxy-3-methyl-4-oxobutyl]amino}-4-oxobutanoate)-(N-pentanoyl-N-{[2′-(1H-tetrazol-1-id-5-yl)[1 ,1′-biphenyl]-4-yl]methyl}-L-valinate) compound of formula-1 , comprising of:a) reacting the mono sodium salt of 4-(((2S,4R)-1-([1,1′-biphenyl]-4-yl)-5-ethoxy-4-methyl-5-oxopentan-2-yl)amino)-4-oxobutanoic acid compound of formula-6 with disodium salt of (S)-2-(N-((2′-(1H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid compound of formula-7 in a suitable solvent,b) obtaining the Trisodium salt of valsartan sacubitril complex by the removal of the solvent from the solution.21. The process as claimed in claim- , wherein ,In step-(b) the suitable solvent is selected from alcohol solvents, ketone solvents, ester solvents, hydrocarbon solvents, nitrile solvents, ether solvents, chloro solvents, polar aprotic solvents, polar solvents like water or mixture thereof.3. A process for the preparation of amorphous Trisodium (4-{[(1S ,3R)-1-([1 ,1′-biphenyl]-4-ylmethyl)-4-ethoxy-3-methyl-4-oxobutyl]amino}-4-oxobutanoate)-(N-pentanoyl-N-{[2′-(1H-tetrazol-1-id-5-yl)[1 ,1′-biphenyl]-4-yl]methyl}-L-valinate) compound of formula-1 , comprising of:a) Dissolving the mono sodium salt of 4-(((2S,4R)-1-([1,1′-biphenyl]-4-yl)-5-ethoxy-4-methyl-5-oxopentan-2-yl)amino)-4-oxobutanoic acid compound of formula-6 and disodium salt of (S)-2-(N-((2′-(1H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl) pentanamido)-3-methylbutanoic acid compound of formula-7 in aqueous methanol,b) distilling off the solvent completely from the reaction mixture obtained in step a) to provide amorphous ...

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Номер записи: 80
14-03-2019 дата публикации

REAGENTS AND METHODS FOR BIOORTHOGONAL LABELING OF BIOMOLECULES IN LIVING CELLS

Номер: US20190077776A1
Автор: Blizzard Robert, MEHL RYAN A.
Принадлежит: Oregon State University

Tetrazine non-canonical amino acids, methods for genetic encoding proteins and polypeptides using the tetrazine amino acids, proteins and polypeptides comprising the tetrazine amino acids, and compositions comprising the proteins and polypeptides having at least one post-translational modification thereof comprising in vivo reaction with the incorporated tetrazine amino acid and a second molecule. 6. The compound of claim 1 , wherein Ris selected from methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , i-propyl claim 1 , n-butyl claim 1 , s-butyl claim 1 , t-butyl claim 1 , n-pentyl claim 1 , and n-hexyl.7. The compound of claim 1 , wherein Ris selected from trifluoromethyl claim 1 , 2-fluoroethyl claim 1 , and methoxy.8. The compound of claim 1 , wherein phenylene is 1 claim 1 ,4-phenylene.9. The compound of claim 1 , wherein phenylene is 1 claim 1 ,3-phenylene.1012-. (canceled)1416-. (canceled)17. The compound of selected from the group consisting of 4-(6-methyl-s-tetrazin-3-yl)phenylalanine (Tet-v2.0-methyl) claim 1 , 4-(6-ethyl-s-tetrazin-3-yl)phenylalanine (Tet-v2.0-ethyl) claim 1 , 4-(6-isopropyl-s-tetrazin-3-yl)phenylalanine (Tet-v2.0-isopropyl) claim 1 , and 4-(6-butyl-s-tetrazin-3-yl)phenylalanine (Tet-v2.0-n-butyl).18. The compound of selected from the group consisting of 3-(6-methyl-s-tetrazin-3-yl)phenylalanine (Tet-v3.0-methyl) claim 5 , 3-(6-ethyl-s-tetrazin-3-yl)phenylalanine (Tet-v3.0-ethyl) claim 5 , 3-(6-isopropyl-s-tetrazin-3-yl)phenylalanine (Tet-v3.0-isopropyl) claim 5 , 3-(6-t-butyl-s-tetrazin-3-yl)phenylalanine (Tet-v3.0-t-butyl) claim 5 , and 3-(6-n-butyl-s-tetrazin-3-yl)phenylalanine (Tet-v3.0-n-butyl).19. A method for making a protein or a polypeptide of interest claim 5 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'incorporating a compound of into a protein or polypeptide.'}20. A method for genetically encoding a protein or a polypeptide of interest claim 5 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, ' ...

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Номер записи: 81
24-03-2016 дата публикации

OXYGEN SCAVENGERS, COMPOSITIONS COMPRISING THE SCAVENGERS, AND ARTICLES MADE FROM THE COMPOSITIONS

Номер: US20160083558A1
Автор: Dauzvardis Matthew J., Li Shenshen
Принадлежит: PLASTIPAK PACKAGING, INC.

The disclosure relates to oxygen scavenging molecules, compositions, methods of making the compositions, articles prepared from the compositions, and methods of making the articles. 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. 3. The composition of claim 1 , wherein the at least one transition metal is present in the composition in an amount of 10 to 400 ppm.4. The composition of claim 1 , wherein the at least one transition metal is cobalt or zinc claim 1 , or a combination thereof.5. The composition of claim 1 , wherein the base polymer comprises a polyester polymer.11. The compound of claim [00102] claim 1 , wherein the compound is a cyclic polymeric compound.17. An article of manufacture comprising a composition according to .18. The article of claim 17 , wherein the article is a preform claim 17 , sheet claim 17 , bottle claim 17 , cup claim 17 , or jar.19. A wall for a package comprising a composition claim 17 , said wall comprising:(a) one or more outer layers; and(b) one or more inner layers;{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein at least one of said inner or at least one of said outer layers comprises a composition according to .'}20. The wall of claim 19 , wherein the first layer is disposed radially outward from said second layer.21. A method for packaging an oxygen sensitive material comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(a) preparing a package having a wall comprising at least one layer, at least one of said layers comprising a composition according to ;'}(b) introducing said oxygen sensitive material into said package; and(c) closing said package.22. A method for producing a packaging material having a wall with oxygen barrier properties comprising:{'claim-ref': {'@idref': 'CLM-00013', 'claim 13'}, 'claim-text': 'wherein said compound is present in an amount of about 0.10 to 10 weight present of said ...

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Номер записи: 82
23-03-2017 дата публикации

METAL/RADIOMETAL-LABELED PSMA INHIBITORS FOR PSMA-TARGETED IMAGING AND RADIOTHERAPY

Номер: US20170081298A1
Автор: Chen Ying, Meade Thomas J., Mease Ronnie C., Pomper Martin G., Ray Sangeeta, ROTZ MATTHEW, Yang Xing
Принадлежит:

Low-molecular weight gadolinium (Gd)-based MR contrast agents for PSMA-specific Ti-weighted MR imaging are disclosed. The (Gd)-based MR contrast agents exhibit high binding affinity for PSMA and exhibit specific Ti contrast enhancement at PSMA+ cells. The PSMA-targeted Gd-based MR contrast agents can be used for PSMA-targeted imaging in vivo. 86Y-labeled PSMA-binding ureas also are provided, wherein the PSMA-binding ureas also are suitable for use with other radiotherapeutics. 4. The compound of wherein the metal is selected from the group consisting of Gd claim 1 , Lu claim 1 , Ac claim 1 , Bi claim 1 , Pb claim 1 , Cu claim 1 , In claim 1 , Sc claim 1 , and Y.5. The compound of claim 1 , wherein the nonradioactive metal is Gd-157 (stable isotope).6. The compound of claim 1 , wherein the radiometal is selected from the group consisting of Lu-177 claim 1 , Ac-225 claim 1 , Bi-213 claim 1 , Bi-212 claim 1 , Pb-212 claim 1 , Cu-67 claim 1 , In-111 claim 1 , Sc-47 claim 1 , and Y-90.7. The compound of claim 1 , wherein the radiometal is selected from the group consisting of Y-86 and Sc-44.8. The compound of claim 1 , wherein the radiometal is selected from the group consisting of Lu-177 and In-111.12. The method of claim 9 , wherein the metal is selected from the group consisting of Gd claim 9 , Lu claim 9 , Ac claim 9 , Bi claim 9 , Pb claim 9 , Cu claim 9 , In claim 9 , Sc and Y.13. The method of claim 9 , wherein imaging comprises magnetic resonance imaging (MRI) and the nonradioactive metal is Gd-157 (stable isotope).14. The method of claim 9 , wherein the method comprises treating one or more prostate-specific membrane antigen (PSMA) tumors or cells and the radiometal is selected from the group consisting of Lu-177 claim 9 , Ac-225 claim 9 , Bi-212 claim 9 , Bi-213 claim 9 , Pb-212 claim 9 , Cu-67 claim 9 , In-111 claim 9 , Sc-47 claim 9 , and Y-90.15. The method of claim 9 , wherein the imaging comprises positron emission tomography (PET) imaging and the ...

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Номер записи: 83
26-03-2015 дата публикации

Substituted N-(tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamide compounds and their use as herbicides

Номер: US20150087519A1
Автор: EVANS Richard Roger, Hutzler Johannes, Kraus Helmut, Kreuz Klaus, Lerchl Jens, NEWTON Trevor William, PARRA RAPADO Liliana, Pasternak Maciej, SEITZ Thomas, WITSCHEL Matthias
Принадлежит:

N-(tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides of formula I and their use as herbicides, 125-. (canceled)27: The compound as claimed in claim 26 , where R is selected from the group consisting of C-C-alkyl claim 26 , C-C-alkoxy-C-C-alkyl claim 26 , C-C-cycloalkyl claim 26 , C-C-haloalkyl claim 26 , R—C(═O)—C-C-alkyl claim 26 , RO—C(═O)—C-C-alkyl claim 26 , RRN—C(═O)—C-C-alkyl and R—C(═O)NH—C-C-alkyl claim 26 , where{'sup': 'c', 'sub': 1', '4', '1', '4, 'Ris C-C-alkyl or C-C-haloalkyl,'}{'sup': 'd', 'sub': 1', '4, 'Ris C-C-alkyl,'}{'sup': 'e', 'sub': 1', '4, 'Ris hydrogen or C-C-alkyl,'}{'sup': 'f', 'sub': 1', '4, 'Ris hydrogen or C-C-alkyl, or'}{'sup': e', 'f, 'R, Rtogether with the nitrogen atom, to which they are bound may form a 5-, 6 or 7-membered, saturated N-bound heterocyclic radical, which may carry as a ring member a further heteroatom selected from O, S and N and which is unsubstituted or may carry 1, 2, 3 or 4 methyl groups,'}{'sup': 'k', 'sub': 1', '4, 'Ris C-C-alkyl.'}28: The compound as claimed in claim 26 , where R is phenyl or heterocyclyl claim 26 , where heterocyclyl is a 5- or 6-membered monocyclic or 8- claim 26 , 9- or 10-membered bicyclic saturated claim 26 , partially unsaturated or aromatic heterocycle claim 26 , which contains 1 claim 26 , 2 claim 26 , 3 or 4 heteroatoms as ring members claim 26 , which are selected from the group consisting of O claim 26 , N and S claim 26 , where phenyl and heterocyclyl are unsubstituted or substituted by 1 claim 26 , 2 claim 26 , 3 or 4 groups R′ claim 26 , where R′ is selected from the group consisting of halogen claim 26 , methyl claim 26 , ethyl claim 26 , methoxy and trifluoromethyl.29: The compound as claimed in claim 26 , where R is R—S(O)—C-C-alkyl claim 26 , where Ris C-C-alkyl claim 26 , C-C-haloalkyl claim 26 , C-C-alkenyl claim 26 , C-C-haloalkenyl claim 26 , C-C-alkynyl claim 26 , C-C-cycloalkyl claim 26 , phenyl or heterocyclyl claim 26 , where heterocyclyl is a 6-membered aromatic ...

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Номер записи: 84
12-06-2014 дата публикации

COMPOUNDS, COMPOSITION, METHODS, TARGETS FOR CANCER THERAPY

Номер: US20140163088A1
Автор: Yu Ming
Принадлежит:

This invention describes methods and pharmaceutical compositions for combinational cancer treatments that are capable of inducing JNK phosphorylation and induce programmed cell death. It also identified genes as target for anti-cancer drug development and enhancement of the chemotherapeutic drug effect for the treatment of cancer. This invention points to a novel method and principle for a new avenue of developing more efficient and low or non cytotoxic cancer treatment. 2. The pharmaceutical compound of claim 1 , wherein the at least one functional group capable of uncoupling cell surface oxidative phosphorylation comprises DNP.4. The pharmaceutical compound of claim 1 , wherein the at least one functional group capable of keeping the compound impermeable to cell plasma membrane comprises WST-3 (2-(4-Iodophenyl)-3-(2 claim 1 ,4-dinitrophenyl)-5-(2 claim 1 ,4-disufophenyl)-2H-tetrazolium).5. A pharmaceutical composition for treating cancer comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a first agent comprising a compound of ; and'}a second agent that blocks at least one of HIF, cell hypoxia responses, NF-κB, C1(2 and IKK activities.6. The pharmaceutical composition of claim 5 , wherein the second agent comprises a flavonoid.7. The pharmaceutical composition of claim 5 , wherein the second agent comprises apigenin.8. The pharmaceutical composition of claim 5 , wherein the second gent comprises an IKK inhibitor claim 5 , a CK2 inhibitor claim 5 , a HIF inhibitor claim 5 , or a tNOX inhibitor.9. The pharmaceutical composition of claim 13 , wherein the IKK inhibitor is selected from the group consisting of BMS-345541 claim 13 , SC-514 claim 13 , IKK-2 Inhibitor IV[5-(p-Fluoropheny0-2-uerido]thiophene-3-carboxamide claim 13 , IKK Inhibitor VII claim 13 , IKK Inhibitor II claim 13 , Wedelolactone claim 13 , IKK-2 Inhibitor V N-(3 claim 13 ,5-Bis-trifluoromethylphenyl)-5-chloro-2-hydrozybenzamide IMD-0354 claim 13 , and IKK-2 Inhibitor VI (5-Phenyl-2-ureido) ...

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Номер записи: 85
21-03-2019 дата публикации

Use of Tetrazolinones for Combating Resistant Phytopathogenic Fungi on Fruits

Номер: US20190082694A1
Автор: Gewehr Markus, Montag Jurith
Принадлежит:

The present invention relates to the use of use of a tetrazolinone fungicide for combating phytopathogenic fungi on fruits, such fungi containing a G143A mutation in the mitochondrial cytochrome b gene conferring resistance to Qo inhibitors. 110-. (canceled)11. A method for combating phytopathogenic fungi on fruits , wherein the fungi , their habitat , breeding grounds , their locus or the plants to be protected against fungal attack , the soil or plant propagation material are treated with an effective amount of a compound of 1-[2-[[1-(4-chlorophenyl)pyrazol-3-yl]oxymethyl]-3-methyl-phenyl]-4-methyl-tetrazol-5-one (compound I) , such fungi containing a G143A mutation in the mitochondrial cytochrome b gene conferring resistance to Qo inhibitors.12. The method of claim 11 , wherein the fruit plant is apple.13. The method of claim 11 , wherein the fruit plant is grape.14Uncinula necator.. The method of claim 13 , wherein the phytopathogenic fungi is15Plasmopara viticola.. The method of claim 13 , wherein the phytopathogenic fungi is16Venturia inaequalis.. The method of claim 12 , wherein the phytopathogenic fungi is17. The method of claim 12 , wherein compound I as defined in is applied in form of a mixture with second compound II claim 12 , which is selected from the group consisting of2-[4-(4-chlorophenoxy)-2-(trifluoromethyl)phenyl]-1-(1,2,4-triazol-1-yl)propan-2-ol, 2-[4-(4-chlorophenoxy)-2-(trifluoromethyl)phenyl]-3-methyl-1-(1,2,4-triazol-1-yl)butan-2-ol, 1-[4-(4-chlorophenoxy)-2-(trifluoromethyl)phenyl]-1-cyclopropyl-2-(1,2,4-triazol-1-yl)ethanol, difenoconazole, penconazole, tetraconazole, myclobutanil, fluxapyroxad, boscalid, fluopyram, folpet, mancozeb, metiram, dithianon, folpet, sulfur, copper, metrafenone, ametoctradin, dimethomorph, oxathiapiproline, cyazofamid, cyprodinil, pyrimethanil, iprodione, fludioxonil and fluopicolide.18. The method of claim 17 , wherein compound II is selected from the group consisting of2-[4-(4-chlorophenoxy)-2-( ...

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Номер записи: 86
29-03-2018 дата публикации

Labeled inhibitors of prostate specific membrane antigen (psma) biological evaluation, and use of imaging agents

Номер: US20180085478A1
Автор: Catherine Anne Foss, Martin G. Pomper, Ronnie C. Mease, Sangeeta Ray
Принадлежит: JOHNS HOPKINS UNIVERSITY

The prostate-specific membrane antigen (PSMA) is increasingly recognized as a viable target for imaging and therapy of cancer. Various 99mTc/Re-labeled compounds were prepared by attaching known Tc/Re chelating agents to an amino-functionalized PSMA inhibitor with or without a variable length linker moiety. Ex vivo biodistribution and in vivo imaging demonstrated the degree of specific binding to engineered PSMA+ PC3 PIP tumors.

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Номер записи: 87
21-03-2019 дата публикации

Gadolinium chelate compounds for use in magnetic resonance imaging

Номер: US20190083659A1
Автор: Christoph-Stephan Hilger, Detlev Suelzle, Gregor Jost, Hubertus Pietsch, Jessica LOHRKE, Johannes Platzek, Markus Berger, Olaf Panknin, Thomas Frenzel
Принадлежит: Bayer Pharma AG

A compound having the formula of tetragadolinium [4,10-bis(carboxylatomethyl)-7-{-3,6,12,15-tetraoxo-16-[4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]-9,9-bis({[{2-[4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]propanoyl} amino)acetyl]amino}methyl)-4,7,11,14-tetraazaheptadecan-2-yl}-1,4,7,10-tetraazacyclo dodecan-1-yl]acetate wherein the stereochemistry at the chiral carbon of the four alanine substituents is selected from the group consisting of RRRR, SSSS, RSSS, RRSS, and RRRS stereoisomers, and racemic and diastereomeric mixtures of any thereof, or a tautomer, a hydrate, a solvate, or a salt thereof, or a mixture of same is described. The compounds may be used as an MRI contrast imaging agent.

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Номер записи: 88
29-03-2018 дата публикации

CRYSTALLINE FORM OF AHU377, PREPARATION METHOD AND USE THEREOF

Номер: US20180086695A1
Автор: Chen Minhua, YANG Chaohui, YU Shu, Zhang Liang, Zhang Xiaoyu, ZHANG Yanfeng
Принадлежит: CRYSTAL PHARMATECH CO., LTD

The present disclosure relates to a novel crystalline form of a compound of formula (I), preparation method and use thereof. The novel crystalline form in the present disclosure has good stability, low hygroscopicity, and remarkable purification effect in process. The novel crystalline form of the compound of formula (I) provided by the present disclosure can be used for the preparation of the drug for treating heart failure. 2. The compound of Formula (I) according to claim 1 , wherein the compound of Formula (I) is in a crystalline form.3. The compound of Formula (I) according to claim 1 , wherein the compound of Formula (I) is in an anhydrate claim 1 , a hydrate or a solvate.4. The compound of Formula (I) according to claim 1 , wherein the crystalline form is Form I claim 1 , the X-ray powder diffraction pattern shows characteristic peaks at 2theta values of 17.2±0.2° claim 1 , 16.4±0.2° and 9.8±0.2°.5. The compound of Formula (I) according to claim 4 , wherein the X-ray powder diffraction pattern of Form I also shows characteristic peaks at 2theta values of 12.3°±0.2° claim 4 , 8.2°±0.2° and 4.1°±0.2°.6. The compound of Formula (I) according to claim 4 , wherein the X-ray powder diffraction pattern of Form I also shows characteristic peaks at 2theta values of 13.0°±0.2° claim 4 , 18.4°±0.2° claim 4 , 13.8°±0.2° and 6.1±0.2°.7. The compound of Formula (I) according to claim 1 , wherein the crystalline form is Form I claim 1 , the X-ray powder diffraction pattern shows characteristic peaks at 2theta values of 17.2±0.2° claim 1 , 16.4±0.2° claim 1 , 9.8±0.2° claim 1 , 12.3°±0.2° claim 1 , 8.2°±0.2° claim 1 , 4.1°±0.2° claim 1 , 13.0°±0.2° claim 1 , 18.4°±0.2° claim 1 , 13.8°±0.2° and 6.1±0.2°.8. A process for preparing solid form of the compound of Formula (I) according to claim 1 , wherein the process comprises: the solid form of the compound of Formula (I) is precipitated by crystallization of the sticky oil Formula (I) in a mixture of one or more organic ...

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Номер записи: 89
21-03-2019 дата публикации

POLISHING COMPOSITION, METHOD FOR PRODUCING SAME, POLISHING METHOD, AND METHOD FOR PRODUCING SUBSTRATE

Номер: US20190085208A1
Автор: NISHIMURA Aya, SHINODA Toshio
Принадлежит: FUJIMI INCORPORATED

To provide a polishing composition capable of polishing objects to be polished, such as simple substance silicon, silicon compounds, and metals, at a high polishing removal rate. 1. A polishing composition comprising:a polishing removal accelerator containing a compound having a ring structure configured to contain four or more nitrogen atoms;abrasives; anda liquid medium.2. The polishing composition according to claim 1 , whereina number of ring members of the ring structure is 5 or more and 14 or less.3. The polishing composition according to claim 1 , whereinthe compound having the ring structure contains at least one group selected from the group consisting of an amino group, an amide group, a phenyl group, a carboxy group, a phosphate group, a sulfo group, and a thiol group.4. The polishing composition according to claim 1 , whereinthe compound having the ring structure is at least one type selected from the group consisting of tetrazole and a derivative of the tetrazole.5. The polishing composition according to claim 4 , whereinthe tetrazole and the derivative of the tetrazole include at least one type selected from the group consisting of 1H-tetrazole, 5-amino-1H-tetrazole, 5-phenyl-1H-tetrazole, and 5,5-bistetrazole diammonium.6. The polishing composition according to claim 1 , whereina concentration of the compound having the ring structure is 1 mmol/L or more and 100 mmol/L or less.7. The polishing composition according to claim 1 , whereinthe polishing composition is used for polishing of a substrate having a positively charged region when contacting the polishing composition in a state where pH is 6 or less.8. A method for producing the polishing composition according to claim 1 , the method comprising:mixing the polishing removal accelerator, the abrasives, and the liquid medium.9. A polishing method comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'polishing an object to he polished using the polishing composition according to .'}10. A ...

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Номер записи: 90
30-03-2017 дата публикации

Compositions, Methods of Use, And Methods of Treatment

Номер: US20170088524A1
Автор: Chen Yu, Jaishankar Priyadarshini, Lauterwasser Erica M. W., Nichols Derek, Renslo Adam R.
Принадлежит:

Embodiments of the present disclosure, in one aspect, relate to a beta-lactamase inhibitor, pharmaceutical compositions including a beta-lactamase inhibitor, methods of treatment of a condition (e.g., infection) or disease, methods of treatment using compositions or pharmaceutical compositions, and the like. 1. A composition , comprising a beta-lactamase inhibitor.2. The composition of claim 1 , further comprising an antibiotic.3. The composition of claim 3 , wherein the antibiotic is a beta-lactam antibiotic.11. A pharmaceutical composition comprising a therapeutically effective amount of a beta-lactamase inhibitor claim 3 , or a pharmaceutically acceptable salt of the beta-lactamase inhibitor claim 3 , and a pharmaceutically acceptable carrier claim 3 , to treat a condition.12. The pharmaceutical composition of claim 11 , further comprising an antibiotic.13. The pharmaceutical composition of claim 12 , wherein the antibiotic is a beta-lactam antibiotic.2132-. (canceled) This application is continuation of US patent application entitled “COMPOSITIONS, METHODS OF USE, AND METHODS OF TREATMENT” having Ser. No. 14/370,715 and filed Jul. 3, 2014, which is the 35 U.S.C. §371 national stage of, and claims priority to and the benefit of, PCT application PCT/US2013/020212, filed Jan. 4, 2013, where the PCT application claims priority to and the benefit of U.S. Provisional Application No. 61/583,679, filed on Jan. 6, 2012, herein incorporated by reference in its entirety.Beta-lactam compounds such as penicillins are the most widely used antibiotics due to their effective inhibition of the transpeptidases required for bacterial cell wall synthesis. Beta-lactamases catalyze β-lactam hydrolysis and are primary mediators of bacterial resistance to these compounds. There are four β-lactamase families, Classes A to D, among which Classes A and C are the most commonly observed in the clinic. CTX-M is a new group of Class A β-lactamases that is particularly effective against the ...

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Номер записи: 91
02-04-2015 дата публикации

N-ALKOXYAMIDE CONJUGATES AS IMAGING AGENTS

Номер: US20150094465A1
Автор: Casebier David S., Cesati Richard R., Cheesman Edward H., Harris Thomas D., Looby Richard J., Robinson Simon P., Yalamanchili Padmaja
Принадлежит: Lantheus Medical Imaging, Inc.

The present disclosure is directed to compounds, diagnostic agents, and related methods. In some cases, methods for treating patients are provided. More specifically, the disclosure provides compounds, diagnostic agents, and kits for detecting and/or imaging and/or monitoring elastin rich tissues. In addition, the disclosure provides methods of detecting and/or imaging and/or monitoring the presence of coronary plaque, carotid plaque, iliac/femoral plaque, aortic plaque, renal artery plaque, plaque of any arterial vessel, aneurism, vasculitis, other diseases of the arterial wall, and/or damage or structural changes in ligaments, uterus, lungs or skin, as indicated by changes in total vessel wall area, internal lumen size, and exterior arterial perimeter. 2. A compound as in claim 1 , wherein X is nitrogen.3. A compound as in claim 1 , wherein X is oxygen.4. A compound as in claim 1 , wherein X is sulfur.5. A compound as in claim 1 , wherein X is phosphorus.6. A compound as in claim 1 , wherein:X is nitrogen;{'sup': '1', 'Ris hydrogen, alkyl, arylalkyl, or alkylarylalkyl;'}{'sup': 2', '3, 'Rand Rcan be the same or different and are hydrogen, alkyl, alkylaryl, aryl, arylalkyl, alkylarylalkyl, or heterocyclylalkyl;'}{'sup': '4', 'Ris alkyl, alkylaryl, aryl, arylalkyl, or alkylarylalkyl,'}{'sup': 1', '2', '3', '4, 'wherein at least one of R, R, R, and Ris substituted with a chelator moiety;'}9. A compound as in claim 8 , whereinn is 1 or 2;{'sup': 'y', 'Ris hydrogen; and'}{'sup': 'z', 'Ris selected from alkyl, aryl, cycloalkyl, and heteroaryl.'}10. A compound as in claim 1 , wherein Rcomprises the at least one chelator moiety.11. A compound as in claim 1 , wherein Ror Rcomprises the at least one chelator moiety.12. A compound as in claim 1 , wherein Rcomprises the at least one chelator moiety.18. A compound as in claim 17 , wherein one of Dand Dis a hydrogen and the other is a chelator moiety.20. A compound as in claim 19 , whereino, r, s, t, and u are each 1; andp and ...

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Номер записи: 92
05-05-2022 дата публикации

METAL/RADIOMETAL-LABELED PSMA INHIBITORS FOR PSMA-TARGETED IMAGING AND RADIOTHERAPY

Номер: US20220135529A1
Автор: Chen Ying, Meade Thomas J., Mease Ronnie C., Pomper Martin G., Ray Sangeeta, ROTZ MATTHEW, Yang Xing
Принадлежит:

Low-molecular weight gadolinium (Gd)-based MR contrast agents for PSMA-specific T-weighted MR imaging are disclosed. The (Gd)-based MR contrast agents exhibit high binding affinity for PSMA and exhibit specific Tcontrast enhancement at PSMA+ cells. The PSMA-targeted Gd-based MR contrast agents can be used for PSMA-targeted imaging in vivo. Y-labeled PSMA-binding ureas also are provided, wherein the PSMA-binding ureas also are suitable for use with other radiotherapeutics.

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Номер записи: 93
05-05-2022 дата публикации

SYNTHESIS OF 5-NITROTETRAZOLE

Номер: US20220135530A1
Автор: Manship Timothy D., Piercey Davin Glenn, Smith Dawson Michael
Принадлежит: PURDUE RESEARCH FOUNDATION

This disclosure shows the ability of a readily-available oxidizer to achieve oxidation of 5-amino-1H-tetrazole (5-AT) to 5-nitrotetrazole (5-NT) in high yields in a single pot synthesis. This strategy reduces the synthesis of this important energetic material down to a single step and eliminates highly sensitive diazonium and copper salt primary explosive intermediates. The overall yield of this process is 48-53% and the resultant aqueous solution of product effectively used for the preparation of nitrotetrazole-containing primary explosive DBX-1. Unlike current methods of nitrotetrazole preparation, the novel method is entirely solution-based and prepares a final solution of sodium nitrotetrazolate, never once needing to handle energetic intermediates or products, making it a much safer method of nitrotetrazole preparation.

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Номер записи: 94
26-06-2014 дата публикации

N1-Cyclic Amine-N5-Substituted Phenyl Biguanide Derivatives, Methods of Preparing the Same and Pharmaceutical Composition Comprising the Same

Номер: US20140179660A1
Автор: KIM Duck, Kim Sung Wuk, KIM Yong Eun, LEE Ji Sun, MIN Chang Hee, OH Ju Hoon, PARK Se Hwan
Принадлежит: HANALL BIOPHARMA CO., LTD.

An N1-cyclic amine-N5-substituted phenyl biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome. 2. The compound of Formula 1 or the pharmaceutically acceptable salt thereof of claim 1 ,wherein R1 and R2 are taken together with nitrogen to which they are attached to form 4- to 7-membered heterocycloalkyl;n is an integer ranging from 0 to 5;when there is more than one R3, each R3 is independently selected from the group consisting of hydrogen, halogen, hydroxy, C1-6alkyl, C1-6alkoxy, C1-6alkylthio, amino, amide, sulfonamide, nitro, heteroaryl, cyano, sulfonic acid and sulfamoyl; andR1 and R2, or R3 are each independently unsubstituted or substituted with at least one substituent selected from the group consisting of halogen, hydroxy and C1-6alkyl.3. The compound of Formula 1 or the pharmaceutically acceptable salt thereof of claim 1 ,wherein R1 and R2 are taken together with nitrogen to which they are attached to form 3- to 8-membered heterocycloalkyl selected from the group consisting of azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl and aziridinyl ...

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Номер записи: 95
16-04-2015 дата публикации

PSMA-TARGETING COMPOUNDS AND USES THEREOF

Номер: US20150104387A1
Автор: Chen Ying, Mease Ronnie C., Pomper Martin G., Ray Sangeeta
Принадлежит: THE JOHNS HOPKINS UNIVERSITY

Prostate-specific membrane antigen (PSMA) targeting compounds are described. Uses of the compounds for imaging, therapy, cell sorting, and tumor mapping are also described. 423-. (canceled)25. (canceled)26. A compound according to claim 1 , having a chelated metal claim 1 , wherein the chelated metal is Tc claim 1 , In claim 1 , Ga claim 1 , Y claim 1 , Lu claim 1 , Re claim 1 , Cu claim 1 , Ac claim 1 , Bi claim 1 , Pb claim 1 , Sm claim 1 , Sc claim 1 , Co claim 1 , Ho claim 1 , Gd claim 1 , Eu claim 1 , Tb claim 1 , or Dy.27. (canceled)28. (canceled)30. (canceled)31. (canceled)3244-. (canceled)45. (canceled)46. (canceled)47. (canceled)48. (canceled)49. (canceled)5274-. (canceled)75. A compound according to wherein FG is a fluorescent dye moiety which emits in the near infrared spectrum.76. A compound according to wherein FG comprises carbocyanine claim 1 , indocarbocyanine claim 1 , oxacarbocyanine claim 1 , thiacarbocyanine and merocyanine claim 1 , polymethine claim 1 , coumarine claim 1 , rhodamine claim 1 , xanthene claim 1 , fluorescein claim 1 , boron-dipyrromethane (BODIPY) claim 1 , Cy5 claim 1 , Cy5.5 claim 1 , Cy7 claim 1 , VivoTag-680 claim 1 , VivoTag-S680 claim 1 , VivoTag-S750 claim 1 , AlexaFluor660 claim 1 , AlexaFluor680 claim 1 , AlexaFluor700 claim 1 , AlexaFluor750AlexaFluor790 claim 1 , Dy677 claim 1 , Dy676 claim 1 , Dy682 claim 1 , Dy752 claim 1 , Dy780 claim 1 , DyLight547 claim 1 , Dylight647 claim 1 , HiLyte Fluor 647 claim 1 , HiLyte Fluor 680 claim 1 , HiLyte Fluor 750 claim 1 , IRDye 800CW claim 1 , IRDye 800RS claim 1 , IRDye 700DX claim 1 , ADS780WS claim 1 , ADS830WS claim 1 , and ADS832WS.81102-. (canceled)104112-. (canceled)116145-. (canceled)146. A method of imaging one or more cells claim 1 , organs or tissues by exposing the cell to or administering to an organism an effective amount of a compound according to claim 1 , where the compound includes a fluorescent dye moiety claim 1 , or a metal isotope suitable for imaging.147. ...

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Номер записи: 96
21-04-2016 дата публикации

Substituted N-(Tetrazol-5-yl)- and N-(Triazol-5-yl)arylcarboxamide Compounds and Their Use as Herbicides

Номер: US20160108008A1
Автор: CALO Frederick, EVANS Richard Roger, Kraus Helmut, Kreuz Klaus, Lerchl Jens, Massa Dario, Mietzner Thomas, NEWTON Trevor William, Pasternak Maciej, SEITZ Thomas, WITSCHEL Matthias
Принадлежит: BASF SE

N-(tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides of formula I and their use as herbicides, 117-. (canceled)19. The compound of claim 18 , wherein R is selected from the group consisting of C-C-alkyl claim 18 , C-C-alkoxy-C-C-alkyl claim 18 , C-C-cycloalkyl claim 18 , C-C-haloalkyl claim 18 , R—C(═O)—C-C-alkyl claim 18 , RO—C(═O)—C-C-alkyl claim 18 , RRN—C(═O)—C-C-alkyl and R—C(═O)NH—C-C-alkyl claim 18 , wherein{'sup': 'c', 'sub': 1', '4', '1', '4, 'Ris C-C-alkyl or C-C-haloalkyl,'}{'sup': 'd', 'sub': 1', '4, 'Ris C-C-alkyl,'}{'sup': 'e', 'sub': 1', '4, 'Ris hydrogen or C-C-alkyl,'}{'sup': 'f', 'sub': 1', '4, 'Ris hydrogen or C-C-alkyl, or'}{'sup': e', 'f, 'R, Rtogether with the nitrogen atom, to which they are bound may form a 5-, 6 or 7-membered, saturated N-bound heterocyclic radical, which may carry as a ring member a further heteroatom selected from O, S and N and which is unsubstituted or may carry 1, 2, 3 or 4 methyl groups,'}{'sup': 'k', 'sub': 1', '4, 'Ris C-C-alkyl.'}20. The compound of claim 18 , wherein R is selected from the group consisting of C-C-alkyl claim 18 , C-C-cycloalkyl claim 18 , C-C-haloalkyl and C-C-alkoxy-C-C-alkyl.21. The compound of claim 18 , wherein R is selected from the group consisting of C-C-alkyl and C-C-alkoxy-C-C-alkyl.2217. The compound of claim 18 , wherein Ris selected from the group consisting of cyano claim 18 , halogen claim 18 , nitro claim 18 , C-C-alkyl claim 18 , C-C-alkenyl claim 18 , C-C-alkynyl claim 18 , C-C-haloalkyl claim 18 , C-C-alkoxy claim 18 , C-C-alkoxy-C-C-alkyl claim 18 , C-C-haloalkoxy-C-C-alkyl claim 18 , C-C-alkoxy-C-C-alkoxy-Z claim 18 , C-C-alkylthio-C-C-alkyl claim 18 , C-C-alkylthio-C-C-alkylthio-Z claim 18 , C-C-alkenyloxy claim 18 , C-C-alkynyloxy claim 18 , C-C-haloalkoxy claim 18 , C-C-haloalkoxy-C-C-alkoxy and R1-S(O) claim 18 , wherein k and Zare as defined in claim and wherein Ris selected from the group consisting of C-C-alkyl and C-C-haloalkyl.23. The compound of claim 18 , wherein ...

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Номер записи: 97
03-07-2014 дата публикации

Macrocyclic Compounds And Metal Complexes For Bioimaging And Biomedical Applications

Номер: US20140187527A1
Автор: Bhagwat Bhalchandra Vishnu, CHANG Cheng Allen, Liu Ren-Shyan
Принадлежит: NATIONAL YANG MING UNIVERSITY

The present disclosure provides a novel class of macrocyclic compounds and their metal complexes formed with transition metal ion, lanthanide metal ions and other metal ions (e.g., Al, Ga, Y, In, Sn, Tl, Pb and Bi) and their applications in the fields of contrast agents, artificial nucleases, fluorescence probes, nuclear medicines and other biomedical applications in the therapeutics or diagnostics. 4. The compound of claim 1 , further comprising at least one group of formula (IV):{'br': None, 'sub': s', 't', 'p, '-W-(X—Y)—\u2003\u2003(IV)'}that bounds the compound of formula (I) to a biomolecule. [{'sub': 2', '2', '2', '2', '2', '2', '8', '2', '2', '8', '8', '8', '8', '8', '8', '8, 'W is —O—, —S—, —CH—, —SO—, SO—, —CO—, —NHNH—, —CONH—, —NHCO—, —NHCONH—, —CONHCO—, —NHCONHO—, —COO—, —COCH—, —CHCO—, —NHO—, —ONH—, —CH═CH—, —CHNH—, —NHCH—, —NH—, —NR, —NH(C═NH)NH—, —CH═N—, —CH═N—O—, —N═CH—, —SONH—, —NHSO—, —NH—CS—, —NHCSNH—, —NH(C═NH)NH—O—, —OCO—, —S—S—, —N═N—, alkynyl, methylene carbamate, methylene thiocarbamate, methylene isourea, methylene isothiourea, methylene guanidine, —C═C(R)—COOR, —C═C(R)—COR, —C═NH—, —C═NOH, —C═NR, —C═NOR, allyl-OCOR, allyl ester, phenylene, alkylene, ethynydiyl, ethylenediyl, a polymerizable group, a boron, a silicon, phosphorous, selenium, haloacetamido, isothiocyanate, maleimido, dichlorotriazinylamino, dichlorotriazinyl, thioester, pyridyldithio, aminooxy, amino, hydrazide, carboxylic acid, or acid halide;'}, {'sub': '8', 'Ris alkyl, cycloalkyl, or aryl;'}, 'X and Y are same or different and independently alkyl, cycloalkyl, aryl, or heterocylic, wherein any two carbon atoms are optionally interrupted with one or more N, O, S, Si, P, Se or B; and', 's, t, and p are an integer from 0 to 100., 'wherein5. The compound of claim 4 , wherein X and Y further comprises positively charged carboxylate or negatively charged ammonium moieties6. The compound of claim 4 , wherein the biomolecule is proteins claim 4 , protein-proteins claim 4 , ...

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Номер записи: 98
03-07-2014 дата публикации

ANTI-AMYLOID COMPOUNDS AND METHODS

Номер: US20140187556A1
Автор: Banfield Scott C., BARDEN Christopher J., Reed Mark A., YADAV Arun
Принадлежит: Treventis Corporation

Anti-amyloid compounds are provided along with methods of use thereof. 2. The compound of in which the compound is according to Formula Ia.3. The compound of in which the compound is according to Formula Ib.4. The compound of in which the compound is according to Formula Ic.5. The compound of in which the compound is according to Formula Id.6. The compound of in which the compound is according to Formula Ie.7. The compound of in which the compound is according to Formula If.8. The compound of in which E is carbon.9. The compound of in which E is nitrogen.10. The compound of in which Ris nitro and Ris selected from the group consisting of ethanol-1-yl claim 3 , methanol claim 3 , 2 claim 3 ,2 claim 3 ,2-trifluoro-1-hydroxyethanol-1-yl claim 3 , and 2 claim 3 ,2 claim 3 ,2-trifluoroethanol-1-yl.11. The compound of in which the compound is 1-(3′-(benzylamino)-4′-nitro-[1 claim 10 ,1′-biphenyl]-3-yl)-2 claim 10 ,2 claim 10 ,2-trifluoroethanol.12. The compound of in which the compound is 1-(3′-(benzylamino)-4′-nitro-[1 claim 10 ,1′-biphenyl]-3-yl)-2 claim 10 ,2 claim 10 ,2-trifluoroethane-1 claim 10 ,1-diol.13. The compound of in which Ris nitro and Ris C-linked tetrazole.14. The compound of in which Ris nitro.15. The compound of in which Ris selected from the group consisting of sulfonamide claim 14 , alkylamide claim 14 , dialkylamide claim 14 , benzyl alkylamide claim 14 , N-pyrrolidinamide claim 14 , (N′-methanonylpiperazine)amide claim 14 , (N′-methylpiperazine)amide claim 14 , morphilinamide claim 14 , and piperidineamide.16. The compound of claim 1 , wherein compound inhibits the aggregation of an amyloidogenic protein.17. The compound of for use in the preparation of a pharmaceutically effective dosage form the treatment of amyloid diseases.18. The compound of claim 16 , wherein said amyloid disease is selected from the group consisting of Alzheimer's disease claim 16 , Parkinson's disease claim 16 , Huntington's disease claim 16 , and prion diseases.19. A ...

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Номер записи: 99
19-04-2018 дата публикации

PREPARATION OF HIGH-PURITY GADOBUTROL

Номер: US20180105537A1
Автор: PLATZEK Johannes, Trentmann Wilhelm
Принадлежит:

A process for producing high-purity gadobutrol in a purity (according to HPLC) of more than 99.7 or 99.8 or 99.9% and the use for preparing a pharmaceutical formulation for parenteral administration is described. The process is carried out using specifically controlled crystallization conditions. 1. A process for producing a high-purity gadobutrol (N-(1-hydroxymethyl-2 ,3-dihydroxypropyl)-1 ,4 ,7-triscarboxymethyl-1 ,4 ,7 ,10-tetraazacyclododecane) , the process comprising:crystallizing a crude gadobutrol product from a first ethanol solution having a water content of 7.0 to 9.5%;isolating a crystallized crude gadobutrol;treating an aqueous solution of the crystallized crude gadobutrol on an ion exchange column cascade until the gadobutrol eluate has a conductivity of less than 40 μS/cm;concentrating the gadobutrol eluate having the conductivity of less than 40 μS/cm to provide a concentrated gadobutrol eluate;crystallizing the concentrated gadobutrol eluate from a second ethanol solution having a water content of 10.0 to 12.0% to give a purified gadobutrol; andisolating and drying the purified gadobutrol to give a high-purity gadobutrol.2. The process of claim 1 , wherein crystallizing the crude gadobutrol product comprises: heating the first ethanol solution having the water content of 7.0 to 9.5% under reflux; and cooling the first ethanol solution having the water content of 7.0 to 9.5% to form a crystallized crude gadobutrol.3. The process of claim 2 , wherein the first ethanol solution has a water content of 8.0 to 9.0%.4. The process of claim 1 , wherein the ion exchange column cascade comprises an acidic ion exchange column followed by a basic ion exchange column.5. The process of claim 1 , wherein treating the aqueous solution of the crystallized crude gadobutrol comprises repeatedly treating to the ion exchange column cascade until the gadobutrol eluate has a conductivity of less than 20 μS/cm.6. The process of claim 1 , wherein crystallizing the ...

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Номер записи: 100