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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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25-09-2012 дата публикации

Substituted 1H-pyrazolo[3,4-D]pyrimidine-6-amine compounds

Номер: US0008273754B2

The present invention relates to substituted 1H-pyrazolo-[3,4-d]pyrimidine-6-amine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted 1H-pyrazolo-[3,4-d]pyrimidine-6-amine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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30-09-2010 дата публикации

SUBSTITUTED PYRAZOLO-PYRIMIDINE COMPOUNDS

Номер: US20100249110A1
Принадлежит: ArQule, Inc.

The present invention relates to substituted pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.

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02-04-2013 дата публикации

Substituted indolo-pyridinone compounds

Номер: US0008410144B2

The present invention relates to substituted indolo-pyridinone compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted indolo-pyridinone compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.

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09-12-2014 дата публикации

Substituted pyrazolo-pyrrolo-pyridine-dione compounds

Номер: US0008906928B2

The present invention relates to substituted pyrazolo-pyrrolo-pyridine-dione compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrazolo-pyrrolo-pyridine-dione compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.

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01-01-2013 дата публикации

Substituted pyrazolo-pyrimidine compounds

Номер: US0008343983B2

The present invention relates to substituted pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.

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21-04-2015 дата публикации

Substituted tricyclic pyrazolo-pyrimidine compounds

Номер: US0009012466B2
Принадлежит: ArQule Inc., ARQULE INC, ARQULE, INC., ARQULE INC.

The present invention relates to substituted tricyclic pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tricyclic pyrazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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11-03-2021 дата публикации

TRICYCLIC KINASE INHIBITORS AND USE THEREOF

Номер: US20210070731A1
Принадлежит:

The present application provides novel compounds that are inhibitors of kinases, including AMPK-related kinases like NUAK1, NUAK2, SIK1, SIK2, SIK3, MARK1, MARK2, MARK3, MARK4, as well as AURKA, AURKB, AURKC, CLK1, CLK2, DCAMKL2, MAPK7, MKNK2, PIK3CD, PKN3, RET, TAOK1, TAOK2, TAOK3, ULK2 and their mutants. The application also provides compositions, including pharmaceutical compositions, kits that include compounds, and methods of making and using compounds. The compounds provided herein are useful in treating diseases, disorders, or conditions that are mediated by these kinases. 1. A compound of formula:{'sup': 1', '2', '3', '4', '7', '8', '9', '10', '10, 'Each G, G, G, G, G, G, Gand Gis independently selected from N and CR;'}{'sup': 5', 'a', 'a', 'a', 'a', '100, 'sub': 2', '2', '1-6', '2-6', '2-6', '1-6', '2-6', '2-6, 'Gis selected from —S—, —O—, —NR—, —C(O)—, —C(O)O—, —C(O)NR—, S(O)NR—, —S(O)NR—, —S(O)—, —S(O)—, Calkylene, Calkenylene and Calkynylene; wherein each Calkylene, Calkenylene and Calkynylene is substituted with one to six R;'}{'sup': 6', '100, 'sub': 4-7', '6-10', '6-10, 'Gis selected from Cmembered heterocycloalkyl, Caryl, 5-10 membered heteroaryl containing 1 to 4 heteroatoms selected from the group consisting of N, O, and S, and 4-10 membered heterocyclyl containing 1 to 4 heteroatoms selected from the group consisting of N, O, and S; wherein each Caryl, 5-10 membered heteroaryl and 4-10 membered heterocyclyl is optionally substituted with one to four R;'}{'sup': 1', 'a', 'b', 'b', 'a', 'a', 'a', 'b', 'a', 'b', 'a', 'a', 'a', 'b', 'a', 'b', '100, 'sub': 2', '2', '1-6', '2- 6', '2-6', '3-8', '6-10', '1-6', '2-6', '2-6', '3-8', '6-10, 'Ris selected from absent, hydrogen, cyano, hydroxy, amino, —C(O)R, —C(O)OR, —C(O)NR, —N(R)C(O)R, —S(O)NRR, —S(O)NRR, —S(O)R, —S(O)R, — NRR, —OR, —SR, Calkyl, Calkenyl, Calkynyl, Ccycloalkyl, Caryl, 5-10 membered heteroaryl containing 1 to 4 heteroatoms selected from the group consisting of N, O, and S and 4-10 membered ...

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22-01-2013 дата публикации

Substituted 5,6-dihydro-6-phenylbenzo[F]isoquinolin-2-amine compounds

Номер: US0008357694B2

The present invention relates to substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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13-03-2014 дата публикации

Substituted Imidazopyridinyl-Aminopyridine Compounds

Номер: US20140073635A1
Принадлежит:

The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. 3. A method of synthesizing a compound of .4. A method of synthesizing a compound of .5. A method of treating a cell proliferative disorder by administering to a subject in need thereof claim 1 , a therapeutically effective amount of a compound of claim 1 , or a salt or ester thereof claim 1 , in combination with a pharmaceutically acceptable carrier or excipient.6. A method of treating a cell proliferative disorder by administering to a subject in need thereof claim 2 , a therapeutically effective amount of a compound of claim 2 , or a salt or ester thereof claim 2 , in combination with a pharmaceutically acceptable carrier or excipient.9. A method of synthesizing a compound of .10. A method of synthesizing a compound of .11. A method of treating a cell proliferative disorder by administering to a subject in need thereof claim 7 , a therapeutically effective amount of a compound of claim 7 , or a salt or ester thereof claim 7 , in combination with a pharmaceutically acceptable carrier or excipient.12. A method of treating a cell proliferative disorder by administering to a subject in need thereof claim 8 , a therapeutically effective amount of a compound of claim 8 , or a salt or ester thereof claim 8 , in combination with a pharmaceutically acceptable carrier or excipient. This application is a continuation of U.S. Ser. No. 13/529,459, filed Jun. 21, 2012, which claims priority to, and the benefit of, U.S. Ser. No. 61/500,889, filed Jun. 24, 2011. The contents of each of these applications are incorporated herein by reference in their entirety. ...

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26-08-2014 дата публикации

Substituted imidazopyridinyl compounds

Номер: US0008815854B2
Принадлежит: ArQule, Inc.

The present invention relates to substituted imidazopyridinyl compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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27-12-2012 дата публикации

Substituted Imidazopyridinyl-Aminopyridine Compounds

Номер: US20120329791A1
Принадлежит: ArQuele, Inc.

The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. 2. The compound of claim 1 , wherein X is NRR′; R′ is H; Ris (CH)R; m is 1 or 2; and Ris unsubstituted or substituted heterocycle selected from the group consisting of pyrrolidinyl claim 1 , imidazolidinyl claim 1 , pyrazolidinyl claim 1 , oxazolidinyl claim 1 , isoxazolidinyl claim 1 , triazolidinyl claim 1 , tetrahyrofuranyl claim 1 , piperidinyl claim 1 , piperazinyl claim 1 , and morpholinyl.3. The compound of claim 1 , wherein X is NRR′; R′ is H; and Ris unsubstituted phenyl or phenyl substituted with a substituent selected from the group consisting of hydroxyl claim 1 , halogen claim 1 , cyano claim 1 , nitro claim 1 , unsubstituted or substituted amino claim 1 , unsubstituted or substituted C-Calkyl claim 1 , unsubstituted or substituted C-Calkoxy claim 1 , and unsubstituted or substituted heterocycle comprising one 5- or 6-member ring and 1-3 heteroatoms selected from N claim 1 , O and S.4. The compound of claim 1 , wherein X is NRR′; and Rand R′ claim 1 , together with the nitrogen atom to which they are attached claim 1 , form an unsubstituted morpholine or a morpholine substituted with a substituent selected from the group consisting of hydroxyl claim 1 , halogen claim 1 , cyano claim 1 , nitro claim 1 , unsubstituted or substituted amino claim 1 , unsubstituted or substituted C-Calkyl claim 1 , and unsubstituted or substituted C-Calkoxy.5. The compound of claim 1 , wherein X is OR; and Ris unsubstituted phenyl or phenyl substituted with a substituent selected from the group consisting of hydroxyl claim 1 , halogen claim 1 , cyano claim 1 ...

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25-04-2017 дата публикации

Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof

Номер: US0009630968B1
Принадлежит: ArQule, Inc., ARQULE INC

The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, tautomer, prodrug, solvate, metabolite, polymorph, analog or derivative thereof, which modulates the activity of BTK, a pharmaceutical composition comprising the compound of Formula (I), and a method of treating or preventing a disease in which BTK plays a role.

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14-07-2011 дата публикации

Substituted Imidazopyridinyl-Aminopyridine Compounds

Номер: US20110172203A1
Принадлежит: ArQule, Inc.

The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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01-11-2011 дата публикации

Substituted tetrahydropyrazolo-pyrido-azepine compounds

Номер: US0008049005B2
Принадлежит: ArQule, Inc., ARQULE INC, ARQULE, INC.

The present invention relates to substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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20-05-2021 дата публикации

TETRAHYDROPYRANYL AMINO-PYRROLOPYRIMIDINONE AND METHODS OF USE THEREOF

Номер: US20210145837A1
Принадлежит: ArQule, Inc.

... or a pharmaceutically acceptable salt thereof, tautomer, prodrug, solvate, metabolite, polymorph, analog or derivative thereof, which modulates the activity of BTK, a pharmaceutical composition comprising the compound of Formula (I), and a method of treating or preventing a disease in which BTK plays a role.

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06-08-2013 дата публикации

Substituted imidazopyridinyl-aminopyridine compounds

Номер: US0008501770B2

The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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12-11-2013 дата публикации

Substituted pyrrolo-aminopyrimidine compounds

Номер: US0008580803B2

The present invention relates to substituted pyrrolo-aminopyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrrolo-aminopyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. The substituted pyrrolo-aminopyrimidine compounds have the following general formula:

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20-08-2013 дата публикации

Compositions and methods for the treatment of cancer

Номер: US0008513292B2

The present invention relates to pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound or pyrrolidine-2,5-dione compound of the present invention. (Ia) (Ib) (IIa) (IIIb) Where U is independently selected from: (I) or (II) where U is independently selected from: ...

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24-02-2015 дата публикации

Substituted imidazopyridinyl-aminopyridine compounds

Номер: US0008962619B2
Принадлежит: ArQule, Inc., ARQULE INC, ARQULE, INC.

The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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27-12-2012 дата публикации

Substituted Imidazopyridinyl Compounds

Номер: US20120329793A1
Принадлежит: ArQule, Inc.

The present invention relates to substituted imidazopyridinyl compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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19-01-2012 дата публикации

Substituted Tetrahydropyrazolo-Pyrido-Azepine Compounds

Номер: US20120015935A1
Принадлежит: ArQule, Inc.

The present invention relates to substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. 6. The method of any one of claims 1 , wherein said cell proliferative disorder is a precancerous condition claims 1 , a hematologic tumor or malignancy claims 1 , a solid tumor claims 1 , or a cancer.7. The method of claim 6 , wherein said cancer is a metastatic cancer.8. The method of claim 1 , wherein said subject is a human.9. The method of claim 1 , further comprising administering a therapeutically effective amount of a second anti-proliferative agent.10. The method of claim 1 , further comprising administering a radiation therapy. This application is a divisional application of U.S. Ser. No. 12/751,383, filed on Mar. 31, 2010, allowed, which claims priority to U.S. Ser. No. 61/165,044, filed on Mar. 31, 2009, the contents of each of which are incorporated herein by reference in their entirety.Cancer is the second leading cause of death in the United States, exceeded only by heart disease. (2004, American Cancer Society, Inc.). Despite recent advances in cancer diagnosis and treatment, surgery and radiotherapy may be curative if a cancer is found early, but current drug therapies for metastatic disease are mostly palliative and seldom offer a long-term cure. Even with new chemotherapies entering the market, the need continues for new drugs effective in monotherapy or in combination with existing agents as first line therapy, and as second and third line therapies in treatment of resistant tumors.Cancer cells are by definition heterogeneous. For example, within a single tissue or cell type, multiple mutational “mechanisms” may lead to the ...

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08-07-2010 дата публикации

SUBSTITUTED 1H-PYRAZOLO[3,4-D]PYRIMIDINE-6-AMINE COMPOUNDS

Номер: US20100172867A1
Принадлежит: ArQule, Inc.

The present invention relates to substituted 1H-pyrazolo-[3,4-d]pyrimidine-6-amine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted 1H-pyrazolo-[3,4-d]pyrimidine-6-amine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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30-09-2010 дата публикации

SUBSTITUTED DIPYRIDO-PYRIMIDO-DIAZEPINE AND BENZO-PYRIDO-PYRIMIDO COMPOUNDS

Номер: US20100249108A1
Принадлежит: ArQule, Inc.

The present invention relates to substituted dipyrido-pyrimido-diazepine compounds, substituted benzo-pyrido-pyrimido-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted dipyrido-pyrimido-diazepine compounds, substituted benzo-pyrido-pyrimido-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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22-07-2010 дата публикации

Compositions and Methods for the Treatment of Cancer

Номер: US20100183603A1
Принадлежит: ARQULE, INC.

The present invention relates to pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound or pyrrolidine-2,5-dione compound of the present invention. (Ia) (Ib) (IIa) (IIIb) Where U is independently selected from: (I) or (II) where U is independently selected from: ...

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23-10-2012 дата публикации

Substituted tetrahydropyrazolo-pyrido-azepine compounds

Номер: US0008293892B2

The present invention relates to substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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08-01-2013 дата публикации

Substituted dipyrido-pyrimido-diazepine and benzo-pyrido-pyrimido compounds

Номер: US0008349827B2

The present invention relates to substituted dipyrido-pyrimido-diazepine compounds, substituted benzo-pyrido-pyrimido-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted dipyrido-pyrimido-diazepine compounds, substituted benzo-pyrido-pyrimido-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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30-09-2010 дата публикации

SUBSTITUTED INDOLO-PYRIDINONE COMPOUNDS

Номер: US20100249127A1
Принадлежит: ArQule, Inc.

The present invention relates to substituted indolo-pyridinone compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted indolo-pyridinone compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.

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23-09-2010 дата публикации

SUBSTITUTED 5,6-DIHYDRO-6-PHENYLBENZO[F]ISOQUINOLIN-2-AMINE COMPOUNDS

Номер: US20100239525A1
Принадлежит: ArQule, Inc.

The present invention relates to substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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26-06-2008 дата публикации

Sigma Receptor Ligands

Номер: US20080153917A1
Принадлежит: UCB PHARMA, S.A.

The present invention concerns phenylcyclopentylacetamides and phenylcyclopropylcarboxamides and analogues thereof, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

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11-09-2012 дата публикации

Substituted imidazolyl-5,6-dihydrobenzo[N]isoquinoline compounds

Номер: US0008263610B2

The present invention relates to substituted imidazolyl-5,6-dihydrobenzo[n]isoquinoline compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazolyl-5,6-dihydrobenzo[n]isoquinoline compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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02-04-2019 дата публикации

Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof

Номер: US0010245263B2
Принадлежит: ArQule, Inc., ARQULE INC

The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, tautomer, prodrug, solvate, metabolite, polymorph, analog or derivative thereof, which modulates the activity of BTK, a pharmaceutical composition comprising the compound of Formula (I), and a method of treating or preventing a disease in which BTK plays a role.

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02-03-2021 дата публикации

Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof

Номер: US0010933065B2
Принадлежит: ArQule Inc., ARQULE INC, ArQule, Inc.

The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, tautomer, prodrug, solvate, metabolite, polymorph, analog or derivative thereof, which modulates the activity of BTK, a pharmaceutical composition comprising the compound of Formula (I), and a method of treating or preventing a disease in which BTK plays a role.

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23-09-2010 дата публикации

SUBSTITUTED IMIDAZOLYL-5,6-DIHYDROBENZO[N]ISOQUINOLINE COMPOUNDS

Номер: US20100239526A1
Принадлежит: ArQule, Inc.

The present invention relates to substituted imidazolyl-5,6-dihydrobenzo[n]isoquinoline compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazolyl-5,6-dihydrobenzo[n]isoquinoline compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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30-06-2011 дата публикации

Substituted Pyrrolo-Aminopyrimidine Compounds

Номер: US20110160203A1
Принадлежит: ArQule, Inc.

The present invention relates to substituted pyrrolo-aminopyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrrolo-aminopyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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30-09-2010 дата публикации

SUBSTITUTED TETRAHYDROPYRAZOLO-PYRIDO-AZEPINE COMPOUNDS

Номер: US20100249109A1
Принадлежит: ArQule, Inc.

The present invention relates to substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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01-06-2021 дата публикации

Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof

Номер: US0011020400B2
Принадлежит: ArQule, Inc., ARQULE INC

The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, tautomer, prodrug, solvate, metabolite, polymorph, analog or derivative thereof, which modulates the activity of BTK, a pharmaceutical composition comprising the compound of Formula (I), and a method of treating or preventing a disease in which BTK plays a role.

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30-09-2010 дата публикации

SUBSTITUTED PYRAZOLO-PYRROLO-PYRIDINE-DIONE COMPOUNDS

Номер: US20100249120A1
Принадлежит: ArQule, Inc.

The present invention relates to substituted pyrazolo-pyrrolo-pyridine-dione compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrazolo-pyrrolo-pyridine-dione compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.

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06-12-2007 дата публикации

RAF inhibitors and their uses

Номер: US20070281955A1
Принадлежит: Arqule Inc

The present invention provides imidazooxazole and imidazothiazole compounds and their synthesis. The compounds of the present invention are capable of inhibiting the activity of RAF kinase, such as B-RAF V600E . The compounds are useful for the treatment of cell proliferative disorders such as cancer.

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27-02-2020 дата публикации

TETRAHYDROPYRANYL AMINO-PYRROLOPYRIMIDINONE AND METHODS OF USE THEREOF

Номер: US20200061071A1
Принадлежит:

The application relates to a compound of Formula (I): 2. The method of claim 1 , wherein the mutant BTK comprises a drug-resistant mutation.3. The method of claim 2 , wherein the drug-resistant mutation is a mutation at amino acid 481.4. The method of claim 2 , wherein the drug-resistant mutation is C481S.5. The method of claim 1 , wherein the cancer is resistant to a BTK inhibitor.6. The method of claim 5 , wherein the BTK inhibitor is ibrutinib.7. The method of claim 1 , wherein the cancer is selected from a cancer of the breast claim 1 , ovary claim 1 , cervix claim 1 , prostate claim 1 , testis claim 1 , esophagus claim 1 , larynx claim 1 , stomach claim 1 , skin claim 1 , lung claim 1 , bone claim 1 , pancreas claim 1 , colon claim 1 , thyroid claim 1 , biliary passage claim 1 , hairy cells claim 1 , buccal cavity claim 1 , naso-pharyngeal claim 1 , lip claim 1 , tongue claim 1 , mouth claim 1 , large intestine claim 1 , small intestine claim 1 , colon-rectum claim 1 , rectum claim 1 , brain and central nervous system claim 1 , bronchus claim 1 , liver claim 1 , intrahepatic bile duct claim 1 , urinary bladder claim 1 , uterine corpus claim 1 , kidney claim 1 , renal pelvis claim 1 , oral cavity claim 1 , pharynx claim 1 , glioblastoma claim 1 , neuroblastoma claim 1 , keratoacanthoma claim 1 , epidermoid carcinoma claim 1 , large cell carcinoma claim 1 , non-small cell lung carcinoma (NSCLC) claim 1 , small cell carcinoma claim 1 , lung adenocarcinoma claim 1 , adenoma claim 1 , adenocarcinoma claim 1 , follicular carcinoma claim 1 , undifferentiated carcinoma claim 1 , papillary carcinoma claim 1 , seminoma claim 1 , melanoma claim 1 , sarcoma claim 1 , bladder carcinoma claim 1 , liver carcinoma claim 1 , kidney carcinoma claim 1 , myeloid disorders claim 1 , lymphoma claim 1 , Hodgkin's leukemia claim 1 , hepatocellular cancer claim 1 , glioma claim 1 , endometrial cancer claim 1 , multiple myeloma claim 1 , acute myelogenous leukemia claim 1 , chronic ...

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29-06-2017 дата публикации

Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof

Номер: US20170182053A1
Принадлежит: Arqule Inc

The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, tautomer, prodrug, solvate, metabolite, polymorph, analog or derivative thereof, which modulates the activity of BTK, a pharmaceutical composition comprising the compound of Formula (I), and a method of treating or preventing a disease in which BTK plays a role.

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18-09-2014 дата публикации

Substituted Tricyclic Pyrazolo-Pyrimidine Compounds

Номер: US20140275023A1
Принадлежит: Arqule Inc

The present invention relates to substituted tricyclic pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tricyclic pyrazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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27-06-2019 дата публикации

Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof

Номер: US20190192520A1
Принадлежит: Arqule Inc

The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, tautomer, prodrug, solvate, metabolite, polymorph, analog or derivative thereof, which modulates the activity of BTK, a pharmaceutical composition comprising the compound of Formula (I), and a method of treating or preventing a disease in which BTK plays a role.

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27-10-2011 дата публикации

Substituted 5,6-dihydro-6-phenylbenzo[f] isoquinolin-2-amine compounds

Номер: WO2010078421A8
Принадлежит: ArQule, Inc.

The present invention relates to substituted 5,6-dihydro-6- phenylbenzo[f]isoquinolin-2-amine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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16-03-2006 дата публикации

Sigma receptor ligands

Номер: WO2006027252A1
Принадлежит: Ucb Pharma, Sa

The present invention concerns phenylcyclopentylacetamides and phenylcyclopropylcarboxamides and analogues thereof, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

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07-10-2010 дата публикации

Substituted indolo-pyridinone compounds

Номер: WO2010114896A1
Принадлежит: ArQule, Inc.

The present invention relates to substituted indolo-pyridinone compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted indolo-pyridinone compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.

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14-01-2009 дата публикации

Raf inhibitors and their uses

Номер: EP2013218A2
Принадлежит: Arqule Inc

The present invention provides imidazooxazole and imidazothiazole compounds and their synthesis. The compounds of the present invention are capable of inhibiting the activity of RAF kinase, such as B-RAFV600E. The compounds are useful for the treatment of cell proliferative disorders such as cancer.

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24-09-2019 дата публикации

substituted pyrrolo-aminopyrimide compounds

Номер: BR112012016376A2
Принадлежит: Arqule Inc

compostos de pirollo-aminopiridina substituída. a presente invenção refere-se aos compostos de pirollo-aminopiridina substituída e métodos de sintetização destes compostos. a presente invenção também se refere às composições farmacêuticas contendo os compostos de pirrolo-aminopiridina substituída e métodos de tratar as desordens das células proliferativas, tais como câncer, administrando estes compostos e as composições farmacêuticas aos indivíduos em necessidade do mesmo. substituted pyrollo-aminopyridine compounds. The present invention relates to substituted pyrollo-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrrolo-aminopyridine compounds and methods of treating proliferative cell disorders such as cancer by administering these compounds and pharmaceutical compositions to individuals in need thereof.

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25-06-2020 дата публикации

Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof

Номер: AU2020203690A1
Принадлежит: Arqule Inc

The application relates to a compound of Formula (I): 'NH OPh N' H (I) or a pharmaceutically acceptable salt thereof, tautomer, prodrug, solvate, metabolite, polymorph, analog or derivative thereof, which modulates the activity of BTK, a pharmaceutical composition comprising the compound of Formula (I), and a method of treating or preventing a disease in which BTK plays a role.

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07-07-2011 дата публикации

Substituted pyrrolo-aminopyrimidine compounds

Номер: CA2785716A1
Принадлежит: Arqule Inc

The present invention relates to substituted pyrrolo-aminopyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrrolo-aminopyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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07-10-2010 дата публикации

Peri-fused pyrazolo-pyrimidine compounds

Номер: WO2010114905A1
Принадлежит: ArQule, Inc.

The present invention relates to substituted pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.

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07-07-2011 дата публикации

Substituted imidazopyridinyl-aminopyridine compounds

Номер: WO2011082270A2
Принадлежит: Arqule. Inc.

The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl- aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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31-10-2018 дата публикации

Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof

Номер: EP3394065A1
Принадлежит: Arqule Inc

The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, tautomer, prodrug, solvate, metabolite, polymorph, analog or derivative thereof, which modulates the activity of BTK, a pharmaceutical composition comprising the compound of Formula (I), and a method of treating or preventing a disease in which BTK plays a role.

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07-12-2011 дата публикации

Indolyl pyrrolidines for the treatment of cancer

Номер: EP2392574A1
Принадлежит: Arqule Inc

The present invention relates to pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound or pyrrolidine-2,5-dione compound of the present invention. where U is:

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01-01-2011 дата публикации

Substituted indolo-pyridinone compounds

Номер: TW201100398A
Принадлежит: Arqule Inc

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07-10-2010 дата публикации

Substituted indolo-pyridinone compounds

Номер: CA2756870A1
Принадлежит: Arqule Inc

The present invention relates to substituted indolo-pyridinone compounds and methods of synthesizing these com-pounds. The present invention also relates to pharmaceutical compositions containing substituted indolo-pyridinone compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compo-sitions to subjects in need thereof.

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07-10-2010 дата публикации

Substituted dipyrido-pyrimido-diazepine and benzo-pyrido-pyrimido compounds

Номер: CA2756807A1
Принадлежит: Arqule Inc

The present invention relates to substituted dipyrido-pyrimido-diazepine compounds of formula (I), substituted benzo-pyrido-pyrimido-diazepine compounds of formula (I) and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted dipyrido-pyrimido-diazepine compounds, substituted benzo--pyrido-pyrimido- diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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07-10-2010 дата публикации

Substituted tetrahydropyrazolo-pyrido-azepin compounds

Номер: CA2756809A1
Принадлежит: Arqule Inc

The present invention relates to substituted tetrahydropyrazolo-pyrido-azepine compounds of formula (I) and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof, or a pharmaceutically acceptable salt or ester thereof, wherein: X1, X2; and X3, together with the two carbon atoms numbered "1" and "2", form a ring selected from (a), (b) and (c).

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26-02-2009 дата публикации

Hdac inhibitors

Номер: CA2695452A1
Принадлежит: Individual

The present invention provides hydroxamic acid compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the hydroxamic acid compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a thera-peutically effective amount of a compound of the present invention.

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08-02-2012 дата публикации

Peri-fused pyrazolo-pyrimidine compounds

Номер: EP2414359A1
Принадлежит: Arqule Inc

The present invention relates to substituted pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.

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14-10-2010 дата публикации

HDAC Inhibitors

Номер: US20100261710A1
Принадлежит: Arqule Inc

The present invention provides hydroxamic acid compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the hydroxamic acid compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound of the present invention.

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12-06-2013 дата публикации

Substituted pyrrolo-aminopyrimidine compounds

Номер: EP2519525A4
Принадлежит: Arqule Inc

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08-07-2010 дата публикации

Substituted pyrazolo [3, 4-b] pyridine compounds

Номер: CA2748276A1
Принадлежит: Arqule Inc

The present invention relates to substituted imidazoly 1-5,6- dihydrobenzo[n]isoquinoline compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazolyl-5,6-dihydrobenzo[n]isoquinoline compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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31-12-2008 дата публикации

Compositions and methods for treatment of cancer

Номер: CA2912546A1
Принадлежит: Arqule Inc

The present invention relates to pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound of formula (Ia), (lb), (IIa) or (llb) (see formula Ia) (see formula Ib) (see formula IIa) (see formula IIb) where U is (see above formula)

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11-05-2021 дата публикации

5,6-dihydro-6-phenylbenzo(f)isoquinoline-2-amine substituted compounds and pharmaceutical compositions comprising said compounds

Номер: BRPI0923786C1
Принадлежит: Arqule Inc

compostos 5,6-dihidro-6-fenilbenzo(f) isoquinolina-2- amina substituidos. a presente invenção refere-se a compostos 5,6-dihidro-6-fenilbenzo [f] isoquinolin-2-amina substituídos e aos métodos de sintetizar esses compostos. a presente invenção também se relaciona com composições farmacêuticas contendo compostos 5,6-dihidro-6-fenilbenzo [f] isoquinolin-2-amina substituídos e métodos de tratamento de distúrbios de proliferação celular, tais como câncer, pela administração desses compostos e composições farmacêuticas a indivíduos em necessidade do mesmo. substituted 5,6-dihydro-6-phenylbenzo(f)isoquinoline-2-amine compounds. The present invention relates to substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of synthesizing such compounds. the present invention also relates to pharmaceutical compositions containing substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of treating cell proliferation disorders, such as cancer, by administering such compounds and pharmaceutical compositions to individuals in need of it.

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07-10-2010 дата публикации

Pyrazolo-pyrrolopyridine-dione derivatives useful in the treatment of cancer

Номер: CA2756810A1
Принадлежит: Arqule Inc

The present invention relates to substituted pyrazolo-pyrrolo-pyridine-dione compounds of formula (I) and meth-ods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrazolo-pyrrolo-pyridine-dione compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.

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07-07-2011 дата публикации

Substituted pyrrolo-aminopyrimidine compounds

Номер: WO2011082273A2
Принадлежит: ArQule, Inc.

The present invention relates to substituted pyrrolo-aminopyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrrolo-aminopyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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21-07-2011 дата публикации

Substituted 5,6-dihydro-6-phenylbenzo[f] isoquinolin-2-amine compounds

Номер: AU2009335010A1
Принадлежит: Arqule Inc

The present invention relates to substituted 5,6-dihydro-6- phenylbenzo[f]isoquinolin-2-amine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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15-09-2011 дата публикации

Indolylpyrrolidine zur behandlung von krebs

Номер: ATE522531T1
Принадлежит: Arqule Inc

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29-08-2023 дата публикации

Composto tetra-hidropiranil amino-pirrolpirimidinona, composição farmacêutica e uso dos mesmos

Номер: BR112018012828B1
Принадлежит: Arqule, Inc

TETRA-HIDROPIRANIL AMINO-PIRROLPIRIMIDINONA, COMPOSIÇÃO FARMACÊUTICA E USO DOS MESMOS. A presente invenção refere-se a um composto de Fórmula (I) ou um sal do mesmo, tautômero, pró-fármaco, solvato, metabólito, polimorfo, análogo ou derivado farmaceuticamente aceitável, que modula a atividade de BTK, uma composição farmacêutica compreendendo o composto de Fórmula (I), e um método de tratamento ou prevenção de uma doença na qual BTK desempenha um papel.

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10-10-2023 дата публикации

Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof

Номер: CA3008446C
Принадлежит: Arqule Inc

The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, tautomer, prodrug, solvate, metabolite, polymorph, analog or derivative thereof, which modulates the activity of BTK, a pharmaceutical composition comprising the compound of Formula (I), and a method of treating or preventing a disease in which BTK plays a role.

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27-05-2022 дата публикации

Τετραϋδροπυρανυλ αμινο-πυρρολοπυριμιδινονη και μεθοδοι χρησης αυτης

Номер: CY1124210T1
Принадлежит: ArQule, Inc.

Η αίτηση αφορά σε ένωση του Τύπου (Ι) ή φαρμακευτικώς αποδεκτό άλας αυτής, ταυτομερές, προφάρμακο, διαλύτωμα, μεταβολίτη, πολύμορφο, ανάλογο ή παράγωγο αυτής, που ρυθμίζει τη δραστικότητα της ΒΤΚ, φαρμακευτική σύνθεση που περιλαμβάνει την ένωση του Τύπου (Ι), και μέθοδο θεραπείας ή πρόληψης ασθένειας στην οποία η ΒΤΚ παίζει ένα ρόλο.

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27-06-2024 дата публикации

Kdm1a inhibitors for the treatment of disease

Номер: WO2024137358A1
Принадлежит: Imago Biosciences, Inc.

Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.

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28-08-2024 дата публикации

Kdm1a inhibitors for the treatment of disease

Номер: EP4419504A1
Принадлежит: Imago Biosciences Inc

Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.

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31-05-2024 дата публикации

Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof

Номер: NZ743384A
Принадлежит: Arqule Inc

The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, tautomer, prodrug, solvate, metabolite, polymorph, analog or derivative thereof, which modulates the activity of BTK, a pharmaceutical composition comprising the compound of Formula (I), and a method of treating or preventing a disease in which BTK plays a role.

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