- HETEROBICYCLIC COMPOUNDS FOR INHIBITING THE ACTIVITY OF SHP2
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A compound of formula (I):wherein Ring A, Q, R1,R2, R3, R4, R5, R6, R7, R8, R9, R10, R11,X, a,b, c and d are as defined in the specification.
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Paragraph 0528-0530
(2020/02/16)
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- INHIBITING AGENTS FOR BRUTON'S TYROSINE KINASE
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Provided are compounds of Formula (I), or pharmaceutically acceptable salts thereof, and methods for their use and production.
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- PHARMACEUTICAL COMPOUNDS
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The invention provides new pyrazine derivatives of formula (I), or a tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined herein. The invention also provides pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
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Page/Page column 155
(2019/09/18)
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- DIHYDROISOQUINOLINE-2(1H)-CARBOXAMIDE AND RELATED COMPOUNDS AND THEIR USE IN TREATING MEDICAL CONDITIONS
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The invention provides dihydroisoquinoline-2(1H)-carboxamide and related compounds, pharmaceutical compositions, and their use in the treatment of medical conditions, such as cancer, and in inhibiting HPK1 activity.
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Paragraph 000411
(2019/11/04)
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- INHIBITING AGENTS FOR BRUTON'S TYROSINE KINASE
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Provided are compounds of Formula (I), or pharmaceutically acceptable salts thereof, methods for use as Bruton's tyrosine kinase and methods of production.
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- ANDROGEN RECEPTOR ANTAGONISTS AND USES THEREOF
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Disclosed are substituted thioimidazolidinone compounds and pharmaceutical compositions comprising such compounds. The compounds and compositions can be used for treatment of androgen receptor-associated diseases or disorders, such as prostate cancer, benign prostatic hypertrophy, male hair loss and hypertrichosis.
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Page/Page column 82-83
(2012/09/22)
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- ANDROGEN RECEPTOR ANTAGONISTS AND USES THEREOF
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The present invention relates to novel substituted thioimidazolidinone compounds and pharmaceutical compositions comprising such compounds for treatment of androgen receptor-associated diseases or disorders, such as prostate cancer, benign prostatic hypertrophy, male hair loss, muscle loss, acne and hirsutism.
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Page/Page column 61
(2011/04/18)
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- Cyclic amine compounds
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The present invention relates to pharmaceutical agents which are agents for the prophylaxis or treatment of hypogonadism, male climacteric disorder, frailty, cachexia or osteoporosis; the pharmaceutical agents frailty suppressants, muscle strength enhance
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Page/Page column 49
(2009/03/07)
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- Tandem optimization of target activity and elimination of mutagenic potential in a potent series of N-aryl bicyclic hydantoin-based selective androgen receptor modulators
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Pharmacokinetic studies in cynomolgus monkeys with a novel prototype selective androgen receptor modulator revealed trace amounts of an aniline fragment released through hydrolytic metabolism. This aniline fragment was determined to be mutagenic in an Ames assay. Subsequent concurrent optimization for target activity and avoidance of mutagenicity led to the identification of a pharmacologically superior clinical candidate without mutagenic potential.
- Hamann, Lawrence G.,Manfredi, Mark C.,Sun, Chongqing,Krystek Jr., Stanley R.,Huang, Yanting,Bi, Yingzhi,Augeri, David J.,Wang, Tammy,Zou, Yan,Betebenner, David. A.,Fura, Aberra,Seethala, Ramakrishna,Golla, Rajasree,Kuhns, Joyce E.,Lupisella, John A.,Darienzo, Celia J.,Custer, Laura L.,Price, Jennifer L.,Johnson, James M.,Biller, Scott A.,Zahler, Robert,Ostrowski, Jacek
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p. 1860 - 1864
(2008/02/04)
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