公开(公告)号：EP2276761B1

公开(公告)日：2015-07-29

申请号：EP09734272.9

申请日：2009-04-22

申请人： Rigel Pharmaceuticals, Inc.

发明人： YU, Jiaxin ,  HONG, Hui ,  DARWISH, Ihab, S. ,  XU, Xiang ,  SINGH, Rajinder

IPC分类号： C07D471/04 ,  C07D401/12 ,  C07D401/14 ,  A61K31/4427 ,  A61K31/4523 ,  A61P3/00 ,  A61P9/00 ,  C07D401/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D487/08 ,  C07D211/58

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  C07D211/58 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D487/08

公开(公告)号：EP3265454A1

公开(公告)日：2018-01-10

申请号：EP16710547.7

申请日：2016-02-26

申请人： Rigel Pharmaceuticals, Inc. ,  Bristol-Myers Squibb Company

发明人： KINSELLA, Todd ,  GELMAN, Marina ,  HONG, Hui ,  DARWISH, Ihab, S. ,  SINGH, Rajinder ,  YU, Jiaxin ,  BORZILLERI, Robert, M. ,  VELAPARTHI, Upender ,  LIU, Peiying ,  DARNE, Chetan ,  RAHAMAN, Hasibur ,  WARRIER, Jayakumar, Sankara

IPC分类号： C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  A61K31/4164 ,  A61K31/426 ,  A61P35/00

摘要： Disclosed are imidazole and thiazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, A, Z, R1 and R′ are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-β, and can be used to treat disease by blocking TGF-β signaling.

公开(公告)号：EP2231600A1

公开(公告)日：2010-09-29

申请号：EP08848677.4

申请日：2008-11-17

申请人： Rigel Pharmaceuticals, Inc.

发明人： HONG, Hui ,  XU, Xiang ,  YU, Jiaxin ,  SINGH, Rajinder ,  DARWISH, Ihab, S. ,  THOTA, Sambaiah

IPC分类号： C07D211/46 ,  C07D211/58 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  A61K31/4427 ,  A61K31/4523 ,  A61P3/00 ,  A61P9/00

CPC分类号： C07D401/14 ,  C07D211/46 ,  C07D211/58 ,  C07D401/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

摘要： Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, E, T, n and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.

公开(公告)号：EP2231666A1

公开(公告)日：2010-09-29

申请号：EP08860063.0

申请日：2008-12-12

申请人： Rigel Pharmaceuticals, Inc.

发明人： DARWISH, Ihab, S. ,  YU, Jiaxin ,  HONG, Hui ,  SINGH, Rajinder ,  THOTA, Sambaiah ,  XU, Xiang

IPC分类号： C07D471/04 ,  C07D401/12 ,  C07D401/14 ,  A61K31/4427 ,  A61K31/4523 ,  A61P3/00 ,  A61P9/00 ,  C07D401/06

CPC分类号： C07D471/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14

摘要： Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, D, E, J, T, p, q and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.

公开(公告)号：EP1740556A1

公开(公告)日：2007-01-10

申请号：EP05726121.6

申请日：2005-03-25

申请人： Rigel Pharmaceuticals, Inc.

发明人： SINGH, Rajinder ,  GOFF, Dane ,  KOLLURI, Rao, S., S. ,  DARWISH, Ihab, S. ,  PARTRIDGE, John ,  COOPER, Robin ,  LU, Henry, H. ,  PARK, Gary

IPC分类号： C07D261/08 ,  C07D413/04 ,  A61K31/4439 ,  A61P31/12

CPC分类号： C07D413/04 ,  C07D261/08 ,  C07D413/12 ,  C07D413/14 ,  C07F9/65583

摘要： The present invention relates to substituted prodrug and compositions thereof useful for treating or preventing Hepatitis C virus (HCV) infections. In particular, the present invention relates to prodrugs of substituted diphenyl-, diheteroaryl- and mixed phenyl heteroaryl substituted five-membered heterocycle compounds, compositions comprising the compounds and the use of such compounds and compositions to inhibit HCV replication and/or proliferation as a therapeutic approach towards the treatment and/or prevention of HCV infections in humans and animals.

公开(公告)号：EP1554271A1

公开(公告)日：2005-07-20

申请号：EP03781338.3

申请日：2003-10-15

申请人： Rigel Pharmaceuticals, Inc.

发明人： SINGH, Rajinder ,  DARWISH, Ihab, S. ,  KOLLURI, Rao S. S. ,  THOTA, Sambaiah ,  LU, Henry, H.

IPC分类号： C07D409/12 ,  C07D401/12 ,  C07D407/12 ,  C07D417/12 ,  C07D209/08 ,  A61K31/404

CPC分类号： C07D401/04 ,  C07D209/08 ,  C07D209/18 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

摘要： The present invention comprises indole-derivatives that are inhibitors of HCV. Composition comprising the compounds in combination with a pharmaceutically acceptable carrier are also disclosed, as are methods of using the compounds and compositions to inhibit HCV infection of a cell, particular in the form of treating HCV infection in a mammal.

公开(公告)号：EP3265454B1

公开(公告)日：2020-02-26

申请号：EP16710547.7

申请日：2016-02-26

申请人： Rigel Pharmaceuticals, Inc. ,  Bristol-Myers Squibb Company

发明人： KINSELLA, Todd ,  GELMAN, Marina ,  HONG, Hui ,  DARWISH, Ihab, S. ,  SINGH, Rajinder ,  YU, Jiaxin ,  BORZILLERI, Robert, M. ,  VELAPARTHI, Upender ,  LIU, Peiying ,  DARNE, Chetan ,  RAHAMAN, Hasibur ,  WARRIER, Jayakumar, Sankara

IPC分类号： C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  A61K31/4164 ,  A61K31/426 ,  A61P35/00

公开(公告)号：EP3221318A1

公开(公告)日：2017-09-27

申请号：EP15801080.1

申请日：2015-11-16

申请人： Rigel Pharmaceuticals, Inc.

发明人： SINGH, Rajinder ,  KINSELLA, Todd ,  YU, Jiaxin ,  GELMAN, Marina ,  DARWISH, Ihab, S.

IPC分类号： C07D487/04 ,  C07D498/04 ,  C07D519/00 ,  A61P35/00 ,  A61K31/437 ,  A61K31/4365 ,  A61K31/428 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/517 ,  A61K31/424 ,  A61K31/519 ,  A61K31/4188

CPC分类号： C07D519/00 ,  C07D487/04 ,  C07D498/04

摘要： Disclosed are imidazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure Formula (I) and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein A, Z, X, R1, R2 m, p and a are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-β, and can be used to treat disease by blocking TGF-β signaling.

摘要翻译： 公开了咪唑化合物，以及药物组合物及其使用方法。 一个实施方案是具有结构式（I）的化合物及其药学上可接受的盐，前药和N-氧化物（及其溶剂化物和水合物），其中A，Z，X，R 1，R 2 m，p和a如本文所述 。 在某些实施方案中，本文公开的化合物抑制TGF-β，并且可用于通过阻断TGF-β信号传导来治疗疾病。

公开(公告)号：EP2276761A1

公开(公告)日：2011-01-26

申请号：EP09734272.9

申请日：2009-04-22

申请人： Rigel Pharmaceuticals, Inc.

发明人： YU, Jiaxin ,  HONG, Hui ,  DARWISH, Ihab, S. ,  XU, Xiang ,  SINGH, Rajinder

IPC分类号： C07D471/04 ,  C07D401/12 ,  C07D401/14 ,  A61K31/4427 ,  A61K31/4523 ,  A61P3/00 ,  A61P9/00 ,  C07D401/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D487/08 ,  C07D211/58

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  C07D211/58 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D487/08

摘要： Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R
1 , R
2 , R
3 , R
4 , D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.

公开(公告)号：EP2391616B1

公开(公告)日：2016-03-30

申请号：EP10703206.2

申请日：2010-01-28

申请人： Rigel Pharmaceuticals, Inc.

发明人： DARWISH, Ihab, S. ,  HONG, Hui ,  SINGH, Rajinder ,  XU, Xiang

IPC分类号： C07D401/12 ,  A61K31/501 ,  A61P3/00 ,  A61P9/00

CPC分类号： C07D401/12 ,  C07D401/14