公开(公告)号：EP3259264A1

公开(公告)日：2017-12-27

申请号：EP16711043.6

申请日：2016-02-15

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

发明人： DING, Pingyu ,  GELMAN, Marina ,  KINSELLA, Todd ,  SINGH, Rajinder ,  BHAMIDIPATI, Somasekhar ,  VELAPARTHI, Upender ,  BORZILLERI, Robert, M. ,  RAHAMAN, Hasibur ,  WARRIER, Jayakumar, Sankara

IPC分类号： C07D401/14 ,  C07D471/04 ,  C07D487/04 ,  A61K31/44 ,  A61P21/00

CPC分类号： C07D401/14 ,  C07B59/002 ,  C07B2200/05 ,  C07C53/06 ,  C07C53/18 ,  C07D471/04 ,  C07D487/04

摘要： and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein R1, Z and n are as described herein. In certain embodiments, a compound disclosed herein inhibits GDF8, and can be used to treat disease by blocking GDF8 signaling.

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：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：EP2903978A1

公开(公告)日：2015-08-12

申请号：EP13780264.1

申请日：2013-10-04

申请人： Rigel Pharmaceuticals, Inc.

发明人： BHAMIDIPATI, Somasekhar ,  GELMAN, Marina ,  DING, Pingyu ,  SINGH, Rajinder ,  CLOUGH, Jeffrey ,  KINSELLA, Todd ,  PAYAN, Donald

IPC分类号： C07D401/14 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D453/02 ,  C07D487/04 ,  C07D498/04 ,  C07D213/26

CPC分类号： C07D401/04 ,  C07D213/26 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D453/02 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  C07F9/65038

摘要： Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.

公开(公告)号：EP3277673A1

公开(公告)日：2018-02-07

申请号：EP16715730.4

申请日：2016-03-30

申请人： Rigel Pharmaceuticals, Inc.

发明人： GELMAN, Marina ,  KINSELLA, Todd ,  BHAMIDIPATI, Somasekhar ,  DARWISH, Ihab ,  SINGH, Rajinder ,  YU, Jiaxin

IPC分类号： C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  A61K31/4162 ,  A61K31/425 ,  A61P5/00 ,  A61P9/00 ,  A61P11/00 ,  A61P13/00 ,  A61P15/00 ,  A61P17/00 ,  A61P19/00 ,  A61P25/00 ,  A61P27/00 ,  A61P35/00

CPC分类号： C07D487/04 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  C07D471/04 ,  C07D519/00

摘要： Disclosed are pyrazole 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 A, X, Z, m, p, and R2 are as described herein. In certain embodiments, a compound disclosed herein inhibits the activity of one or more members of the TGF-β superfamily, and can be used to treat disease by blocking such activity.

公开(公告)号：EP3129367B1

公开(公告)日：2019-09-04

申请号：EP15716690.1

申请日：2015-04-02

申请人： Rigel Pharmaceuticals, Inc.

发明人： SINGH, Rajinder ,  BHAMIDIPATI, Somasekhar ,  DING, Pingyu ,  PAYAN, Donald ,  GELMAN, Marina ,  KINSELLA, Todd

IPC分类号： C07D401/14 ,  C07D401/04 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  A61K31/4427 ,  A61P35/00

公开(公告)号：EP3283479A1

公开(公告)日：2018-02-21

申请号：EP16715725.4

申请日：2016-03-29

申请人： Rigel Pharmaceuticals, Inc.

发明人： GELMAN, Marina ,  DING, Pingyu ,  KINSELLA, Todd ,  SINGH, Rajinder ,  BHAMIDIPATI, Somasekhar ,  CLOUGH, Jeffrey

IPC分类号： C07D403/12 ,  A61K31/505 ,  A61P35/00

CPC分类号： C07D403/12 ,  A61P35/02 ,  C07D401/12 ,  C07D471/04

摘要： Disclosed are aryl pyrimidine compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure (I) and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein A, Z, R and R' are as described herein. In certain embodiments, a compound disclosed herein inhibits the activity of one or more members of the TGF-β superfamily, and can be used to treat disease by blocking such activity.

公开(公告)号：EP3129367A1

公开(公告)日：2017-02-15

申请号：EP15716690.1

申请日：2015-04-02

申请人： Rigel Pharmaceuticals, Inc.

发明人： SINGH, Rajinder ,  BHAMIDIPATI, Somasekhar ,  DING, Pingyu ,  PAYAN, Donald ,  GELMAN, Marina ,  KINSELLA, Todd

IPC分类号： C07D401/14 ,  C07D401/04 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  A61K31/4427 ,  A61P35/00

CPC分类号： C07D401/04 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/635 ,  A61K31/695 ,  A61K39/39541 ,  A61K45/06 ,  A61K2039/505 ,  C07D401/14 ,  C07D405/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07F7/0812 ,  C07K16/2818

摘要： The invention described herein comprises compounds of formula (IV) and a method of treating cancer comprising administering to a subject having cancer one of the compounds in conjunction with another therapeutic treatment of cancer. The compounds (IV) inhibit signaling by a member of the TGF-β superfamily such as Nodal or Activin.

摘要翻译： 本文描述的本发明包括式（IV）的化合物和治疗癌症的方法，其包括对具有癌症的受试者与另一种治疗性癌症的治疗结合给药。 化合物（IV）抑制TGF-β超家族的成员如Nodal或激活素的信号传导。

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。