公开(公告)号：EP2370415A2

公开(公告)日：2011-10-05

申请号：EP09835863.3

申请日：2009-12-23

申请人： Rigel Pharmaceuticals, Inc.

发明人： BHAMIDIPATI, Somasekhar ,  LI, Hui ,  SINGH, Rajinder ,  TAYLOR, Vanessa ,  CLOUGH, Jeffrey ,  MCMURTRIE, Darren

IPC分类号： C07D239/22 ,  A61K31/505 ,  A61P37/06

CPC分类号： C07D239/48

摘要： The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.

公开(公告)号：EP2316459A1

公开(公告)日：2011-05-04

申请号：EP10010732.5

申请日：2003-07-29

申请人： Rigel Pharmaceuticals, Inc.

发明人： Singh, Rajinder ,  Argade, Ankush ,  Payan, Donald G. ,  Clough, Jeffrey ,  Keim, Holger ,  Sylvain, Catherine ,  Li, Hui ,  Bhamidipati, Somasekhar

IPC分类号： A61K31/506 ,  A61K31/519 ,  A61P35/00 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D498/04

CPC分类号： A61K31/506 ,  A61K31/519 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D498/04

摘要： The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.

摘要翻译： 本发明提供用2,4-嘧啶二胺化合物治疗或预防自身免疫疾病的方法，以及治疗，预防或改善与这些疾病相关的症状的方法。 可以用化合物治疗或预防的自身免疫性疾病的具体实例包括类风湿性关节炎和/或其相关症状，系统性红斑狼疮和/或其相关症状和多发性硬化症和/或其相关症状。

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：EP2205592A1

公开(公告)日：2010-07-14

申请号：EP07870108.3

申请日：2007-12-29

申请人： Rigel Pharmaceuticals, Inc.

发明人： GOFF, Dane ,  ZHANG, Jing ,  SINGH, Rajinder ,  HOLLAND, Sacha ,  YU, Jiaxin ,  HECKRODT, Thilo ,  DING, Pingyu ,  LITVAK, Joane

IPC分类号： C07D403/04 ,  C07D403/14 ,  C07D471/18 ,  C07D491/14 ,  A61K31/4196 ,  A61P19/00 ,  A61P35/00

CPC分类号： A61K31/4439 ,  A61K31/4196 ,  A61K31/4375 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D471/08 ,  C07D471/18 ,  C07D491/14

摘要： Polycyclic aryl and polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl catalytic activity are also disclosed.

公开(公告)号：EP1856135B1

公开(公告)日：2009-12-09

申请号：EP06718943.1

申请日：2006-01-19

申请人： Rigel Pharmaceuticals, Inc.

发明人： SINGH, Rajinder ,  BHAMIDIPATI, Somasekhar ,  MASUDA, Esteban ,  STELLA, Valentino J. ,  SUN, Thomas

IPC分类号： C07F9/6561 ,  C07D498/04 ,  A61K31/675 ,  A61K31/5383 ,  A61P37/00

CPC分类号： C07D498/04 ,  A61K31/5383 ,  A61K31/675 ,  C07F9/65583 ,  C07F9/6561 ,  C07F9/65742

摘要： The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.

公开(公告)号：EP1534286B1

公开(公告)日：2009-12-09

申请号：EP03784871

申请日：2003-07-29

申请人： RIGEL PHARMACEUTICALS INC

发明人： SINGH RAJINDER ,  ARGADE ANKUSH ,  PAYAN DONALD G ,  CLOUGH JEFFREY ,  KEIM HOLGER ,  SYLVAIN CATHERINE ,  LI HUI ,  BHAMIDIPATI SOMASEKHAR

IPC分类号： A61K31/506 ,  A61K31/519 ,  A61P37/00

CPC分类号： A61K31/506 ,  A61K31/519 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D498/04 ,  Y10S514/825 ,  Y10S514/903

摘要： The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systematic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.

公开(公告)号：EP2078010A2

公开(公告)日：2009-07-15

申请号：EP07870107.5

申请日：2007-12-29

申请人： Rigel Pharmaceuticals, Inc.

发明人： GOFF, Dane ,  ZHANG, Jing ,  SINGH, Rajinder ,  HOLLAND, Sacha ,  YU, Jiaxin ,  HECKRODT, Thilo ,  DING, Pingyu ,  LITVAK, Joane

IPC分类号： C07D403/04 ,  C07D403/14 ,  C07D471/18 ,  C07D491/14 ,  A61K31/4196 ,  A61P19/00 ,  A61P35/00 ,  C07D401/14 ,  C07D405/14 ,  C07D417/04 ,  C07D417/14 ,  C07D451/04 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D491/04 ,  C07D491/20 ,  C07D495/04 ,  C07D519/00

CPC分类号： C07D401/14 ,  A61K31/502 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/04 ,  C07D417/14 ,  C07D451/04 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D491/04 ,  C07D491/20 ,  C07D495/04 ,  C07D519/00

摘要： Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.

公开(公告)号：EP2010181A1

公开(公告)日：2009-01-07

申请号：EP07759007.3

申请日：2007-03-21

申请人： Rigel Pharmaceuticals, Inc.

发明人： MASUDA, Esteban ,  PAYAN, Donald, G. ,  GROSSBARD, Elliott, B.

IPC分类号： A61K31/505 ,  A61P35/02

CPC分类号： A61K31/505 ,  A61K31/5383 ,  A61K31/542

摘要： The present disclosure provides methods for the treatment of cell proliferative disorders by administration of a Syk kinase or Syk/Flt-3 kinase inhibitor. Cell proliferative disorders treatable by the methods include, hematopoietic neoplasms and virally associated tumors. The compounds are also directed to therapeutic or prophylactic inhibition of tumor metastasis.

公开(公告)号：EP1427812B1

公开(公告)日：2008-11-19

申请号：EP02763580.4

申请日：2002-08-29

申请人： Rigel Pharmaceuticals, Inc.

发明人： ROSSI, Alexander, B.

IPC分类号： C12N5/02 ,  C12N5/08 ,  C12N5/00

CPC分类号： C12N5/0642 ,  C12N2501/125 ,  C12N2501/23 ,  C12N2501/26 ,  C12N2503/02

摘要： Provided are methods for producing and screening proliferated populations of CD34-negative progenitor cells, mucosal mast cells, connective tissue-type mast cells and basophil cells. The methods generate uniform proliferated populations of cells. The proliferated populations contain a uniform population of a size suitable for use in high throughput screening methods, for example, screening for agents that alter exocytosis. The invention includes screening the proliferated populations with at least one candidate bioactive agent, and evaluating the cells to detect a cell with an altered phenotype. The invention also includes isolating a candidate bioactive agent that causes the altered phenotype. Additionally, cells formed according to the described methods are also encompassed by the invention.

公开(公告)号：EP1261705B1

公开(公告)日：2008-09-24

申请号：EP00993043.9

申请日：2000-11-13

申请人： Rigel Pharmaceuticals, Inc.

发明人： KINSELLA, Todd, M.

IPC分类号： C12N15/12 ,  C12N15/62 ,  C12N15/86 ,  C12N5/10 ,  C07K14/435 ,  C07K14/475 ,  C12Q1/68 ,  G01N33/50 ,  G01N33/533

CPC分类号： G01N33/5023 ,  C07K14/475 ,  C07K2317/24 ,  C07K2319/00 ,  C12Q1/6897 ,  G01N33/5008