公开(公告)号：EP2598500A1

公开(公告)日：2013-06-05

申请号：EP11745858.8

申请日：2011-07-27

申请人： Rigel Pharmaceuticals, Inc.

发明人： LI, Hui ,  HECKRODT, Thilo, J. ,  CHEN, Yan ,  MCMURTRIE, Darren, John ,  TAYLOR, Vanessa ,  SINGH, Rajinder ,  DING, Pingyu ,  YEN, Rose

IPC分类号： C07D413/12 ,  C07D413/14 ,  A61K31/506 ,  A61P27/00 ,  A61P37/06

CPC分类号： C07D413/12 ,  C07B59/002 ,  C07B2200/05 ,  C07F9/65583

摘要： Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds.

摘要翻译： 公开了式I化合物，含有它们的组合物，以及用于化合物和组合物用于治疗JAK途径的调节或JAK激酶，特别是JAK 2和JAK 3的抑制在治疗上有用的条件的方法。 还公开了制备该化合物的方法。

公开(公告)号：EP2558474A1

公开(公告)日：2013-02-20

申请号：EP11730116.8

申请日：2011-04-13

申请人： Rigel Pharmaceuticals, Inc.

发明人： YU, Jiaxin ,  CLOUGH, Jeffrey ,  SINGH, Rajinder

IPC分类号： C07D498/04 ,  A61K31/5383 ,  A61P37/00 ,  A61P29/00

CPC分类号： C07D498/04

摘要： The present disclosure provides biologically active 2,4-pyrimidinediamme compounds of formulae (I) and (II): and salts thereof, compositions comprising these compounds, and methods of using these compounds in a variety of applications.

公开(公告)号：EP2114955B1

公开(公告)日：2013-02-13

申请号：EP07866125.3

申请日：2007-12-28

申请人： Rigel Pharmaceuticals, Inc.

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

IPC分类号： C07D495/04 ,  A61K31/4196 ,  A61P19/00 ,  C07D249/14 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D491/04 ,  C07D471/18 ,  C07D401/12 ,  C07D403/12 ,  C07D409/14

CPC分类号： C07D495/04 ,  C07D249/14 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D453/06 ,  C07D471/18

公开(公告)号：EP2484679A2

公开(公告)日：2012-08-08

申请号：EP12002451.8

申请日：2007-12-28

申请人： Rigel Pharmaceuticals, Inc.

发明人： Goff, Ding ,  Zhang, Jing ,  Singh, Rajinder ,  Holland, Sacha ,  Yu, Jiaxin ,  Heckrodt, Thilo ,  Ding, Pingyu ,  Litvak, Joane

IPC分类号： C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D495/04 ,  C07D519/00 ,  C07D487/04 ,  A61K31/4196 ,  A61P19/00 ,  C07D401/14 ,  C07D403/14

CPC分类号： C07D495/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00

摘要： N 3 -Heteroaryl substituted triazoles and N 5 -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.

摘要翻译： 公开了N 3 - 杂芳基取代的三唑和N 5 - 杂芳基取代的三唑和含有这些化合物的药物组合物，用于抑制受体蛋白酪氨酸激酶Ax1的活性。 还公开了使用该化合物治疗与Axl活性相关的疾病或病症的方法。

公开(公告)号：EP2454265A2

公开(公告)日：2012-05-23

申请号：EP10737424.1

申请日：2010-07-16

申请人： Rigel Pharmaceuticals, Inc.

发明人： BHAMIDIPATI, Somasekhar ,  SINGH, Rajinder ,  CLOUGH, Jeffrey

IPC分类号： C07D498/04 ,  C07F9/09 ,  A61K31/5383 ,  A61P37/08 ,  A61P17/02 ,  A61P29/00 ,  A61P19/02 ,  A61P37/00 ,  A61P21/04 ,  A61P1/04

CPC分类号： C07D498/04 ,  C07B59/002 ,  C07F9/6561 ,  C07F9/65742

摘要： The present disclosure provides biologically active deuterated 2,4-pyrimidinediamine compounds Formula (1) and prodrugs thereof, compositions comprising the deuterated compounds, intermediates and methods for synthesizing the deuterated compounds and methods of using the deuterated compounds in a variety of applications.

公开(公告)号：EP1814878B1

公开(公告)日：2012-01-04

申请号：EP05857021.9

申请日：2005-11-23

申请人： Rigel Pharmaceuticals, Inc.

发明人： COOPER, Robin ,  SINGH, Rajinder ,  CLOUGH, Jeffrey

IPC分类号： C07D413/12 ,  C07D413/14 ,  A61K31/5386 ,  A61P37/00

CPC分类号： C07D239/48 ,  C07D413/12 ,  C07D413/14

摘要： The present invention provides methods of treating or preventing autoimmune diseases with spiro 2,4-pyrimidinediamine compounds of Formula (I), 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 lupus erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.

公开(公告)号：EP2389372A1

公开(公告)日：2011-11-30

申请号：EP10701189.2

申请日：2010-01-22

申请人： Rigel Pharmaceuticals, Inc.

发明人： LI, Hui ,  HECKRODT, Thilo, J. ,  CHEN, Yan ,  MCMURTRIE, Darren, John ,  TAYLOR, Vanessa ,  SINGH, Rajinder ,  DING, Pingyu ,  THOTA, Sambaiah ,  YEN, Rose

IPC分类号： C07D401/12 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D451/02 ,  C07D471/04 ,  C07D471/08 ,  C07D491/08 ,  C07D498/04 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/54

CPC分类号： C07D413/12 ,  A61K31/155 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/54 ,  A61K31/541 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/551 ,  A61K31/635 ,  A61K31/675 ,  A61K45/06 ,  C07D401/14 ,  C07D403/12 ,  C07D413/04 ,  C07D413/14 ,  C07D419/14 ,  C07D451/02 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/08 ,  C07D498/04 ,  C07F9/65583

摘要： Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.

公开(公告)号：EP2387572A2

公开(公告)日：2011-11-23

申请号：EP10732030.1

申请日：2010-01-13

申请人： Rigel Pharmaceuticals, Inc.

发明人： ZHAO, Haoran ,  KOLLURI, Rao ,  VALDEZ, Carlos ,  TSO, Kin ,  SINGH, Rajinder ,  RAMPHAL, John

IPC分类号： C07D413/14 ,  C07D413/12 ,  A61K31/506 ,  A61K31/407 ,  A61P3/00 ,  A61P9/00 ,  A61P29/00

CPC分类号： C07D498/04 ,  A61K31/5383 ,  C07D498/14

摘要： This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

公开(公告)号：EP2387565A2

公开(公告)日：2011-11-23

申请号：EP10732053.3

申请日：2010-01-13

申请人： Rigel Pharmaceuticals, Inc.

发明人： GURURAJA, Tarikere ,  PAYAN, Donald ,  TSO, Kin ,  KINOSHITA, Taisei ,  DING, Rongxian ,  SINGH, Rajinder ,  YUNG, Stephanie ,  LI, Hui ,  MASUDA, Esteban

IPC分类号： C07D239/32 ,  C07D239/30 ,  C07D403/12 ,  A61K31/495 ,  A61P29/00

CPC分类号： C07D451/04

摘要： 2,4-Pyrimidinediamine compounds represented by formula (I), methods for preparing the same and methods for treating an inflammatory disorder and for inhibiting the production of IL-23 and/or stimulating the production of IL-10 using the same are disclosed.

公开(公告)号：EP2382210A2

公开(公告)日：2011-11-02

申请号：EP09837134.7

申请日：2009-12-29

申请人： Rigel Pharmaceuticals, Inc.

发明人： SINGH, Rajinder ,  ATUEGBU, Andy ,  RAMPHAL, John ,  LI, Hui ,  GELMAN, Marina ,  CLOUGH, Jeffrey ,  VALDEZ, Carlos ,  BHAMIDIPATI, Somasekhar ,  THOTA, Sambaiah ,  MCMURTRIE, Darren

IPC分类号： C07D413/14

CPC分类号： A61K31/5383 ,  A61K45/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D487/08 ,  C07D498/04

摘要： The present invention provides pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also provided are pharmaceutical compositions comprising these compounds and methods of treating diseases associated with kinase activity, in particular enhanced PLK1 catalytic activity, such as diseases associated with abnormal cell proliferation, including neoplastic disorders.