公开(公告)号：EP2283009B1

公开(公告)日：2012-08-29

申请号：EP09745673.5

申请日：2009-05-06

申请人： F. Hoffmann-La Roche AG

发明人： ARZENO, Humberto Bartolome ,  DUNN, James Patrick ,  GOLDSTEIN, David Michael ,  GONG, Leyi ,  HAN, Xiaochun ,  HOGG, Joan Heather ,  JAHANGIR, Alam ,  PALMER, Wylie Solang ,  REUTER, Deborah Carol ,  SILVA, Tania ,  TIVITMAHAISOON, Parcharee ,  TREJO-MARTIN, Teresa Alejandra ,  WU, Shao-Yong

IPC分类号： C07D401/14 ,  A61K31/506 ,  A61P29/00

CPC分类号： C07D401/14

公开(公告)号：EP2283009A1

公开(公告)日：2011-02-16

申请号：EP09745673.5

申请日：2009-05-06

申请人： F. Hoffmann-La Roche AG

发明人： ARZENO, Humberto Bartolome ,  DUNN, James Patrick ,  GOLDSTEIN, David Michael ,  GONG, Leyi ,  HAN, Xiaochun ,  HOGG, Joan Heather ,  JAHANGIR, Alam ,  PALMER, Wylie Solang ,  REUTER, Deborah Carol ,  SILVA, Tania ,  TIVITMAHAISOON, Parcharee ,  TREJO-MARTIN, Teresa Alejandra ,  WU, Shao-Yong

IPC分类号： C07D401/14 ,  A61K31/506 ,  A61P29/00

CPC分类号： C07D401/14

摘要： The invention relates to prodrugs of JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses prodrugs of JNK inhibitors, as described below in formula (I), wherein m, n, p, q, Q, r, R
1 , R
2 , R
3 , X, X
1 , X
2 , X
3 , X
4 , X
5 , Y
1 , Y
2 , Z
1 , and Z
2 are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.

公开(公告)号：EP2872490B1

公开(公告)日：2018-02-07

申请号：EP13736570.6

申请日：2013-07-11

申请人： F. Hoffmann-La Roche AG

发明人： HAN, Xiaochun ,  LOU, Yan ,  MICHOUD, Christophe ,  MISCHKE, Steven Gregory ,  REMISZEWSKI, Stacy ,  RUPERT, Kenneth Carey

IPC分类号： C07D223/16 ,  C07D401/06 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D405/10 ,  C07D405/12 ,  C07D409/06 ,  C07D413/06 ,  C07D413/10 ,  C07D417/06 ,  C07D417/10 ,  C07D471/04 ,  A61K31/55 ,  A61P35/00

CPC分类号： C07D223/16 ,  C07D401/06 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D405/10 ,  C07D405/12 ,  C07D409/06 ,  C07D413/06 ,  C07D413/10 ,  C07D417/06 ,  C07D417/10 ,  C07D471/04

摘要： Disclosed are compounds of Formula (I) or pharmaceutically acceptable salts thereof, wherein W, X, Y, Z, R1, R2, R3 and R4 are described in this application, and methods of using said compounds in the treatment of cancer.

公开(公告)号：EP2280969A1

公开(公告)日：2011-02-09

申请号：EP09738024.0

申请日：2009-04-20

申请人： F. Hoffmann-La Roche AG

发明人： BROOKFIELD, Frederick ,  DILLON, Michael, Patrick ,  EUSTACHE, Florence ,  GOLDSTEIN, David, Michael ,  GONG, Leyi ,  HAN, Xiaochun ,  HOGG, Joan, Heather ,  PARK, Jaehyeon ,  REUTER, Deborah, Carol ,  SJOGREN, Eric, Brian

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： This application discloses novel pyrimidinyl pyridone derivatives according to formula (I), wherein A, R
1 , R
2 , R
3 , and m are defined as described herein, which inhibit JNK. The compounds disclosed herein are useful to modulate the activity of JNK and treat diseases associated with excessive JNK activity. The compounds are useful to treat autoimmune, inflammatory, metabolic, and neurological diseases as well as cancer. Also disclosed are compositions comprising the compound of formula (I) and methods of treatment comprising administering a therapeutically effective amount of the compound of formula I to a subject in need thereof.

摘要翻译： 该申请公开了根据式（I）的新型嘧啶基吡啶酮衍生物，其中A，R 1，R 2，R 3和m如本文所述定义，其抑制JNK。 本文公开的化合物可用于调节JNK的活性并治疗与过量的JNK活性相关的疾病。 该化合物可用于治疗自身免疫疾病，炎症，代谢疾病和神经疾病以及癌症。 还公开了包含式（I）化合物的组合物和治疗方法，其包括将治疗有效量的式I化合物给予有需要的受试者。