公开(公告)号：EP1778718A1

公开(公告)日：2007-05-02

申请号：EP05768304.7

申请日：2005-07-05

申请人： GENENTECH, INC.

发明人： COHEN, Frederick ,  DESHAYES, Kurt ,  FAIRBROTHER, Wayne, J. ,  FENG, Bainian ,  FLYGARE, John ,  GAZZARD, Lewis, J. ,  TSUI, Vickie, Hsiao-Wei

IPC分类号： C07K5/08 ,  A61K38/06 ,  A61P35/00

CPC分类号： C07D417/14 ,  A61K31/55 ,  A61K38/177 ,  C07D403/12 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D495/04 ,  C07D513/04 ,  C07K5/06026 ,  C07K5/0806 ,  C07K5/0827 ,  C07K7/06 ,  C12N5/0693

摘要： The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4’, R5, R5’, R6 and R6’ are as described herein.

公开(公告)号：EP3041474B1

公开(公告)日：2020-03-18

申请号：EP14766355.3

申请日：2014-09-04

申请人： Genentech, Inc. ,  Constellation Pharmaceuticals, Inc.

发明人： ALBRECHT, Brian, K. ,  BELLON, Steven, F. ,  GEHLING, Victor, S. ,  HARMANGE, Jean-Christophe ,  LEBLANC, Yves ,  LIANG, Jun ,  MAGNUSON, Steven, R. ,  TSUI, Vickie, Hsiao-Wei ,  ZHANG, Birong

IPC分类号： A61K31/519 ,  A61P35/00

公开(公告)号：EP1778718B1

公开(公告)日：2014-10-08

申请号：EP05768304.7

申请日：2005-07-05

申请人： Genentech, Inc.

发明人： COHEN, Frederick ,  DESHAYES, Kurt ,  FAIRBROTHER, Wayne, J. ,  FENG, Bainian ,  FLYGARE, John ,  GAZZARD, Lewis, J. ,  TSUI, Vickie, Hsiao-Wei

IPC分类号： C07K5/08 ,  A61K38/06 ,  A61P35/00

CPC分类号： C07D417/14 ,  A61K31/55 ,  A61K38/177 ,  C07D403/12 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D495/04 ,  C07D513/04 ,  C07K5/06026 ,  C07K5/0806 ,  C07K5/0827 ,  C07K7/06 ,  C12N5/0693

公开(公告)号：EP3041474A1

公开(公告)日：2016-07-13

申请号：EP14766355.3

申请日：2014-09-04

申请人： Genentech, Inc. ,  Constellation Pharmaceuticals, Inc.

发明人： ALBRECHT, Brian, K. ,  BELLON, Steven, F. ,  GEHLING, Victor, S. ,  HARMANGE, Jean-Christophe ,  LEBLANC, Yves ,  LIANG, Jun ,  MAGNUSON, Steven, R. ,  TSUI, Vickie, Hsiao-Wei ,  ZHANG, Birong

IPC分类号： A61K31/519 ,  A61P35/00

摘要： The present invention relates to compounds formula (I): and to salts thereof, wherein R1-R4 and A have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of histone demethylases, such as KDM5. Also included are pharmaceutically acceptable compositions comprising the compounds of the present invention and methods of using said compositions in the treatment of various disorders.

公开(公告)号：EP1740173A1

公开(公告)日：2007-01-10

申请号：EP05725976.4

申请日：2005-03-22

申请人： GENENTECH, INC.

发明人： COHEN, Frederick ,  FAIRBROTHER, Wayne ,  FLYGARE, John ,  TSUI, Vickie, Hsiao-Wei ,  KETELTAS, Stephen, Franz

IPC分类号： A61K31/403 ,  C07D203/02 ,  C07D409/12

CPC分类号： C07K5/06026 ,  C07K14/4747

摘要： The invention provides novel inhibitors of IAP that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula (I) in which X1 and X2 are independently O or S; L is a bond or -C(X3)-, -C(X3)NR12, -C(X3)O- wherein X3 is O or S and R12 is H or R1; R1 is alkyl, a carbocycle, carbocycle-substituted alkyl, a heterocycle or heterocycle-substituted alkyl, wherein each is optionally substituted with halogen, hydroxyl, mercapto, carboxyl, alkyl, haloalkyl, alkoxy, alkylsulfonyl, amino, nitro, aryl and heteroaryl; R2 is alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, a heterocycle or heterocyclylalkyl; R3 is H or alkyl; R4 and R4' are independently H, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, or heteroaralkyl wherein each is optionally substituted with halogen, hydroxyl, mercapto, carboxyl, alkyl, alkoxy, amino and nitro; R5, and R5' are each independently H or alkyl; R6 is H or alkyl; and salts and solvates thereof.