公开(公告)号：EP2049500A1

公开(公告)日：2009-04-22

申请号：EP07799329.3

申请日：2007-07-05

申请人： Array Biopharma, Inc. ,  Genentech, Inc.

发明人： MITCHELL, Ian S. ,  BLAKE, James F. ,  XU, Rui ,  KALLAN, Nicholas C. ,  XIAO, Dengming ,  SPENCER, Keith Lee ,  BENCSIK, Josef R. ,  LIANG, Jun ,  SAFINA, Brian ,  LI, Jun ,  CHABOT, Christine ,  BANKA, Anna.L. ,  WALLACE, Eli. M. ,  SCHLACHTER, Stephen.T.

IPC分类号： C07D239/70 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  A61K31/517 ,  A61P35/00

CPC分类号： C07D409/14 ,  A61K31/517 ,  A61K31/5377 ,  A61K45/06 ,  C07D239/70 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D409/12

摘要： The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Formula (I). Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

公开(公告)号：EP2049500B1

公开(公告)日：2011-09-07

申请号：EP07799329.3

申请日：2007-07-05

申请人： Array Biopharma, Inc. ,  Genentech, Inc.

发明人： MITCHELL, Ian S. ,  BLAKE, James F. ,  XU, Rui ,  KALLAN, Nicholas C. ,  XIAO, Dengming ,  SPENCER, Keith Lee ,  BENCSIK, Josef R. ,  LIANG, Jun ,  SAFINA, Brian ,  LI, Jun ,  CHABOT, Christine ,  BANKA, Anna.L. ,  WALLACE, Eli. M. ,  SCHLACHTER, Stephen.T.

IPC分类号： C07D239/70 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  A61K31/517 ,  A61P35/00

CPC分类号： C07D409/14 ,  A61K31/517 ,  A61K31/5377 ,  A61K45/06 ,  C07D239/70 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D409/12

摘要： The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Formula (I). Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

公开(公告)号：EP3074377B1

公开(公告)日：2018-10-17

申请号：EP14865855.2

申请日：2014-11-26

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

发明人： ANDREZ, Jean-Christophe ,  BICHLER, Paul Robert ,  CHEN, Chien-An ,  CHOWDHURY, Sultan ,  DECKER, Shannon Marie ,  DEHNHARDT, Christoph Martin ,  FOCKEN, Thilo ,  GRIMWOOD, Michael Edward ,  HEMEON, Ivan William ,  JIA, Qi ,  LI, Jun ,  LIU, Zhiguo ,  ORTWINE, Daniel F. ,  SAFINA, Brian ,  SUTHERLIN, Daniel ,  SHENG, Tao ,  SUN, Shaoyi ,  WHITE, Andrew D. ,  WILSON, Michael Scott ,  ZENOVA, Alla Yurevna ,  ZHU, Jiuxiang

IPC分类号： C07D211/42 ,  C07D211/22

CPC分类号： A61K31/445 ,  A61K31/337 ,  A61K31/397 ,  A61K31/4015 ,  A61K31/415 ,  A61K31/4412 ,  A61K31/4523 ,  A61K31/4545 ,  A61K31/495 ,  C07D205/04 ,  C07D205/12 ,  C07D207/12 ,  C07D211/22 ,  C07D211/32 ,  C07D211/42 ,  C07D211/54 ,  C07D211/60 ,  C07D211/96 ,  C07D233/68 ,  C07D237/08 ,  C07D241/04 ,  C07D265/30 ,  C07D295/155 ,  C07D295/26 ,  C07D305/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07D417/06 ,  C07D451/02 ,  C07D451/06 ,  C07D453/02 ,  C07D487/08 ,  C07F7/0812

摘要： The invention provides compounds having the general formula I: and pharmaceutically acceptable salts thereof, wherein the variables RA, RAA, subscript n, ring A, X2, L, subscript m, X1, R1, R2, R3, R4, R5, and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compactions.

公开(公告)号：EP3074377A1

公开(公告)日：2016-10-05

申请号：EP14865855.2

申请日：2014-11-26

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

发明人： ANDREZ, Jean-Christophe ,  BICHLER, Paul Robert ,  CHEN, Chien-An ,  CHOWDHURY, Sultan ,  DECKER, Shannon Marie ,  DEHNHARDT, Christoph Martin ,  FOCKEN, Thilo ,  GRIMWOOD, Michael Edward ,  HEMEON, Ivan William ,  JIA, Qi ,  LI, Jun ,  LIU, Zhiguo ,  ORTWINE, Daniel F. ,  SAFINA, Brian ,  SUTHERLIN, Daniel ,  SHENG, Tao ,  SUN, Shaoyi ,  WHITE, Andrew D. ,  WILSON, Michael Scott ,  ZENOVA, Alla Yurevna ,  ZHU, Jiuxiang

IPC分类号： C07D205/04 ,  C07D207/12 ,  C07D211/42 ,  C07D233/68 ,  C07D237/08 ,  C07D241/04 ,  C07D305/08 ,  A61K31/337 ,  A61K31/397 ,  A61K31/415 ,  A61K31/4412 ,  A61K31/495 ,  A61K31/4015 ,  A61P25/04

CPC分类号： A61K31/445 ,  A61K31/337 ,  A61K31/397 ,  A61K31/4015 ,  A61K31/415 ,  A61K31/4412 ,  A61K31/4523 ,  A61K31/4545 ,  A61K31/495 ,  C07D205/04 ,  C07D207/12 ,  C07D211/22 ,  C07D211/32 ,  C07D211/42 ,  C07D211/54 ,  C07D211/60 ,  C07D233/68 ,  C07D237/08 ,  C07D241/04 ,  C07D265/30 ,  C07D305/08 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D453/02 ,  C07D487/08 ,  C07F7/0812

摘要： The invention provides compounds having the general formula I: and pharmaceutically acceptable salts thereof, wherein the variables RA, RAA, subscript n, ring A, X2, L, subscript m, X1, R1, R2, R3, R4, R5, and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compactions.

摘要翻译： 其中变量RA，RAA，亚基n，环A，X2，L，下标m，X1，R1，R2，R3，R4，R5和RN具有本文所述的含义， 化合物和使用这些化合物和组合物的方法。

公开(公告)号：EP2855428A1

公开(公告)日：2015-04-08

申请号：EP13726976.7

申请日：2013-05-21

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

发明人： ANDREZ, Jean-Christophe ,  CHOWDHURY, Sultan ,  DECKER, Shannon ,  DEHNHARDT, Christoph, Martin ,  FOCKEN, Thilo ,  GRIMWOOD, Michael, Edward ,  HEMEON, Ivan, William ,  JIA, Qi ,  LI, Jun ,  ORTWINE, Daniel, F. ,  SAFINA, Brian ,  SHENG, Tao ,  SUN, Shaoyi ,  SUTHERLIN, Daniel, P. ,  WILSON, Michael, Scott ,  ZENOVA, Alla, Yurevna

IPC分类号： C07C311/51 ,  C07D207/08 ,  C07D213/82 ,  C07D307/12 ,  A61K31/44 ,  A61K31/445 ,  A61K31/18 ,  A61P25/04

CPC分类号： C07D491/107 ,  A61K31/18 ,  A61K31/397 ,  A61K31/40 ,  A61K31/41 ,  A61K31/4164 ,  A61K31/44 ,  A61K31/5375 ,  C07B2200/05 ,  C07C307/06 ,  C07C311/51 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2601/18 ,  C07C2602/10 ,  C07C2602/18 ,  C07C2602/20 ,  C07C2602/42 ,  C07C2602/44 ,  C07C2602/50 ,  C07C2603/66 ,  C07C2603/68 ,  C07C2603/74 ,  C07D205/04 ,  C07D207/46 ,  C07D207/48 ,  C07D209/52 ,  C07D211/22 ,  C07D211/96 ,  C07D213/64 ,  C07D213/82 ,  C07D233/84 ,  C07D257/04 ,  C07D265/30 ,  C07D295/192 ,  C07D295/26 ,  C07D307/12 ,  C07D307/18 ,  C07D309/08 ,  C07D311/58 ,  C07D311/70 ,  C07D311/72 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D451/02 ,  C07D471/08

摘要： The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

摘要翻译： 本发明提供具有以下通式的新化合物及其药学上可接受的盐，其中变量RA，下标n，环A，X2，L，下标m，X1，B，R1，R2，R3，R4，R5和RN具有 本文所述的含义，以及含有这些化合物的组合物和使用这些化合物和组合物的方法。

公开(公告)号：EP3450428A1

公开(公告)日：2019-03-06

申请号：EP18197734.9

申请日：2014-11-26

申请人： GENENTECH, INC. ,  Xenon Pharmaceuticals Inc.

发明人： ANDREZ, Jean-Christophe ,  BICHLER, Paul Robert ,  CHEN, Chien-An ,  CHOWDHURY, Sultan ,  DECKER, Shannon Marie ,  DEHNHARDT, Christoph Martin ,  FOCKEN, Thilo ,  GRIMWOOD, Michael Edward ,  HEMEON, Ivan William ,  JIA, Qi ,  LI, Jun ,  LIU, Zhiguo ,  ORTWINE, Daniel F. ,  SAFINA, Brian ,  SUTHERLIN, Daniel ,  SHENG, Tao ,  SUN, Shaoyi ,  WHITE, Andrew D. ,  WILSON, Michael Scott ,  ZENOVA, Alla Yurevna ,  ZHU, Jiuxiang

IPC分类号： C07D401/04 ,  C07D405/04 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07D417/06 ,  C07D451/02 ,  C07D451/06 ,  C07D205/12 ,  C07D295/155 ,  C07D211/96 ,  C07D295/26

摘要： The invention provides compounds having the general formula I:

and pharmaceutically acceptable salts thereof, wherein the variables R A , R AA , subscript n, ring A, X 2 , L, subscript m, X 1 , R 1 , R 2 , R 3 , R 4 , R 5 , and R N have the meaning as described herein; compositions containing such compounds; and such compounds and compositions for use in methods of treatment.

公开(公告)号：EP3297989A1

公开(公告)日：2018-03-28

申请号：EP16728782.0

申请日：2016-05-20

申请人： GENENTECH, INC. ,  Xenon Pharmaceuticals Inc.

发明人： CHOWDHURY, Sultan ,  DEHNHARDT, Christoph Martin ,  HASAN, Abid ,  HEMEON, Ivan William ,  JIA, Qi ,  LI, Jun ,  LIU, Zhiguo ,  ORTWINE, Daniel F. ,  SAFINA, Brian ,  SUTHERLIN, Daniel ,  SUN, Shaoyi ,  WHITE, Andrew D. ,  GONG, Wei ,  ZENOVA, Alla Yurevna ,  ZHU, Jiuxiang

IPC分类号： C07D211/22 ,  C07D211/38 ,  C07D211/48 ,  C07D211/62 ,  A61K31/445 ,  A61P25/00

CPC分类号： C07D211/22 ,  C07D211/34 ,  C07D211/38 ,  C07D211/42 ,  C07D211/48 ,  C07D211/62 ,  C07D221/20 ,  C07D401/04 ,  C07D401/08 ,  C07D401/12 ,  C07D405/08

摘要： The invention provides compounds having activity as sodium channel (e.g., NaV1.7) inhibitors that are useful for treating sodium channel-mediated diseases or conditions, such as pain, as well as other diseases and conditions associated with the mediation of sodium channels, and compositions containing such compounds and methods for using such compounds and compositions.