公开(公告)号：EP2445903A1

公开(公告)日：2012-05-02

申请号：EP10730132.7

申请日：2010-06-24

申请人： Novartis AG

发明人： BOCK, Mark G. ,  GAUL, Christoph ,  GUMMADI, Venkateshwar Rao ,  SENGUPTA, Saumitra

IPC分类号： C07D403/04 ,  C07D403/14 ,  C07D407/14 ,  C07D409/14 ,  C07D417/14 ,  A61K31/4178 ,  A61P35/00

CPC分类号： A61K31/4439 ,  A61K31/444 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

摘要： The present invention provides compounds of Formula (I) and (II), or a pharmaceutically acceptable salts thereof, where R
53 , R
54 , p, q and n are as defined herein. The compounds of the present invention have been found to be useful as 17α-hydroxylase/C
17,20 -lyase inhibitors.

公开(公告)号：EP2598486A1

公开(公告)日：2013-06-05

申请号：EP11741554.7

申请日：2011-07-27

申请人： Novartis AG

发明人： BARNES, David, Weninger ,  BEBERNITZ, Gregory, Raymond ,  CLAIRMONT, Kevin ,  COHEN, Scott, Louis ,  DAMON, Robert, Edson, II. ,  DAY, Robert, Francis ,  DODD, Stephanie, Kay ,  GAUL, Christoph ,  GULGEZE EFTHYMIOU, Hatice, Belgin ,  JAIN, Monish ,  KARKI, Rajeshri Ganesh ,  KIRMAN, Louise, Clare ,  LIN, Kai ,  MAO, Justin Yik Ching ,  PATEL, Tajesh Jayprakash ,  RAYMER, Brian, Kenneth ,  SU, Liansheng

IPC分类号： C07D215/36 ,  C07D235/18 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04 ,  C07D413/12 ,  C07D471/04 ,  C07D513/04 ,  C07D263/57 ,  A61K31/404 ,  A61K31/4184

CPC分类号： A61K31/542 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0095 ,  A61K9/08 ,  A61K9/1075 ,  A61K31/404 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D209/24 ,  C07D215/36 ,  C07D235/08 ,  C07D235/12 ,  C07D235/16 ,  C07D235/18 ,  C07D235/30 ,  C07D263/57 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D413/12 ,  C07D471/04 ,  C07D513/04 ,  C12N9/93 ,  C12Y604/01002

摘要： The present invention provides compounds of formula (I); or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing the compounds of formula (I), their therapeutic uses, combinations with other of pharmacologically active agents, and a pharmaceutical compositions.

摘要翻译： 本发明提供式（I）化合物; 或其药学上可接受的盐，其中变量如本文所定义。 本发明提供了制备式（I）化合物，其治疗用途，与其他药理活性剂的组合以及药物组合物的方法。

公开(公告)号：EP2155201B1

公开(公告)日：2012-08-01

申请号：EP08760632.3

申请日：2008-06-06

申请人： Novartis AG

发明人： GERSPACHER, Marc ,  FURET, Pascal ,  VANGREVELINGHE, Eric ,  PISSOT SOLDERMANN, Carole ,  GAUL, Christoph ,  HOLZER, Philipp

IPC分类号： A61K31/498 ,  A61K31/5377 ,  A61K31/541 ,  C07D241/42 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  A61P35/00 ,  A61P35/02 ,  A61P21/00 ,  A61P17/06 ,  A61P17/00 ,  A61P19/02

CPC分类号： A61K31/498 ,  A61K31/5377 ,  A61K31/541 ,  C07D241/42 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14

摘要： The present invention relates to quinoxaline compound of the formula (I): wherein R1 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R; R2 is caryl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R8 R3, R4, and R5 are each independently hydrogen or R9; R6 is hydrogen; and R7, R8 and R9 are each independently selected from organic and inorganic substituents, their use in therapy of diseases, in particular diseases mediated by the tyrosine kinase activity of Janus kinases, including JAK-2 and JAK-3 kinases.

公开(公告)号：EP2247591A1

公开(公告)日：2010-11-10

申请号：EP09708802.5

申请日：2009-02-04

申请人： Novartis AG

发明人： GAUL, Christoph ,  GERSPACHER, Marc ,  HOLZER, Philipp ,  PISSOT SOLDERMANN, Carole

IPC分类号： C07D487/04 ,  A61K31/519

CPC分类号： C07D487/04

摘要： The invention relates to compounds of formula (I) and salts thereof formula (I), wherein the substituens are as defined in the specification, processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases.

公开(公告)号：EP2144909A1

公开(公告)日：2010-01-20

申请号：EP08735845.3

申请日：2008-04-04

申请人： Novartis AG

发明人： DOBLER, Markus Rolf ,  JEWELL, JR., Charles Francis ,  MEREDITH, Erik ,  MONOVICH, Lauren G. ,  SISKA, Sarah ,  VON MATT, Anette ,  VAN EIS, Maurice ,  YOON, Taeyoung ,  GAUL, Christoph ,  CAPPARELLI, Michael Paul

IPC分类号： C07D471/04 ,  C07D519/00 ,  A61K31/4375 ,  A61P35/00

CPC分类号： C07D471/04

摘要： The present invention provides a compound of formula I: (formula I) said compound is inhibitor of selective subset of kinases belonging to the AGC or calmodulin kinase family, such as for example MARK1/2/3, PKD-1/2/3, PKN-1/2, CDK-9, CaMKII, ROCK-I/II, inhibitors of histone deacetylase (HDAC) phosphorylation, or inhibitors of other kinases. Finally, the present invention also provides a pharmaceutical composition.

公开(公告)号：EP2144908A1

公开(公告)日：2010-01-20

申请号：EP08735844.6

申请日：2008-04-04

申请人： Novartis AG

发明人： VAN EIS, Maurice ,  SCHULER, Walter ,  VON MATT, Anette ,  SOLDERMANN, Nicolas ,  MONOVICH, Lauren G. ,  GAUL, Christoph

IPC分类号： C07D471/04 ,  A61K31/4745

CPC分类号： C07D471/04

摘要： The present invention relates to novel organic compounds comprising a naphthyridine which may be mediators of a selective subset of kinases belonging to the AGC kinase family, such as for example PKC, PKD, PKN-1/2, CDK-9, MRCK-beat, PASK, PRKX, ROCK-I/II or mediators of other kinases, the selectivity of which would be depending on the structural variation thereof.

公开(公告)号：EP2445903B1

公开(公告)日：2014-03-26

申请号：EP10730132.7

申请日：2010-06-24

申请人： Novartis AG

发明人： BOCK, Mark G. ,  GAUL, Christoph ,  GUMMADI, Venkateshwar Rao ,  SENGUPTA, Saumitra

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D417/14 ,  C07D409/14 ,  C07D407/14 ,  C07D413/14 ,  C07D405/14 ,  A61K31/4178 ,  A61P35/00

CPC分类号： A61K31/4439 ,  A61K31/444 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

公开(公告)号：EP2702052A1

公开(公告)日：2014-03-05

申请号：EP12718554.4

申请日：2012-04-27

申请人： Novartis AG

发明人： BOCK, Mark Gary ,  GAUL, Christoph ,  GUMMADI, Venkateshwar Rao ,  SENGUPTA, Saumitra

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D409/14 ,  A61K31/444 ,  A61K31/4436 ,  A61K31/506 ,  A61K31/4439 ,  A61P35/00

CPC分类号： A61K31/506 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

摘要： The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R
1 , R
2 , R
3 , R
4 , R
5 and R
6 are as defined herein. The compounds of the present invention have been found to be useful as 17α-hydroxylase/C
17,20 -lyase inhibitors.

摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5和R 6如本文所定义。 已经发现本发明的化合物可用作17α-羟化酶/ C17,20-裂解酶抑制剂。

公开(公告)号：EP2155201A2

公开(公告)日：2010-02-24

申请号：EP08760632.3

申请日：2008-06-06

申请人： Novartis AG

发明人： GERSPACHER, Marc ,  FURET, Pascal ,  VANGREVELINGHE, Eric ,  PISSOT SOLDERMANN, Carole ,  GAUL, Christoph ,  HOLZER, Philipp

IPC分类号： A61K31/498 ,  A61K31/5377 ,  A61K31/541 ,  C07D241/42 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  A61P35/00 ,  A61P35/02 ,  A61P21/00 ,  A61P17/06 ,  A61P17/00 ,  A61P19/02

CPC分类号： A61K31/498 ,  A61K31/5377 ,  A61K31/541 ,  C07D241/42 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14

摘要： The present invention relates to quinoxaline compound of the formula (I): wherein R1 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R; R2 is caryl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R8 R3, R4, and R5 are each independently hydrogen or R9; R6 is hydrogen; and R7, R8 and R9 are each independently selected from organic and inorganic substituents, their use in therapy of diseases, in particular diseases mediated by the tyrosine kinase activity of Janus kinases, including JAK-2 and JAK-3 kinases.

公开(公告)号：EP2089393A1

公开(公告)日：2009-08-19

申请号：EP07819423.0

申请日：2007-10-29

申请人： NOVARTIS AG

发明人： FERRAND, Sandrine ,  GLICKMAN, Fraser ,  LEBLANC, Catherine ,  RITCHIE, Cathy ,  SHAW, Duncan ,  STIEFL, Nikolaus Johannes ,  FURET, Pascal ,  IMBACH, Patricia ,  STAUFFER, Frédéric ,  CAPRARO, Hans-Georg ,  GESSIER, François ,  GAUL, Christoph ,  ALBAUGH, Pamela A. ,  CHOPIUK, Greg

IPC分类号： C07D487/04 ,  A61K31/5025 ,  A61P9/00 ,  A61P19/00 ,  A61P25/00

CPC分类号： C07D487/04

摘要： A compound of Formula Ia or Ib in free or salt or solvate form, where R1, R2, R3, R4, R5 R20, R24, R25, X, Y and Z have the meanings as indicated in the specification, are useful for treating diseases mediated by the ALK-5 and/or ALK-4 receptor. These compounds are also useful for treating diseases mediated by the Pi3k receptor, the JAK-2 receptor and the TRK receptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.