公开(公告)号：EP1575950A1

公开(公告)日：2005-09-21

申请号：EP03789283.3

申请日：2003-12-15

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： DENHOLM, Alastair ,  KELLER, Thomas, Hugo ,  MCCARTHY, Clive ,  PRESS, Neil, John ,  TAYLOR, Roger, John

IPC分类号： C07D471/04 ,  A61K31/4375 ,  A61P29/00

CPC分类号： C07D471/04

摘要： Compounds of Formula (I) in free or salt form, wherein R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by of phosphodiesterase type 4 or the down-regulation or inhibition of TNF-α release, particularly obstructive or inflammatory airways diseases. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

公开(公告)号：EP1805181B1

公开(公告)日：2012-08-29

申请号：EP05797944.5

申请日：2005-10-21

申请人： Novartis AG

发明人： FAIRHURST, Robin, Alec ,  TAYLOR, Roger, John ,  SINGH, Paul

IPC分类号： C07D473/16 ,  C07D473/32 ,  C07D473/40 ,  A61K31/52 ,  A61P29/00

CPC分类号： C07D473/32 ,  C07D473/16 ,  C07D473/40

公开(公告)号：EP2132186A1

公开(公告)日：2009-12-16

申请号：EP08717374.6

申请日：2008-03-04

申请人： Novartis AG

发明人： TAYLOR, Roger, John

IPC分类号： C07D239/54 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12 ,  C07D495/04 ,  A61K31/517 ,  A61P11/00 ,  A61P37/00

CPC分类号： C07D495/14 ,  C07D215/36 ,  C07D239/54 ,  C07D239/80 ,  C07D239/96 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12 ,  C07D471/04 ,  C07D495/04

摘要： A compound of formula (I): in free or salt form, wherein A, R1, R3, Qa, Qb and Q are as defined herein, for the treatment of a disease mediated by the S1P2 or S1P3 receptor, such as inflammatory or obstructive airways disease.

公开(公告)号：EP2018382A2

公开(公告)日：2009-01-28

申请号：EP07724369.9

申请日：2007-04-19

申请人： NOVARTIS AG

发明人： FAIRHURST, Robin, Alec ,  TAYLOR, Roger, John

IPC分类号： C07D473/16 ,  C07D473/34 ,  A61K31/522 ,  A61P29/00

CPC分类号： C07D473/16 ,  C07D473/34

摘要： A compound of formula (I) and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.

公开(公告)号：EP2755652A1

公开(公告)日：2014-07-23

申请号：EP12783311.9

申请日：2012-09-14

申请人： Novartis AG

发明人： BALA, Kamlesh, Jagdis ,  BUDD, Emma ,  EDWARDS, Lee ,  HOWSHAM, Catherine ,  LEGRAND, Darren, Mark ,  TAYLOR, Roger, John

IPC分类号： A61K31/415 ,  A61K31/4439 ,  A61K31/497 ,  A61P11/06

CPC分类号： C07D487/04 ,  A61K31/415 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/5377 ,  A61K45/06 ,  C07D231/40 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/14

摘要： A compound of Formula I and pharmaceutically acceptable salts and solvates thereof, wherein R
1 , R
2 , R
3 , R
a , A, B, D and E are all as defined herein. The compounds modulate the activity of CFTR and are useful in the treatment of inflammatory or obstructive airways diseases or mucosal hydration, including, for example cystic fibrosis. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

摘要翻译： 式I的化合物及其药学上可接受的盐和溶剂化物，其中R1，R2，R3，Ra，A，B，D和E全部如本文所定义。 该化合物调节CFTR的活性，并且可用于治疗炎性或阻塞性气道疾病或粘膜水合，包括例如囊性纤维化。 还描述了含有化合物的药物组合物和用于制备化合物的方法。

公开(公告)号：EP2044070B1

公开(公告)日：2012-08-22

申请号：EP07765174.3

申请日：2007-07-11

申请人： Novartis AG

发明人： FAIRHURST, Robin, Alec ,  TAYLOR, Roger, John

IPC分类号： C07D473/16 ,  C07H19/167 ,  A61K31/52 ,  A61P11/00

CPC分类号： C07D473/16

摘要： Compounds of formula (I):or stereoisomers or pharmaceutically acceptable salts thereof, wherein W, R1,R 2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.

公开(公告)号：EP1529038A1

公开(公告)日：2005-05-11

申请号：EP03787754.5

申请日：2003-08-08

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： CUENOUD, Bernard ,  FAIRHURST, Robin, Alec ,  TAYLOR, Roger, John

IPC分类号： C07D277/68 ,  C07D417/12 ,  A61K31/428 ,  A61P29/00

CPC分类号： C07D417/12 ,  A61K31/428 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D277/68

摘要： Compounds of Formula (I) in free or salt or solvate form, wherein X has the meaning indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the ß2-adrenoreceptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

公开(公告)号：EP2013211B1

公开(公告)日：2012-03-14

申请号：EP07724372.3

申请日：2007-04-19

申请人： Novartis AG

发明人： FAIRHURST, Robin, Alec ,  TAYLOR, Roger, John ,  COX, Brian

IPC分类号： C07D473/16 ,  C07D473/18 ,  C07D473/34 ,  C07H19/167 ,  A61P29/00 ,  A61K31/52 ,  A61K31/7076

CPC分类号： C07D473/16 ,  C07D473/34

摘要： Purine derivatives of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are as defined herein. The compounds are useful for the treatment of a condition mediated by activation of the adenosine A2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions comprising a purine derivative as active ingredient and a process for the preparation of these compounds.

公开(公告)号：EP1529038B1

公开(公告)日：2009-10-07

申请号：EP03787754.5

申请日：2003-08-08

申请人： NOVARTIS AG ,  Novartis Pharma GmbH

发明人： CUENOUD, Bernard ,  FAIRHURST, Robin, Alec ,  TAYLOR, Roger, John

IPC分类号： C07D277/68 ,  C07D417/12 ,  A61K31/428 ,  A61P29/00

CPC分类号： C07D417/12 ,  A61K31/428 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D277/68

摘要： Compounds of Formula (I) in free or salt or solvate form, wherein X has the meaning indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the ß2-adrenoreceptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

公开(公告)号：EP2013199A1

公开(公告)日：2009-01-14

申请号：EP07845239.8

申请日：2007-04-19

申请人： NOVARTIS AG

发明人： FAIRHURST, Robin, Alec ,  TAYLOR, Roger, John

IPC分类号： C07D403/08 ,  C07D473/00 ,  A61K31/52

CPC分类号： C07D473/34 ,  C07D473/40

摘要： A compound of formula (I) and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.