公开(公告)号：EP2132187A2

公开(公告)日：2009-12-16

申请号：EP08725019.7

申请日：2008-01-31

申请人： Theravance, Inc.

发明人： CHOI, Seok-ki ,  FATHEREE, Paul R. ,  HEGDE, Sharath ,  HUDSON, Ryan ,  JENDZA, Keith ,  MARQUESS, Daniel ,  MCKINNELL, Robert Murray ,  SASIKUMAR, Vivek

IPC分类号： C07D257/04 ,  C07C323/41 ,  C07C323/60 ,  C07C259/06 ,  A61K31/41 ,  A61K31/195 ,  A61K31/18 ,  A61P9/12

CPC分类号： C07C237/20 ,  C07C243/32 ,  C07C319/12 ,  C07C323/22 ,  C07C323/41 ,  C07C323/60 ,  C07C2601/14 ,  C07D257/04

摘要： The invention is directed to compounds of formula (I): wherein Ar, r, R3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula (I) have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.

摘要翻译： 本发明涉及式I化合物：其中Ar，r，R 3，X和R 5-7如说明书中所定义，及其药学上可接受的盐。 式I化合物具有AT1受体拮抗剂活性和去甲普林抑制活性。 本发明还涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。

公开(公告)号：EP2162442B1

公开(公告)日：2012-12-19

申请号：EP08768064.1

申请日：2008-06-04

申请人： Theravance, Inc.

发明人： ALLEGRETTI, Paul ,  CHOI, Seok-Ki ,  FATHEREE, Paul, R. ,  GENDRON, Roland ,  HUDSON, Ryan ,  JENDZA, Keith ,  MCKINNELL, Robert, Murray ,  MCMURTRIE, Darren ,  OLSON, Brooke

IPC分类号： C07D235/08 ,  C07D401/12 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  A61P9/12 ,  A61K31/4184 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/496 ,  A61K31/5377

CPC分类号： A61K31/4184 ,  A61K31/4439 ,  A61K31/5377 ,  A61K45/06 ,  C07D235/08 ,  C07D401/12 ,  C07D403/10 ,  C07D403/12 ,  C07D405/10 ,  C07D405/12

公开(公告)号：EP2146963A2

公开(公告)日：2010-01-27

申请号：EP08743204.3

申请日：2008-04-23

申请人： Theravance, Inc.

发明人： ALLEGRETTI, Paul ,  CHOI, Seok-ki ,  GENDRON, Roland ,  FATHEREE, Paul R. ,  JENDZA, Keith ,  MCKINNELL, Robert Murray ,  MCMURTRIE, Darren ,  OLSON, Brooke

IPC分类号： C07D213/64 ,  C07D233/64 ,  C07D233/68 ,  C07D233/70 ,  C07D401/10 ,  C07D401/12 ,  C07D409/06 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/4412 ,  A61P9/00

CPC分类号： C07D233/70 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/417 ,  A61K31/4188 ,  A61K31/4196 ,  A61K31/4412 ,  A61K45/00 ,  A61K45/06 ,  C07D207/36 ,  C07D207/46 ,  C07D213/64 ,  C07D213/89 ,  C07D231/14 ,  C07D233/64 ,  C07D233/68 ,  C07D233/90 ,  C07D249/08 ,  C07D255/02 ,  C07D401/12 ,  C07D403/10 ,  C07D513/04 ,  C07D513/14

摘要： The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

公开(公告)号：EP2162442A1

公开(公告)日：2010-03-17

申请号：EP08768064.1

申请日：2008-06-04

申请人： Theravance, Inc.

发明人： ALLEGRETTI, Paul ,  CHOI, Seok-Ki ,  FATHEREE, Paul, R. ,  GENDRON, Roland ,  HUDSON, Ryan ,  JENDZA, Keith ,  MCKINNELL, Robert, Murray ,  MCMURTRIE, Darren ,  OLSON, Brooke

IPC分类号： C07D235/08 ,  C07D401/12 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  A61P9/12 ,  A61K31/4184 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/496 ,  A61K31/5377

CPC分类号： A61K31/4184 ,  A61K31/4439 ,  A61K31/5377 ,  A61K45/06 ,  C07D235/08 ,  C07D401/12 ,  C07D403/10 ,  C07D403/12 ,  C07D405/10 ,  C07D405/12

摘要： The invention is directed to compounds having the formula: (I) wherein: Ar, r, n, X, R2-3 and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.