公开(公告)号：EP1633707A1

公开(公告)日：2006-03-15

申请号：EP04776527.6

申请日：2004-06-10

申请人： Theravance, Inc.

发明人： MAMMEN, Mathai ,  HUGHES, Adam ,  JI, Yu-Hua ,  LI, Li ,  ZHANG, Weijiang

IPC分类号： C07D207/08 ,  C07D211/34 ,  A61K31/40 ,  A61P11/06

CPC分类号： C07D207/08 ,  A61K31/40 ,  C07D207/09 ,  C07D207/16 ,  C07D211/34

摘要： This invention is directed to compounds of formula (I): wherein R1-R5 and a-e are as defined in the specification; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof. The invention also directed to pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors using such compounds.

公开(公告)号：EP1641744A2

公开(公告)日：2006-04-05

申请号：EP04753431.8

申请日：2004-05-26

申请人： Theravance, Inc.

发明人： STERGIADES, Ioanna ,  YOST, Edward ,  HUBBARD, Cristin ,  ZHANG, Weijiang

IPC分类号： C07C233/43 ,  A61K31/167 ,  A61P11/08

CPC分类号： C07C233/43 ,  C07B2200/13

摘要： The invention provides a novel β2 adrenergic receptor agonist in crystalline salt form. The invention also provides pharmaceutical compositions comprising the novel β2 adrenergic receptor agonist in crystalline salt form, formulations containing the pharmaceutical compositions, methods of using the crystalline salt to treat diseases associated with β2 adrenergic receptor activity, and processes useful for preparing such crystalline compounds.

公开(公告)号：EP2773634A1

公开(公告)日：2014-09-10

申请号：EP12783835.7

申请日：2012-11-02

申请人： Theravance, Inc.

发明人： LONG, Daniel D. ,  MCKINNELL, Robert Murray ,  JIANG, Lan ,  LOO, Mandy ,  LEPACK, Kassandra ,  VAN ORDEN, Lori Jean ,  OGAWA, Gavin ,  HUANG, Xiaojun ,  ZHANG, Weijiang

IPC分类号： C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D491/113 ,  A61K31/4439 ,  A61K31/4433 ,  A61P31/12 ,  A61P31/14

CPC分类号： A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D491/113

摘要： The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.

公开(公告)号：EP2350019B1

公开(公告)日：2013-07-24

申请号：EP09793120.8

申请日：2009-09-29

申请人： Theravance, Inc.

发明人： CHAO, Robert ,  ZHANG, Weijiang

IPC分类号： C07D233/70 ,  A61K31/415 ,  A61P9/12

CPC分类号： C07D233/70

公开(公告)号：EP2350019A1

公开(公告)日：2011-08-03

申请号：EP09793120.8

申请日：2009-09-29

申请人： Theravance, Inc.

发明人： CHAO, Robert ,  ZHANG, Weijiang

IPC分类号： C07D233/70 ,  A61K31/415 ,  A61P9/12

CPC分类号： C07D233/70

摘要： The invention provides a crystalline freebase form of 4'-{2-ethoxy-4-ethyl-5-[((
S )-2-mercapto-4-methylpentanoylamino)methyl]imidazol-1-ylmethyl}-3'-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compound, processes and intermediates for preparing the crystalline compound, and methods of using the crystalline compound to treat diseases such as hypertension.

摘要翻译： 本发明提供了4' - {2-乙氧基-4-乙基-5 - [（（S）-2-巯基-4-甲基戊酰基氨基）甲基]咪唑-1-基甲基} -3'-氟联苯-4-基 - 2-羧酸。 本发明还提供了包含结晶化合物的药物组合物，用于制备结晶化合物的方法和中间体，以及使用该结晶化合物治疗诸如高血压的疾病的方法。

公开(公告)号：EP1532104A1

公开(公告)日：2005-05-25

申请号：EP03771813.7

申请日：2003-07-25

申请人： Theravance, Inc.

发明人： LINSELL, Martin, S. ,  JACOBSEN, John, R. ,  KHOSSRAVI, Davar ,  PABORJI, Mehdi ,  ZHANG, Weijiang

IPC分类号： C07C233/43 ,  A61K31/165 ,  A61P11/00 ,  C07C209/16

CPC分类号： C07C213/04 ,  C07C215/30 ,  C07C233/43

摘要： The invention provides a crystalline salt form of a novel β2 adrenergic receptor agonist. The invention also provides pharmaceutical compositions comprising the crystalline form, formulations containing the pharmaceutical compositions, methods of using the crystalline salt form to treat diseases associated with β2 adrenergic receptor activity, and processes useful for preparing such a crystalline compound.

公开(公告)号：EP2635571A1

公开(公告)日：2013-09-11

申请号：EP11784875.4

申请日：2011-11-03

申请人： Theravance, Inc.

发明人： MCKINNELL, Robert Murray ,  LONG, Daniel D. ,  VAN ORDEN, Lori Jean ,  JIANG, Lan ,  LOO, Mandy ,  SAITO, Daisuke Roland ,  ZIPFEL, Sheila ,  STANGELAND, Eric L. ,  LEPACK, Kassandra ,  OGAWA, Gavin ,  HUANG, Xiaojun ,  ZHANG, Weijiang

IPC分类号： C07D403/14 ,  A61K31/4025 ,  A61K31/12

CPC分类号： C07D401/14 ,  A61K31/496 ,  A61K45/06 ,  C07D403/14

摘要： The invention provides compounds of formula (I) wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.

公开(公告)号：EP2483246A1

公开(公告)日：2012-08-08

申请号：EP10763266.3

申请日：2010-09-28

申请人： Theravance, Inc.

发明人： ZHANG, Weijiang ,  COLSON, Pierre-Jean ,  FASS, Timothy

IPC分类号： C07D233/68 ,  C07D233/70 ,  A61K31/4164 ,  A61P29/00

CPC分类号： C07D233/70 ,  C07D233/68 ,  Y02P20/55

摘要： The invention provides processes for preparing intermediates useful for preparing compounds of the formula (IV), or a salt thereof, where R
1-3 are as defined in the specification.

摘要翻译： 本发明提供了制备用于制备式（IV）化合物或其盐的中间体的方法，其中R 1-3如说明书中所定义。

公开(公告)号：EP1805168A1

公开(公告)日：2007-07-11

申请号：EP05818550.5

申请日：2005-10-27

申请人： Theravance, Inc.

发明人： PETERSON, Matthew John ,  LEE, Junning ,  LEE, Richard J. ,  ZHANG, Weijiang

IPC分类号： C07D401/12

CPC分类号： C07D401/14 ,  C07D401/06

摘要： Processes and intermediates for preparing substituted 4-amino-1-(pyridylmethyl)piperidine and related compounds in high yield and high purity are described. The substituted 4-amino-1-(pyridylmethyl)piperidine and related compounds prepared by the described processes are useful as muscarinic receptor antagonists.

公开(公告)号：EP1680416A2

公开(公告)日：2006-07-19

申请号：EP04817483.3

申请日：2004-10-28

申请人： Theravance, Inc.

发明人： WILSON, Richard, D. ,  CONGDON, Julie ,  MAMMEN, Mathai ,  ZHANG, Weijiang ,  CHAO, Robert

IPC分类号： C07D401/14

CPC分类号： C07C309/35 ,  C07D401/14

摘要： This invention provides naphthalene-1,5-disulfonic acid salts of 4-{N-[7-(3-(S)-1-carbamoyl-1,1-diphenylmethyl)pyrrolidin-1-yl)hept-1-yl]-N-(isopropyl)amino}-1-(4-methoxypyrid-3-ylmethyl)piperidine, which salts are useful as muscarinic receptor antagonists. This invention is also directed to pharmaceutical compositions comprising these salt forms, methods of using these salt forms for treating medical conditions mediated by muscarinic receptors; and processes for preparing these salt forms.