公开(公告)号：EP1687257B1

公开(公告)日：2009-04-15

申请号：EP04784634.0

申请日：2004-09-21

申请人： Theravance, Inc.

发明人： LINSELL, Martin, S. ,  JACOBSEN, John, R. ,  SAITO, Daisuke, Roland

IPC分类号： C07C233/43 ,  C07D215/24 ,  A61K31/167 ,  A61K31/4704 ,  A61P11/08

CPC分类号： C07C233/43 ,  C07D215/26 ,  C07D215/38

摘要： The invention provides novel β2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with β2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.

公开(公告)号：EP1276759B1

公开(公告)日：2008-07-30

申请号：EP01930978.0

申请日：2001-05-01

申请人： Theravance, Inc.

发明人： LINSELL, Martin, S.

IPC分类号： C07K9/00

CPC分类号： B82Y5/00 ,  A61K9/0014 ,  A61K9/0019 ,  A61K38/00 ,  A61K47/40 ,  C07K9/008

摘要： The invention provides a novel reductive alkylation method useful for selectively alkylating saccharide-amines of glycopeptide antibiotics.

公开(公告)号：EP1899324A2

公开(公告)日：2008-03-19

申请号：EP06760341.5

申请日：2006-05-24

申请人： Theravance, Inc.

发明人： MCKINNELL, Robert, Murray ,  GENDRON, Roland ,  JIANG, Lan ,  CHOI, Seok-ki ,  LONG, Daniel, D. ,  FATHEREE, Paul, R. ,  MARQUESS, Daniel ,  DALZIEL, Sean, M. ,  PHIZACKERLEY, Kirsten, M.

IPC分类号： C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  A61K31/4545 ,  A61P1/00

CPC分类号： C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  G01N33/5058

摘要： The invention relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.

公开(公告)号：EP1644382B1

公开(公告)日：2008-03-05

申请号：EP04778030.9

申请日：2004-07-09

申请人： Theravance, Inc.

发明人： FATHEREE, Paul, R. ,  LINSELL, Martin S. ,  MARQUESS, Daniel ,  TRAPP, Sean, G. ,  MORAN, Edmund, J. ,  AGGEN, James B.

IPC分类号： C07D501/00 ,  C07K9/00 ,  A61K31/545 ,  A61P31/04

CPC分类号： C07K7/64 ,  C07D501/00 ,  C07K9/008

公开(公告)号：EP1856049A1

公开(公告)日：2007-11-21

申请号：EP06737554.3

申请日：2006-03-09

申请人： Theravance, Inc.

发明人： JI, Yu-Hua ,  HUSFELD, Craig ,  MAMMEN, Mathai ,  MU, YongQi ,  STANGELAND, Eric, L.

IPC分类号： C07D211/46 ,  C07D409/12 ,  C07D405/12 ,  C07D401/12 ,  C07D211/62 ,  A61K31/445 ,  A61K31/4525 ,  A61K31/454 ,  A61K31/4545 ,  C07D487/08

CPC分类号： C07D211/58 ,  C07D211/46 ,  C07D211/62 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D487/08 ,  C07D487/10

摘要： The invention provides compounds of Formula I wherein a, b, c, d, f, W, Q, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

摘要翻译： 本发明提供了式I化合物，其中a，b，c，d，f，W，Q，Y，R 1，R 2和R 3如说明书中所定义。 式I化合物是毒蕈碱受体拮抗剂。 本发明还提供了含有这些化合物的药物组合物，制备这些化合物的方法和中间体以及使用这些化合物治疗肺部疾病的方法。

公开(公告)号：EP1848716A1

公开(公告)日：2007-10-31

申请号：EP06735182.5

申请日：2006-02-16

申请人： Theravance, Inc.

发明人： FATHEREE, Paul R. ,  TURNER, Derek S. ,  CHAO, Robert ,  LIU, Jyanwei ,  ZHANG, Hao ,  GENOV, Daniel ,  LEE, Junning

IPC分类号： C07D451/04 ,  A61K31/46

CPC分类号： C07D451/04

摘要： The invention provides crystalline halide salts of 1 isopropyl-1H-indazole-3-carboxylic acid {(1S,3R,5R)-8-[2-(4-acetylpiperazin-1-yl)ethyl]-8-azabicyclo[3.2.1]oct-3-yl}amide and solvates thereof. The invention also provides pharmaceutical compositions comprising such salts, methods of using such crystalline salts to treat diseases associated with 5 HT4 receptor activity, and processes useful for preparing such crystalline salts.

公开(公告)号：EP1831211A1

公开(公告)日：2007-09-12

申请号：EP05854933.8

申请日：2005-12-21

申请人： Theravance, Inc.

发明人： FATHEREE, Paul, R. ,  GENDRON, Roland ,  GOLDBLUM, Adam ,  LONG, Daniel ,  MARQUESS, Daniel ,  TURNER, Derek, S. ,  CHOI, Seok-ki

IPC分类号： C07D451/04 ,  A61K31/46 ,  A61P9/00

CPC分类号： C07D451/04

摘要： The invention provides novel indazole-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5 HT4 receptor activity, and processes and intermediates useful for preparing such compounds.

摘要翻译： 本发明提供了新的吲唑 - 甲酰胺5-HT 4受体激动剂化合物。 本发明还提供包含此类化合物的药物组合物，使用此类化合物治疗与HT 4受体活性有关的疾病的方法，以及可用于制备此类化合物的方法和中间体。

公开(公告)号：EP1723115A1

公开(公告)日：2006-11-22

申请号：EP05730718.3

申请日：2005-03-10

申请人： Theravance, Inc.

发明人： MAMMEN, Mathai ,  JI, Yu-Hua ,  MU, YongQi

IPC分类号： C07D211/62 ,  C07D409/14 ,  A61K31/445 ,  A61K31/4535 ,  A61P11/00

CPC分类号： C07D211/62 ,  C07D409/14

摘要： This invention provides compounds of formula (I), wherein a, b, c, d, m, n, p, s, t, Ar1, R1, R2, R3, R4, R6, R7, R8, and W are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

摘要翻译： 本发明提供式（I）的化合物，其中a，b，c，d，m，n，p，s，t，Ar 1，R 1，R 2，R 3，R 4，R 6，R 7， 在说明书中。 式I化合物是毒蕈碱受体拮抗剂。 本发明还提供了含有这些化合物的药物组合物，制备这些化合物的方法和中间体以及使用这些化合物治疗肺部疾病的方法。

公开(公告)号：EP1723110A1

公开(公告)日：2006-11-22

申请号：EP05725289.2

申请日：2005-03-10

申请人： Theravance, Inc.

发明人： MAMMEN, Mathai ,  JI, Yu-Hua ,  MU, YongQi ,  MISCHKI, Trevor ,  MALATHONG, Viengkham

IPC分类号： C07D211/46 ,  A61K31/445 ,  A61P11/00

CPC分类号： C07D211/46

摘要： This invention provides compounds of formula I: [Insert structure here] I wherein a, b, c, m, p, s, t, W, Ar1, X1, R1, R2, R3, R4, R6, and R7 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

摘要翻译： 本发明提供了式I化合物：其中a，b，c，m，p，s，t，W，Ar1，X1，R1，R2，R3，R4，R6和R7如上定义 在说明书中。 式I化合物是毒蕈碱受体拮抗剂。 本发明还提供了含有这些化合物的药物组合物，制备这些化合物的方法和中间体以及使用这些化合物治疗肺部疾病的方法。

公开(公告)号：EP1706371A1

公开(公告)日：2006-10-04

申请号：EP05711348.2

申请日：2005-01-11

申请人： Theravance, Inc.

发明人： MCKINNELL, Robert Murray ,  JACOBSEN, John R. ,  TRAPP, Sean G. ,  SAITO, Daisuke Roland

IPC分类号： C07C215/60 ,  C07D243/10 ,  C07D265/30

CPC分类号： C07C233/43 ,  C07D215/24 ,  C07D265/30

摘要： The invention provides novel β2-adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with β2-adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.