公开(公告)号：EP2358676A1

公开(公告)日：2011-08-24

申请号：EP09752988.7

申请日：2009-11-13

申请人： Theravance, Inc.

发明人： PATTERSON, Lori Jean ,  CHAO, Robert ,  RAPTA, Miroslav

IPC分类号： C07D211/22 ,  A61K31/4409 ,  A61P25/00

CPC分类号： A61K31/4465 ,  C07D211/22 ,  C07D211/32

摘要： The invention provides a crystalline hydrochloride salt of 4-[2-(2,4,6-trifluorophenoxymethyl)phenyl]piperidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.

公开(公告)号：EP1706371B1

公开(公告)日：2011-04-06

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.

公开(公告)号：EP2280933A1

公开(公告)日：2011-02-09

申请号：EP09727561.4

申请日：2009-03-31

申请人： Theravance, Inc.

发明人： TRAPP, Sean, G. ,  LEADBETTER, Michael, R. ,  LONG, Daniel, D. ,  JIANG, Lan ,  AXT, Sabine

IPC分类号： C07C233/36 ,  C07C233/78 ,  C07C235/10 ,  C07C237/48 ,  C07C255/24 ,  C07C275/24 ,  C07C275/34 ,  C07C311/14 ,  C07D307/68 ,  C07D333/38 ,  A61P1/00 ,  A61P25/04 ,  A61K31/16 ,  A61K31/13 ,  C07C335/16

CPC分类号： C07C237/48 ,  C07C233/36 ,  C07C233/37 ,  C07C233/40 ,  C07C233/62 ,  C07C233/78 ,  C07C235/10 ,  C07C255/24 ,  C07C275/14 ,  C07C275/18 ,  C07C275/24 ,  C07C275/28 ,  C07C275/30 ,  C07C275/34 ,  C07C311/05 ,  C07C311/14 ,  C07C311/16 ,  C07C311/18 ,  C07C311/46 ,  C07C317/44 ,  C07C335/08 ,  C07C335/12 ,  C07C335/16 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/10 ,  C07D203/02 ,  C07D203/26

摘要： The invention provides amino- and amido-aminotetralin compounds of formula (I) wherein R
1 , R
2 , R
3 , R
4 , R
5 , R
6 , R
7 , and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

公开(公告)号：EP1831211B1

公开(公告)日：2010-06-02

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.

公开(公告)号：EP2173746A2

公开(公告)日：2010-04-14

申请号：EP08794481.5

申请日：2008-07-15

申请人： Theravance, Inc.

发明人： COLSON, Pierre-Jean ,  YU, Ying ,  LONG, Daniel, D. ,  STERGIADES, Ioanna

IPC分类号： C07D451/02

CPC分类号： C07D451/06 ,  C07D451/02 ,  Y02P20/55

摘要： The invention provides an efficient method for preparing 3-endo-(S- azabicyclo[3.2.1]oct-3-yl)benzamide by hydrogenation, under controlled conditions, of an amino-protected 3-(8-azabicyclo[3.2.1]oct-2-en-3-yl)benzamide intermediate in which the amino-protecting group is removable by catalytic hydrogenation.

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：EP2121594A1

公开(公告)日：2009-11-25

申请号：EP08725911.5

申请日：2008-02-21

申请人： Theravance, Inc.

发明人： JI, Yu-hua ,  HUSFELD, Craig ,  LANGE, Christopher ,  LEE, Rick ,  MU, Yongqi

IPC分类号： C07D207/08 ,  C07D207/09 ,  A61K31/40 ,  A61P11/00

CPC分类号： C07D207/09 ,  C07D207/08 ,  C07D207/48

摘要： The invention provides compounds of formula (I) in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R 1-6, a-e and Q are as defined in the specification,. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.

公开(公告)号：EP1856050B1

公开(公告)日：2009-11-25

申请号：EP06737787.9

申请日：2006-03-09

申请人： Theravance, Inc.

发明人： AXT, Sabine ,  CHURCH, Timothy J. ,  MALATHONG, Viengkham

IPC分类号： C07D211/46 ,  A61K31/45 ,  A61P11/06

CPC分类号： C07D401/12 ,  A61K9/0073 ,  A61K9/14 ,  A61K9/19 ,  A61K31/4545 ,  A61K31/56 ,  A61K31/58 ,  A61K45/00 ,  A61K45/06 ,  A61M15/00 ,  A61M2202/064 ,  C07B2200/13 ,  C07D211/62 ,  C07D211/94

摘要： The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.

公开(公告)号：EP1648413B1

公开(公告)日：2009-10-07

申请号：EP04757141.9

申请日：2004-07-21

申请人： Theravance, Inc.

发明人： JENKINS, Thomas E. ,  BOLTON, Jennifer

IPC分类号： A61K9/107 ,  A61K31/216

CPC分类号： A61K9/1075 ,  A61K31/20 ,  A61K31/216 ,  A61K31/325 ,  Y10S514/816 ,  Y10S514/937

摘要： The invention provides pharmaceutical compositions comprising a phenylacetic acid ester compound useful for inducing or maintaining general anesthesia or sedation in mammals, methods for preparing such compositions, and methods for inducing or maintaining anesthesia or sedation using such compositions.

公开(公告)号：EP1626970B1

公开(公告)日：2009-07-08

申请号：EP04753585.1

申请日：2004-05-27

申请人： Theravance, Inc.

发明人： MAMMEN, Mathai ,  HUGHES, Adam

IPC分类号： C07D451/02 ,  A61K31/472

CPC分类号： C07D451/02 ,  A61K31/46 ,  A61K31/4743 ,  C07D451/12 ,  C07D471/08

摘要： This invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a phan-naceutically acceptable salt or solvate or stereoisomer thereof The compounds of this invention possess both β2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.