公开(公告)号：EP2231589B1

公开(公告)日：2013-02-13

申请号：EP08859523.6

申请日：2008-12-10

申请人： Theravance, Inc.

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

IPC分类号： C07C229/28 ,  C07C229/34 ,  C07C237/06 ,  C07C237/14 ,  C07C237/20 ,  C07C237/48 ,  C07D295/185 ,  A61K31/165 ,  A61K31/166 ,  A61K31/197 ,  A61K31/216 ,  A61K31/45 ,  A61K31/495 ,  A61P1/00

CPC分类号： C07C237/48 ,  A61K9/0019 ,  A61K9/0075 ,  A61K9/10 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/4858 ,  A61K9/4866 ,  A61K47/12 ,  A61K47/14 ,  A61K47/26 ,  C07C229/28 ,  C07C229/34 ,  C07C237/06 ,  C07C237/14 ,  C07C237/20 ,  C07C2601/14 ,  C07C2602/10 ,  C07D295/185

公开(公告)号：EP2185553B1

公开(公告)日：2012-06-27

申请号：EP08795592.8

申请日：2008-08-26

申请人： Theravance, Inc.

发明人： LONG, Daniel D. ,  SAITO, Daisuke Roland ,  VAN DYKE, Priscilla ,  JIANG, Lan ,  CHURCH, Timothy J. ,  JACOBSEN, John R.

IPC分类号： C07D451/02 ,  A61K31/46 ,  A61P25/04

CPC分类号： C07D451/02

摘要： The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): (I) wherein R1, R2, R3, and α 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：EP2225210B1

公开(公告)日：2012-04-25

申请号：EP08859870.1

申请日：2008-12-08

申请人： Theravance, Inc.

发明人： CHOI, Seok-ki ,  FATHEREE, Paul R. ,  MCKINNELL, Robert Murray ,  OLSON, Brooke

IPC分类号： C07D235/08 ,  C07D235/26 ,  C07D403/10 ,  A61K31/4184 ,  A61P9/00

CPC分类号： C07D235/08 ,  C07D235/26 ,  C07D403/10

摘要： The invention relates to compounds having the formula: (I) wherein Ar, r, n, X, R2, R2', R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.

公开(公告)号：EP2376427A1

公开(公告)日：2011-10-19

申请号：EP09793383.2

申请日：2009-12-09

申请人： Theravance, Inc.

发明人： DALZIEL, Sean ,  RAPTA, Miroslav

IPC分类号： C07C231/24 ,  C07C237/48

CPC分类号： C07C229/38 ,  C07C237/48 ,  C07C2601/14 ,  C07C2602/10

摘要： The invention provides crystalline solid forms of (S)-4-((2S,3S)-7-carbamoyl-1,1-diethyl-3-methoxy-1,2,3,4-tetrahydronaphthalen-2-ylamino)-2-cyclohexylmethyl-butyric acid. The invention also provides pharmaceutical compositions comprising such crystalline solid forms, methods of using such crystalline solid forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline solid forms.

摘要翻译： 本发明提供了（S）-4 - （（2S，3S）-7-氨基甲酰基-1,1-二乙基-3-甲氧基-1,2,3,4-四氢萘-2-基氨基）-2 - 环己基甲基 - 丁酸。 本发明还提供包含此类结晶固体形式的药物组合物，使用此类结晶固体形式治疗与μ阿片受体活性相关的疾病的方法，以及可用于制备此类结晶固体形式的方法。

公开(公告)号：EP1509492B1

公开(公告)日：2011-08-31

申请号：EP03799743.4

申请日：2003-01-24

申请人： Theravance, Inc.

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

IPC分类号： C07C235/20 ,  C07C69/734 ,  A61K31/216 ,  A61P23/00

CPC分类号： A61K31/24 ,  A61K31/216 ,  C07C69/734 ,  C07C235/20

摘要： The invention provides compounds compositions and methods useful for inducing or maintaining general anesthesia or sedation in mammals.

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：EP2334651A2

公开(公告)日：2011-06-22

申请号：EP09790756.2

申请日：2009-07-23

申请人： Theravance, Inc.

发明人： CHOI, Seok-ki ,  FATHEREE, Paul R. ,  GENDRON, Roland ,  MCKINNELL, Robert Murray ,  BLAIR, Brooke

IPC分类号： C07D233/64 ,  C07D233/68 ,  C07D233/90 ,  C07D249/08 ,  C07D249/10 ,  C07D401/14 ,  C07D403/10 ,  A61K31/4174 ,  A61K31/4178 ,  A61K31/4196 ,  A61P9/12

CPC分类号： A61K31/4196 ,  A61K45/06 ,  C07D233/64 ,  C07D233/68 ,  C07D233/90 ,  C07D249/08 ,  C07D249/10 ,  C07D401/06 ,  C07D401/14 ,  C07D403/10

摘要： In one aspect, the invention relates to compounds having the formula: (I) wherein: Ar, r, Z, X, R
3 , and R
5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT
1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

公开(公告)号：EP2001876B1

公开(公告)日：2011-05-18

申请号：EP07752111.0

申请日：2007-02-28

申请人： Theravance, Inc.

发明人： LONG, Daniel ,  CHURCH, Timothy J. ,  JACOBSEN, John R. ,  JIANG, Lan ,  SAITO, Daisuke Roland ,  STERGIADES, Ioanna ,  VAN DYKE, Priscilla

IPC分类号： C07D451/02

CPC分类号： C07D451/02 ,  A61K31/439 ,  A61K31/46 ,  A61K31/485 ,  A61K45/06

摘要： The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate 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：EP1984362B1

公开(公告)日：2011-05-11

申请号：EP07750777.0

申请日：2007-02-15

申请人： Theravance, Inc.

发明人： GENOV, Daniel ,  LEE, Junning ,  LIU, Jyanwei

IPC分类号： C07D451/04 ,  C07D451/06 ,  A61K31/46 ,  A61P1/00 ,  A61P25/00

CPC分类号： C07D451/04 ,  C07D451/06

摘要： The invention provides 8-azabicyclo[3.2.1]octyl intermediates of formula (I): useful for the preparation of 5-HT4 receptor agonist compounds. The invention also provides processes for the preparation of such useful intermediates.

公开(公告)号：EP2195313A1

公开(公告)日：2010-06-16

申请号：EP08795593.6

申请日：2008-08-26

申请人： Theravance, Inc.

发明人： LONG, Daniel, D. ,  JIANG, Lan ,  SAITO, Daisuke, Roland ,  VAN DYKE, Priscilla

IPC分类号： C07D451/02 ,  A61K31/33 ,  A61P1/00

CPC分类号： C07D451/02

摘要： The invention provides heteroarylene substituted 8-azabicyclo[3.2.1]octane compounds of formula (I): (I) wherein R1, R2, A, and m 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.