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1.发明授权2 -AMINOTETRALIN DERIVATIVES AS MU OPIOID RECEPTOR ANTAGONISTS 有权2-AMINOTETRALINDERIVATE ALS ANTAGONISTEN DES MU-OPIOID-REZEPTORS
公开(公告)号：EP2280933B1
公开(公告)日：2013-07-24
申请号：EP09727561.4
申请日：2009-03-31
申请人： Theravance, Inc.
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
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2.发明公开COMBINATIONS OF AN ARYL ANILINE BETA-2 ADRENERGIC RECEPTOR AGONIST AND A CORTICOSTEROID 有权组合的ARYLANILIN-β-2-肾上腺素受体激动剂和皮质类固醇
公开(公告)号：EP1641465A2
公开(公告)日：2006-04-05
申请号：EP04809361.1
申请日：2004-05-07
申请人： Theravance, Inc.
发明人： MORAN, Edmund, J. , JACOBSEN, John, R. , LEADBETTER, Michael, R. , NODWELL, Matthew, B. , TRAPP, Sean, G. , AGGEN, James, B. , CHURCH, Timothy, J.
IPC分类号： A61K31/58 , A61K31/136 , A61K31/277 , A61K31/325 , A61K31/33 , A61K31/343 , A61K31/35 , A61K31/36 , A61K31/381 , A61K31/385 , A61K31/405 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/47
CPC分类号： A61K31/4706 , A61K31/136 , A61K31/277 , A61K31/325 , A61K31/33 , A61K31/343 , A61K31/35 , A61K31/36 , A61K31/381 , A61K31/385 , A61K31/405 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/47 , A61K31/4704 , A61K31/4709 , A61K31/58 , C07C213/04 , C07C215/34 , C07C215/60 , C07C217/84 , C07C229/38 , C07C233/43 , C07C317/36 , C07D213/75 , C07D215/227 , C07D215/26 , C07D231/22 , C07D239/38 , C07D239/42 , C07D239/47 , C07D239/69 , C07D277/46 , C07D311/80 , C07D321/10 , C07D401/12 , C07D409/12 , C07D413/12 , A61K2300/00
摘要： The invention provides novel β2 adrenergic receptor agonist compounds of formula (I): wherein R1 - R13 and w have any of the values described in the specification. The invention also provides combinations of such compounds and other therapeutic agents, pharmaceutical compositions comprising such compounds and combinations, methods of using such compounds to treat diseases associated with β2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.
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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.
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.-
4.发明公开3-CARBOXYPROPYL-AMINOTETRALIN DERIVATIVES AS MU OPIOID RECEPTOR ANTAGONISTS 有权作为阿片受体拮抗剂的3-羧基丙氨酰胺基衍生物
公开(公告)号：EP2231585A2
公开(公告)日：2010-09-29
申请号：EP08859864.4
申请日：2008-12-10
申请人： Theravance, Inc.
发明人： TRAPP, Sean, G. , LEADBETTER, Michael, R. , LONG, Daniel, D. , JACOBSEN, John, R. , VAN DYKE, Priscilla , COLSON, Pierre-Jean , RAPTA, Miroslav , YU, Ying
IPC分类号： C07C215/64 , C07C229/28 , C07C237/48 , A61K31/216 , A61K31/197 , A61P1/00
CPC分类号： C07C237/48 , A61K9/0075 , A61K9/2054 , A61K9/4858 , A61K31/197 , A61K31/485 , A61K45/06 , A61K47/02 , A61K47/12 , C07B2200/07 , C07C215/64 , C07C229/28 , C07C229/34 , C07C2601/14 , C07C2602/10 , Y10T436/173845
摘要： The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I): (I) wherein R
1 , R
2 , R
3 , R
4 , R
5 , and R
6 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.摘要翻译： 本发明提供了式（I）的3-羧丙基 - 氨基四氢化萘化合物或其药学上可接受的盐：其中R 1，R 2，R 3，R 4，R 5和R 6在说明书中定义的式 ，它们是μ阿片受体的拮抗剂。 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μ阿片受体活性相关的病症的方法，以及可用于制备此类化合物的方法和中间体。
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5.发明授权COMBINATIONS OF AN ARYL ANILINE BETA-2 ADRENERGIC RECEPTOR AGONIST AND A CORTICOSTEROID 有权组合的ARYLANILIN-β-2-肾上腺素受体激动剂和皮质类固醇
公开(公告)号：EP1641465B1
公开(公告)日：2009-11-04
申请号：EP04809361.1
申请日：2004-05-07
申请人： Theravance, Inc.
发明人： MORAN, Edmund, J. , JACOBSEN, John, R. , LEADBETTER, Michael, R. , NODWELL, Matthew, B. , TRAPP, Sean, G. , AGGEN, James, B. , CHURCH, Timothy, J.
IPC分类号： A61K31/58 , A61K31/136 , A61K31/277 , A61K31/325 , A61K31/33 , A61K31/343 , A61K31/35 , A61K31/36 , A61K31/381 , A61K31/385 , A61K31/405 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/47
CPC分类号： A61K31/4706 , A61K31/136 , A61K31/277 , A61K31/325 , A61K31/33 , A61K31/343 , A61K31/35 , A61K31/36 , A61K31/381 , A61K31/385 , A61K31/405 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/47 , A61K31/4704 , A61K31/4709 , A61K31/58 , C07C213/04 , C07C215/34 , C07C215/60 , C07C217/84 , C07C229/38 , C07C233/43 , C07C317/36 , C07D213/75 , C07D215/227 , C07D215/26 , C07D231/22 , C07D239/38 , C07D239/42 , C07D239/47 , C07D239/69 , C07D277/46 , C07D311/80 , C07D321/10 , C07D401/12 , C07D409/12 , C07D413/12 , A61K2300/00
摘要： The invention provides novel β2 adrenergic receptor agonist compounds of formula (I): wherein R1 - R13 and w have any of the values described in the specification. The invention also provides combinations of such compounds and other therapeutic agents, pharmaceutical compositions comprising such compounds and combinations, methods of using such compounds to treat diseases associated with β2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.
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公开(公告)号：EP1446379B1
公开(公告)日：2009-04-29
申请号：EP02780622.3
申请日：2002-11-12
申请人： Theravance, Inc.
发明人： MORAN, Edmund, J. , JACOBSEN, John, R. , LEADBETTER, Michael, R. , NODWELL, Matthew, B. , TRAPP, Sean, G. , AGGEN, James , CHURCH, Timothy, J.
IPC分类号： C07C229/60
CPC分类号： C07D213/75 , C07C215/60 , C07C217/84 , C07C229/38 , C07C233/43 , C07C317/36 , C07D213/76 , C07D215/227 , C07D215/26 , C07D231/22 , C07D239/38 , C07D239/42 , C07D239/47 , C07D277/46 , C07D277/52 , C07D295/26 , C07D311/80 , C07D319/18 , C07D321/10 , C07D401/12 , C07D409/12 , C07D413/12
摘要： The invention provides novel β2 adrenergic receptor agonist compounds of formula (I): wherein R1-R13 and w have any of the values described in the specification. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with β¿2? adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.
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7.发明授权3-CARBOXYPROPYL-AMINOTETRALIN DERIVATIVES AS MU OPIOID RECEPTOR ANTAGONISTS 有权3-羧基丙基氨基丙酸酯衍生物ALS ANTAGONISTEN DES MU-OPIOID-REZEPTORS
公开(公告)号：EP2231585B1
公开(公告)日：2013-02-13
申请号：EP08859864.4
申请日：2008-12-10
申请人： Theravance, Inc.
发明人： TRAPP, Sean, G. , LEADBETTER, Michael, R. , LONG, Daniel, D. , JACOBSEN, John, R. , VAN DYKE, Priscilla , COLSON, Pierre-Jean , RAPTA, Miroslav , YU, Ying
IPC分类号： C07C215/64 , C07C229/28 , C07C237/48 , A61K31/216 , A61K31/197 , A61P1/00
CPC分类号： C07C237/48 , A61K9/0075 , A61K9/2054 , A61K9/4858 , A61K31/197 , A61K31/485 , A61K45/06 , A61K47/02 , A61K47/12 , C07B2200/07 , C07C215/64 , C07C229/28 , C07C229/34 , C07C2601/14 , C07C2602/10 , Y10T436/173845
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公开(公告)号：EP1446379A1
公开(公告)日：2004-08-18
申请号：EP02780622.3
申请日：2002-11-12
申请人： Theravance, Inc.
发明人： MORAN, Edmund, J. , JACOBSEN, John, R. , LEADBETTER, Michael, R. , NODWELL, Matthew, B. , TRAPP, Sean, G. , AGGEN, James , CHURCH, Timothy, J.
IPC分类号： C07C229/60
CPC分类号： C07D213/75 , C07C215/60 , C07C217/84 , C07C229/38 , C07C233/43 , C07C317/36 , C07D213/76 , C07D215/227 , C07D215/26 , C07D231/22 , C07D239/38 , C07D239/42 , C07D239/47 , C07D277/46 , C07D277/52 , C07D295/26 , C07D311/80 , C07D319/18 , C07D321/10 , C07D401/12 , C07D409/12 , C07D413/12
摘要： The invention provides novel β2 adrenergic receptor agonist compounds of formula (I): wherein R1-R13 and w have any of the values described in the specification. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with β¿2? adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.
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公开(公告)号：EP1292611B1
公开(公告)日：2008-03-12
申请号：EP01932807.9
申请日：2001-05-01
申请人： Theravance, Inc.
发明人： LINSELL, Martin, S. , FATHEREE, Paul, R. , JUDICE, J., Kevin , LEADBETTER, Michael, R. , ZHU, Yan
CPC分类号： B82Y5/00 , A61K9/0014 , A61K9/0019 , A61K38/00 , A61K47/40 , A61K47/6951 , C07K9/008
摘要： Disclosed are glycopeptide derivatives substituted at the C-terminus and/or the R terminus with a substituent that comprises one or more saccharide groups and a carboxy group; and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial agents.
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公开(公告)号：EP1292612B1
公开(公告)日：2006-08-23
申请号：EP01934967.9
申请日：2001-05-01
申请人： Theravance, Inc.
CPC分类号： C07K9/008 , A61K9/0014 , A61K9/0019 , A61K9/0095 , A61K9/02 , A61K9/19 , A61K9/2018 , A61K9/4858 , A61K38/14 , A61K47/06 , A61K47/12 , A61K47/26 , A61K47/40 , A61K47/6951 , B82Y5/00
摘要： Disclosed are glycopeptides that are substituted with one or more substituents each comprising one or more phosphono groups; and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial agents.
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