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1.发明申请公开(公告)号：US20090221589A1
公开(公告)日：2009-09-03
申请号：US12097931
申请日：2006-12-18
IPC分类号： A61K31/4164 , A61K31/502 , A61K31/4439 , A61K31/422 , A61K31/4178 , A61K31/4184 , A61K31/4196 , A61P13/10
CPC分类号： A61K31/135
摘要： The present invention relates to the use of new beta-agonists of general formula (Ia) or (Ib) wherein the groups R1 to R12 and R1 to R7, respectively, have the meanings given in the claims and specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, for preparing a medicament for the treatment of overactive bladder.
摘要翻译： 本发明涉及通式（Ia）或（Ib）的新的β-激动剂的用途，其中R1至R12和R1至R7分别具有权利要求和说明书中给出的含义，互变异构体，对映异构体 ，非对映异构体，其混合物，其前药及其盐，特别是其与无机或有机酸或碱的生理上可接受的盐，用于制备治疗膀胱过动症的药物。
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2.发明授权Beta-agonists, processes for preparing them and their use as pharmaceutical compositions 有权β-激动剂，制备它们的方法及其作为药物组合物的用途公开(公告)号：US07214698B2
公开(公告)日：2007-05-08
申请号：US11276649
申请日：2006-03-09
IPC分类号： A61K31/4164
CPC分类号： C07D233/64 , C07D233/84 , C07D249/08 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12
摘要： The present invention relates to new beta-agonists of general formula 1: wherein the groups R1 to R12 have the meanings given in the claims and specification, the isomers thereof, processes for preparing these compounds and their use as pharmaceutical compositions.
摘要翻译： 本发明涉及通式1的新β-激动剂：其中R 1至R 12基团具有权利要求书和说明书中给出的含义，其异构体， 制备这些化合物的方法及其作为药物组合物的用途。
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3.发明授权Beta-agonists, methods for the preparation thereof and their use as pharmaceutical compositions 有权β-激动剂，其制备方法及其作为药物组合物的用途公开(公告)号：US07977334B2
公开(公告)日：2011-07-12
申请号：US12113780
申请日：2008-05-01
IPC分类号： A61K31/50 , C07D249/04
CPC分类号： C07D249/08 , C07D233/36 , C07D233/64 , C07D233/68 , C07D233/90 , C07D235/06 , C07D237/32 , C07D249/06 , C07D401/04 , C07D403/10 , C07D409/04 , C07D413/04
摘要： The present invention relates to new beta-agonists of general formula (I) wherein the groups R1 to R7 have the meanings given in the claims and specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, processes for preparing these compounds and their use as pharmaceutical compositions.
摘要翻译： 本发明涉及通式（I）的新β-激动剂，其中基团R 1至R 7具有权利要求和说明书中给出的含义，互变异构体，对映体，非对映体，其混合物，其前药和盐 特别是其与无机或有机酸或碱的生理上可接受的盐，制备这些化合物的方法及其作为药物组合物的用途。
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4.发明授权Indol-containing beta-agonists, methods for the preparation thereof and their use as pharmaceutical compositions 有权含吲哚的β-激动剂，其制备方法及其作为药物组合物的用途公开(公告)号：US07754756B2
公开(公告)日：2010-07-13
申请号：US11550830
申请日：2006-10-19
申请人： Rainer Walter , Bradford S. Hamilton , Thomas Trieselmann , Matthew R. Netherton , Marco Santagostino , Ingo Konetzki
发明人： Rainer Walter , Bradford S. Hamilton , Thomas Trieselmann , Matthew R. Netherton , Marco Santagostino , Ingo Konetzki
IPC分类号： A61K31/4045 , A61K31/404 , C07D209/24 , C07D209/18 , C07D413/02
CPC分类号： C07D209/08 , C07D209/18 , C07D209/42 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D413/12
摘要： The present invention relates to new beta-agonists of general formula (I) wherein the groups R1 and R2 have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers, solvates, hydrates, mixtures thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, methods of preparing these compounds and their use as pharmaceutical compositions.
摘要翻译： 本发明涉及通式（I）的新β-激动剂，其中基团R 1和R 2具有权利要求和说明书中给出的含义，互变异构体，外消旋体，对映异构体，非对映异构体，溶剂合物，水合物，其混合物，其前药 其盐，特别是其与无机或有机酸或碱的生理学上可接受的盐，制备这些化合物的方法及其作为药物组合物的用途。
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5.发明申请Beta-agonists, methods for the preparation thereof and their use as pharmaceutical compositions 有权β-激动剂，其制备方法及其作为药物组合物的用途公开(公告)号：US20080234278A1
公开(公告)日：2008-09-25
申请号：US12113780
申请日：2008-05-01
IPC分类号： A61K31/502 , C07D233/61 , A61K31/4172 , A61P43/00 , C07D237/32
CPC分类号： C07D249/08 , C07D233/36 , C07D233/64 , C07D233/68 , C07D233/90 , C07D235/06 , C07D237/32 , C07D249/06 , C07D401/04 , C07D403/10 , C07D409/04 , C07D413/04
摘要： The present invention relates to new beta-agonists of general formula (I) wherein the groups R1 to R7 have the meanings given in the claims and specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, processes for preparing these compounds and their use as pharmaceutical compositions.
摘要翻译： 本发明涉及通式（I）的新的β-激动剂，其中基团R 1至R 7具有权利要求和说明书中给出的含义，互变异构体， 对映异构体，非对映异构体，其混合物，其前药及其盐，特别是其与无机或有机酸或碱的生理学上可接受的盐，制备这些化合物的方法及其作为药物组合物的用途。
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6.发明申请Novel Beta-Agonists, Process for Their Preparation and Their Use as Medicaments 审中-公开新型β-激动剂，其制备方法及其用作药物公开(公告)号：US20080300290A1
公开(公告)日：2008-12-04
申请号：US12091823
申请日：2006-10-27
申请人： Rainer Walter , Thomas Trieselmann , Matthew R. Netherton , Marco Santagostino , Bradford S. Hamilton
发明人： Rainer Walter , Thomas Trieselmann , Matthew R. Netherton , Marco Santagostino , Bradford S. Hamilton
IPC分类号： A61K31/4164 , C07D233/61 , A61P3/04 , A61P3/10
CPC分类号： C07D233/64
摘要： Compounds of general formula (I) which are selective beta-3-agonists and useful for the treatment of obesity and type II diabetes. Exemplary compounds are: [4-(1-{3-[2-(3-phenylsulphonylamino-phenyl)-2-hydroxy-ethylamino]-3-methyl-butyl}-1H-imidazol-4-yl)-phenyl]-acetic acid and methyl [4-(1-{3-[2-(3-phenylsulphonylamino-phenyl)-2-hydroxy-ethylamino]-3-methyl-butyl}-1H-imidazol-4-yl)-phenyl]-acetate.
摘要翻译： 作为选择性β-3-激动剂并可用于治疗肥胖和II型糖尿病的通式（I）的化合物。 示例性化合物是：[4-（1- {3- [2-（3-苯基磺酰基氨基 - 苯基）-2-羟基 - 乙基氨基] -3-甲基 - 丁基} -1H-咪唑-4-基） - 苯基] 乙酸和[4-（1- {3- [2-（3-苯基磺酰基氨基 - 苯基）-2-羟基 - 乙基氨基] -3-甲基 - 丁基} -1H-咪唑-4-基） - 苯基] 乙酸盐。
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7.发明申请公开(公告)号：US20080269281A1
公开(公告)日：2008-10-30
申请号：US12091828
申请日：2006-10-27
IPC分类号： A61K31/437 , C07D471/04 , A61P3/10 , A61P3/04
CPC分类号： C07D471/04
摘要： Compounds of the formula which are selective beta-3-agonists and useful for the treatment of obesity and type II diabetes. Exemplary compounds are: ethyl 3-{3-[(R)-2-(3-benzenesulphonylamino-phenyl)-2-hydroxy-ethylamino]-3-methyl-butyl}-3H-imidazo[4,5-b]pyridine-5-carboxylate and 3-{3-[(R)-2-(3-benzenesulphonylamino-phenyl)-2-hydroxy-ethylamino]-3-methyl-butyl}-3H-imidazo[4,5-b]pyridine-5-carboxylic acid.
摘要翻译： 作为选择性β-3-激动剂并可用于治疗肥胖和II型糖尿病的式的化合物。 示例性化合物是：3- {3 - [（R）-2-（3-苯磺酰氨基 - 苯基）-2-羟基 - 乙基氨基] -3-甲基 - 丁基} -3H-咪唑并[4,5-b]吡啶 -5-羧酸乙酯和3- {3 - [（R）-2-（3-苯磺酰基氨基 - 苯基）-2-羟基 - 乙基氨基] -3-甲基 - 丁基} -3H-咪唑并[4,5-b]吡啶 -5-羧酸。
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8.发明授权Aryl- and heteroarylcarbonyl derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use 有权苯并吡喃和相关支架的芳基和杂芳基羰基衍生物，含有这些化合物的药物及其应用公开(公告)号：US08859580B2
公开(公告)日：2014-10-14
申请号：US12742680
申请日：2008-11-14
申请人： Frank Himmelsbach , Matthias Eckhardt , Bradford S. Hamilton , Armin Heckel , Joerg Kley , Thorsten Lehmann-Lintz , Herbert Nar , Stefan Peters , Annette Schuler-Metz , Matthias Zentgraf
发明人： Frank Himmelsbach , Matthias Eckhardt , Bradford S. Hamilton , Armin Heckel , Joerg Kley , Thorsten Lehmann-Lintz , Herbert Nar , Stefan Peters , Annette Schuler-Metz , Matthias Zentgraf
IPC分类号： C07D221/26 , C07D417/06 , C07D401/06 , C07D471/08 , C07D498/08 , C07D413/14 , C07D413/06 , C07D405/06 , C07D401/14 , C07D451/06 , C07D403/06
CPC分类号： C07D221/26 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/06 , C07D413/06 , C07D413/14 , C07D417/06 , C07D451/06 , C07D471/08 , C07D498/08
摘要： The present invention relates to compounds defined by formula I wherein the groups R1 to R3, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.
摘要翻译： 本发明涉及由式I定义的化合物，其中R 1至R 3，X，m，n和o基团如权利要求1中所定义，具有有价值的药理学活性。 特别地，化合物是11β-羟基类固醇脱氢酶（HSD）1的抑制剂，因此适用于治疗和预防可受该酶抑制影响的疾病，如代谢疾病，特别是2型糖尿病，肥胖症和血脂异常。
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公开(公告)号：US08846613B2
公开(公告)日：2014-09-30
申请号：US14048880
申请日：2013-10-08
IPC分类号： A61K31/5355 , A61K45/06 , A61K31/7048 , A61K31/522 , A61K31/155 , A61K31/422 , A61K31/427
CPC分类号： A61K31/5355 , A61K31/155 , A61K31/422 , A61K31/427 , A61K31/522 , A61K31/7048 , A61K45/06 , A61K2300/00
摘要： The invention relates to a pharmaceutical composition comprising 1.a and/or 1.b according to claim 1 in combination with at least one second therapeutic agent 2 which is suitable in the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance and hyperglycemia. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions.
摘要翻译： 本发明涉及包含根据权利要求1的1.a和/或1.b与至少一种第二治疗剂2组合的药物组合物，其适用于治疗或预防选自1型糖尿病的一种或多种病症 ，2型糖尿病，糖耐量异常和高血糖。 此外，本发明涉及用于预防或治疗代谢紊乱及相关病症的方法。
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10.发明申请Urea derivatives of substituted nortropanes, medicaments containing such compounds and their use 有权取代的正丙胺的脲衍生物，含有这些化合物的药物及其用途公开(公告)号：US20110275595A1
公开(公告)日：2011-11-10
申请号：US13124259
申请日：2009-10-22
IPC分类号： A61K31/695 , A61K31/501 , A61K31/46 , C07D451/02 , C07F7/02 , A61P3/00 , A61P3/10 , A61K31/5377 , A61P3/04
CPC分类号： C07D451/02 , C07D519/00
摘要： The present invention relates to compounds defined by formula I wherein the groups R1, Y1 to Y4, V, W, and X are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
摘要翻译： 本发明涉及由式I定义的化合物，其中基团R1，Y1至Y4，V，W和X如权利要求1所定义，具有有价值的药理活性。 特别地，化合物是11β-羟基类固醇脱氢酶（HSD）1的抑制剂，因此适用于治疗和预防可受该酶抑制影响的疾病，例如代谢疾病，特别是2型糖尿病，肥胖症和 血脂异常
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