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公开(公告)号：US08642585B2
公开(公告)日：2014-02-04
申请号：US13803237
申请日：2013-03-14
申请人： Matthias Eckhardt , Sara Frattini , Dieter Hamprecht , Frank Himmelsbach , Elke Langkopf , Iain Lingard , Stefan Peters , Holger Wagner
发明人： Matthias Eckhardt , Sara Frattini , Dieter Hamprecht , Frank Himmelsbach , Elke Langkopf , Iain Lingard , Stefan Peters , Holger Wagner
IPC分类号： A61K31/553 , C07D267/10 , A61K31/443 , C07D405/02 , A61K31/4155 , C07D231/10 , A61K31/422 , C07D263/30 , A61K31/4178 , C07D233/54 , A61K31/4245 , C07D271/06 , A61K31/427 , C07D277/20 , A61K31/501 , C07D403/02 , A61K31/5377 , C07D413/14 , A61K31/497 , C07D307/77 , A61K31/343 , C07D257/02 , A61K31/506 , A61K31/41 , C07D249/08 , A61K31/4196 , A61K31/4025 , C07D409/02 , A61K31/382 , C07D413/02
CPC分类号： C07D405/12 , A61K31/343 , A61K31/351 , A61K31/382 , A61K31/397 , A61K31/4025 , A61K31/41 , A61K31/4155 , A61K31/4178 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/443 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K31/541 , A61K31/553 , A61K45/06 , C07D307/80 , C07D405/14 , C07D407/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
摘要翻译： 本发明涉及通式I的化合物，其中R1，R2和m基团如权利要求1中所定义，其具有有价值的药理学性质，特别是与GPR40受体结合并调节其活性。 该化合物适用于治疗和预防可受该受体影响的疾病，如代谢疾病，特别是2型糖尿病。
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72.发明申请ARYL-AND HETEROARYLCARBONYL DERIVATIVES OF HEXAHYDROINDENOPYRIDINE AND OCTAHYDROBENZOQUINOLINE 有权四氢呋喃并吡咯啉的亚芳基和异丁烯基衍生物公开(公告)号：US20140031544A1
公开(公告)日：2014-01-30
申请号：US13922889
申请日：2013-06-20
IPC分类号： C07D401/06 , C07D498/04 , C07D221/06 , C07D471/04 , C07D417/06
CPC分类号： C07D221/10 , C07D221/06 , C07D221/16 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/14 , C07D417/06 , C07D471/04 , C07D498/04
摘要： The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m 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，其中变量R1，R2，R3，R4和m如权利要求1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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73.发明授权Aryl- and heteroarylcarbonyl derivatives of substituted nortropanes, medicaments containing such compounds and their use 有权取代的正丙胺的芳基和杂芳基羰基衍生物，含有这些化合物的药物及其用途公开(公告)号：US08609690B2
公开(公告)日：2013-12-17
申请号：US13059233
申请日：2009-08-21
IPC分类号： A61K31/541 , C07D451/02 , A61K31/46 , A61K31/498 , A61K31/519
CPC分类号： C07D451/02 , C07D519/00
摘要： The present invention relates to compounds defined by formula (I) wherein the groups R1 and R2 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和R2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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74.发明授权Glucopyranosyl-substituted benzonitrile derivatives, pharmaceutical compositions containing such compounds, their use and process for their manufacture 有权吡喃葡糖基取代的苄腈衍生物，含有这些化合物的药物组合物，其用途和制备方法公开(公告)号：US08557782B2
公开(公告)日：2013-10-15
申请号：US12796866
申请日：2010-06-09
CPC分类号： C07H7/04 , A61K9/0019 , A61K9/02 , A61K9/2018 , A61K9/4866 , C07D309/10
摘要： Glucopyranosyl-substituted benzonitrile derivatives defined according to claim 1, including the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.
摘要翻译： 根据权利要求1所述的吡喃葡萄糖基取代的苄腈衍生物，包括互变异构体，其立体异构体，其混合物及其盐。 根据本发明的化合物适用于治疗代谢性疾病。
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75.发明授权1,1′-diadamantyl carboxylic acids, medicaments containing such compounds and their use 有权1,1'-二十二烷基羧酸，含有这些化合物的药物及其用途公开(公告)号：US08309597B2
公开(公告)日：2012-11-13
申请号：US13054949
申请日：2009-07-24
IPC分类号： A61K31/40 , A61K31/445 , A61K31/397 , A61K31/5375 , C07D211/08 , C07D205/04 , C07D265/30
CPC分类号： C07D295/185 , C07C62/06 , C07C62/38 , C07C69/00 , C07C69/753 , C07C211/35 , C07C233/32 , C07C233/57 , C07C233/58 , C07C233/60 , C07C255/45 , C07C271/24 , C07C2601/08 , C07C2601/14 , C07C2603/74 , C07D205/04 , C07D207/08 , C07D209/08 , C07D209/44 , C07D211/56 , C07D213/64 , C07D217/04 , C07D223/16 , C07D235/16 , C07D239/74 , C07D241/04 , C07D257/04 , C07D263/56 , C07D271/06
摘要： The present invention relates to compounds defined by formula (I) wherein the group R is 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.
摘要翻译： 本发明涉及由式（I）定义的化合物，其中基团R如权利要求1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被该酶抑制影响的疾病，如代谢疾病。
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76.发明申请Aryl- and Heteroarylcarbonyl derivatives of substituted nortropanes, medicaments containing such compounds and their use 有权取代的正丙胺的芳基和杂芳基羰基衍生物，含有这些化合物的药物及其用途公开(公告)号：US20120115853A1
公开(公告)日：2012-05-10
申请号：US13059233
申请日：2009-08-21
IPC分类号： A61K31/541 , C07D451/02 , A61K31/46 , A61K31/498 , A61K31/519
CPC分类号： C07D451/02 , C07D519/00
摘要： The present invention relates to compounds defined by formula (I) wherein the groups R1 and R2 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和R2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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77.发明授权Glucopyranosyl-substituted ((hetero)cycloalkylethynyl-benzyl)-benzene derivatives, medicaments containing such compounds, their use and process for their manufacture 有权吡喃葡糖基取代的（（杂）环烷基乙炔基 - 苄基） - 苯衍生物，含有这些化合物的药物，它们的用途和制备方法公开(公告)号：US07851602B2
公开(公告)日：2010-12-14
申请号：US11494162
申请日：2006-07-27
IPC分类号： A61K31/7028 , A61K31/7034 , C07H7/04
CPC分类号： C07H15/203 , A61K31/7034
摘要： Glucopyranosyl-substituted ((hetero)cycloalkylethynyl-benzyl)-benzene derivatives of the general formula I where the groups R1 to R6 as well as R7a, R7b, R7c are defined according to claim 1, including the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.
摘要翻译： 其中基团R1至R6以及R7a，R7b，R7c的通式I的吡喃葡糖基取代的（（杂）环烷基乙炔基 - 苄基） - 苯衍生物根据权利要求1定义，包括互变异构体，其立体异构体，混合物 及其盐。 根据本发明的化合物适用于治疗代谢性疾病。
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78.发明授权Processes for preparing of glucopyranosyl-substituted (ethynyl-benzyl)-benzene derivatives and intermediates thereof 有权制备吡喃葡萄糖基取代的（乙炔基 - 苄基） - 苯衍生物的方法及其中间体公开(公告)号：US07847074B2
公开(公告)日：2010-12-07
申请号：US11531898
申请日：2006-09-14
CPC分类号： C07H7/04
摘要： The present invention relates to processes for preparing the compounds of general formula I, wherein the groups R1, R2 and R3 are defined according to claim 1 and to intermediates of said processes.
摘要翻译： 本发明涉及制备通式Ⅰ化合物的方法，其中R 1，R 2和R 3基团根据权利要求1定义，和所述方法的中间体。
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79.发明授权Glucopyranosyl-substituted benzonitrile derivatives, pharmaceutical compositions containing such compounds, their use and process for their manufacture 有权吡喃葡糖基取代的苄腈衍生物，含有这些化合物的药物组合物，其用途和制备方法公开(公告)号：US07745414B2
公开(公告)日：2010-06-29
申请号：US11674839
申请日：2007-02-14
CPC分类号： C07D309/10 , C07H7/04
摘要： Glucopyranosyl-substituted benzonitrile derivatives as defined herein, including the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.
摘要翻译： 本文定义的吡喃葡糖基取代的苄腈衍生物，包括互变异构体，其立体异构体，其混合物及其盐。 根据本发明的化合物适用于治疗代谢性疾病。
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80.发明申请TETRASUBSTITUTED CLUCOPYRANOSYLATED BENZENE DERIVATIVES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, THEIR USE AND PROCESS FOR THEIR MANUFACTURE 有权四环素衍生的苯并噻唑衍生物，含有这些化合物的药物，其使用及其制造方法公开(公告)号：US20100093654A1
公开(公告)日：2010-04-15
申请号：US12527774
申请日：2008-02-20
IPC分类号： A61K31/7034 , C07H15/203 , A61P3/10
CPC分类号： C07H7/04
摘要： Tetrasubstituted glucopyranosylated benzene derivatives of general formula (I) as defined according to claim 1, including the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.
摘要翻译： 包括互变异构体，其立体异构体，其混合物及其盐的如权利要求1所定义的通式（I）的四取代吡喃葡糖基化苯衍生物。 根据本发明的化合物适用于治疗代谢性疾病。
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