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61.发明申请Glucopyranosyl-substituted ((hetero)arylethynyl-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）芳基乙炔基 - 苄基） - 苯衍生物，含有这些化合物的药物，它们的用途和制造方法公开(公告)号：US20060189548A1
公开(公告)日：2006-08-24
申请号：US11359846
申请日：2006-02-22
IPC分类号： A61K31/7052 , C07H17/02
CPC分类号： C07D309/10 , C07D405/10 , C07D409/10 , C07D413/10 , C07D417/10
摘要： Glucopyranosyl-substituted (hetero)arylethynyl-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： 基团R 1至R 6以及R 7a的通式I的吡喃葡糖基取代的（杂）芳基乙炔基 - 苯衍生物， R 7b，R 7c，如权利要求1所定义，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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62.发明申请D-xylopyranosyl-phenyl-substituted cycles, medicaments containing such compounds, their use and process for their manufacture 有权D-吡喃木糖基 - 苯基取代的周期，含有这些化合物的药物，它们的用途和制造方法公开(公告)号：US20060025349A1
公开(公告)日：2006-02-02
申请号：US11190315
申请日：2005-07-27
IPC分类号： A61K31/704 , A61K31/70 , C07H17/02
CPC分类号： C07H7/04 , C07D309/10 , C07D309/12 , C07D309/22 , C07D405/10 , C07D405/12 , C07D407/10 , C07D407/12
摘要： D-Glucopyranosyl-phenyl-substituted cycles of general formula I wherein the groups R1 to R6, Z, Cy and R7a, R7b, R7c, R7d are defined as in claim 1, have an inhibiting effect on the sodium-dependent glucose cotransporter SGLT. The present invention also relates to pharmaceutical compositions for the treatment of metabolic disorders.
摘要翻译： 通式I的D-吡喃葡糖基 - 苯基取代的环，其中基团R 1至R 6，Z，Cy和R 7a，R R 7，R 7，R 7，R 7，如权利要求1中所定义，对钠依赖性葡萄糖转运蛋白SGLT具有抑制作用。 本发明还涉及用于治疗代谢紊乱的药物组合物。
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63.发明申请D-xylopyranosyl-substituted phenyl derivatives, medicaments containing such compounds, their use and process for their manufacture 有权D-吡喃木糖基取代的苯基衍生物，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：US20060009400A1
公开(公告)日：2006-01-12
申请号：US11168905
申请日：2005-06-28
IPC分类号： C07H17/02 , A61K31/704
摘要： A D-Xylopyranosyl-substituted phenyl compound of general formula I wherein the groups R1 to R5, X, Z and R7a, R7b, R7c are defined as in claim 1, have an inhibiting effect on the sodium-dependent glucose cotransporter SGLT. The present invention also relates to pharmaceutical compositions for the treatment of metabolic disorders.
摘要翻译： 通式I的D-吡喃葡萄糖基取代的苯基化合物，其中基团R 1至R 5，X，Z和R 7a，R 如权利要求1中所定义，R 7，R 7c对钠依赖性葡萄糖转运蛋白SGLT具有抑制作用。 本发明还涉及用于治疗代谢紊乱的药物组合物。
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![2-Amino-imidazo[4,5-d]pyridazin-4-ones, their preparation and their use as pharmaceutical compositions](/abs-image/US/2005/10/20/US20050234235A1/abs.jpg.150x150.jpg)
64.发明申请2-Amino-imidazo[4,5-d]pyridazin-4-ones, their preparation and their use as pharmaceutical compositions 有权2-氨基 - 咪唑并[4,5-d]哒嗪-4-酮，它们的制备及其作为药物组合物的用途公开(公告)号：US20050234235A1
公开(公告)日：2005-10-20
申请号：US11102048
申请日：2005-04-08
申请人： Matthias Eckhardt , Frank Himmelsbach , Elke Langkopf , Norbert Hauel , Mohammad Tadayyon , Leo Thomas
发明人： Matthias Eckhardt , Frank Himmelsbach , Elke Langkopf , Norbert Hauel , Mohammad Tadayyon , Leo Thomas
IPC分类号： A61K31/503 , C07D487/02
CPC分类号： C07D487/04 , C07D471/04
摘要： The present invention relates to 2-amino-imidazo[4,5-d]pyridazin-4-ones and 2-amino-imidazo[4,5-c]pyridin-4-ones of general formula wherein R1 to R4 and X are defined as in claims 1 to 6, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译： 本发明涉及以下通式的2-氨基 - 咪唑并[4,5-d]哒嗪-4-酮和2-氨基 - 咪唑并[4,5-c]吡啶-4-酮，其中R 1， R 4和X如权利要求1至6中所定义，其互变异构体，对映异构体，非对映异构体，其混合物及其盐具有有价值的药理学性质，特别是抑制 对二肽基肽酶-IV（DPP-IV）酶活性的影响。
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65.发明申请Glucopyranosyl-substituted phenyl derivatives, medicaments containing such compounds, their use and process for their manufacture 有权吡喃葡糖基取代的苯基衍生物，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：US20050209166A1
公开(公告)日：2005-09-22
申请号：US11080150
申请日：2005-03-15
IPC分类号： A61K31/70 , A61K31/7004 , A61P3/00 , C07D309/10 , C07H15/04 , C07H15/20 , C07H15/26
CPC分类号： C07H23/00 , A61K9/0019 , A61K9/02 , A61K9/2018 , A61K9/4866 , C07D309/10 , C07H15/04 , C07H15/20 , C07H15/26
摘要： Glucopyranosyl-substituted benzene derivatives of general formula I where the groups R1 to R6 as well as R7a, R7b, R7c are defined herein and 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： 通式I的吡喃葡糖基取代的苯衍生物，其中基团R 1至R 6以及R 7a，R 7b， 本文所定义的R 7c和互变异构体，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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66.发明申请Imidazopyridazinediones, their preparation and their use as pharmaceutical compositions 有权咪唑并哒嗪酮，其制备及其作为药物组合物的用途公开(公告)号：US20050203095A1
公开(公告)日：2005-09-15
申请号：US11075791
申请日：2005-03-09
申请人： Matthias Eckhardt , Frank Himmelsbach , Iris Kauffmann-Hefner , Elke Langkopf , Mohammad Tadayyon , Leo Thomas
发明人： Matthias Eckhardt , Frank Himmelsbach , Iris Kauffmann-Hefner , Elke Langkopf , Mohammad Tadayyon , Leo Thomas
IPC分类号： A61K31/503 , C07D487/02
CPC分类号： C07D487/04
摘要： The invention relates to substituted imidazopyridazinediones of general formula wherein R1 and R4 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译： 本发明涉及通式的取代咪唑并哒嗪酮，其中R 1和R 4定义如权利要求1，互变异构体，对映异构体，非对映异构体，其混合物和 其具有有价值的药理学性质，特别是对二肽基肽酶-IV（DPP-IV）的活性的抑制作用。
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67.发明申请New substituted imidazo-pyridinones and imidazo-pyridazinones, the preparation thereof and their use as pharmaceutical compositions 有权新的取代的咪唑并 - 吡啶酮和咪唑并哒嗪酮，其制备及其作为药物组合物的用途公开(公告)号：US20050020574A1
公开(公告)日：2005-01-27
申请号：US10726214
申请日：2003-12-02
申请人： Norbert Hauel , Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Roland Maier , Michael Mark , Mohammad Tadayyon , Iris Kauffmann-Hefner
发明人： Norbert Hauel , Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Roland Maier , Michael Mark , Mohammad Tadayyon , Iris Kauffmann-Hefner
IPC分类号： C07D471/04 , C07D487/04 , C07D519/00 , C07D471/02 , A61K31/4745 , A61K31/503 , A61K31/55 , C07D487/02
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein R1 to R4 are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译： 本发明涉及通式的取代的咪唑并 - 吡啶酮和咪唑并哒嗪酮，其中R 1至R 4如权利要求1所定义，互变异构体，立体异构体，其混合物及其盐具有有价值的 药理特性，特别是酶二肽肽酶-IV（DPP-IV）的活性的抑制作用。
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68.发明授权公开(公告)号：US09328072B2
公开(公告)日：2016-05-03
申请号：US13922889
申请日：2013-06-20
IPC分类号： C07D401/06 , C07D417/06 , C07D413/14 , C07D221/06 , C07D471/04 , C07D221/10 , C07D401/12 , C07D401/14 , C07D405/14 , C07D498/04
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.
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69.发明授权Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use 有权苯并呋喃和相关支架的脂环族羧酸衍生物，含有这些化合物的药物及其应用公开(公告)号：US09073870B2
公开(公告)日：2015-07-07
申请号：US14191951
申请日：2014-02-27
IPC分类号： A61K31/439 , C07D221/22 , C07D221/26 , C07D471/18 , C07D491/18 , C07D401/06 , C07D401/08 , C07D401/12 , C07D405/06 , C07D405/12 , C07D491/08
CPC分类号： C07D221/26 , C07D221/22 , C07D401/06 , C07D401/08 , C07D401/12 , C07D405/06 , C07D405/12 , C07D471/18 , C07D491/08 , C07D491/18
摘要： The present invention relates to compounds defined by formula I wherein the groups A, B, 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，其中基团A，B，X，m，n和o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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70.发明授权公开(公告)号：US08933072B2
公开(公告)日：2015-01-13
申请号：US13703708
申请日：2011-06-15
申请人： Matthias Eckhardt , Frank Himmelsbach , Katerina Leftheris , Suresh B. Singh , Colin M. Tice , Zhenrong Xu , Yuanjie Ye , Linghang Zhuang
发明人： Matthias Eckhardt , Frank Himmelsbach , Katerina Leftheris , Suresh B. Singh , Colin M. Tice , Zhenrong Xu , Yuanjie Ye , Linghang Zhuang
IPC分类号： C07D413/14 , C07D413/12 , C07D413/10 , A61K31/5355
CPC分类号： C07D417/14 , A61K31/5355 , C07D413/10 , C07D413/14
摘要： Disclosed are compounds represented by Formula (I): or pharmaceutically acceptable salts, enantiomers or diastereomers thereof. Also disclosed are pharmaceutical compositions comprising the compounds of Formula (I) or pharmaceutically acceptable salts, enantiomers or diastereomers thereof for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. Values for the variables of Formula (I) are defined herein.
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