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41.发明授权Substituted imidazo-pyridinones and imidazo-pyridazinones, the preparation thereof and their use as pharmaceutical compositions 有权取代的咪唑并 - 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：US07109192B2
公开(公告)日：2006-09-19
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： C07D487/04 , C07D471/04 , A61K31/5025 , A61K31/437
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定义如权利要求1，互变异构体，立体异构体， 其具有有价值的药理学特性的其混合物及其盐，特别是酶二肽基肽酶-IV（DPP-IV）的活性的抑制作用。
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42.发明申请Bicyclic imidazole derivatives, the preparation thereof and their use as pharmaceutical compositions 有权双环咪唑衍生物，其制备及其作为药物组合物的用途公开(公告)号：US20050143377A1
公开(公告)日：2005-06-30
申请号：US11018894
申请日：2004-12-21
申请人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Norbert Hauel , Mohammad Tadayyon , Leo Thomas
发明人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Norbert Hauel , Mohammad Tadayyon , Leo Thomas
IPC分类号： A61K31/519 , A61K31/522 , A61K31/5377 , A61P3/00 , A61P19/00 , C07D473/02 , C07D473/04 , C07D473/06 , C07D487/04
CPC分类号： C07D473/04 , C07D473/06 , C07D487/04
摘要： The present invention relates to bicyclic imidazole compounds of general formula wherein R1 to R3 and A are defined as in claims 1 to 8, the tautomers, the enantiomers, the stereoisomers, 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： 本发明涉及通式的双环咪唑化合物，其中R 1至R 3和A如权利要求1至8中所定义，互变异构体，对映异构体，立体异构体 ，其混合物及其盐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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43.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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![8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions](/abs-image/US/2014/04/15/US08697868B2/abs.jpg.150x150.jpg)
44.发明授权8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions 有权8- [3-氨基 - 哌啶-1-基] - 黄嘌呤，它们的制备及其作为药物组合物的用途公开(公告)号：US08697868B2
公开(公告)日：2014-04-15
申请号：US12360392
申请日：2009-01-27
IPC分类号： C07D473/00 , C07D473/02 , C07D473/04
CPC分类号： C07D473/04
摘要： Disclosed are substituted xanthines of the formula wherein R is defined as in claim 1, the tautomers, the stereoisomers, 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： 公开了下式的取代黄嘌呤：其中R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学性质，特别是对二肽基肽酶-IV酶活性的抑制作用 DPP-IV）。
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![8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions](/abs-image/US/2014/03/04/US08664232B2/abs.jpg.150x150.jpg)
45.发明授权8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions 有权8- [3-氨基 - 哌啶-1-基] - 黄嘌呤，其制备及其作为药物组合物的用途公开(公告)号：US08664232B2
公开(公告)日：2014-03-04
申请号：US13448495
申请日：2012-04-17
申请人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Michael Mark , Roland Maier , Ralf R. H. Lotz , Mohammad Tadayyon
发明人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Michael Mark , Roland Maier , Ralf R. H. Lotz , Mohammad Tadayyon
IPC分类号： A01N43/90 , C07D473/00
CPC分类号： C07D473/04 , C07D473/06 , C07D473/08 , C07D519/00
摘要： The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, the tautomers, the stereoisomers, the mixtures, the prodrugs 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： 本发明涉及通式为其中R1至R3如本文所定义的取代黄嘌呤，其互变异构体，立体异构体，混合物，其前药及其盐具有有价值的药理学性质，特别是对 酶二肽肽酶-IV（DPP-IV）。
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46.发明授权Aryl- and heteroarylcarbonyl derivatives of hexahydroindenopyridine and octahydrobenzoquinoline 有权六氢茚基吡啶和八氢苯并喹啉的芳基和杂芳基羰基衍生物公开(公告)号：US08497281B2
公开(公告)日：2013-07-30
申请号：US12940387
申请日：2010-11-05
IPC分类号： C07D401/06 , A61K31/352
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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47.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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48.发明申请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：US20110269791A1
公开(公告)日：2011-11-03
申请号：US12991722
申请日：2009-05-12
申请人： Stefan Peters , Matthias Eckhardt , Bradford S. Hamilton , Frank Himmelsbach , Joerg Kley , Thorsten Lehmann-Lintz
发明人： Stefan Peters , Matthias Eckhardt , Bradford S. Hamilton , Frank Himmelsbach , Joerg Kley , Thorsten Lehmann-Lintz
IPC分类号： A61K31/439 , A61K31/4985 , A61P3/10 , A61K31/397 , A61P3/00 , A61P3/06 , C07D471/04 , C07D221/26
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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49.发明授权Imidazopyridazinone and imidazopyridone derivatives, the preparation thereof and their use as pharmaceutical compositions 有权咪唑并哒嗪酮和咪唑并吡酮衍生物，其制备及其作为药物组合物的用途公开(公告)号：US08034941B2
公开(公告)日：2011-10-11
申请号：US12489716
申请日：2009-06-23
申请人： Matthias Eckhardt , Norbert Hauel , Elke Langkopf , Frank Himmelsbach , Iris Kauffmann-Hefner , Mohammad Tadayyon , Michael Mark
发明人： Matthias Eckhardt , Norbert Hauel , Elke Langkopf , Frank Himmelsbach , Iris Kauffmann-Hefner , Mohammad Tadayyon , Michael Mark
IPC分类号： C07D515/02
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 Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, 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的咪唑并 - 吡啶酮和咪唑并哒嗪酮，其中Y和R 1至R 4如权利要求1所定义，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， 特别是对二肽基肽酶-IV（DPP-IV）的活性的抑制作用。
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50.发明授权Tetrasubstituted glucopyranosylated benzene derivatives, medicaments containing such compounds, their use and process for their manufacture 有权四取代的吡喃葡萄糖基化苯衍生物，含有此类化合物的药物，其用途及其制备方法公开(公告)号：US07879807B2
公开(公告)日：2011-02-01
申请号：US12527774
申请日：2008-02-20
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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