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51.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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52.发明授权Benzothiazoles and benzoxazoles, drugs containing them, their use and methods of preparing them 失效苯并噻唑和苯并恶唑，含有它们的药物，其用途和制备方法
公开(公告)号：US5919807A
公开(公告)日：1999-07-06
申请号：US945612
申请日：1997-10-28
申请人： Peter Muller , Rudolph Hurnaus , Roland Maier , Michael Mark , Bernhard Eisele , Ralph-Michael Budzinski , Leo Thomas , Gerhard Hallermayer
发明人： Peter Muller , Rudolph Hurnaus , Roland Maier , Michael Mark , Bernhard Eisele , Ralph-Michael Budzinski , Leo Thomas , Gerhard Hallermayer
IPC分类号： A23K20/137 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61P1/16 , A61P3/06 , A61P3/08 , A61P31/04 , A61P35/00 , C07D263/56 , C07D277/64 , C07D277/66 , C07D277/68 , C07D277/74 , C07D277/76 , C07D277/82 , C07D417/04 , C07D417/12
CPC分类号： C07D263/56 , A23K20/137 , C07D277/64 , C07D277/66 , C07D277/68 , C07D277/74 , C07D277/76 , C07D417/04 , C07D417/12
摘要： The invention relates to benzothiazoles and benzoxazoles of general formula ##STR1## wherein R.sup.1 to R.sup.3, X, Z and n are defined as in claim 1, the enantiomers, diastereomers and salts thereof, particularly the physiologically acceptable acid addition salts thereof which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.
摘要翻译： PCT No.PCT / EP96 / 01827 Sec。 371日期1997年10月28日第 102（e）1997年10月28日PCT PCT 1996年5月2日PCT公布。 公开号WO96 / 35681 日期：1996年11月14日本发明涉及以下通式的苯并噻唑和苯并恶唑：其中R1至R3，X，Z和n如权利要求1所定义，其对映体，非对映异构体及其盐，特别是其生理上可接受的酸加成盐， 有价值的性质，特别是对胆固醇生物合成的抑制作用，含有这些化合物的药物组合物，其用途及其制备方法。
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53.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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公开(公告)号：US20110092510A1
公开(公告)日：2011-04-21
申请号：US12995474
申请日：2009-06-02
申请人： Thomas Klein , Michael Mark , Heiko Niessen , Leo Thomas
发明人： Thomas Klein , Michael Mark , Heiko Niessen , Leo Thomas
IPC分类号： A61K31/4985 , A61K31/40 , A61K31/403 , A61K31/506 , A61K31/52 , A61K31/5025 , A61K31/519 , A61K31/4439 , A61P3/00 , A61P9/10 , A61P29/00 , A61P9/12
CPC分类号： A61K31/40 , A61K31/155 , A61K31/403 , A61K31/41 , A61K31/4184 , A61K31/4196 , A61K31/422 , A61K31/4375 , A61K31/4439 , A61K31/4985 , A61K31/5025 , A61K31/506 , A61K31/513 , A61K31/519 , A61K31/522 , A61K31/53 , A61K45/06 , A61P1/16 , A61K2300/00
摘要： The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for treating and/or preventing non alcoholic fatty liver diseases (NAFLD).
摘要翻译： 本发明涉及某些DPP-4抑制剂特别适用于治疗和/或预防非酒精性脂肪肝疾病（NAFLD）的发现。
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55.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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56.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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57.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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![8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical composition](/abs-image/US/2010/01/12/US07645763B2/abs.jpg.150x150.jpg)
58.发明授权8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical composition 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：US07645763B2
公开(公告)日：2010-01-12
申请号：US11062518
申请日：2005-02-22
IPC分类号： C07D473/06 , C07D519/00 , A61K31/522 , A61P3/10 , A61P3/04
CPC分类号： C07D473/06
摘要： The present invention relates to substituted xanthines of general formula wherein R1 and R2 are defined as in the claims, 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： 本发明涉及通式的取代黄嘌呤：其中R 1和R 2如权利要求中所定义，其互变异构体，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 酶二肽肽酶-IV（DPP-IV）。
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![2-amino-imidazo[4,5-d]pyridazin-4-ones, their preparation and their use as pharmaceutical compositions](/abs-image/US/2009/01/13/US07476671B2/abs.jpg.150x150.jpg)
59.发明授权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：US07476671B2
公开(公告)日：2009-01-13
申请号：US11609621
申请日：2006-12-12
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： A61K31/5355 , A61K31/497 , A61K31/4439 , A61K31/4166 , C07D491/04 , C07D487/04 , C07D471/04 , A61P3/10
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R1至R4和X为 如权利要求1至6中定义的互变异构体，对映异构体，非对映体，其混合物及其盐，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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![Crystalline form of 1'-(1-methylethyl)-4'-[(2-fluoro-4-methoxyphenyl)methyl]-5'-methyl-1H-pyrazol-3'-O-beta-D-glucopyranoside, a method for its preparation and the use thereof for preparing medicaments](/abs-image/US/2007/10/18/US20070244176A1/abs.jpg.150x150.jpg)
60.发明申请Crystalline form of 1'-(1-methylethyl)-4'-[(2-fluoro-4-methoxyphenyl)methyl]-5'-methyl-1H-pyrazol-3'-O-beta-D-glucopyranoside, a method for its preparation and the use thereof for preparing medicaments 失效1' - （1-甲基乙基）-4' - [（2-氟-4-甲氧基苯基）甲基] -5'-甲基-1H-吡唑-3'-O-β-D-吡喃葡萄糖苷的结晶形式， 用于其制备和用于制备药物的用途公开(公告)号：US20070244176A1
公开(公告)日：2007-10-18
申请号：US11621859
申请日：2007-01-10
申请人： Gerd Kraemer , Hans-Juergen Martin , Gebhard Adelgoss , Klaus Dugi , Adil Duran , Peter Eickelmann , Steffen Maier , Sabine Pinnetti , Regine Ritter , Gebhard Schilcher , Ruediger Streicher , Leo Thomas
发明人： Gerd Kraemer , Hans-Juergen Martin , Gebhard Adelgoss , Klaus Dugi , Adil Duran , Peter Eickelmann , Steffen Maier , Sabine Pinnetti , Regine Ritter , Gebhard Schilcher , Ruediger Streicher , Leo Thomas
IPC分类号： A61K31/415 , C07D231/00
CPC分类号： C07H17/02
摘要： The invention relates to a crystalline form of 1′-(1-methylethyl)-4′-[(2-fluoro-4-methoxyphenyl)methyl]-5′-methyl-1H-pyrazol-3′-O-β-D-glucopyranoside, to a method for the preparation thereof, as well as to the use thereof for preparing medicaments.
摘要翻译： 本发明涉及1' - （1-甲基乙基）-4' - [（2-氟-4-甲氧基苯基）甲基] -5'-甲基-1H-吡唑-3'-O-β-D - 吡喃葡萄糖苷，其制备方法，以及其用于制备药物的用途。
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