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公开(公告)号：US20140163025A1
公开(公告)日：2014-06-12
申请号：US14093583
申请日：2013-12-02
申请人： Matthias ECKHARDT , Sara FRATTINI , Elke LANGKOPF , Holger WAGNER
发明人： Matthias ECKHARDT , Sara FRATTINI , Elke LANGKOPF , Holger WAGNER
IPC分类号： A61K31/5377 , A61K31/343 , A61K31/4025 , C07D405/12 , A61K45/06 , A61K31/41 , C07D405/14 , A61K31/443 , A61K31/4155 , C07D307/80 , A61K31/4178
CPC分类号： A61K31/343 , A61K31/085 , A61K31/09 , A61K31/192 , A61K31/34 , A61K31/351 , A61K31/357 , A61K31/36 , A61K31/4025 , A61K31/404 , A61K31/41 , A61K31/4155 , A61K31/416 , A61K31/4178 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/443 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D307/80 , C07D401/12 , C07D405/12 , C07D405/14 , C07D407/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to compounds of general formula I, wherein the groups (Het)Ar and R1 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，其中基团（Het）Ar和R 1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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公开(公告)号：US20130252937A1
公开(公告)日：2013-09-26
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： C07D405/12 , A61K31/343 , C07D307/80 , A61K31/351 , A61K31/506 , C07D413/12 , A61K31/422 , A61K31/4155 , A61K31/443 , A61K31/397 , C07D409/12 , A61K31/382 , C07D417/12 , A61K31/427 , A61K31/541 , A61K31/4025 , A61K31/4196 , A61K31/513 , A61K31/501 , A61K31/41 , C07D405/14 , A61K31/497 , C07D413/14 , A61K31/553 , A61K31/5377 , A61K31/4178 , A61K31/4245 , A61K45/06 , C07D407/12
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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公开(公告)号：US20140148462A1
公开(公告)日：2014-05-29
申请号：US14088493
申请日：2013-11-25
申请人： Matthias ECKHARDT , Elke LANGKOPF , Holger WAGNER
发明人： Matthias ECKHARDT , Elke LANGKOPF , Holger WAGNER
IPC分类号： A61K31/506 , A61K31/343 , C07D401/12 , A61K31/443 , C07D403/12 , A61K45/06 , C07D417/12 , A61K31/428 , C07D405/12 , A61K31/4184 , A61K31/501 , C07D307/80 , A61K31/497
CPC分类号： A61K31/506 , A61K31/343 , A61K31/4184 , A61K31/428 , A61K31/443 , A61K31/497 , A61K31/501 , A61K45/06 , C07D307/80 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to compounds of general formula I, wherein the group (Het)Ar is 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（Het）Ar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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4.发明申请Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions 审中-公开黄嘌呤衍生物，其制备及其作为药物组合物的用途公开(公告)号：US20100204250A1
公开(公告)日：2010-08-12
申请号：US12767855
申请日：2010-04-27
申请人： Frank HIMMELSBACH , Michael MARK , Matthias ECKHARDT , Elke LANGKOPF , Roland MAIER , Ralf LOTZ
发明人： Frank HIMMELSBACH , Michael MARK , Matthias ECKHARDT , Elke LANGKOPF , Roland MAIER , Ralf LOTZ
IPC分类号： A61K31/522 , C07D473/28 , A61P3/04 , A61P3/08
CPC分类号： C07D473/08 , C07D473/04 , C07D473/06 , C07D473/10 , C07D473/12
摘要： The present invention relates to substituted xanthines of general formula wherein R1 to R4 are as defined herein, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs 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R4如本文所定义的取代黄嘌呤，其互变异构体及其立体异构体，其混合物，其前体药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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5.发明申请IMIDAZOLES AND TRIAZOLES, THEIR PREPARATION, AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS 有权咪唑和三唑，其制备及其作为药物组合物的用途公开(公告)号：US20080312243A1
公开(公告)日：2008-12-18
申请号：US12192589
申请日：2008-08-15
IPC分类号： A61K31/4439 , A61K31/498 , A61P3/10
CPC分类号： C07D471/04 , C07D249/14 , C07D401/04 , C07D401/12 , C07D401/14
摘要： The present invention relates to imidazoles and triazoles of general formula wherein R1 to R4 and X are defined as in claims 1 to 8, 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： 本发明涉及通式的咪唑和三唑，其中R 1至R 4和X如权利要求1至8中所定义，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）的活性具有抑制作用。
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6.发明申请XANTHINE DERIVATIVES, THE PREPARATION THEREOF AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS 审中-公开XANTHINE衍生物，其制备方法及其作为药物组合物的用途公开(公告)号：US20100144703A1
公开(公告)日：2010-06-10
申请号：US12706739
申请日：2010-02-17
申请人： Frank HIMMELSBACH , Elke LANGKOPF , Matthias ECKHARDT , Roland MAIER , Michael MARK , Mohammad TADAYYON , Ralf R. H. LOTZ
发明人： Frank HIMMELSBACH , Elke LANGKOPF , Matthias ECKHARDT , Roland MAIER , Michael MARK , Mohammad TADAYYON , Ralf R. H. LOTZ
IPC分类号： A61K31/553 , C07D473/04 , A61K31/522 , A61K31/5513 , A61K31/554
CPC分类号： C07D473/06
摘要： Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs 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： 公开了以下通式的取代黄嘌呤：其中R1至R4定义如下，其互变异构体，立体异构体，其混合物，其前体药物及其盐具有有价值的药理学性质，特别是对酶二肽基肽酶的活性的抑制作用 -IV（DPP-IV）。
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7.发明申请XANTHINE DERIVATIVES, THE PREPARATION THEREOF AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS 有权XANTHINE衍生物，其制备方法及其作为药物组合物的用途公开(公告)号：US20090093457A1
公开(公告)日：2009-04-09
申请号：US12331720
申请日：2008-12-10
申请人： Frank HIMMELSBACH , Elke LANGKOPF , Matthias ECKHARDT , Roland MAIER , Michael MARK , Mohammad TADAYYON , Ralf R. H. LOTZ
发明人： Frank HIMMELSBACH , Elke LANGKOPF , Matthias ECKHARDT , Roland MAIER , Michael MARK , Mohammad TADAYYON , Ralf R. H. LOTZ
IPC分类号： A61K31/522 , C07D473/04 , C07D265/14 , C07D279/16 , A61K31/54 , A61K31/554 , A61P3/00 , A61K31/5513 , A61K31/536 , C07D243/12 , C07D285/36
CPC分类号： C07D473/06
摘要： Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs 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： 公开了以下通式的取代黄嘌呤：其中R1至R4定义如下，其互变异构体，立体异构体，其混合物，其前体药物及其盐具有有价值的药理学性质，特别是对酶二肽基肽酶的活性的抑制作用 -IV（DPP-IV）。
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8.发明申请Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions 审中-公开黄嘌呤衍生物，其制备及其作为药物组合物的用途公开(公告)号：US20120252783A1
公开(公告)日：2012-10-04
申请号：US13523939
申请日：2012-06-15
申请人： Frank HIMMELSBACH , Michael MARK , Matthias ECKHARDT , Elke LANGKOPF , Roland MAIER , Ralf LOTZ
发明人： Frank HIMMELSBACH , Michael MARK , Matthias ECKHARDT , Elke LANGKOPF , Roland MAIER , Ralf LOTZ
IPC分类号： A61K31/522 , A61K31/55 , A61P3/10 , A61K31/5377 , A61P3/04 , C07D473/08 , C07D473/06
CPC分类号： C07D473/08 , C07D473/04 , C07D473/06 , C07D473/10 , C07D473/12
摘要： The present invention relates to substituted xanthines of general formula wherein R1 to R4 are as defined herein, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs 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R4如本文所定义的取代黄嘌呤，其互变异构体及其立体异构体，其混合物，其前体药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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![8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions](/abs-image/US/2012/08/16/US20120208831A1/abs.jpg.150x150.jpg)
公开(公告)号：US20120208831A1
公开(公告)日：2012-08-16
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
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).
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10.发明申请公开(公告)号：US20120040982A1
公开(公告)日：2012-02-16
申请号：US13280396
申请日：2011-10-25
申请人： Frank HIMMELSBACH , Michael MARK , Matthias ECKHARDT , Elke LANGKOPF , Roland MAIER , Ralf LOTZ
发明人： Frank HIMMELSBACH , Michael MARK , Matthias ECKHARDT , Elke LANGKOPF , Roland MAIER , Ralf LOTZ
IPC分类号： A61K31/5377 , A61P3/10 , C07D413/14 , A61P3/04 , A61K31/522 , C07D473/00
CPC分类号： C07D473/08 , C07D473/04 , C07D473/06 , C07D473/10 , C07D473/12
摘要： The present invention relates to substituted xanthines of general formula wherein R1 to R4 are as defined herein, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
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