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31.发明授权Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions 有权黄嘌呤衍生物，其制备及其作为药物组合物的用途公开(公告)号：US07696212B2
公开(公告)日：2010-04-13
申请号：US12331720
申请日：2008-12-10
申请人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Roland Maier , Ralf Lotz , Michael Mark , Mohammad Tadayyon
发明人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Roland Maier , Ralf Lotz , Michael Mark , Mohammad Tadayyon
IPC分类号： C07D473/06 , C07D519/00 , A61K31/522 , A61K31/538 , A61K31/536 , A61K31/5415 , A61K31/5513 , A61P3/10 , A61P3/04
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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32.发明授权Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions 有权黄嘌呤衍生物，其制备及其作为药物组合物的用途公开(公告)号：US07560450B2
公开(公告)日：2009-07-14
申请号：US10716141
申请日：2003-11-18
申请人： Matthias Eckhardt , Frank Himmelsbach , Elke Langkopf , Roland Maier , Michael Mark , Mohammad Tadayyon
发明人： Matthias Eckhardt , Frank Himmelsbach , Elke Langkopf , Roland Maier , Michael Mark , Mohammad Tadayyon
IPC分类号： C07D473/06 , A61K31/522 , A61P3/10 , A61P3/04
CPC分类号： C07D473/04 , C07D473/06 , C07D473/08
摘要： The present invention relates to substituted xanthines of general formula 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： 本发明涉及具有有价值的药理学特性的互变异构体，立体异构体，其混合物，其前体药物及其盐的通式的取代黄嘌呤，特别是对酶二肽基肽酶-IV（DPP- IV）。
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33.发明授权Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions 有权黄嘌呤衍生物，其制备及其作为药物组合物的用途公开(公告)号：US07482337B2
公开(公告)日：2009-01-27
申请号：US10695597
申请日：2003-10-28
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： C07D473/06 , C07D519/00 , A61K31/522 , A61K31/538 , A61K31/536 , A61K31/5415 , A61K31/5513 , A61P3/10 , A61P3/04
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-[3-AMINO-PIPERIDIN-1-YL]-XANTHINES, THE PREPARATION THEREOF AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS](/abs-image/US/2008/10/16/US20080255159A1/abs.jpg.150x150.jpg)
34.发明申请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] - 辛糖，其制备方法及其作为药物组合物的用途公开(公告)号：US20080255159A1
公开(公告)日：2008-10-16
申请号：US12143219
申请日：2008-06-20
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： A61K31/522 , C07D473/04 , A61P3/10 , A61P3/04
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 defined as in claims 1 to 16, 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： 本发明涉及以下通式的取代黄嘌呤：其中R 1至R 3定义如权利要求1至16中所定义，互变异构体，立体异构体，混合物，前体药物 其具有有价值的药理学特性的盐，特别是对二肽基肽酶-IV（DPP-IV）的活性的抑制作用。
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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)
35.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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36.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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37.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：US07566707B2
公开(公告)日：2009-07-28
申请号：US10865719
申请日：2004-06-10
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： A61P7/12 , A61P3/04 , A61P19/00 , A61K31/55 , A61K31/553 , A61K31/554 , A61K31/54 , A61K31/535 , A61K31/495 , A61K31/50 , C07D223/00 , C07D273/00 , C07D285/00 , C07D243/00 , C07D267/00 , C07D281/00 , C07D291/00 , C07D498/00 , C07D513/00 , C07D515/00 , C07D487/00 , C07D491/00 , C07D279/00 , C07D265/00
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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![8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions](/abs-image/US/2008/08/05/US07407955B2/abs.jpg.150x150.jpg)
38.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：US07407955B2
公开(公告)日：2008-08-05
申请号：US10639036
申请日：2003-08-12
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： C07D473/06 , A61K31/52 , A61P3/10 , A61P19/02 , A61P3/04 , C07D519/00
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 defined as in claims 1 to 16, 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： 本发明涉及以下通式的取代黄嘌呤：其中R 1至R 3定义如权利要求1至16中所定义，互变异构体，立体异构体，混合物，前体药物 其具有有价值的药理学特性的盐，特别是对二肽基肽酶-IV（DPP-IV）的活性的抑制作用。
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39.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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公开(公告)号：US08809376B2
公开(公告)日：2014-08-19
申请号：US13869144
申请日：2013-04-24
IPC分类号： A61K31/44 , C07D307/87
CPC分类号： C07D307/80 , A61K31/343 , A61K31/443 , A61K45/06 , C07D405/12 , A61K2300/00
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.
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