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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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公开(公告)号：US08642585B2
公开(公告)日：2014-02-04
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： A61K31/553 , C07D267/10 , A61K31/443 , C07D405/02 , A61K31/4155 , C07D231/10 , A61K31/422 , C07D263/30 , A61K31/4178 , C07D233/54 , A61K31/4245 , C07D271/06 , A61K31/427 , C07D277/20 , A61K31/501 , C07D403/02 , A61K31/5377 , C07D413/14 , A61K31/497 , C07D307/77 , A61K31/343 , C07D257/02 , A61K31/506 , A61K31/41 , C07D249/08 , A61K31/4196 , A61K31/4025 , C07D409/02 , A61K31/382 , C07D413/02
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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![Piperazin-1-yl and 2-([1,4]diazepan-1-yl)-imidazo[4,5-d]-pyridazin-4-ones, the preparation thereof and their use as pharmaceutical compositions](/abs-image/US/2007/05/15/US07217711B2/abs.jpg.150x150.jpg)
3.发明授权Piperazin-1-yl and 2-([1,4]diazepan-1-yl)-imidazo[4,5-d]-pyridazin-4-ones, the preparation thereof and their use as pharmaceutical compositions 有权哌嗪-1-基和2 - （[1,4]二氮杂环庚烷-1-基） - 咪唑并[4,5-d] - 哒嗪-4-酮的制备及其作为药物组合物的用途公开(公告)号：US07217711B2
公开(公告)日：2007-05-15
申请号：US11016176
申请日：2004-12-17
申请人： Matthias Eckhardt , Norbert Hauel , Frank Himmelsbach , Iris Kauffmann-Hefner , Elke Langkopf , Mohammad Tadayyon , Leo Thomas
发明人： Matthias Eckhardt , Norbert Hauel , Frank Himmelsbach , Iris Kauffmann-Hefner , Elke Langkopf , Mohammad Tadayyon , Leo Thomas
IPC分类号： C07D487/04 , A61K31/5025 , A61P3/10
CPC分类号： C07D487/04
摘要： The present invention relates to substituted imidazo[4,5-d]pyridazin-4-ones of general formula wherein R1 to R3 and n are defined as in claims 1 to 8, the tautomers, enantiomers, diastereomers, 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取代咪唑并[4,5-d]哒嗪-4-酮：其中R 1至R 3和n如权利要求1中所定义 至8，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，特别是对二肽基肽酶-IV（DPP-IV）的活性的抑制作用。
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4.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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5.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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![8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions](/abs-image/US/2012/02/21/US08119648B2/abs.jpg.150x150.jpg)
公开(公告)号：US08119648B2
公开(公告)日：2012-02-21
申请号：US12143219
申请日：2008-06-20
申请人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Michael Mark , Roland Maier , Ralf Lotz
发明人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Michael Mark , Roland Maier , Ralf Lotz
IPC分类号： A61P3/10 , A61P3/04 , A61P19/02 , C07D473/06 , C07D519/00 , A61K31/53
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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7.发明授权Imidazoles and triazoles, their preparation, and their use as pharmaceutical compositions 有权咪唑和三唑，它们的制备及其作为药物组合物的用途公开(公告)号：US07906539B2
公开(公告)日：2011-03-15
申请号：US12192589
申请日：2008-08-15
IPC分类号： A61K31/41 , A61K31/426 , A61K31/4192 , C07D249/08 , C07D233/00
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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![8-(piperazin-1yl)- and 8-([1,4]diazepan-1yl)-xanthines, the preparation thereof and their use as pharmaceutical composition](/abs-image/US/2009/06/23/US07550455B2/abs.jpg.150x150.jpg)
8.发明授权8-(piperazin-1yl)- and 8-([1,4]diazepan-1yl)-xanthines, the preparation thereof and their use as pharmaceutical composition 有权8-（哌嗪-1-基） - 和8 - （[1,4]二氮杂环庚烷-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：US07550455B2
公开(公告)日：2009-06-23
申请号：US10979468
申请日：2004-11-02
IPC分类号： C07D473/06 , C07D519/00 , A61K31/522 , A61P3/10 , A61P3/04
CPC分类号： C07D519/00 , C07D473/04
摘要： The present invention relates to substituted xanthines of the general formula in which R1 to R3 and n are as defined in claims 1 to 8, their tautomers, their enantiomers, their diastereomers, their mixtures, their prodrugs and their salts, which have valuable pharmacological properties, in particular an inhibitory action 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至R 3和n如权利要求1至8中所定义，其互变异构体，其对映异构体，它们的非对映异构体，其混合物，其前药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, their preparation and their use as pharmaceutical compositions](/abs-image/US/2009/03/10/US07501426B2/abs.jpg.150x150.jpg)
9.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：US07501426B2
公开(公告)日：2009-03-10
申请号：US11060703
申请日：2005-02-17
IPC分类号： C07D473/06 , A61K31/522 , A61P3/10 , A61P19/02 , A61P3/04
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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10.发明授权3-methyl-7-butinyl-xanthines, the preparation thereof and their use as pharmaceutical compositions 有权3-甲基-7-丁烯基 - 黄嘌呤，其制备及其作为药物组合物的用途公开(公告)号：US07495002B2
公开(公告)日：2009-02-24
申请号：US11218056
申请日：2005-09-01
申请人： Elke Langkopf , Matthias Eckhardt , Frank Himmelsbach , Mohammad Tadayyon , Leo Thomas , Ralf R. H. Lotz
发明人： Elke Langkopf , Matthias Eckhardt , Frank Himmelsbach , Mohammad Tadayyon , Leo Thomas , Ralf R. H. Lotz
IPC分类号： C07D473/06 , C07D519/00 , A61K31/522 , A61P3/10
CPC分类号： C07D473/00
摘要： The present invention relates to new substituted xanthines of general formula wherein R1, R2 and X are defined as in the claims, 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： 本发明涉及通式的新的取代黄嘌呤：其中R 1，R 2和X如权利要求中所定义，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，特别是抑制 对二肽基肽酶-IV（DPP-IV）酶活性的影响。
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