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公开(公告)号：US08778926B2
公开(公告)日：2014-07-15
申请号：US13354356
申请日：2012-01-20
申请人： Frank Himmelsbach , Elke Langkopf , Bernd Nosse
发明人： Frank Himmelsbach , Elke Langkopf , Bernd Nosse
IPC分类号： A61K31/506 , C07D491/048 , C07D413/14 , C07D407/14
CPC分类号： C07D407/14 , C07D413/14 , C07D491/048
摘要： The present invention relates to compounds of general formula I, wherein the groups R1, LP, LQ, X1, X2, X3, A, n and m are as defined in the application. The compounds of formula I have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
摘要翻译： 本发明涉及通式I的化合物，其中基团R1，LP，LQ，X1，X2，X3，A，n和m如申请中所定义。 式I化合物具有有价值的药理学性质，特别是与GPR119受体结合并调节其活性。
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公开(公告)号：US08669271B2
公开(公告)日：2014-03-11
申请号：US13327823
申请日：2011-12-16
IPC分类号： A01N43/42 , A61K31/44 , A01N43/08 , A61K31/34 , C07D471/02 , C07D307/87 , C07D307/93
CPC分类号： C07D407/04 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/048
摘要： The present invention relates to compounds of formula I, wherein the groups R1, LP, LQ, X1, X2, X3, Ar and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
摘要翻译： 本发明涉及式I化合物，其中基团R1，LP，LQ，X1，X2，X3，Ar和n如申请中所定义，其具有有价值的药理学性质，特别是与GPR119受体和 调节其活动。
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3.发明授权N-cyclopropyl-N-piperidinyl-amide derivatives, pharmaceutical compositions and uses thereof 有权N-环丙基-N-哌啶基 - 酰胺衍生物，药物组合物及其用途公开(公告)号：US08921398B2
公开(公告)日：2014-12-30
申请号：US13489557
申请日：2012-06-06
申请人： Armin Heckel , Frank Himmelsbach , Elke Langkopf , Bernd Nosse , Neil J. Ashweek , Nicole Harriott
发明人： Armin Heckel , Frank Himmelsbach , Elke Langkopf , Bernd Nosse , Neil J. Ashweek , Nicole Harriott
IPC分类号： C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , A61K31/4468 , A61K31/497 , C07D401/12 , C07D401/14
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , Y10S514/866 , Y10S514/909
摘要： The present invention relates to compounds of general formula I, wherein R1, LP, HetAr, Ar, and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
摘要翻译： 本发明涉及通式Ⅰ化合物，其中R1，LP，HetAr，Ar和n如申请中所定义，其具有有价值的药理学性质，特别是与GPR119受体结合并调节其活性。
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公开(公告)号：US08822471B2
公开(公告)日：2014-09-02
申请号：US13418376
申请日：2012-03-13
申请人： Bernd Nosse , Andreas Blum , Steffen Breitfelder , Armin Heckel , Frank Himmelsbach , Elke Langkopf , Bernd Wellenzohn , Neil J. Ashweek , Nicole Harriott
发明人： Bernd Nosse , Andreas Blum , Steffen Breitfelder , Armin Heckel , Frank Himmelsbach , Elke Langkopf , Bernd Wellenzohn , Neil J. Ashweek , Nicole Harriott
IPC分类号： A61K31/4545 , A61K31/506 , A61K31/501 , C07D413/14 , C07D413/04 , C07D417/14
CPC分类号： C07D413/14 , C07D413/04 , C07D417/14
摘要： The present invention relates to compounds of general formula I, wherein the groups R1, LP, LQ, Ar, m and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
摘要翻译： 本发明涉及通式I的化合物，其中R1，LP，LQ，Ar，m和n基团如本申请中所定义，其具有有价值的药理学性质，特别是与GPR119受体结合并调节其活性 。
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公开(公告)号：US09492436B2
公开(公告)日：2016-11-15
申请号：US14331359
申请日：2014-07-15
IPC分类号： C07D471/02 , A61K31/437 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/541 , A61K45/06 , C07D493/04 , C07D519/00
CPC分类号： A61K31/437 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/541 , A61K45/06 , C07D493/04 , C07D519/00
摘要： The present invention relates to compounds of general formula I, wherein the group R1, R2, X and Y are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the AMP-activated protein kinase (AMPK) 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，X和Y基团如权利要求1中所定义，其具有有价值的药理学性质，特别是结合AMP活化蛋白激酶（AMPK）并调节其 活动。 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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![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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