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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)
71.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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72.发明授权Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds 有权具有MCH拮抗活性的炔烃化合物和包含这些化合物的药物公开(公告)号：US07524862B2
公开(公告)日：2009-04-28
申请号：US11104914
申请日：2005-04-13
申请人： Dirk Stenkamp , Stephan Georg Mueller , Philipp Lustenberger , Thorsten Lehmann-Lintz , Gerald Juergen Roth , Klaus Rudolf , Marcus Schindler , Leo Thomas , Ralf Lotz
发明人： Dirk Stenkamp , Stephan Georg Mueller , Philipp Lustenberger , Thorsten Lehmann-Lintz , Gerald Juergen Roth , Klaus Rudolf , Marcus Schindler , Leo Thomas , Ralf Lotz
IPC分类号： A61K31/47 , A61K31/44 , C07D215/38 , C07D491/02 , C07D405/00
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14
摘要： Alkyne compounds of formula I wherein A, B, W, X, Y, Z, R1, and R2 have the meanings given herein, which have MCH-receptor antagonistic activity and are useful for preparing pharmaceutical compositions for the treatment of metabolic disorders and/or eating disorders, particularly obesity and diabetes.
摘要翻译： 式I的炔烃化合物，其中A，B，W，X，Y，Z，R 1和R 2具有本文给出的含义，其具有MCH受体拮抗活性并且可用于制备用于治疗代谢紊乱和/ 或进食障碍，特别是肥胖和糖尿病。
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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)
73.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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74.发明授权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：US07183280B2
公开(公告)日：2007-02-27
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： A61K31/5025 , A61K31/519 , 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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75.发明申请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：US20060079541A1
公开(公告)日：2006-04-13
申请号：US11218056
申请日：2005-09-01
申请人： Elke Langkopf , Matthias Eckhardt , Frank Himmelsbach , Mohammad Tadayyon , Leo Thomas , Ralf Lotz
发明人： Elke Langkopf , Matthias Eckhardt , Frank Himmelsbach , Mohammad Tadayyon , Leo Thomas , Ralf Lotz
IPC分类号： A61K31/522 , C07D473/04
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： 本发明涉及以下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， 其具有有价值的药理学特性的其混合物及其盐，特别是对二肽基肽酶-IV（DPP-IV）的活性的抑制作用。
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公开(公告)号：US20050245500A1
公开(公告)日：2005-11-03
申请号：US11071797
申请日：2005-03-03
申请人： Gerald Roth , Philipp Lustenberger , Dirk Stenkamp , Stephan Mueller , Thorsten Lehmann-Lintz , Marcus Schindler , Leo Thomas , Ralf Lotz , Marco Santagostino
发明人： Gerald Roth , Philipp Lustenberger , Dirk Stenkamp , Stephan Mueller , Thorsten Lehmann-Lintz , Marcus Schindler , Leo Thomas , Ralf Lotz , Marco Santagostino
IPC分类号： A61K31/454 , A61K31/4709 , A61K31/4747 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/55 , C07C235/74 , C07D205/04 , C07D207/08 , C07D207/20 , C07D209/08 , C07D211/42 , C07D211/46 , C07D211/48 , C07D211/52 , C07D211/58 , C07D211/62 , C07D221/20 , C07D263/56 , C07D295/092 , C07D295/135 , C07D401/12 , C07D413/02 , C07D417/02 , C07D43/02
CPC分类号： C07D207/08 , C07C235/74 , C07D205/04 , C07D207/20 , C07D209/08 , C07D211/42 , C07D211/46 , C07D211/48 , C07D211/52 , C07D211/58 , C07D211/62 , C07D221/20 , C07D263/56 , C07D295/088 , C07D295/135 , C07D401/12
摘要： Compounds of formula I wherein the groups and residues A, B, b, X, Y, Z, R1, R2, R3, R5a and R5b have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one amide according to the invention. As a result of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia, and diabetes.
摘要翻译： 式I化合物，其中基团和残基A，B，b，X，Y，Z，R 1，R 2，R 3， R 5a和R 5b具有权利要求1中给出的含义。 本发明还涉及含有至少一种本发明酰胺的药物组合物。 由于它们的MCH受体拮抗活性，根据本发明的药物组合物适用于治疗代谢紊乱和/或进食障碍，特别是肥胖症，贪食症，厌食症，食欲过盛和糖尿病。
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![8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions](/abs-image/US/2005/10/20/US20050234108A1/abs.jpg.150x150.jpg)
77.发明申请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：US20050234108A1
公开(公告)日：2005-10-20
申请号：US11060703
申请日：2005-02-17
IPC分类号： A61K31/44
CPC分类号： C07D473/04
摘要： The present invention relates to substituted xanthines of general 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： 本发明涉及通式的取代黄嘌呤，其中R如权利要求1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，特别是对酶二肽基肽酶的活性的抑制作用 -IV（DPP-IV）。
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78.发明申请Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds 有权具有MCH拮抗活性的炔烃化合物和包含这些化合物的药物公开(公告)号：US20050234101A1
公开(公告)日：2005-10-20
申请号：US11104889
申请日：2005-04-13
申请人： Dirk Stenkamp , Stephan Mueller , Philipp Lustenberger , Thorsten Lehmann-Lintz , Gerald Roth , Klaus Rudolf , Marcus Schindler , Leo Thomas , Ralf Lotz
发明人： Dirk Stenkamp , Stephan Mueller , Philipp Lustenberger , Thorsten Lehmann-Lintz , Gerald Roth , Klaus Rudolf , Marcus Schindler , Leo Thomas , Ralf Lotz
IPC分类号： C07D213/30 , C07D213/38 , C07D213/74 , C07D213/75 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D409/10 , C07D409/14 , C07D451/06 , A61K31/4545 , A61K31/44 , A61K31/4439 , C07D41/02
CPC分类号： C07D213/30 , C07D213/38 , C07D213/74 , C07D213/75 , C07D401/06 , C07D401/10 , C07D401/12 , C07D409/10 , C07D409/14 , C07D451/06
摘要： Alkyne compounds having MCH-receptor antagonistic activity, which are useful for preparing pharmaceutical compositions for the treatment of metabolic disorders and/or eating disorders, particularly obesity and diabetes.
摘要翻译： 具有MCH受体拮抗活性的炔烃化合物，其可用于制备用于治疗代谢紊乱和/或进食障碍，特别是肥胖和糖尿病的药物组合物。
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![New piperazin-1-yl and 2-([1,4]diazepan-1-yl)-imidazo[4,5-d]-pyridazin-4-ones, the preparation thereof and their use as pharmaceutial compositions](/abs-image/US/2005/08/04/US20050171093A1/abs.jpg.150x150.jpg)
79.发明申请New piperazin-1-yl and 2-([1,4]diazepan-1-yl)-imidazo[4,5-d]-pyridazin-4-ones, the preparation thereof and their use as pharmaceutial compositions 有权新的哌嗪-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：US20050171093A1
公开(公告)日：2005-08-04
申请号：US11016176
申请日：2004-12-17
申请人： Matthias Eckhardt , Norbert Hauel , Frank Himmelsbach , Iris Kauffman-Hefner , Elke Langkopf , Mohammad Tadayyon , Leo Thomas
发明人： Matthias Eckhardt , Norbert Hauel , Frank Himmelsbach , Iris Kauffman-Hefner , Elke Langkopf , Mohammad Tadayyon , Leo Thomas
IPC分类号： A61K31/503 , A61K31/5377 , A61K31/551 , C07D487/02 , C07D487/04
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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![6,7,8,9-tetrahydro-5H-1,4,7,10a-tetraaza-cyclohept[f]indene derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them](/abs-image/US/2016/05/24/US09346816B2/abs.jpg.150x150.jpg)
80.发明授权6,7,8,9-tetrahydro-5H-1,4,7,10a-tetraaza-cyclohept[f]indene derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them 有权6,7,8,9-四氢-5H-1,4,7,10a-四氮杂 - 环庚烯并[f]茚衍生物，含有这些化合物的药物组合物，它们的用途和制备方法公开(公告)号：US09346816B2
公开(公告)日：2016-05-24
申请号：US14072324
申请日：2013-11-05
申请人： Stephan-Georg Mueller , Christopher John Brown , Alexander Heifetz , Bernd Nosse , Juergen Prestle , Natacha Prevost , Klaus Rudolf , Stefan Scheuerer , Marcus Schindler , Dirk Stenkamp , Leo Thomas , Heather Tye
发明人： Stephan-Georg Mueller , Christopher John Brown , Alexander Heifetz , Bernd Nosse , Juergen Prestle , Natacha Prevost , Klaus Rudolf , Stefan Scheuerer , Marcus Schindler , Dirk Stenkamp , Leo Thomas , Heather Tye
IPC分类号： A61K31/55 , C07D487/14
CPC分类号： C07D487/14
摘要： The present invention relates to compounds defined by formula I wherein the groups X, Y, W and R1 to R4 are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are agonists of the 5-HT2C receptor, and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this receptor, such as metabolic and CNS-related disorders.
摘要翻译： 本发明涉及由式I定义的化合物，其中基团X，Y，W和R 1至R 4如权利要求1所定义，具有有价值的药理学活性。 特别地，这些化合物是5-HT 2C受体的激动剂，因此适用于治疗和预防可被受体抑制影响的疾病，如代谢和CNS相关疾病。
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