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1. 发明授权

US07750005B2 Substituted hexahydropyrazino [1,2-A] pyrimidine-4,7-dione derivatives, process for their preparation and their use as medicaments 有权
标题翻译：取代的六氢吡嗪并[1,2-A]嘧啶-4,7-二酮衍生物，其制备方法及其用作药物
公开(公告)号：US07750005B2
公开(公告)日：2010-07-06
申请号：US12124503
申请日：2008-05-21
申请人： Stefanie Flohr , Siegfried Stengelin , Matthias Gossel , Thomas Klabunde , Pavel Safar , James Spoonamore , Martin Smrcina
发明人： Stefanie Flohr , Siegfried Stengelin , Matthias Gossel , Thomas Klabunde , Pavel Safar , James Spoonamore , Martin Smrcina
IPC分类号： C07D487/00 , A61K31/495 , A01N43/60
CPC分类号： C07D487/04
摘要： The invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives and to the physiologically tolerated salts and physiologically functional derivatives thereof.Compounds of the formula I in which the radicals have the stated meanings, and the physiologically tolerated salts thereof and processes for preparing them are described. The compounds are suitable for example as anorectic agents.
摘要翻译：本发明涉及取代的六氢吡嗪并[1,2-a]嘧啶-4,7-二酮衍生物及其生理上耐受的盐和生理功能衍生物。描述了其中基团具有所述含义的式I化合物及其生理上耐受的盐及其制备方法。该化合物适合于例如厌食剂。

2. 发明授权

US07652007B2 Nitrogen-substituted hexahydropyrazino[1,2-A]pyrimidine-4,7-dione derivatives, processes for their preparation and their use as medicaments 有权
标题翻译：氮取代六氢吡嗪并[1,2-A]嘧啶-4,7-二酮衍生物，其制备方法及其作为药物的用途
公开(公告)号：US07652007B2
公开(公告)日：2010-01-26
申请号：US10779439
申请日：2004-02-13
申请人： Stefanie Flohr , Siegfried Stengelin , Matthias Gossel , Thomas Klabunde , Petra Stahl , Pavel Safar , James Spoonamore , Martin Smrcina , Joseph Klein , Gregory Merriman , Brian Whiteley , Carolina Lanter , Kenneth Bordeau , Zhaoxia Yang
发明人： Stefanie Flohr , Siegfried Stengelin , Matthias Gossel , Thomas Klabunde , Petra Stahl , Pavel Safar , James Spoonamore , Martin Smrcina , Joseph Klein , Gregory Merriman , Brian Whiteley , Carolina Lanter , Kenneth Bordeau , Zhaoxia Yang
IPC分类号： C07D487/00 , A61K31/495 , A01N43/60
CPC分类号： C07D487/04
摘要： Nitrogen-substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives, processes for the preparation and their use as medicamentsThe invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives and to the physiologically tolerated salts and physiologically functional derivatives thereof.Compounds of the formula I in which the radicals have the stated meanings, and the physiologically tolerated salts thereof and processes for preparing them are described. The compounds are suitable for example as anorectic agents.
摘要翻译：氮取代六氢吡嗪并[1,2-a]嘧啶-4,7-二酮衍生物，其制备方法及其作为药物的用途本发明涉及取代的六氢吡嗪并[1,2-a]嘧啶-4,7-二酮衍生物以及其生理上耐受的盐和生理功能衍生物。描述了其中基团具有所述含义的式I化合物及其生理上耐受的盐及其制备方法。该化合物适合于例如厌食剂。

3. 发明申请

US20050085483A1 Nitrogen-substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives, processes for their preparation and their use as medicaments 有权
标题翻译：氮取代六氢吡嗪并[1,2-a]嘧啶-4,7-二酮衍生物，其制备方法及其用作药物
公开(公告)号：US20050085483A1
公开(公告)日：2005-04-21
申请号：US10779439
申请日：2004-02-13
申请人： Stefanie Flohr , Siegfried Stengelin , Matthias Gossel , Thomas Klabunde , Petra Stahl , Pavel Safar , James Spoonamore , Martin Smrcina , Joseph Klein , Gregory Merriman , Brian Whiteley , Carolina Lanter , Kenneth Bordeau , Zhaoxia Yang
发明人： Stefanie Flohr , Siegfried Stengelin , Matthias Gossel , Thomas Klabunde , Petra Stahl , Pavel Safar , James Spoonamore , Martin Smrcina , Joseph Klein , Gregory Merriman , Brian Whiteley , Carolina Lanter , Kenneth Bordeau , Zhaoxia Yang
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： Nitrogen-substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives, processes for the preparation and their use as medicaments The invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives and to the physiologically tolerated salts and physiologically functional derivatives thereof. in which the radicals have the stated meanings, and the physiologically tolerated salts thereof and processes for preparing them are described. The compounds are suitable for example as anorectic agents.
摘要翻译：氮取代六氢吡嗪并[1,2-a]嘧啶-4,7-二酮衍生物，其制备方法及其作为药物的用途本发明涉及取代的六氢吡嗪并[1,2-a]嘧啶-4,7-二酮衍生物以及其生理上耐受的盐和生理功能衍生物。其中基团具有所述含义，并且描述了其生理上耐受的盐及其制备方法。该化合物适合于例如厌食剂。

4. 发明申请

US20080221113A1 SUBSTITUTED HEXAHYDROPYRAZINO [1,2-A] PYRIMIDINE-4,7-DIONE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS MEDICAMENTS 有权
标题翻译：取代的HEXAHYDROPYRAZINO [1,2-A]嘧啶-4,7-二酮衍生物，其制备方法及其作为药物的用途
公开(公告)号：US20080221113A1
公开(公告)日：2008-09-11
申请号：US12124503
申请日：2008-05-21
申请人： Stefanie Flohr , Siegfried Stengelin , Matthias Gossel , Thomas Klabunde , Pavel Safar , James Spoonamore , Martin Smrcina
发明人： Stefanie Flohr , Siegfried Stengelin , Matthias Gossel , Thomas Klabunde , Pavel Safar , James Spoonamore , Martin Smrcina
IPC分类号： A61K31/4985 , C07D471/04 , A61P3/04 , A61P3/10 , A61P15/00
CPC分类号： C07D487/04
摘要： Substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives, processes for their preparation and their use as medicamentsThe invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives and to the physiologically tolerated salts and physiologically functional derivatives thereof.Compounds of the formula I in which the radicals have the stated meanings, and the physiologically tolerated salts thereof and processes for preparing them are described. The compounds are suitable for example as anorectic agents.
摘要翻译：取代的六氢吡嗪并[1,2-a]嘧啶-4,7-二酮衍生物，其制备方法及其作为药物的用途本发明涉及取代的六氢吡嗪并[1,2-a]嘧啶-4,7-二酮衍生物，生理上耐受的盐及其生理功能衍生物。描述了其中基团具有所述含义的式I化合物及其生理上耐受的盐及其制备方法。该化合物适合于例如厌食剂。

5. 发明授权

US07390814B2 Substituted hexahydropyrazino [1,2-a] pyrimidine-4,7-dione derivatives, process for their preparation and their use as medicaments 有权
标题翻译：取代的六氢吡嗪并[1,2-a]嘧啶-4,7-二酮衍生物，其制备方法和用作药物
公开(公告)号：US07390814B2
公开(公告)日：2008-06-24
申请号：US10778554
申请日：2004-02-13
申请人： Stefanie Flohr , Siegfried Stengelin , Matthias Gossel , Thomas Klabunde , Pavel Safar , James Spoonamore , Martin Smrcina
发明人： Stefanie Flohr , Siegfried Stengelin , Matthias Gossel , Thomas Klabunde , Pavel Safar , James Spoonamore , Martin Smrcina
IPC分类号： A01N43/90 , C07D239/70
CPC分类号： C07D487/04
摘要： Substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives, processes for their preparation and their use as medicamentsThe invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives and to the physiologically tolerated salts and physiologically functional derivatives thereof.Compounds of the formula I in which the radicals have the stated meanings, and the physiologically tolerated salts thereof and processes for preparing them are described. The compounds are suitable for example as anorectic agents.
摘要翻译：取代的六氢吡嗪并[1,2-a]嘧啶-4,7-二酮衍生物，其制备方法及其作为药物的用途本发明涉及取代的六氢吡嗪并[1,2-a]嘧啶-4,7-二酮衍生物，生理上耐受的盐及其生理功能衍生物。描述了其中基团具有所述含义的式I化合物及其生理上耐受的盐及其制备方法。该化合物适合于例如厌食剂。

6. 发明授权

US07994168B2 Hexahydro-pyrazino[1,2-A]pyrimidine-4,7-dione derivatives substituted with amino acids 有权
标题翻译：用氨基酸取代的六氢 - 吡嗪并[1,2-A]嘧啶-4,7-二酮衍生物
公开(公告)号：US07994168B2
公开(公告)日：2011-08-09
申请号：US11677067
申请日：2007-02-21
申请人： Petra Lennig , Siegfried Stengelin , Thomas Klabunde , Matthias Gossel , Pavel Safar , James Spoonamore , Gregory Merriman , Joseph T Klein , Brian Whiteley , Carolina Lanter , Kenneth Bordeau , Zhaoxia Yang , Martin Smrcina
发明人： Petra Lennig , Siegfried Stengelin , Thomas Klabunde , Matthias Gossel , Pavel Safar , James Spoonamore , Gregory Merriman , Joseph T Klein , Brian Whiteley , Carolina Lanter , Kenneth Bordeau , Zhaoxia Yang , Martin Smrcina
IPC分类号： C07D487/04 , A61K31/4985 , A61P3/04
CPC分类号： C07D487/04
摘要： The invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives substituted with amino acids, and to the physiologically tolerated salts thereof, processes for their preparation and their use as medicaments.
摘要翻译：本发明涉及被氨基酸取代的取代六氢吡嗪并[1,2-a]嘧啶-4,7-二酮衍生物及其生理学上可耐受的盐，其制备方法及其用作药物。

7. 发明申请

US20070197539A1 HEXAHYDRO-PYRAZINO[1,2-A]PYRIMIDINE-4,7-DIONE DERIVATIVES SUBSTITUTED WITH AMINO ACIDS 有权
标题翻译：用氨基酸取代的十六氢吡嗪并[1,2-A]嘧啶-4,7-二酮衍生物
公开(公告)号：US20070197539A1
公开(公告)日：2007-08-23
申请号：US11677067
申请日：2007-02-21
申请人： Petra Lennig , Siegfried Stengelin , Thomas Klabunde , Matthias Gossel , Pavel Safar , Martin Smrcina , James Spoonamore , Gregory Merriman , Joseph Klein , Brian Whiteley , Carolina Lanter , Kenneth Bordeau , Zhaoxia Yang
发明人： Petra Lennig , Siegfried Stengelin , Thomas Klabunde , Matthias Gossel , Pavel Safar , Martin Smrcina , James Spoonamore , Gregory Merriman , Joseph Klein , Brian Whiteley , Carolina Lanter , Kenneth Bordeau , Zhaoxia Yang
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives substituted with amino acids, and to the physiologically tolerated salts thereof, processes for their preparation and their use as medicaments
摘要翻译：本发明涉及被氨基酸取代的取代六氢吡嗪并[1,2-a]嘧啶-4,7-二酮衍生物及其生理学上可耐受的盐，其制备方法及其用作药物

8. 发明授权

US07323457B2 Substituted sulfonamides and ureas useful for inhibiting kinase activity 失效
公开(公告)号：US07323457B2
公开(公告)日：2008-01-29
申请号：US11738725
申请日：2007-04-23
申请人： Pavel Safar , Armin Walser , Stephen James Shimshock
发明人： Pavel Safar , Armin Walser , Stephen James Shimshock
IPC分类号： A61K31/5513 , C07D243/08
CPC分类号： C07C257/18 , A61K38/00 , C07D209/42 , C07D211/62 , C07D295/135 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07K5/0207 , C07K5/021
摘要： Sulfonamide and urea compounds having an inhibitory effect on Src kinase including enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates of said compound, said compound having the general structure shown in Formula II are disclosed and claimed:

9. 发明授权

US06500803B1 Factor VIIa inhibitors 有权
标题翻译：因子VIIa抑制剂
公开(公告)号：US06500803B1
公开(公告)日：2002-12-31
申请号：US09588651
申请日：2000-06-07
申请人： Otmar Klingler , Manfred Schudok , Gerhard Zoller , Uwe Heinelt , Elisabeth Defossa , Hans Matter , Pavel Safar
发明人： Otmar Klingler , Manfred Schudok , Gerhard Zoller , Uwe Heinelt , Elisabeth Defossa , Hans Matter , Pavel Safar
IPC分类号： A61K3805
CPC分类号： C07K5/06086 , A61K38/00
摘要： The present invention relates to compounds of formula I, in which R1, R2, R91, R92, R93, R94, R95, R96, R97, r, s, and t have the meanings indicated in the claims. Compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of conditions in which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
摘要翻译：本发明涉及式Ⅰ化合物，其中R1，R2，R91，R92，R93，R94，R95，R96，R97，r，s和t具有权利要求中所示的含义。式I化合物是有价值的药理活性化合物。它们具有强烈的抗血栓形成作用，并且适用于例如治疗和预防血栓栓塞性疾病或再狭窄。它们是血液凝固酶因子VIIa的可逆抑制剂，并且通常可以在其中存在不需要的因子VIIa活性的条件下或用于治疗或预防预期因子VIIa的抑制的病症。本发明还涉及制备式I化合物的方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

10. 发明授权

US07393849B2 Substituted sulfonamides and ureas useful for inhibiting kinase activity 失效
标题翻译：可用于抑制激酶活性的取代磺酰胺和脲
公开(公告)号：US07393849B2
公开(公告)日：2008-07-01
申请号：US11738733
申请日：2007-04-23
申请人： Pavel Safar , Armin Walser , Stephen James Shimshock
发明人： Pavel Safar , Armin Walser , Stephen James Shimshock
IPC分类号： A61K31/496 , A61K31/4545 , C07D211/06 , C07D241/04 , C07D401/04
CPC分类号： C07C257/18 , A61K38/00 , C07D209/42 , C07D211/62 , C07D295/135 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07K5/0207 , C07K5/021
摘要： Sulfonamide and urea compounds having an inhibitory effect on Src kinase including enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates of said compound, said compound having the general structure shown in Formula II are disclosed and claimed:
摘要翻译：具有对Src激酶具有抑制作用的磺酰胺和脲化合物，包括其对映体，立体异构体和互变异构体，以及所述化合物的药学上可接受的盐或溶剂合物，所述化合物具有式II所示的一般结构，

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