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1. 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。

2. 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

3. 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。

4. 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。

5. 发明申请

US20070265278A1 2-PHENYL-INDOLES AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 2-PHENYL-INDOLES作为PROSTAGLANDIN D2受体拮抗剂
公开(公告)号：US20070265278A1
公开(公告)日：2007-11-15
申请号：US11782890
申请日：2007-07-25
申请人： Keith HARRIS , Hans-Jochen Lang , Rose Mathew , Stephen Shimshock , Thaddeus Nieduzak , Sharon Jackson , Zhaoxia Yang , Kenneth Bordeau
发明人： Keith HARRIS , Hans-Jochen Lang , Rose Mathew , Stephen Shimshock , Thaddeus Nieduzak , Sharon Jackson , Zhaoxia Yang , Kenneth Bordeau
IPC分类号： A61K31/404 , A61K31/4245 , A61K31/435 , A61K31/4453 , A61K31/47 , A61K31/495 , A61P1/04 , A61P37/08 , A61P9/00 , C07D209/04 , C07D271/113 , C07D401/12
CPC分类号： C07D209/12 , C07D209/18 , C07D209/22 , C07D209/24 , C07D405/12 , C07D413/06
摘要： The present invention is directed to a compound of Formula (XVI): (please replace Formula (I) with Formula (XVI) as shown below) wherein R, R2, R3, R4, R5, R6, R7 and n are as defined herein, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, a pharmaceutically acceptable prodrug thereof, or a pharmaceutically acceptable salt, hydrate or solvate of the prodrug, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds according to Formula (XVI) in admixture with a pharmaceutically acceptable carrier, a method of treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which are generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like by administering to said patient a pharmaceutically effective amount of a compound according to Formula (XVI).
摘要翻译：本发明涉及式（ⅩⅥ）化合物：（如下所示，用式（ⅩⅥ）表示的式（I）表示）其中R，R 2，R 3， R 4，R 4，R 5，R 6，R 7和n如本文所定义，或其药学上可接受的盐，水合物或溶剂化物，其药学上可接受的前药，或药学上可接受的盐，水合物或溶剂化物，药物组合物，其包含药学上有效量的根据式（XVI）的一种或多种化合物与药学上可接受的载体混合，治疗患有PGD2介导的病症的患者的方法，包括但不限于过敏性疾病（例如过敏性鼻炎，过敏性结膜炎，特应性皮炎，支气管哮喘和食物过敏），全身肥大细胞增多症，伴有系统性肥大细胞活化，过敏性休克，支气管收缩，支气管炎，荨麻疹，湿疹，伴有瘙痒的疾病（如特应性皮炎和荨麻疹），伴随瘙痒的行为（如刮伤和殴打）而产生的疾病（如白内障，视网膜脱离，炎症，感染和睡眠障碍），炎症，慢性阻塞性肺疾病，缺血再灌注损伤，脑血管意外，慢性类风湿性关节炎，胸膜炎，溃疡性结肠炎等，通过向所述患者施用药学有效量的根据式（XVI）的化合物。

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