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1. 发明申请

WO2008014186A1 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：WO2008014186A1
公开(公告)日：2008-01-31
申请号：PCT/US2007/073945
申请日：2007-07-20
申请人： SANOFI-AVENTIS , YANG, Zhaoxia , REILING, Stephan , NIEDUZAK, Thaddeus R. , MATHEW, Rose M. , JACKSON, Sharon , HARRIS, Keith J.
发明人： YANG, Zhaoxia , REILING, Stephan , NIEDUZAK, Thaddeus R. , MATHEW, Rose M. , JACKSON, Sharon , HARRIS, Keith J.
IPC分类号： C07D209/18 , A61K31/404 , A61P11/06 , A61P27/14 , A61P37/06 , A61P37/08
CPC分类号： C07D209/18
摘要： The present invention is directed to 2-phenyl-indole compounds (A), their preparation, pharmaceutical compositions containing these compounds, and their pharmaceutical use in 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, eczema, urticaria 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.
摘要翻译：本发明涉及2-苯基 - 吲哚化合物（A），其制备方法，含有这些化合物的药物组合物及其在治疗患有PGD2介导的病症的患者中的药物用途，包括但不限于过敏性疾病（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），系统性肥大细胞增多症，伴有系统性肥大细胞活化的疾病，过敏性休克，支气管收缩，支气管炎，湿疹，伴有瘙痒的荨麻疹疾病（如特应性皮炎和荨麻疹），由于伴随瘙痒的行为（如搔抓和殴打），炎症，慢性阻塞性肺疾病，缺血再灌注损伤，脑血管疾病等引起的二次产生的疾病（如白内障，视网膜脱离，炎症，感染和睡眠障碍）事故，慢性类风湿性关节炎，胸膜炎，溃疡性结肠炎等。

2. 发明申请

WO2006081343A1 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：WO2006081343A1
公开(公告)日：2006-08-03
申请号：PCT/US2006/002736
申请日：2006-01-25
申请人： AVENTIS PHARMACEUTICALS INC. , HARRIS, Keith, J. , LANG, Hans-Jochen , MATHEW, Rose, M. , SHIMSHOCK, Stephen, J. , NIEDUZAK, Thaddeus, R. , JACKSON, Sharon , YANG, Zhaoxia , BORDEAU, Kenneth, J.
发明人： HARRIS, Keith, J. , LANG, Hans-Jochen , MATHEW, Rose, M. , SHIMSHOCK, Stephen, J. , NIEDUZAK, Thaddeus, R. , JACKSON, Sharon , YANG, Zhaoxia , BORDEAU, Kenneth, J.
IPC分类号： C07D209/12 , C07D209/18 , C07D209/22 , C07D209/24 , C07D413/06 , A61K31/404 , A61K31/405 , A61K31/4245 , A61P11/00
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) wherein R, R 2 , R 3 , R 4 , R 5 , R 6 , R 7 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）的化合物，其中R 1，R 2，R 3，R 4，R 4， 5，R 6，R 7和n如本文所定义，或其药学上可接受的盐，水合物或溶剂合物，其药学上可接受的前药，或药学上可接受的盐，水合物或溶剂合物，包含药学上有效量的一种或多种根据式（XVI）的化合物与药学上可接受的载体混合的药物组合物，治疗患有PGD2的患者的方法包括但不限于过敏性疾病（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），系统性肥大细胞增多症，伴有系统性肥大细胞活化的疾病，过敏反应，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（如搔抓和殴打），炎症，慢性阻塞性肺疾病，局部缺血再灌注损伤等二次产生的疾病（如白内障，视网膜脱离，炎症，感染和睡眠障碍），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。

3. 发明申请

WO2006024390A1 MIT AMINOSÄUREN SUBSTITUIERTE HEXAHYDRO-PYRAZINO[1,2-A]PYRIMIDIN-4, 7-DIONDERIVATE 审中-公开
标题翻译：与咪唑类六氢 - 吡嗪并[1,2-a]嘧啶4,7二酮衍生物氨基酸
公开(公告)号：WO2006024390A1
公开(公告)日：2006-03-09
申请号：PCT/EP2005/008873
申请日：2005-08-16
申请人： SANOFI-AVENTIS DEUTSCHLAND GMBH , LENNIG, Petra , STENGELIN, Siegfried , KLABUNDE, Thomas , GOSSEL, Matthias , SAFAR, Pavel , SMRCINA, Martin , SPOONAMORE, James , MERRIMAN, Gregory , KLEIN, Joseph, T. , WHITELEY, Brian , LANTER, Carolina , BORDEAU, Kenneth , YANG, Zhaoxia
发明人： LENNIG, Petra , STENGELIN, Siegfried , KLABUNDE, Thomas , GOSSEL, Matthias , SAFAR, Pavel , SMRCINA, Martin , SPOONAMORE, James , MERRIMAN, Gregory , KLEIN, Joseph, T. , WHITELEY, Brian , LANTER, Carolina , BORDEAU, Kenneth , YANG, Zhaoxia
IPC分类号： C07D487/04 , A61K31/4985 , A61P43/00
CPC分类号： C07D487/04
摘要： Die Erfindung betrifft substituierte Hexahydro-pyrazino[1,2-a]pyrimidin-4,7-dionderivate sowie deren physiologisch verträgliche Salze und physiologisch funktionelle Derivate. Es werden Verbindungen der Formel (I), worin die Reste die angegebenen Bedeutungen haben, sowie deren physiologisch verträglichen Salze und Verfahren zu deren Herstellung beschrieben. Die Verbindungen eignen sich z.B. als Anorektika.
摘要翻译：本发明涉及取代的六氢吡嗪并[1,2-a]嘧啶-4,7-二酮衍生物和其生理学可接受的盐和生理学功能衍生物。是式（I）的化合物，其中的基团具有所述的含义，和描述它们的生理学可接受的盐和它们的制备方法。的化合物是合适的，例如，是作为食欲抑制剂。

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