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    • 1. 发明专利
    • Lpa receptor agonist
    • LPA受体激素
    • JP2008297278A
    • 2008-12-11
    • JP2007147257
    • 2007-06-01
    • Astellas Pharma Incアステラス製薬株式会社
    • KAWANAMI EIJIKONDO YUTAKASHISHIKURA JUNICHITAKAHASHI MASAYASUSAKAMOTO KAZUSHISOGA TAKATOSHIORITA MASAYA
    • A61K31/4375A61K31/55A61P13/00A61P13/02A61P13/08A61P25/00A61P25/02A61P25/28A61P43/00C07D455/00C07D471/14C12N15/09G01N33/15G01N33/50
    • PROBLEM TO BE SOLVED: To provide a low-molecular lysophosphatidic acid (LPA) receptor agonist and a prophylactic or therapeutic agent for various kinds of diseases caused by an LPA receptor, containing the agonist as an active ingredient.
      SOLUTION: The LPA receptor agonist is composed of an indoloquinolizine derivative represented by general formula (I) (wherein X is methylene or ethylene; R
      1 is a hydrogen atom or a lower alkyl group or benzyl group which may be substituted; R
      2 and R
      3 are each independently a hydrogen atom or a lower alkyl). The prophylactic or therapeutic agent comprises the agonist as an active ingredient. 12-Benzyl-12b-methyl-1,2,3,4,6,7,12,12b-octahydroindolo[2,3-a]quinolizine which is a new compound represented by general formula (I) (wherein R
      1 is a benzyl group; R
      2 is a methyl group; R
      3 is a hydrogen atom) exhibits, especially, strong LPA receptor agonist action. The prophylactic or therapeutic agent, especially, has effects for treating urinary system diseases, central nervous system diseases or peripheral nervous system diseases caused by the LPA receptor.
      COPYRIGHT: (C)2009,JPO&INPIT
    • 要解决的问题:提供低分子溶血磷脂酸(LPA)受体激动剂和用于由含有激动剂作为活性成分的LPA受体引起的各种疾病的预防或治疗剂。 解决方案:LPA受体激动剂由通式(I)表示的吲哚喹嗪衍生物(其中X为亚甲基或亚乙基; R 1为氢原子或低级烷基或苄基 可以被取代的基团; R 2和R 3各自独立地为氢原子或低级烷基。 预防或治疗剂包含激动剂作为活性成分。 12-苄基-122-甲基-1,2,3,4,6,7,12,12b-八氢吲哚并[2,3-a]喹嗪,它是由通式(I)表示的新化合物(其中R 1 是苄基; R 2 SP 2是甲基; R 3是氢原子)特别表现出强烈的LPA受体激动剂作用。 预防或治疗剂,特别是具有治疗由LPA受体引起的泌尿系统疾病,中枢神经系统疾病或周围神经系统疾病的作用。 版权所有(C)2009,JPO&INPIT