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    • 1. 发明公开
    • SPIROQUINONE COMPOUND AND PHARMACEUTICAL COMPOSITION
    • SPIROCHINONVERBINDUNG UND PHARMAZEUTISCHE ZUSAMMENSETZUNG
    • EP2070919A1
    • 2009-06-17
    • EP07832277.3
    • 2007-11-21
    • Hykes Laboratories LLC
    • YOKOYAMA, ShinjiKANAZAWA, HashimeAOTSUKA, Tomoji
    • C07D339/06A61K31/381A61P1/04A61P1/16A61P3/00A61P3/04A61P3/06A61P3/10A61P5/16A61P9/00A61P9/10A61P13/12A61P19/08A61P29/00A61P35/00A61P43/00
    • C07D339/06
    • A novel spiroquinone derivative having a high ABCA1 stabilization effect and being useful for prophylactic and/or therapeutic agents for various diseases developing hypo-high density lipoproteinemia is obtained. The novel spiroquinone derivative is a compound represented by the following formula:

      wherein R 1a , R 1b , R 1c and R each represents a hydrogen atom, a halogen atom, an alkyl group which may have a substituent, or an alkoxy group which may have a substituent, and R 2a and R 2b each represents a hydrogen atom, or an alkyl group which may have a substituent (e.g., a carboxyl group, an alkoxycarbonyl group, a carbamoyl group, and an N-substituted carbamoyl group), the groups R 2a and R 2b may bond together to form a hydrocarbon ring with an adjacent carbon atom, provided that compounds in which all of the groups R 1a , R 1b , R 1c and R 1d are t-butyl groups, and both of the groups R 2a and R 2b are hydrogen atoms or both of the groups R 2a and R 2b are methyl groups are excluded; or a pharmacologically acceptable salt thereof.
    • 获得具有高ABCA1稳定作用并可用于预防和/或治疗各种发展低密度脂蛋白血症的疾病的新型螺醌衍生物。 新的螺醌衍生物是下式表示的化合物:其中R 1a,R 1b,R 1c和R各自表示氢原子,卤素原子,可以具有取代基的烷基或可具有取代基的烷氧基 取代基,R 2a和R 2b各自表示氢原子或可以具有取代基的烷基(例如羧基,烷氧基羰基,氨基甲酰基和N-取代氨基甲酰基),基团 R 2a和R 2b可以键合在一起形成具有相邻碳原子的烃环,条件是其中所有基团R 1a,R 1b,R 1c和R 1d都是叔丁基的化合物,以及两个基团 R 2a和R 2b是氢原子,或者R 2a和R 2b基团都是甲基; 或其药理学上可接受的盐。