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    • 152. 发明专利
    • Retinoid prodrug compound
    • RETINOID PRODRUG化合物
    • JP2008094727A
    • 2008-04-24
    • JP2006275097
    • 2006-10-06
    • Research Foundation Itsuu Laboratory財団法人乙卯研究所
    • MURATAKE HIDEAKISHUDO KOICHI
    • C07C233/65A61K31/195A61K31/196A61K31/198A61K31/216A61K31/223A61K31/24A61K31/25A61K31/27A61K31/695A61P3/02A61P17/00A61P17/16A61P19/02A61P19/08A61P29/00A61P35/00A61P35/02A61P37/08A61P43/00C07C233/81C07C233/92C07C271/64C07F7/08C07K5/062
    • PROBLEM TO BE SOLVED: To provide a retinoid prodrug compound having properties of being converted into the retinoid after absorption into a living body. SOLUTION: The compound is represented by general formula (I) [wherein, R 1 to R 5 represent each a hydrogen atom, an alkyl group or a trialkylsilyl group; X represents -NH-CO-, -CO-NH-, -N(COR 6 )-CO- or -CO-N(COR 7 )- (wherein, R 6 and R 7 represent each a lower alkoxy group or a carboxy-substituted phenyl group) or the like; and Z represents -Y-CH(R 12 )-COOH or -COOR 13 äwherein, Y represents a single bond, -CH 2 -, -CH(OH)-, -CO-, -CO-NH- or -CO-NH-CH 2 -CO-NH-; R 12 represents a hydrogen atom or a lower alkyl group; and R 13 represents a hydrogen atom, -CH(R 14 )-COOH (wherein, R 14 represents a hydrogen atom, a lower alkyl group or hydroxy group), -[CH 2 CH 2 -O] n -CH 2 -CH 2 -OH, -CH 2 -O-[CH 2 CH 2 -O] m -CH 2 -OH or -[CH(CH 3 )-CO-O] p -CH(CH 3 )-COOH (wherein, n, m or p each represents an integer of 1-100)}] or a salt thereof or an ester thereof. COPYRIGHT: (C)2008,JPO&INPIT
    • 待解决的问题:提供一种具有在吸收进入生物体后被转化为类视黄醇的特性的类视色素前体药物化合物。 解决方案:该化合物由通式(I)表示[其中R 1至R 5各自表示氢原子,烷基或三烷基甲硅烷基 ; X表示-NH-CO-,-CO-NH-,-N(COR 6) - CO-或-CO-N(COR 7) R 6和R 7分别表示低级烷氧基或羧基取代苯基)等。 和Z代表-Y-CH(R 12 SPOR) - COOH或-COOR 13,其中Y表示单键,-CH 2 SB 2 - ,-CH(OH) - , - CO-,-CO-NH-或-CO-NH-CH 2 SB- R 12表示氢原子或低级烷基; 并且R 13是表示氢原子,-CH(R 14)SPO)-COOH(其中,R 14表示氢原子,低级烷基 基团或羟基), - [CH 2 S 2 -O] -CH SB> 2 -OH,-CH 2 -O - [CH 2 SB] 2 / SB> -CH -CH(CH 3)-COOH(其中,n,m或p各自表示1-100的整数)}]或其盐或其酯。 版权所有(C)2008,JPO&INPIT