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    • 4. 发明授权
    • Retinoid prodrug compound
    • 维甲酸前药化合物
    • US08633335B2
    • 2014-01-21
    • US12682966
    • 2007-10-31
    • Hideaki MuratakeKoichi Shudo
    • Hideaki MuratakeKoichi Shudo
    • C07C51/367
    • C07C237/52C07C233/65C07C235/84C07C235/88C07C237/48C07C271/30C07C2602/10C07F7/081
    • A compound represented by the following general formula (I): [R1 to R5 represent hydrogen atom, an alkyl group, or a trialkylsilyl group, X represents —NH—CO—, —CO—NH—, —N(COR6)—CO—, —CO—N(COR7)— (R6 and R7 represent a lower alkoxy group, or a carboxy-substituted phenyl group) etc.; and Z represents —Y—CH(R12)—COOH, —CHO, —CH═CH—COOH, or —COOR13 (Y represents a single bond, —CH2—, —CH(OH)—, —CO—, —CO—NH—, or —CO—NH—CH2—CO—NH—, R12 represents hydrogen atom or a lower alkyl group, and R13 represents hydrogen atom, —CH(R14)—COOH(R14 represents hydrogen atom, a lower alkyl group, or hydroxy group), —[CH2CH2—O]n—CH2—CH2—OH, —CH2—O—[CH2CH2—O]m—CH2—OH, or —[CH(CH3)—CO—O]p—CH(CH3)—COOH (m, n and p represent an integer of 1 to 100))], a salt thereof or an ester thereof, which has a property of being converted into a retinoid after absorption in vivo.
    • 由以下通式(I)表示的化合物:[R1至R5表示氢原子,烷基或三烷基甲硅烷基,X表示-NH-CO-,-CO-NH-,-N(COR6)-CO - ,-CO-N(COR 7) - (R 6和R 7表示低级烷氧基或羧基取代的苯基)等。 Z表示-Y-CH(R 12)-COOH,-CHO,-CH = CH-COOH或-COOR 13(Y表示单键,-CH 2 - , - CH(OH) - , - CO- -NH-或-CO-NH-CH 2 -CO-NH-,R 12表示氢原子或低级烷基,R 13表示氢原子,-CH(R 14)-COOH(R ​​14表示氢原子,低级烷基 ,或羟基), - [CH 2 CH 2 -O] n -CH 2 -CH 2 -OH,-CH 2 -O- [CH 2 CH 2 -O] m -CH 2 -OH或 - [CH(CH 3)-CO-O] CH(CH 3)-COOH(m,n和p表示1〜100的整数))],其盐或其酯,其在体内吸收后具有转化为类视黄醇的性质。
    • 7. 发明申请
    • RETINOID PRODRUG COMPOUND
    • RETINOID PRODRUG化合物
    • US20100286427A1
    • 2010-11-11
    • US12682966
    • 2007-10-31
    • Hideaki MuratakeKoichi Shudo
    • Hideaki MuratakeKoichi Shudo
    • C07F7/10C07C271/62C07C229/52C07C229/44C07C235/84
    • C07C237/52C07C233/65C07C235/84C07C235/88C07C237/48C07C271/30C07C2602/10C07F7/081
    • A compound represented by the following general formula (I): [R1 to R5 represent hydrogen atom, an alkyl group, or a trialkylsilyl group, X represents —NH—CO—, —CO—NH—, —N(COR6)—CO—, —CO—N(COR7)— (R6 and R7 represent a lower alkoxy group, or a carboxy-substituted phenyl group) etc.; and Z represents —Y—CH(R12)—COOH, —CHO, —CH═CH—COOH, or —COOR13 (Y represents a single bond, —CH2—, —CH(OH)—, —CO—, —CO—NH—, or —CO—NH—CH2—CO—NH—, R12 represents hydrogen atom or a lower alkyl group, and R13 represents hydrogen atom, —CH(R14)—COOH(R14 represents hydrogen atom, a lower alkyl group, or hydroxy group), —[CH2CH2—O]n—CH2—CH2—OH, —CH2—O—[CH2CH2—O]m—CH2—OH, or —[CH(CH3)—CO—O]p—CH(CH3)—COOH (m, n and p represent an integer of 1 to 100))], a salt thereof or an ester thereof, which has a property of being converted into a retinoid after absorption in vivo.
    • 由以下通式(I)表示的化合物:[R1至R5表示氢原子,烷基或三烷基甲硅烷基,X表示-NH-CO-,-CO-NH-,-N(COR6)-CO - ,-CO-N(COR 7) - (R 6和R 7表示低级烷氧基或羧基取代的苯基)等。 Z表示-Y-CH(R 12)-COOH,-CHO,-CH = CH-COOH或-COOR 13(Y表示单键,-CH 2 - , - CH(OH) - , - CO- -NH-或-CO-NH-CH 2 -CO-NH-,R 12表示氢原子或低级烷基,R 13表示氢原子,-CH(R 14)-COOH(R ​​14表示氢原子,低级烷基 ,或羟基), - [CH 2 CH 2 -O] n -CH 2 -CH 2 -OH,-CH 2 -O- [CH 2 CH 2 -O] m -CH 2 -OH或 - [CH(CH 3)-CO-O] CH(CH 3)-COOH(m,n和p表示1〜100的整数))],其盐或其酯,其在体内吸收后具有转化为类视黄醇的性质。