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    • 8. 发明授权
    • 3′-ethynylcytidine derivative
    • 3'-乙炔基胞苷衍生物
    • US08058261B2
    • 2011-11-15
    • US12375077
    • 2007-07-23
    • Motoaki TanakaMasakazu Fukushima
    • Motoaki TanakaMasakazu Fukushima
    • A01N43/04A61K31/70
    • C07H19/06
    • To provide a compound which exhibits excellent anti-tumor activity and excellent oral absorption and which is a useful anti-tumor drug.The invention provides a 3′-ethynylcytidine derivative represented by formula (1): (wherein X represents a (substituted) alkylcarbonyl group, a (substituted) alkoxycarbonyl group, or a hydrogen atom; one of Y and Z represents a hydrogen atom or a group represented by (R1)(R2)(R3)Si— and the other represents a group represented by (R4)(R5)(R6)Si—; and R1, R2, R3, R4, R5, and R6 each represent a (substituted) alkyl group, a (substituted) cyclic alkyl group, or a (substituted) aryl group) or a salt thereof.
    • 提供表现出优异的抗肿瘤活性和优异的口服吸收并且是有用的抗肿瘤药物的化合物。 本发明提供由式(1)表示的3'-乙炔基胞苷衍生物:其中X表示(取代)烷基羰基,(取代)烷氧基羰基或氢原子; Y和Z之一表示氢原子或 (R 1)(R 2)(R 3)Si表示的基团,另一个表示由(R 4)(R 5)(R 6)Si - 表示的基团,R 1,R 2,R 3,R 4,R 5和R 6各自表示 (取代的)烷基,(取代的)环烷基或(取代的)芳基)或其盐。
    • 9. 发明申请
    • 3'-ETHYNYLCYTIDINE DERIVATIVE
    • 3'-乙酰基衍生物
    • US20090306008A1
    • 2009-12-10
    • US12375077
    • 2007-07-23
    • Motoaki TanakaMasakazu Fukushima
    • Motoaki TanakaMasakazu Fukushima
    • A61K31/7068C07H19/067A61P35/00
    • C07H19/06
    • To provide a compound which exhibits excellent anti-tumor activity and excellent oral absorption and which is a useful anti-tumor drug.The invention provides a 3′-ethynylcytidine derivative represented by formula (1): (wherein X represents a (substituted) alkylcarbonyl group, a (substituted) alkoxycarbonyl group, or a hydrogen atom; one of Y and Z represents a hydrogen atom or a group represented by (R1)(R2)(R3)Si— and the other represents a group represented by (R4)(R5)(R6)Si—; and R1, R2, R3, R4, R5, and R6 each represent a (substituted) alkyl group, a (substituted) cyclic alkyl group, or a (substituted) aryl group) or a salt thereof.
    • 提供表现出优异的抗肿瘤活性和优异的口服吸收并且是有用的抗肿瘤药物的化合物。 本发明提供由式(1)表示的3'-乙炔基胞苷衍生物:其中X表示(取代)烷基羰基,(取代)烷氧基羰基或氢原子; Y和Z之一表示氢原子或 (R 1)(R 2)(R 3)Si表示的基团,另一个表示由(R 4)(R 5)(R 6)Si - 表示的基团,R 1,R 2,R 3,R 4,R 5和R 6各自表示 (取代的)烷基,(取代的)环烷基或(取代的)芳基)或其盐。