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    • 5. 发明授权
    • Nucleoside and oligonucleotide analogues
    • 核苷和寡核苷酸类似物
    • US07335765B2
    • 2008-02-26
    • US09925673
    • 2001-08-09
    • Masakatsu KanekoKoji MoritaTakeshi Imanishi
    • Masakatsu KanekoKoji MoritaTakeshi Imanishi
    • C07H19/00C07H21/00C07H19/06C70H19/16
    • C07H19/10C07H19/06C07H19/16C07H19/20Y02P20/55Y10T436/143333
    • A compound of the formula (1): wherein R1 and R2 are the same or different and represent a hydrogen atom, a hydroxyl protecting group, a phosphate group, or —P(R3)R4, wherein R3 and R4 are the same or different and represent a hydroxyl group, an amino group, an alkoxy group having from 1 to 4 carbon atoms, a cyanoalkoxy group having from 1 to 5 carbon atoms or an amino group substituted by an alkyl group having from 1 to 4 carbon atoms; A represents an alkylene group having from 1 to 4 carbon atoms and B represents a purin-9-yl group, a 2-oxo-pyrimidin-1-yl group, a substituted purin-9-yl group or a substituted 2-oxo-pyrimidin-1-yl group having a substituent α selected from the group consisting of a hydroxyl group which may be protected, an alkoxy group having from 1 to 4 carbon atoms, a mercapto group which may be protected, an alkylthio group having from 1 to 4 carbon atoms, an alkoxy group having from 1 to 4 carbon atoms, an amino group which may be protected, a mono- or di-alkylamino group which may be substituted by an alkyl group having from 1 to 4 carbon atoms, an alkyl group having from 1 to 4 carbon atoms and a halogen atom; or a salt thereof.
    • 式(1)的化合物:其中R 1和R 2相同或不同,表示氢原子,羟基保护基,磷酸基或 -P(R 3)R 4,其中R 3和R 4相同或不同,表示 羟基,氨基,具有1至4个碳原子的烷氧基,具有1至5个碳原子的氰基烷氧基或被具有1至4个碳原子的烷基取代的氨基; A表示具有1至4个碳原子的亚烷基,B表示嘌呤-9-基,2-氧代 - 嘧啶-1-基,取代的嘌呤-9-基或取代的2-氧代 - 具有选自可被保护的羟基,具有1至4个碳原子的烷氧基,可被保护的巯基的取代基的嘧啶-1-基,具有1至4个碳原子的烷硫基, 4个碳原子,具有1至4个碳原子的烷氧基,可被保护的氨基,可以被具有1至4个碳原子的烷基取代的一烷基或二烷基氨基,烷基 具有1至4个碳原子和卤素原子; 或其盐。