[发明专利]Rapafucin衍生物化合物及其使用方法

权利要求书

1.一种根据式(XIV)的大环化合物：

或其立体异构体、溶剂化物或药学上可接受的盐，

每个n、m和p独立地是选自0至5的整数；

每个R₁、R₂和R₃独立地选自由以下组成的组：H、F、Cl、Br、CF₃、CN、N₃、-N(R₁₂)₂、-N(R₁₂)₃、-CON(R₁₂)₂、NO₂、OH、OCH₃、甲基、乙基、丙基、-COOH、-SO₃H、-PO(OR₁₂)₂、-OPO(OR₁₂)₂、-(CH₂)_qCOOH、-O-(CH₂)_qCOOH、-S-(CH₂)_qCOOH、-CO-(CH₂)_qCOOH、-NR₁₂-(CH₂)_qCOOH、-(CH₂)_qSO₃H、-O-(CH₂)_qSO₃H、-S-(CH₂)_qSO₃H、-CO-(CH₂)_qSO₃H、-NR₁₂-(CH₂)_qSO₃H、-(CH₂)_qN(R₁₂)₂、-O-(CH₂)_qN(R₁₂)₂、-S-(CH₂)_qN(R₁₂)₂、-CO-(CH₂)_qN(R₁₂)₂、-(CH₂)_qN(R₁₂)₃、-O-(CH₂)_qN(R₁₂)₃、-S-(CH₂)_qN(R₁₂)₃、-CO-(CH₂)_qN(R₁₂)₃、-NR₁₂-(CH₂)_qN(R₁₂)₃、-(CH₂)_qCON(R₁₂)₂、-O-(CH₂)_qCON(R₁₂)₂、-S-(CH₂)_qCON(R₁₂)₂、-CO-(CH₂)_qCON(R₁₂)₂、-(CH₂)_qPO(OR₁₂)₂、-O(CH₂)_qPO(OR₁₂)₂、-S(CH₂)_qPO(OR₁₂)₂、-CO(CH₂)_qPO(OR₁₂)₂、-NR₁₂(CH₂)_qPO(OR₁₂)₂、-(CH₂)_qOPO(OR₁₂)₂、-O(CH₂)_qOPO(OR₁₂)₂、-S(CH₂)_qOPO(OR₁₂)₂、-CO(CH₂)_qOPO(OR₁₂)₂以及-NR₁₂(CH₂)_qOPO(OR₁₂)₂；

q是选自0至5的整数；

每个R₄、R₅、R₆、R₇、R₉和R₁₁独立地选自由以下组成的组：H、甲基、乙基、丙基和异丙基；

每个R₈和R₁₀独立地选自由以下组成的组：H、卤素、羟基、C_1-20烷基、N₃、NH₂、NO₂、CF₃、OCF₃、OCHF₂、COC_1-20烷基、CO₂C_1-20烷基、与相邻氮形成的5元或6元环状结构部分、-N(R₁₂)₂、-N(R₁₂)₃、-CON(R₁₂)₂、-COOH、-SO₃H、-PO(OR₁₂)₂、-OPO(OR₁₂)₂、-(CH₂)_qCOOH、-O-(CH₂)_qCOOH、-S-(CH₂)_qCOOH、-CO-(CH₂)_qCOOH、-NR₁₂-(CH₂)_qCOOH、-(CH₂)_qSO₃H、-O-(CH₂)_qSO₃H、-S-(CH₂)_qSO₃H、-CO-(CH₂)_qSO₃H、-NR₁₂-(CH₂)_qSO₃H、-(CH₂)_qN(R₁₂)₂、-O-(CH₂)_qN(R₁₂)₂、-S-(CH₂)_qN(R₁₂)₂、-CO-(CH₂)_qN(R₁₂)₂、-(CH₂)_qN(R₁₂)₃、-O-(CH₂)_qN(R₁₂)₃、-S-(CH₂)_qN(R₁₂)₃、-CO-(CH₂)_qN(R₁₂)₃、-NR₁₂-(CH₂)_qN(R₁₂)₃、-(CH₂)_qCON(R₁₂)₂、-O-(CH₂)_qCON(R₁₂)₂、-S-(CH₂)_qCON(R₁₂)₂、-CO-(CH₂)_qCON(R₁₂)₂、-(CH₂)_qPO(OR₁₂)₂、-O(CH₂)_qPO(OR₁₂)₂、-S(CH₂)_qPO(OR₁₂)₂、-CO(CH₂)_qPO(OR₁₂)₂、-NR₁₂(CH₂)_qPO(OR₁₂)₂、-(CH₂)_qOPO(OR₁₂)₂、-O(CH₂)_qOPO(OR₁₂)₂、-S(CH₂)_qOPO(OR₁₂)₂、-CO(CH₂)_qOPO(OR₁₂)₂以及-NR₁₂(CH₂)_qOPO(OR₁₂)₂；

每个R₁₂独立地选自由以下组成的组：H、甲基、乙基、丙基和异丙基；

条件是R₂、R₃、R₈和R₁₀中的至少一个选自-N(R₁₂)₂、-N(R₁₂)₃、-CON(R₁₂)₂、-COOH、-SO₃H、-PO(OR₁₂)₂、-OPO(OR₁₂)₂、-(CH₂)_qCOOH、-O-(CH₂)_qCOOH、-S-(CH₂)_qCOOH、-CO-(CH₂)_qCOOH、-NR₁₂-(CH₂)_qCOOH、-(CH₂)_qSO₃H、-O-(CH₂)_qSO₃H、-S-(CH₂)_qSO₃H、-CO-(CH₂)_qSO₃H、和-NR₁₂-(CH₂)_qSO₃H、-(CH₂)_qN(R₁₂)₂、-O-(CH₂)_qN(R₁₂)₂、-S-(CH₂)_qN(R₁₂)₂、-CO-(CH₂)_qN(R₁₂)₂、-(CH₂)_qN(R₁₂)₃、-O-(CH₂)_qN(R₁₂)₃、-S-(CH₂)_qN(R₁₂)₃、-CO-(CH₂)_qN(R₁₂)₃、-NR₁₂-(CH₂)_qN(R₁₂)₃、-(CH₂)_qCON(R₁₂)₂、-O-(CH₂)_qCON(R₁₂)₂、-S-(CH₂)_qCON(R₁₂)₂、-CO-(CH₂)_qCON(R₁₂)₂、-(CH₂)_qPO(OR₁₂)₂、-O(CH₂)_qPO(OR₁₂)₂、-S(CH₂)_qPO(OR₁₂)₂、-CO(CH₂)_qPO(OR₁₂)₂、-NR₁₂(CH₂)_qPO(OR₁₂)₂、-(CH₂)_qOPO(OR₁₂)₂、-O(CH₂)_qOPO(OR₁₂)₂、-S(CH₂)_qOPO(OR₁₂)₂、-CO(CH₂)_qOPO(OR₁₂)₂以及-NR₁₂(CH₂)_qOPO(OR₁₂)₂。