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    • 9. 发明授权
    • Tricyclic phthalazine derivatives as phosphodiesterase 4 inhibitors
    • 三环酞嗪衍生物作为磷酸二酯酶4抑制剂
    • US06525055B1
    • 2003-02-25
    • US09830679
    • 2001-04-30
    • Mauro NapoletanoGabriele NorciniFranco PellaciniGabriele Morazzoni
    • Mauro NapoletanoGabriele NorciniFranco PellaciniGabriele Morazzoni
    • A61K315025
    • C07D487/04
    • Tricyclic phthalazine compounds of formula (I) wherein A is a 5-7 membered heterocycle containing from 1 to 4 nitrogen atoms, optionally partially or totally unsaturated, and optionally substituted by a (C1-4)alkyl group in turn optionally substituted; Z is NH, methylene, a C2-6 alkylene chain optionally branched and/or unsaturated and/or interrupted by a C5-7 cycloalkyl residue; Cy is phenyl or heterocycle optionally substituted by one or more substituents, or a COR4 group wherein R4 is hydroxy, alkoxy, amino optionally substituted by one or two (C1-6)alkyl groups or by hydroxy; R is a (C1-6)alkyl or polyfluoro(C1-6)alkyl group; R1 is hydrogen; a (C1-8)-alkyl, (C2-8)-alkenyl or (C2-8)-alkynyl group optionally substituted by hydroxy, oxo, aryl or heterocycle, and optionally interrupted by one or more heteroatoms or heterogroups; a (C1-4)alkoxy group or a (C4-7)cycloalkoxy group optionally containing an oxygen atom and optionally substituted by a polar substituent in the cyclic moiety, aryloxy aryl-(C1-10)-alkoxy; the N—O derivatives and the pharmaceutically acceptable salts thereof are described. The compounds of formula (I) are PDE 4 inhibitors.
    • 式(I)的三环酞嗪化合物,其中A是含有1至4个氮原子的5-7元杂环,任选地部分或完全不饱和,并且任选地被(C 1-4)烷基取代, Z是NH,亚甲基,任选支链和/或不饱和的和/或被C5-7环烷​​基残基中断的C2-6亚烷基链; Cy是任选被一个或多个取代基取代的苯基或杂环,或其中R4是羟基,烷氧基,任选被一个或两个(C 1-6)烷基或羟基取代的氨基的COR 4基团; R为(C 1-6)烷基或多氟(C 1-6)烷基; R1是氢; 任选被羟基,氧代,芳基或杂环取代的(C 1-8) - 烷基,(C 2-8) - 烯基或(C 2-8) - 炔基,并且任选被一个或多个杂原子或杂团中断; 芳氧基芳基 - (C 1-10) - 烷氧基,(C 1-4)烷氧基或任选含有氧原子且任选被环状部分中的极性取代基取代的(C 4-7)环烷氧基; 描述了N-O衍生物及其药学上可接受的盐。 式(I)化合物是PDE 4抑制剂。