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    • 3. 发明授权
    • Phthalazine derivatives as phosphodiesterase 4 inhibitors
    • 酞嗪衍生物作为磷酸二酯酶4抑制剂
    • US06340684B1
    • 2002-01-22
    • US09764983
    • 2001-01-22
    • Mauro NapoletanoGabriele NorciniGiancarlo GranciniFranco PellaciniGabriele Morazzoni
    • Mauro NapoletanoGabriele NorciniGiancarlo GranciniFranco PellaciniGabriele Morazzoni
    • A61K31502
    • C07D401/06C07D237/30C07D237/32C07D237/34C07D405/06
    • The present invention provides a compound selected from the group including: N-3-acetyl-1-(3,5-dichloropyridin-4-ylmethyl)-5-cyclopentyloxy-6-methoxy-4H-phthalazine; 6,7-dimethoxy-1-pyridin-4-ylmethyl-4-thiazol-2-yl-phthalazine; 1-(6,7-dimethoxy-4-pyridin-4-ylmethyl-1H-phthalazin-2-yl)ethanone; 2-methanesulphonyl-6,7-dimethoxy-4-pyridin-4-ylmethyl-1,2-dihydrophthalazine; 2-formyl-6,7-dimethoxy-4-pyridin-4-ylmethyl-1,2-dihydrophthalazine; 1-(6,7-dimethoxy-4-pyridin-4-ylmethyl-1H-phthalazin-2-yl)-1-imidazol-1-ylmethanone; 1-(3,5-dichloro-pyridin-4-ylmethyl)-3-methansulphonyl-6-difluoromethoxy-5-(tetrahydro-furan-2-yloxy)-4H-phthalazine; N→O derivatives thereof; and pharmaceutically acceptable salts thereof. The invention also provides a pharmaceutical composition, which contains a therapeutically effective amount of the above compound in admixture with a pharmaceutically acceptable carrier.
    • 本发明提供了选自以下的化合物:N-3-乙酰基-1-(3,5-二氯吡啶-4-基甲基)-5-环戊基氧基-6-甲氧基-4H-酞嗪; 6,7-二甲氧基-1-吡啶-4-基甲基-4-噻唑-2-基 - 酞嗪; 1-(6,7-二甲氧基-4-吡啶-4-基甲基-1H-酞嗪-2-基)乙酮; 2-甲磺酰基-6,7-二甲氧基-4-吡啶-4-基甲基-1,2-二氢酞嗪; 2-甲酰基-6,7-二甲氧基-4-吡啶-4-基甲基-1,2-二氢酞嗪; 1-(6,7-二甲氧基-4-吡啶-4-基甲基-1H-酞嗪-2-基)-1-咪唑-1-基甲酮; 1-(3,5-二氯 - 吡啶-4-基甲基)-3-甲磺酰基-6-二氟甲氧基-5-(四氢 - 呋喃-2-基氧基)-4H-酞嗪; 其N-> O衍生物; 及其药学上可接受的盐。 本发明还提供一种药物组合物,其含有治疗有效量的上述化合物与药学上可接受的载体的混合物。
    • 5. 发明授权
    • Benzazine derivatives as phosphodiesterase 4 inhibitors
    • 苯并嗪衍生物作为磷酸二酯酶4抑制剂
    • US06358973B1
    • 2002-03-19
    • US09806496
    • 2001-04-13
    • Mauro NapoletanoGabriele NorciniGiancarlo GranciniFranco PellaciniGabriele MorazzoniLorenzo Pradella
    • Mauro NapoletanoGabriele NorciniGiancarlo GranciniFranco PellaciniGabriele MorazzoniLorenzo Pradella
    • C07D4006
    • C07D401/06
    • Compounds of formula I: wherein A is a heterocycle containing a nitrogen atom and optionally saturated or unsaturated and optionally further substituted by an oxo group (═O); R is: hydrogen, cyano, (C1-4)alkoxycarbonyl, carbamoyl; optionally substituted (C4-7)-cycloalkyl, aryl or heterocycle; (C1-8)alkyl, (C2-8)alkenyl or (C2-8)alkynyl optionally branched and/or substituted by (C4-7) cycloalkyl, aryl or heterocycle; aryloxy, heterocyclyloxy, aryl(C1-4)alkoxy, heterocyclyl(C1-4)alkoxy, amino substituted by one or two (C1-4)alkyl group(s), aryl-amino, heterocyclyl-amino, aryl(C1-4)alkyl-amino, or heterocyclyl(C1-4)alkylamino; Y is methylene or ethylene; W is an optionally substituted aryl or heterocycle; R1 is hydrogen, (C4-7)cycloalkyl or a (C2-8)alkyl, (C2-8)alkenyl or (C2-8)alkynyl group optionally substituted by hydroxy, oxo, (C4-7)cycloalkyl, aryl or heterocycle, and optionally interrupted by one or more heteroatom(s) or heterogroup(s); R2 is a (C1-6)alkyl or polyfluoro(C1-6)alkyl group; the N→O derivatives of the compounds of formula I and the pharmaceutically acceptable salts thereof. The compounds of formula (I) are PDE 4 inhibitors and may be used in compositions and methods involving PDE 4 inhibition.
    • 式I化合物:其中A是含有氮原子,任选饱和或不饱和并任选进一步被氧代基(= O)取代的杂环; R为:氢,氰基,(C 1-4)烷氧基羰基,氨基甲酰基; 任选取代的(C 4-7) - 环烷基,芳基或杂环; (C 1-8)烷基,(C 2-8)烯基或任选被(C 4-7)环烷基,芳基或杂环支链和/或取代的(C 2-8)炔基; 芳氧基,杂环氧基,芳基(C 1-4)烷氧基,杂环基(C 1-4)烷氧基,被一个或两个(C 1-4)烷基取代的氨基,芳基 - 氨基,杂环基 - 氨基,芳基 )烷基 - 氨基或杂环基(C 1-4)烷基氨基; Y是亚甲基或亚乙基; W是任选取代的芳基或杂环; R1是氢,(C4-7)环烷基或(C2-8)烷基,(C2-8)烯基或(C2-8)炔基,任选被羟基,氧代,(C 4-7)环烷基,芳基或杂环 并且任选被一个或多个杂原子或杂团中断; R2是(C1-6)烷基或多氟(C1-6)烷基; 式I化合物的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,可用于涉及PDE4抑制的组合物和方法。
    • 8. 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。