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    Phthalazine derivatives as phosphodiesterase 4 inhibitors
    1.
    发明授权
    Phthalazine derivatives as phosphodiesterase 4 inhibitors 失效
    酞嗪衍生物作为磷酸二酯酶4抑制剂

    公开(公告)号：US06340684B1

    公开(公告)日：2002-01-22

    申请号：US09764983

    申请日：2001-01-22

    申请人： Mauro Napoletano ,  Gabriele Norcini ,  Giancarlo Grancini ,  Franco Pellacini ,  Gabriele Morazzoni

    发明人： Mauro Napoletano ,  Gabriele Norcini ,  Giancarlo Grancini ,  Franco Pellacini ,  Gabriele Morazzoni

    IPC分类号： A61K31502

    CPC分类号： C07D401/06 ,  C07D237/30 ,  C07D237/32 ,  C07D237/34 ,  C07D405/06

    摘要： 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.

    摘要翻译： 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。

    Phthalazine derivatives phosphodiesterase 4 inhibitors
    2.
    发明授权
    Phthalazine derivatives phosphodiesterase 4 inhibitors 失效
    酞嗪衍生物磷酸二酯酶4抑制剂

    公开(公告)号：US06329370B1

    公开(公告)日：2001-12-11

    申请号：US09743813

    申请日：2001-01-22

    申请人： Mauro Napoletano ,  Gabriele Norcini ,  Giancarlo Grancini ,  Franco Pellacini ,  Gian Marco Leali ,  Gabriele Morazzoni

    发明人： Mauro Napoletano ,  Gabriele Norcini ,  Giancarlo Grancini ,  Franco Pellacini ,  Gian Marco Leali ,  Gabriele Morazzoni

    IPC分类号： A61K315377

    CPC分类号： C07D401/06 ,  C07D237/30 ,  C07D237/32 ,  C07D237/34 ,  C07D401/14 ,  C07D405/06 ,  C07D417/04 ,  C07D417/14

    摘要： The present invention provides a compound selected from the group including: 1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-4-phenyl-phthalazine; 4-(3,5-dichloro-pyridin-4-ylmethyl)-7-methoxy-1H-phthalazin-2-carboxylic acid methyl ester; benzyl-{3-{1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-phthalazin-5-yl}-prop-2-ynyl}-methyl-amine; 1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-5-(5-morpholin-4-yl-pent-1-ynyl)-phthalazine dihydrochloride; 3-{1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-phthalazin-5-yl}-prop-2-yn-1-ol; 1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-4-morpholin-4-yl-phthalazine; 1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-4-(1,2,4)triazol-1-yl-phthalazine; N→O derivatives thereof; and pharmaceutically acceptable salts thereof. The invention also provides a pharmaceutical composition which includes a therapeutically effective amount of the above compound in admixture with a suitable carrier.

    摘要翻译： 本发明提供了选自以下的化合物：1-（3,5-二氯 - 吡啶-4-基甲基）-6-甲氧基-4-苯基 - 酞嗪; 4-（3,5-二氯 - 吡啶-4-基甲基）-7-甲氧基-1H-酞嗪-2-甲酸甲酯; 苄基 - {3- {1-（3,5-二氯 - 吡啶-4-基甲基）-6-甲氧基 - 二氮杂萘-5-基} - 丙-2-炔基} - 甲基 - 胺; 1-（3,5-二氯 - 吡啶-4-基甲基）-6-甲氧基-5-（5-吗啉-4-基 - 戊-1-炔基） - 酞嗪二盐酸盐; 3- {1-（3,5-二氯 - 吡啶-4-基甲基）-6-甲氧基 - 二氮杂萘-5-基} - 丙-2-炔-1-醇; 1-（3,5-二氯 - 吡啶-4-基甲基）-6-甲氧基-4-吗啉-4-基 - 酞嗪; 1-（3,5-二氯 - 吡啶-4-基甲基）-6-甲氧基-4-（1,2,4）三唑-1-基 - 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，其包含治疗有效量的上述化合物与合适的载体的混合物。

    Phthalazine derivatives phosphodiesterase 4 inhibitors
    3.
    发明授权
    Phthalazine derivatives phosphodiesterase 4 inhibitors 失效

    公开(公告)号：US06492360B1

    公开(公告)日：2002-12-10

    申请号：US09976436

    申请日：2001-10-15

    申请人： Mauro Napoletano ,  Gabriele Norcini ,  Giancarlo Grancini ,  Franco Pellacini ,  Gian Marco Leali ,  Gabriele Morazzoni

    发明人： Mauro Napoletano ,  Gabriele Norcini ,  Giancarlo Grancini ,  Franco Pellacini ,  Gian Marco Leali ,  Gabriele Morazzoni

    IPC分类号： A61K31502

    CPC分类号： C07D401/06 ,  C07D237/30 ,  C07D237/32 ,  C07D237/34 ,  C07D401/14 ,  C07D405/06 ,  C07D417/04 ,  C07D417/14

    摘要： Compounds of formula (I), wherein is a single or double bond; Z is NH, methylene, a (C2-C6)alkylene chain optionally branched and/or unsaturated and/or interrupted by a (C5-C7)cycloalkyl residue; A is phenyl or heterocycle optionally substituted or a COR4 group wherein R4 is hydroxy, (C1-C6)-alkoxy, amino optionally substituted; R is a (C1-C6)alkyl or polyfluoro(C1-C6)alkyl group; R1 is absent when is a double bond or, when is a single bond, is (a) hydrogen; (b) (C1-C6)alkyl optionally substituted; (c) —COR6 wherein R6 is hydrogen, aryl, aryl-(C1-C6)alkyl, amino optionally alkylated or monohydroxylated, hydroxy, (C1-C4)alkoxy, carboxy, (C1-C4)alkoxycarbonyl, formula (1), or (C1-C4)alkyl optionally substituted by heterocycle; (d) (C1-C4)-alkylsulfonyl; R2 represents two hydrogen atoms or a group —O when is a single bond, or, when is a double bond, R2 is hydrogen, cyano, (C1-C4)alkoxycarbonyl, amido, optionally substituted aryl or heterocycle, (C1-C8)alkyl, (C2-C8)alkenyl or (C2-C8)alkynyl optionally branched and/or substituted; aryloxy, heterocyclyloxy, aryl-(C1-C4)alkoxy, heterocyclyloxy-(C1-C4)alkoxy, amino substituted by one or two (C1-C4)-alkyl group(s), arylamino, heterocyclylamino, aryl-(C1-C4)alkylamino, heterocyclyl-(C1-C4)-alkylamino; R3 is hydrogen, or a (C1-C8)alkyl, (C2-C8)alkenyl or (C2-C8)alkynyl group optionally substituted, and optionally interrupted; the N→O derivatives of the compounds of formula (I) and the pharmaceutically acceptable salts thereof are PDE 4 inhibitors.

    Benzazine derivatives as phosphodiesterase 4 inhibitors
    4.
    发明授权
    Benzazine derivatives as phosphodiesterase 4 inhibitors 失效
    苯并嗪衍生物作为磷酸二酯酶4抑制剂

    公开(公告)号：US06358973B1

    公开(公告)日：2002-03-19

    申请号：US09806496

    申请日：2001-04-13

    申请人： Mauro Napoletano ,  Gabriele Norcini ,  Giancarlo Grancini ,  Franco Pellacini ,  Gabriele Morazzoni ,  Lorenzo Pradella

    发明人： Mauro Napoletano ,  Gabriele Norcini ,  Giancarlo Grancini ,  Franco Pellacini ,  Gabriele Morazzoni ,  Lorenzo Pradella

    IPC分类号： C07D4006

    CPC分类号： C07D401/06

    摘要： 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.

    摘要翻译： 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。

    Tricyclic phthalazine derivatives as phosphodiesterase 4 inhibitors
    6.
    发明授权
    Tricyclic phthalazine derivatives as phosphodiesterase 4 inhibitors 失效
    三环酞嗪衍生物作为磷酸二酯酶4抑制剂

    公开(公告)号：US06525055B1

    公开(公告)日：2003-02-25

    申请号：US09830679

    申请日：2001-04-30

    申请人： Mauro Napoletano ,  Gabriele Norcini ,  Franco Pellacini ,  Gabriele Morazzoni

    发明人： Mauro Napoletano ,  Gabriele Norcini ,  Franco Pellacini ,  Gabriele Morazzoni

    IPC分类号： A61K315025

    CPC分类号： C07D487/04

    摘要： 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.

    摘要翻译： 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。