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    Phthalazine derivatives as phosphodiesterase 4-inhibitors
    1.
    发明申请
    Phthalazine derivatives as phosphodiesterase 4-inhibitors 审中-公开
    酞嗪衍生物作为磷酸二酯酶4-抑制剂

    公开(公告)号：US20040043999A1

    公开(公告)日：2004-03-04

    申请号：US10441177

    申请日：2003-05-20

    申请人： Zambon Group S.p.A

    发明人： Mauro Napoletano ,  Gabriele Norcini ,  Daniela Botta ,  Giancarlo Grancini ,  Gabriele Morazzoni ,  Francesco Santangelo ,  Jorge G. Siro Herrero ,  Jose Luis Garcia Navaio ,  Julio G. Alvarez-Builla

    IPC分类号： C07D237/30 ,  A61K031/502

    CPC分类号： C07D401/06 ,  C07D237/30 ,  C07D237/34 ,  C07D401/12 ,  C07D405/12

    摘要： A process for preparing a compound of formula I: 1 wherein G is methylene, ethylene, CONH, amino or a bond; R is H, phenyl or a (C1-4)alkyl group optionally substituted by phenyl; Cy is phenyl or a 5- or 6-membered heterocycle of the group consisting of pyrrole, imidazole, pyrazole, pyrrolidine, pyrroline, imidazoline, imidazolidine, pyrazolidine, pyrazoline, pyridine, pyrazine, pyrimidine, pyridazine, piperazine, piperidine, and triazine, the Cy residue being optionally substituted by one or more substituent(s) selected from the group consisting of keto, nitro, carboxy, fluorine, chlorine, bromine, or iodine; R1 is a (C1-6)alkyl or polyfluoro(C1-6)alkyl group; and R2 is aryl, aryl-(C1-10)-alkyl, (C4-7)cycloalkyl or (C4-7)heterocycle wherein the heteroatom is an oxygen atom.

    摘要翻译： 制备式I化合物的方法：其中G是亚甲基，亚乙基，CONH，氨基或键; R是H，苯基或任选被苯基取代的（C 1-4）烷基; Cy是苯基或由吡咯，咪唑，吡唑，吡咯烷，吡咯啉，咪唑啉，咪唑烷，吡唑烷，吡唑啉，吡啶，吡嗪，嘧啶，哒嗪，哌嗪，哌啶和三嗪组成的组的5-或6-元杂环， Cy残基任选被一个或多个选自酮，硝基，羧基，氟，氯，溴或碘的取代基取代; R1是（C1-6）烷基或多氟（C1-6）烷基; 并且R 2是芳基，芳基 - （C 1-10） - 烷基，（C 4-7）环烷基或（C 4-7）杂环，其中杂原子是氧原子。