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    Semicarbazide derivatives, processes for preparation thereof and pharmaceutical composition comprising the same
    1.
    发明公开
    Semicarbazide derivatives, processes for preparation thereof and pharmaceutical composition comprising the same 失效
    氨基脲衍生物，其制备方法和包含其的药物组合物

    公开(公告)号：EP0144853A3

    公开(公告)日：1986-01-29

    申请号：EP84114005

    申请日：1984-11-20

    申请人： FUJISAWA PHARMACEUTICAL CO., LTD.

    发明人： Nakaguchi, Osamu ,  Shimazaki, Norihiko ,  Kawai, Yoshio ,  Hashimoto, Masashi ,  Nakatuka, Michie

    IPC分类号： C07D211/70 ,  C07D237/04 ,  C07D203/26 ,  C07C133/02 ,  C07C159/00 ,  C07D295/22 ,  A61K31/175 ,  A61K31/445 ,  A61K31/50 ,  A61K31/395

    CPC分类号： C07D213/89 ,  C07D203/26 ,  C07D211/70 ,  C07D237/04 ,  C07D295/32

    摘要： New semicarbazide derivatives of the formula:
    wherein
    R' is hydrogen, R 2 is hydrogen, lower alkyl, ar(lower)alkyl, lower alkenyl or aryl, R 3 is lower alkyl, ar(lower)alkyl, lower alkenyl or aryl, or R 2 and R 3 are taken together to form (C 2 -C 6 )-alkylidene group optionally substituted with aryl or taken together with the adjacent nitrogen atom to form a saturated or unsaturated, 5- or 6-membered heterocyclic group optionally substituted with aryl; or R' and R 2 are taken together with the adjacent nitrogen atoms to form a saturated or unsaturated, 5- or 6-membered heterocyclic group or 1,2-diazaspiroalkane-1,2-diyl group, R 3 is hydrogen, lower alkyl, ar(lower)alkyl, lower alkeny or aryl; R 4 is aryl which may have substituent(s) selected from lower alkyl, halogen, lower alkoxy, lower alkylamino, halo(lower)alkyl, hydroxy, lower alkanoyl, esterified carboxy and carboxy, R 5 is hydrogen or lower alkyl, and X is 0 or S, provided that the lower alkyl group for R 3 is (C 3 -C 6 ) alkyl, when R 2 is hydrogen or (C 1 -C 2 ) alkyl and R 4 is aryl optionally having substituent(s) selected from groups consisting of halogen, lower alkyl, lower alkoxy and halo(lower)alkyl, and pharmaceutically acceptable salts thereof, and processes for preparation thereof and pharmaceutical composition comprising the same. These derivatives and salts thereof are useful as antiinflammatory and analgesic agents.

    摘要翻译： 下式的新氨基脲衍生物：其中R'为氢，R2为氢，低级烷基，芳（低级）烷基，低级链烯基或芳基，R3为低级烷基，芳（低级）烷基，低级链烯基或芳基， R 3一起形成任选被芳基取代或与相邻氮原子一起形成饱和或不饱和的任选被芳基取代的5或6元杂环基的（C 2 -C 6） - 烷叉基; 或者R'和R2与相邻的氮原子一起形成饱和或不饱和的5-或6-元杂环基或1,2-二氮杂螺烷-1,2-二基，R3是氢，低级烷基，芳基 （低级）烷基，低级烯基或芳基; R4是可以具有选自低级烷基，卤素，低级烷氧基，低级烷基氨基，卤代（低级）烷基，羟基，低级烷酰基，酯化羧基和羧基的取代基的芳基，R5是氢或低级烷基，并且X是0 或S，条件是当R 2为氢或（C 1 -C 2）烷基时，R 3的低级烷基为（C 3 -C 6）烷基，且R 4为任选具有选自卤素，低级烷基， 低级烷氧基和卤代（低级）烷基，及其药学上可接受的盐，及其制备方法和包含其的药物组合物。 这些衍生物及其盐可用作抗炎剂和镇痛剂。

    Semicarbazide derivatives, processes for preparation thereof and pharmaceutical composition comprising the same
    4.
    发明公开
    Semicarbazide derivatives, processes for preparation thereof and pharmaceutical composition comprising the same 失效
    氨基脲衍生物，它们的制备方法和含有它们的药物组合物。

    公开(公告)号：EP0144853A2

    公开(公告)日：1985-06-19

    申请号：EP84114005.6

    申请日：1984-11-20

    申请人： FUJISAWA PHARMACEUTICAL CO., LTD.

    发明人： Nakaguchi, Osamu ,  Shimazaki, Norihiko ,  Kawai, Yoshio ,  Hashimoto, Masashi ,  Nakatuka, Michie

    IPC分类号： C07C271/58 ,  C07D211/70 ,  C07D237/04 ,  C07D203/26 ,  A61K31/175 ,  A61K31/445 ,  A61K31/50 ,  A61K31/395

    CPC分类号： C07D213/89 ,  C07D203/26 ,  C07D211/70 ,  C07D237/04 ,  C07D295/32

    摘要： New semicarbazide derivatives of the formula:
    wherein

    R' is hydrogen,
    R 2 is hydrogen, lower alkyl, ar(lower)alkyl, lower alkenyl or aryl,
    R 3 is lower alkyl, ar(lower)alkyl, lower alkenyl or aryl, or
    R 2 and R 3 are taken together to form (C 2 -C 6 )-alkylidene group optionally substituted with aryl or taken together with the adjacent nitrogen atom to form a saturated or unsaturated, 5- or 6-membered heterocyclic group optionally substituted with aryl; or
    R' and R 2 are taken together with the adjacent nitrogen atoms to form a saturated or unsaturated, 5- or 6-membered heterocyclic group or 1,2-diazaspiroalkane-1,2-diyl group,
    R 3 is hydrogen, lower alkyl, ar(lower)alkyl, lower alkeny or aryl;
    R 4 is aryl which may have substituent(s) selected from lower alkyl, halogen, lower alkoxy, lower alkylamino, halo(lower)alkyl, hydroxy, lower alkanoyl, esterified carboxy and carboxy,
    R 5 is hydrogen or lower alkyl, and
    X is 0 or S, provided that the lower alkyl group for R 3 is (C 3 -C 6 ) alkyl, when R 2 is hydrogen or (C 1 -C 2 ) alkyl and R 4 is aryl optionally having substituent(s) selected from groups consisting of halogen, lower alkyl, lower alkoxy and halo(lower)alkyl, and pharmaceutically acceptable salts thereof, and processes for preparation thereof and pharmaceutical composition comprising the same.

    These derivatives and salts thereof are useful as antiinflammatory and analgesic agents.