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    Pharmaceutical composition containing 1,1,3,5-substituted biuret compound
    3.
    发明授权
    Pharmaceutical composition containing 1,1,3,5-substituted biuret compound 失效
    含有1,1,3,5-取代缩二脲化合物的药物组合物

    公开(公告)号：US4371544A

    公开(公告)日：1983-02-01

    申请号：US257418

    申请日：1981-04-24

    申请人： Hajime Fujimura ,  Yasuzo Hiramatsu ,  Takahiro Yabuuchi ,  Masakatu Hisaki ,  Katsuo Takikawa ,  Takaji Honna ,  Hidekazu Miyake ,  Makoto Kajitani

    发明人： Hajime Fujimura ,  Yasuzo Hiramatsu ,  Takahiro Yabuuchi ,  Masakatu Hisaki ,  Katsuo Takikawa ,  Takaji Honna ,  Hidekazu Miyake ,  Makoto Kajitani

    IPC分类号： A61K31/17 ,  C07C275/62 ,  C07D295/215

    CPC分类号： C07D295/215 ,  A61K31/17 ,  C07C275/62 ,  Y10S514/887 ,  Y10S514/916

    摘要： An analgesic, anti-inflammatory or anti-pyretic composition containing 1,1,3,5-substituted biuret compound of the formula, ##STR1## wherein R.sup.1 is a lower alkyl group or a phenyl group; R.sup.2 is a lower alkyl group, a phenyl group or a substituted phenyl group having chlorine atom(s), methyl group(s) or methoxy group(s) as the substituent(s), further R.sup.1 and R.sup.2 may form a single ring containing one or two hetero atoms including the adjacent nitrogen atom; R.sup.3 is a hydrogen atom, a lower alkyl group or a phenyl group; R.sup.4 is a phenyl group, a substituted phenyl group having halogen atom(s), trifluoromethyl group(s), methyl group(s), methoxy group(s), dimethyl-amino group(s), nitro group(s), hydroxyl group(s), acetyl group(s), or methylthio group(s) as the substituent(s), a benzyl group, a cyclohexyl group or a lower alkyl group, as the active ingredient.

    摘要翻译： 含有下式的1,1,3,5-取代缩二脲化合物的镇痛，抗炎或抗热解组合物，其中R1是低级烷基或苯基; R2是低级烷基，苯基或具有氯原子的取代苯基，甲基或甲氧基作为取代基，此外，R 1和R 2可以形成含有 一个或两个杂原子，包括相邻的氮原子; R3是氢原子，低级烷基或苯基; R4是苯基，具有卤素原子的取代苯基，三氟甲基，甲基，甲氧基，二甲基 - 氨基，硝基，羟基 基团，乙酰基或甲硫基作为取代基，苄基，环己基或低级烷基作为活性成分。

    N-substituted guanidino acid derivatives
    8.
    发明授权
    N-substituted guanidino acid derivatives 失效
    N-取代胍基酸衍生物

    公开(公告)号：US3935266A

    公开(公告)日：1976-01-27

    申请号：US192557

    申请日：1971-10-26

    申请人： Sadao Hashimoto ,  Ryuji Sakakibara ,  Yasushi Kurashige ,  Katsuo Takikawa ,  Yoko Osame ,  Hiroshi Minami ,  Takashi Suzue

    发明人： Sadao Hashimoto ,  Ryuji Sakakibara ,  Yasushi Kurashige ,  Katsuo Takikawa ,  Yoko Osame ,  Hiroshi Minami ,  Takashi Suzue

    IPC分类号： A61K31/16 ,  A61K31/165 ,  C07C67/00 ,  C07C239/00 ,  C07C279/14 ,  C07C103/30

    CPC分类号： C07C279/14

    摘要： An N-substituted guanidino acid derivatives having the following formula of ##EQU1## wherein R is an alkyl having 6 to 15 carbon atoms,. a cycloalkyl having 6 to 15 carbon atoms or an aryl(C.sub.6 to C.sub.8)alkyl(C.sub.1 to C.sub.9); A represents R.sup.1 or R.sub.2 CO--, R.sup.1 being an alkyl having 1 to 4 carbon atoms, an alkenyl having 2 to 4 carbon atoms, cyclohexyl, a phenyl containing or not containing a substitute of a lower alkyl, a halogenated lower alkyl, a lower alkoxy, hydroxy or a halogen, or a benzyl containing or not containing a substitute of a lower alkyl, a halogenated lower alkyl, a lower alkoxy, hydroxy or a halogen, and R.sup.2 being an alkyl of 1 to 3 carbon atoms, an alkenyl of 2 to 3 carbon atoms, an aryl of 6 to 8 carbon atoms or an aryl(C.sub.6 to C.sub.8)alkyl(C.sub.1 to C.sub.2); and n is an integer of 4 to 10. The present compounds are excellent in pharmacological activities, particularly in antagonism to bradykinin and histamine, and useful as anti-inflammatory agent.

    摘要翻译： 具有下式的ANH ANGLE CNH（CH 2）n CONHR NH的N-取代胍基衍生物，其中R是具有6至15个碳原子的烷基。 具有6至15个碳原子的环烷基或芳基（C 6至C 8）烷基（C 1至C 9）; A表示R 1或R 2 CO-，R 1为具有1至4个碳原子的烷基，具有2至4个碳原子的烯基，环己基，含有或不含有低级烷基，卤代低级烷基，低级烷氧基 ，羟基或卤素，或含有或不含低级烷基，卤代低级烷基，低级烷氧基，羟基或卤素的取代基的苄基，R 2为1至3个碳原子的烷基，烯基为2 至3个碳原子，6至8个碳原子的芳基或芳基（C6至C8）烷基（C1至C2）; n为4〜10的整数。本发明化合物的药理活性特别优选缓激肽和组胺的拮抗作用，作为抗炎剂有用。