N-substituted guanidino acid derivatives
    2.
    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

    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。