(4-imidazolyl)piperidines, the preparation thereof and their application
in therapy
    13.
    发明授权
    (4-imidazolyl)piperidines, the preparation thereof and their application in therapy 失效
    (4-咪唑基)哌啶,其制备及其在治疗中的应用

    公开(公告)号:US4707487A

    公开(公告)日:1987-11-17

    申请号:US840956

    申请日:1986-03-17

    CPC分类号: C07D401/04

    摘要: Compounds of general formula ##STR1## in which R.sub.1 denotes H, CH.sub.3 or C.sub.2 H.sub.5, R denotes H or R.sub.2 and R.sub.2 denotes an alkyl, piperonyl, 3-(1-benzimidazolonyl)-propyl group; a group of formula ##STR2## in which n is 0, 1, 2, or 3, X is a single bond or alternatively --O--, --S--, --NH--, --CO--, --CH.dbd.CH-- or ##STR3## and R.sub.3 is H, CH.sub.3, F, CN or an acyl group; or alternatively a group of formula ##STR4## in which Z denotes an O or S atom or a divalent group NH, N --CH.sub.3 or N --CN, and R.sub.5 denotes an alkyl group, a cycloalkyl group which can bear a phenyl substituent, a phenyl group which can bear a CH.sub.3 or F substituent, a phenylalkyl(1-3 C) group or a naphthyl, adamantyl or p-toluenesulphonyl group. These compounds are useful to control the release of cerebral histamine and to increase the rate of renewal of cerebral histamine.

    摘要翻译: 其中R 1表示H,CH 3或C 2 H 5的通式为I的化合物,R表示H或R 2,R 2表示烷基,胡椒基,3-(1-苯并咪唑啉酮基) - 丙基; 其中n为0,1,2或3的式为“IMAGE”的基团,X为单键或者为-O - , - S - , - NH - , - CO-, - CH = CH-或 - 并且R 3是H,CH 3,F,CN或酰基; 或另一组式为“IMAGE”的基团,其中Z表示O或S原子或二价基团NH,N -CH 3或N -CN,R 5表示烷基,可带有苯基取代基的环烷基, 可以具有CH3或F取代基的苯基,苯基烷基(1-3C)基或萘基,金刚烷基或对甲苯磺酰基。 这些化合物可用于控制脑组织胺的释放和增加脑组织的更新速率。