(4-imidazolyl)piperidines, the preparation thereof and their app

Details (4-imidazolyl)piperidines, the preparation thereof and their app (4-imidazolyl)piperidines, the preparation thereof and their app

1986-03-17

1987-11-17

Bond, Robert T.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514321, 514322, 546197, 546199, 546210, C07D40104, C07D40514, A61K 31445

Patent

active

047074876

ABSTRACT:
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.

REFERENCES:
patent: 4087531 (1978-05-01), Langbein et al.
patent: 4217350 (1980-08-01), Eichenberger et al.
patent: 4329348 (1982-05-01), Huebner
"Structure-Action Relationship of Histamine Analogs 1. Histamine-Like Comnds With Cyclized Side Chain", Chemical Abstracts, vol. 80, No. 15, Apr. 15, 1974, No. 82801a, p. 389.

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