Piperidine derivatives

Details Piperidine derivatives Piperidine derivatives

1984-07-24

1985-10-29

Bond, Robert T.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

514326, 546213, 546216, 546221, A61K 31445, C07D21146, C07D40904

Patent

active

045501165

ABSTRACT:
Compounds of the general formula I: ##STR1## wherein R.sup.1 represents a thienyl group, or a phenyl group optionally substituted by a halogen (preferably fluorine or chlorine) atom, a lower alkoxy or lower alkyl group, R.sup.2 represents a hydrogen or halogen (preferably fluorine) atom, a lower alkoxy or lower alkyl group, R.sup.3 represents a hydrogen or halogen (preferably fluorine) atom, a lower alkylthio, lower alkoxy or lower alkyl group, or a cycloalkyl group containing 5 or 6 carbon atoms, or a group of the general formula: ##STR2## wherein R.sup.4 and R.sup.5 singly each represents a hydrogen atom or lower alkyl group, R.sup.6 represents a cycloalkyl, hydroxymethyl, carboxy or lower alkoxycarbonyl group, and W represents a carbonyl ##STR3## or a hydroxymethylene [viz. --CH(OH)--] group, and pharmacologically acceptable salts thereof possess potent selective Histamine H.sub.1 -receptor blocking and calcium antagonist properties and are of interest in the treatment of a variety of respiratory, allergenic and cardiovascular disease states. The new compounds can be prepared by various methods based on the condensation of .alpha.-substituted benzyl halides with N-(benzoylpropyl or phenyl-hydroxypropyl)-4-hydroxy piperidines or condensation of di-substituted-methoxy-piperidines with a benzoylpropyl halide or a phenyl-hydroxypropyl-halide followed, where necessary, by removal of protecting groups.

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