N-acryloylpiperazine derivatives, their preparation and their us

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514253, 540607, 544237, 544238, 544284, 544298, 544335, 544353, 544354, 544355, 544362, 544363, 544367, 544368, 544375, 544376, 544379, 544380, 544383, 544386, 544387, 544391, A61K 31495, C07D24104

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active

051927667

ABSTRACT:
Compounds of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 is each --R.sup.5, --CH.dbd.CH--R.sup.5 or --C.tbd.C--R.sup.5, wherein R.sup.5 is optionally substituted aryl or aromatic heterocyclic; R.sup.3 is hydrogen, alkyl, cyano or --R.sup.5 ; X is oxygen or sulfur; A is 1,4-piperazin-1,4-diyl or a 1,4-homopiperazin-1,4-diyl; B' is alkylene, carbonyl, thiocarbonyl, sulfinyl or sulfonyl; and R.sup.4 is optionally substituted phenyl and pharmaceutically acceptable salts thereof have valuable PAF antagonist activity, and may be prepared by reacting a compound containing the piperazine or homopiperazine part of the molecular with a compound containing the other part of the molecule.

REFERENCES:
patent: 4788206 (1988-11-01), Guthrie et al.
patent: 4794183 (1988-12-01), Nakamura et al.
patent: 4891363 (1990-01-01), Nakamura et al.
patent: 5068340 (1991-11-01), Nakamura et al.

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