Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Bacterium or component thereof or substance produced by said...
Patent
1978-05-05
1979-09-11
Coughlan, Jr., Paul M.
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Bacterium or component thereof or substance produced by said...
424249, 424251, 544212, 544295, 544357, 544363, A61K 31495, C07D40112, C07D40114
Patent
active
041675673
ABSTRACT:
Antihypertensive compounds of the formula ll ##STR1## wherein X is chloro or trifluoromethyl; wherein R is an aromatic heterocyclic radical selected from the group consisting of triazinyl, pyrazinyl, pyridinyl, pyrimidinyl or the above radicals substituted by one or two trifluoromethyl, alkyl, alkoxy, dialkylamino, alkylthio, or halo, or 1 to 4 halo atoms for pyridine, or combinations of substituents, in which alkyl and alkoxy are each of 1 to 3 carbon atoms, inclusive, and halo is fluoro, bromo or chloro, or R is the group ##STR2## in which R.sub.1 is phenyl, phenyl-substituted with one or two halogens, trifluoromethylphenyl, phenyl-substituted with one or two alkoxy or alkyl groups, or alkylphenylsulfonyl, in which alkyl, alkoxy, and halo are defined as above; or R is the group SO.sub.2 R.sub.2, in which R.sub.1 is dialkylamino, phenyl, phenyl-substituted with one or two halogens, alkyl, trifluoromethyl or alkoxy groups, in which alkyl, alkoxy and halo are defined as hereinabove, are prepared from compounds of the formula ##STR3## WHEREIN X has the significance as above, by reaction with the selected cyclic amine or by reaction of ##STR4## wherein X is defined as above and a selected R.sub.2 -sulfonyl chloride or R.sub.1 -isocyanate.
The compounds of formula ll and their pharmacologically acceptable acid addition salts are hypotensive agents which are useful for the treatment of hypertension in mammals, including man.
REFERENCES:
patent: 3362956 (1968-01-01), Archer
patent: 3632761 (1972-01-01), Graham
patent: 4025629 (1977-05-01), Coverdale
Armitage Robert A.
Berneis Hans L.
Coughlan, Jr. Paul M.
The Upjohn Company
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