Antihypertensive aminoquinolines

C - Chemistry – Metallurgy – 07 – D

Patent

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260/259, 260/266

C07D 239/00 (2006.01) C07D 215/44 (2006.01) C07D 295/192 (2006.01)

Patent

CA 1082707

ABSTRACT OF THE DISCLOSURE Antihypertensive compounds of the formula 11 Image 11 wherein X is chloro or trifluoromethyl; wherein R is an aromatic heterocyclic radical selected from the group consisting of triazinyl, pyrazinyl, pyri- dinyl, pyrimidinyl or the above radicals substituted by one or two trifluoromethyl. alkyl, alkoxy, dialkyl- amino, alkylthio, or halo, or 1 to 4 halo atoms for pyridine, or uimbinations 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 -?NHR1, in which R1 is znenyl, phenyl- substituted wlth one or two halogens. trifluoro- methylphenyl, phenyl-substituted with one or two alkoxy or alkyl groups, or alkylphenylsul- fonyl, in which alkyl, alkoxy, and halo are defined as above; or R is the group SO2R2, in which R1 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 Image wherein X has the significance as above, by reaction with the selected cyclic amine or by reaction of Image wherein X is defined as above and a selected R2-sulfonyl chloride or R1-isocyanate. The compounds of formula 11 and their pharma- cologically acceptable acid addition salts are hypotensive agents which are useful for the treatment of hypertension in mammals, including man.

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