The Upjohn Co.

Charles E Coverdale

Louis L Skaletzky

Robert James Collins

Novel compounds of the formula: ##STR1## are disclosed with the corresponding hydrates and pharamceutically acceptable acid addition salts thereof, wherein R.sub.1 is halogen, lower alkyl, or trifluoromethyl; R.sub.2 is lower alkyl, substituted or unsubstituted phenyl or benzyl and R.sub.3 is hydrogen. The novel compounds are useful for the treatment of hypertension and anxiety in mammals, including humans. Disclosed also are compositions containing the novel compounds of the invention and methods of their use in the treatment of hypertension and anxiety.

Compositions and method of using quinolylaminobenzoylpiperazino-1-oxides

Novel p-(trifluoromethylquinolylamino)benzamides are provided, for example, p-[(7-trifluoromethyl-4-quinolyl)-amino]-N,N-(3-methyl-3-azapentamethylene )benzamide and 1-[p-[[7-(trifluoromethyl)-4-quinolyl]amino]benzoyl]piperazine dihydrochloride. Also provided are pharmaceutical dosage unit forms for systemic administration and methods for their systemic administration. The compound, dosage unit forms and methods of systemic administration are useful in obtaining antihypertensive and anti-anxiety effects in mammals.

P-(trifluoromethylquinolylamino)benzamides, pharmaceutical dosage forms

Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen or lower alkyl, R.sub.3 represents lower alkyl and A is a monovalent group of formula: ##STR2## wherein Y is hydrogen or the acyl radical of a hydrocarbon carboxylic acid having from 2 to 18 carbon atoms, inclusive, are employed as anticonvulsants in treating mammals, including humans. Novel compounds within the scope of the above formula are also disclosed, wherein R.sub.1 is specifically lower alkyl and provided that R.sub.1 is located in a position ortho or meta to the substituent group A when R.sub.2 is hydrogen. Disclosed also are novel intermediate compounds for preparing the above-described novel compounds of the invention, which correspond thereto but wherein the group A is replaced by a nitro-group.

Compositions and method for treating epilepsy and convulsions

Novel compounds of the formula: ##SPC1## Are disclosed with the corresponding hydrates and pharmaceutically acceptable acid addition salts thereof, wherein R.sub.1 is halogen, lower alkyl, or trifluoromethyl; R.sub.2 is lower alkyl, substituted or unsubstituted phenyl or benzyl and R.sub.3 is hydrogen. The novel compounds are useful for the treatment of hypertension and anxiety in mammals, including humans. Disclosed also are compositions containing the novel compounds of the invention and methods of their use in the treatment of hypertension and anxiety.

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Portage, MI, United States of America

Charles E Coverdale