Roussel Uclaf

Charles J Hedgecock

Elizabeth A Kuo

David P Kay

Wilfred R Tully

Stuart D Jones

Philip T Hambleton

A compound selected from the group consisting of all tautomeric forms of a cycloalkyl-propanamide of the formula ##STR1## wherein R.sub.1 is cycloalkyl of 3 to 6 carbon atoms, R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are individually selected from the group consisting of hydrogen, halogen, --NO.sub.2, azido, --CN, alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, --(CH.sub.2).sub.m --CF.sub.3, --O--(CH.sub.2).sub.m --CF.sub.3, --S--(CH.sub.2).sub.m --CF.sub.3, m is an integer from 0 to 3, --CF.sub.2 --Hal, --OCF.sub.2 --Hal, ##STR2## n is an integer from 1 to 3, Hal, Hal.sub.1, and Hal.sub.2 and Hal.sub.3 are individually halogen, and --COR', R' is --OH or alkyl or alkoxy of 1 to 3 carbon atoms or R.sub.4 and R.sub.5 together are --O--CH.sub.2 --O-- and their non-toxic, pharmaceutically acceptable basic salts having anti-inflammatory activity.

3-cycloalkyl-propanamides

A compound selected from the group consisting of a compound of the formula ##STR1## wherein Y is a nitrogen atom or carbon atom bearing Z, Z is selected from the group consisting of hydrogen, halogen, --C.ident.N, --N.sub.3 and --C(Hal).sub.3, Hal is a halogen, X is cycloalkyl of 3 to 6 carbon atoms or hydrogen with the proviso that when X is hydrogen, Y must be nitrogen, R is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, phenyl and substituted phenyl and their non-toxic, pharmaceutically acceptable acid addition salts, a process and intermediate for preparing them, having tranquillizing properties.

7-cyclopropyl-imidazodiazepines

A compound selected from the group consisting of all tautomeric forms of a cycloalky-propanamide of the formula ##STR1## wherein R.sub.1 is cycloalkyl of 3 to 6 carbon atoms, R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are individually selected from the group consisting of hydrogen, halogen, --NO.sub.2, azido, --CN, alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, --(CH.sub.2).sub.m --CF.sub.3, --O--(CH.sub.2).sub.m --CF.sub.3, --S--(CH.sub.2).sub.m --CF.sub.3, m is an integer from 0 to 3, --CF.sub.2 --Hal, --OCF.sub.2 --Hal, ##STR2## n is an integer from 1 to 3, Hal, Hal.sub.1, Hal.sub.2 and Hal.sub.3 are individually halogen, and --COR', R' is --OH or alkyl or alkoxy of 1 to 3 carbon atoms or R.sub.4 and R.sub.5 together are --O--CH.sub.2 --O-- and their non-toxic, pharmaceutically acceptable basic salts having anti-inflammatory activity.

A compound selected from the group consisting of a compound of the formula ##STR1## wherein the R.sub.1 s are the same and are alkyl of 1 to 3 carbon atoms or together are alkylene of 2 to 5 carbon atoms, X, Y and W are individually --O-- or --S--, R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and phenyl optionally substituted with at least one member of the group consisting of halogen, alkyl and alkoxy of 1 to 3 carbon atoms and --CF.sub.3, R.sub.4 and R.sub.5 are individually selected from the group consisting of hydrogen, halogen, --OH, alkyl and alkoxy of 1 to 3 carbon atoms and --CF.sub.3 with the proviso that when R.sub.1 and R.sub.2 are alkyl, X and Y are the same and their non-toxic, pharmaceutically acceptable acid addition salts having benzodiazepine inverse agonist properties.

Novel imidazobenzodiazepines

A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of ##STR2## R.sub.4, R.sub.5, R.sub.7 and R.sub.8 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, R.sub.6 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, phenyl, halogen, alkoxycarbonyl of 2 to 5 carbon atoms, cyano, ##STR3## R' and R' are individually alkyl of 1 to 5 carbon atoms, R.sub.2 and R.sub.3 together form a member of the group consisting of ##STR4## m is 1, 2 or 3, X.sub.1 and X.sub.2 are individually selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, alkenyl of 2 to 5 carbon atoms, alkoxy of 1 to 5 carbon atoms, aralkoxy, aryloxy, halogen, azido and nitro or taken together form methylenedioxy and their non-toxic, pharmaceutically acceptable acid additon salts capable of treating memory disorders.

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Wootton Bassett, United Kingdom

Charles J Hedgecock