Roussel Uclaf

Colin R Gardner

Roger J Gillespie

Wilfred R Tully

David A Rowlands

Stephen Clements-Jewery

Ian R Ager

Robert M Deacon

John R Hedgecock

A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is thiazol-2-yl optionally substituted by 1 or 2 alkyl of 1 to 3 carbon atoms optionally substituted by one or more fluorine or --COOAlk, Alk is alkyl of 1 to 3 carbon atoms, R.sub.2 and R.sub.3 are individually selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms and alkenyl of 2 to 5 carbon atoms or R.sub.2 and R.sub.3 together form alkylene of 3 to 5 carbon atoms, X is oxygen or sulfur and R.sub.4 is alkyl of 1 to 3 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having minor tranquillizing activity and useful for the treatment of obesity and cognitive impairment.

2-thiazolyl-imidazo[1,2,-a]pyrimidines

A compound selected from the group consisting a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of phenyl, cycloalkyl of 4 to 6 carbon atoms and ##STR2## R.sub.4 and R.sub.5 are individually hydrogen or 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, amido and mono- and dialkylamido of 1 to 5 alkyl carbon atoms, R.sub.2 and R.sub.3 are individually selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and cycloalkyl of 3 to 5 carbon atoms or taken together form alkylene of 3 to 5 carbon atoms, X and Y are individually selected form the group consisting of hydrogen, halogen, --NO.sub.2, azido, --CN, --CF.sub.3 and alkyl and alkoxy of 1 to 3 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts capable of inducing an affinity for benzodiazepine receptors and a novel process and novel intermediates for their preparation.

Novel imidazobenzodiazepines

Novel benzothiopyranopyridinones of the formula ##STR1## wherein A,B,C and D are individually selected from the group consisting of hydrogen, alkyl and alkoxy of 1 to 6 carbon atoms, nitro, halogen, amino and acylamino of 2 to 7 carbon atoms or A and B or C and D taken with the carbon atoms to which they are attached form a benzene ring, R is selected from the group consisting of hydrogen and R', R' is selected from the group consisting of alkyl of 1 to 9 carbon atoms, alkenyl of 2 to 9 carbon atoms optionally substituted with an --OH, cycloalkyl of 3 to 9 carbon atoms, phenyl, aralkyl of 7 to 9 carbon atoms and --(CH.sub.2).sub.n --Z, n is an integer from 1 to 4, Z is selected from the group consisting of cycloalkyl and cycloalkenyl of 3 to 9 carbon atoms, dioxanyl, 2-oxobenzimidazolyl, benzoyl, halo substituted benzoyl, cyano, alkoxy carbonyl of 2 to 7 carbon atoms and carbamoyl and their non-toxic, pharmaceutically acceptable acid addition salts having antipsychotic and antidepressant and antidopaminergic activity.

Benzothiopyranopyridinones

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Newbury Berks, United Kingdom

Colin R Gardner