PROCESS FOR THE PREPARATION OF NOVEL BENZOTHIOPYRANOPYRIDINONES AND THEIR SALTS

• Main Authors: CLEMENTS-JEWERY, STEPHEN, GILLESPIE, ROGER J, ROWLANDS, DAVID A, GARDNER, COLIN R, AGER, IAN R
• Format: Patent
• Language: English; French
• Published: 08.04.1986
• Edition: 4
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

L'invention concerne la préparation de nouvelles benzothiopyranopyridinones, ainsi que de leurs sels, de formule (I): < IMG > (I) où A, B, C et D, identiques ou différents, représentent hydrogène, alcoyle (1-6c), alcoxy (1-6c), NO2, NH2, acylamino (2-7c) ou halogène ou l'un de A et B ou C et D forment un cycle benzénique, R est hydrogène ou R', R' étant alcoyle (1-3c) ou alcényle (2-9c) éventuellement substitué par hydroxy, ou R' étant cycloalcoyle (3-9c), phényle, aralcoyle (7-9c) ou -(CH2)n-Z, n étant 1, 2, 3 ou 4 et Z cycloalcoyle ou cycloalcényle (3-9c), dioxanyl, 2-oxo benzimidazolyl, benzoyle, halobenzoyl, alcoxycarbonyl (2-7c), cyano ou carbamoyl. Les produits (I) et leurs sels pharmaceutiquement acceptables peuvent être utilisés comme médicaments, notamment antidopaminergiques, antidépresseurs et antipsychotiques. Novel benzothiopyranopyridinones of the formula I 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 -(CH2)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.