N-4,5-di:hydro-2-thiazolyl 4-hydroxy 3-quinoline-carboxamide derivs. - anxiolytics having strong affinity for benzodiazepine receptors, opt. used in association with neuroleptics or antidepressants

摘要

N-(4,5-Dihydro-2-thiazolyl)- 6- or 7-R1-2-R-4-hydroxy -3-quinoline- carboxamide derivs. of formula (I) and their acid addition salts are new. (Where R is H or 1-4C alkyl; R1 is in position 6 or 7 and is H, halo, 1-4C linear alkyl, 3-5C branched alkyl, 1-4C alkoxy, trifluoromethylthio, methylthio, trifluoromethoxy or trifluoromethyl). Cpds. (I) are anxiolytics used to treat anxiety, such as chronic anxiety associated with insomnia, behaviour problems, distress etc. or used in association with neuroleptics or antidepressants to treat psychotic or depressive states. (I) have a strong affinity for the benzodiazepine receptors and may be administered orally or parenterally. Activity and toxicity tests are described. (I) where (a) R is H or methyl and R1 is H and (b) R is H and R1 is 6-ethyl or 6-chloro including their acid addn. salts are specifically claimed.