NEW 8-METHYL-7H-1,3-DIOXOLO[4,5-H][2,3]-BENZODIAZEPINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AS ACTIVE COMPONENT, AND PROCESS FOR PRODUCING THEM

摘要

1,3-Dioxolo[4,5-h][2,3] benzodiazepine derivatives (I) are new. 1,3-Dioxolo [4,5-h] [2,3] benzodiazepine derivatives of formula (I) and their acid addition salts are new. (i) A, B = H; R1 = (CH2)n-CO(CH2)mR; R = halo, pyridyl or NR3R4; R3, R4 = H, cycloalkyl, alkoxy, amino, phenyl (optionally substituted by one or two alkyl), alkyl (optionally substituted by phenyl ) or saturated 5-6 membered heterocycle containing 1-3 N or one N plus one O (optionally substituted by phenyl, itself optionally substituted by 1-3 alkoxy); or NR3R4 = (un)saturated 5-6 membered heterocycle optionally containing a further N or S (optionally substituted by phenyl, itself optionally substituted by 1-3 alkoxy); n = 0-2; m = 0-2; or (ii) A + B = a bond; R1 = CO(CH2)pR6; R6 = halo, phenoxy, alkoxy or NR7R8; R7, R8 = H, guanyl, cycloalkyl or alkyl (optionally substituted by phenyl, itself optionally substituted by 1-3 alkoxy) or 5-6 membered saturated heterocycle containing 1 or more N or one N plus one O; or NR7R8 = oxo-pyrrolidinyl, phthalimido (optionally substituted) or saturated 5-6 membered heterocycle containing one or more N or one N plus one O (optionally substituted by 1-3 of OH, phenyl (optionally substituted by 1-3 halo or alkoxy), phenoxy (optionally substituted by 1-3 halo or alkoxy) or phenoxyalkyl (optionally ring-substituted as for phenoxy and/or substituted in the alkyl by 1 or 2 OH); p = 0-2; R2 = NO2, NH2 or (1-4C) alkanoylamino; alkyl moieties have 1-4C and cycloalkyl 3-6C.