813-74-1Relevant articles and documents
Fluck,Horn
, p. 273,274,277 (1973)
CONDENSED DIAZEPINONES, THEIR COMPOSITIONS AND METHODS OF USE AS PHARMACEUTICALS
-
, (2008/06/13)
Disclosed are novel condensed diazepinones of formula I STR1 wherein B is a fused ring selected from STR2 X is--CH--or, when B is ortho-phenylene, X can also be nitrogen; A 1 is C 1-C. sub.2 alkylene; A 2 is C 1-C 2 when it is in the 2-position relative to the saturated heterocyclic ring nitrogen or a single bond or methylene when it is in the 3-or 4-position; R 1 is C 1-C 3 alkyl; R 2 is C. sub.1-C 7 alkyl, optionally hydroxy-substituted on at least one of its second to seventh carbon, or C 3-C 7 cycloalkyl, optionally hydroxy substituted, or C 3-C 7 cycloalkylmethyl; or R 1 and R 2 can, together with the nitrogen therebetween, be a 4-to 7-membered saturated monocyclic, heterocyclic ring which can optionally include an oxygen or N--CH 3 ; R 3 is hydrogen, chlorine, or methyl; R 4 is hydrogen or C 1-C 4 alkyl, R 5 is hydrogen, chlorine or C 1-C 4 alkyl; and Z is a single bond, oxygen, methylene or 1,2-ethylene; and NR 1 R 2--N oxides and nontoxic, pharmaceutically acceptable addition salts thereof. Also disclosed are pyrrolobenzodiazepinone intermediates, pharmaceutical compositions containing the condensed diazepinones and methods of using them to treat cardiovascular disorders, particularly bradycardia and bradyarrhythmia.