Substituted diazolo[b][1,5]benzodiazepines and their use as CNS agents
AssigneeLilly Industries Limited
InventorsJiban K. Chakrabarti, Terrence M. Hotten
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AssigneeLilly Industries Limited
InventorsJiban K. Chakrabarti, Terrence M. Hotten
Estimating the term…
Compounds are described of the formula ##STR1## or an acid addition salt thereof; in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, halogen, C.sub.1-4 haloalkyl, C.sub.1-4 alkanoyl, nitro, amino, C.sub.2-4 acylamino, cyano, hydroxyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, C.sub.1-4 haloalkoxy or a group of the formula --SO.sub.2 N(R.sup.8).sub.2, --SO.sub.2 R.sup.8 or --SO.sub.3 R.sup.8 where R.sup.8 is C.sub.1-4 alkyl, C.sub.1-4 haloalkyl or optionally substituted phenyl; in which R.sup.5 is a group of the formula ##STR2## where R.sup.9 is hydrogen, C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, C.sub.2-4 alkenyl, C.sub.1-4 alkanoyl, benzyl, cyano or optionally substituted phenyl, where R.sup.10 is hydrogen, C.sub.1-4 alkyl or optionally substituted phenyl and where n is 0 or 1; in which R.sup.6 is hydrogen, C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl. C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, benzyl, C.sub.1-6 alkanoyl, C.sub.1-4 carbalkoxy or benzoyl; and in which R.sup.7 is one of the values of R.sup.6 or halogen, nitro, cyano, amino or C.sub.1-4 acylamino. The compounds are active as pharmaceuticals and particularly in the treatment of disorders of the central nervous system.
A compound of the formula ##STR18## in which R.sup.1, R.sup.2 and R.sup.3 independently represent hydrogen, halogen or C.sub.1-4 haloalkyl, R.sup.6 is C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl or C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, R.sup.7 is hydrogen and R.sup.9 is hydrogen, C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl or benzyl.
Dependencies are inferred from the claim text.