Imidazodiazepines
AssigneeHoffmann-La Roche Inc.
InventorsThierry Godel, Walter Hunkeler, Heinz Stadler, Ulrich Widmer
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AssigneeHoffmann-La Roche Inc.
InventorsThierry Godel, Walter Hunkeler, Heinz Stadler, Ulrich Widmer
Estimating the term…
The invention relates to compounds of the formula ##STR1## wherein A together with the two carbon atoms denoted by .alpha. and .beta. is one of the residues ##STR2## Q is one of the residues ##STR3## R.sup.1 and R.sup.2 each independently are hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower hydroxyalkyl, lower alkoxy-lower alkyl, (C.sub.3 -C.sub.6)-cycloalkyl, (C.sub.3 -C.sub.6)-cycloalkyl-lower alkyl, amino-lower alkyl, lower alkylamino-lower alkyl, di-lower alkylamino-lower alkyl or aryl-lower alkyl or together with the nitrogen atom are a 5- to 8-membered membered heterocycle optionally containing a further hetero atom or a fused benzene ring, R.sup.3 is hydrogen and R.sup.4 is lower alkyl or R.sup.3 and R.sup.4 together are dimethylene or trimethylene and R.sup.5 and R.sup.6 each independently are hydrogen, halogen, trifluoromethyl, lower alkoxy or nitro, the compounds of formula I having the (S) configuration with reference to the carbon atom denoted by .gamma. when R.sup.3 and R.sup.4 together are dimethylene or trimethylene, and pharmaceutically acceptable acid addition salts thereof. These compounds and salts have pronounced anxiolytic, anticonvulsant, muscle relaxant and sedative-hypnotic properties.
A compound of the formula ##STR18## wherein A together with the two carbon atoms denoted by .alpha. and .beta. is one of the residues ##STR19## Q is one of the residues ##STR20## R.sup.1 and R.sup.2 each independently are hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower hydroxyalkyl, lower alkoxy-lower alkyl, (C.sub.3 -C.sub.6)-cycloalkyl, (C.sub.3 -C.sub.6)-cycloalkyl-lower alkyl, amino-lower alkyl, lower alkylamino-lower alkyl, di-lower alkylamino-lower alkyl or aryl-lower alkyl or together with the nitrogen atom are 1-pyrrolidinyl, 1-pyrrolinyl, piperidino, 2,6-dimethylpiperidino, 3,3-dimethylpiperidino, hexamethyleneimin-1-yl, heptamethyleneimin-1-yl, morpholino, 4-methyl-1-piperazinyl, or isoindolin-2-yl,
A pharmaceutical composition comprising an effective amount of a compound of the formula ##STR21## wherein A together with the two carbon atoms denoted by .alpha. and .beta. is one of the residues ##STR22## Q is one of the residues ##STR23## R.sup.1 and R.sup.2 each independently are hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower hydroxyalkyl, lower alkoxy-lower alkyl, (C.sub.3 -C.sub.6)-cycloalkyl, (C.sub.3 -C.sub.6)-cycloalkyl-lower alkyl, amino-lower alkyl, lower alkylamino-lower alkyl, di-lower alkylamino-lower alkyl or aryl-lower alkyl or together with the nitrogen atom are 1-pyrrolidinyl, 1-pyrrolinyl, piperidino, 2,6-dimethylpiperidino, 3,3-dimethylpiperidino, hexamethyleneimin-1-yl, heptamethyleneimin-1-yl, morpholino, 4-methyl-1-piperazinyl, or isoindolin-2-yl,
A method of treating convulsion, anxiety states, muscle tensions, tension states and insomnia which comprises administering to a patient in need of such treatment an effective amount of a compound of the formula ##STR24## wherein A together with the two carbon atoms denoted by .alpha. and .beta. is one of the residues ##STR25## Q is one of the residues ##STR26## R.sup.1 and R.sup.2 each independently are hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower hydroxyalkyl, lower alkoxy-lower alkyl, (C.sub.3 -C.sub.6)-cycloalkyl, (C.sub.3 -C.sub.6)-cycloalkyl-lower alkyl, amino-lower alkyl, lower alkylamino-lower alkyl, di-lower alkylamino-lower alkyl or aryl-lower alkyl or together with the nitrogen atom are a 5- to 8-membered heterocycle optionally containing a further hetero atom or a fused benzene ring,
Dependencies are inferred from the claim text.