Oxazolyl- and thiazolylimidazo-benzo- and thienodiazepines and their use as medicaments
AssigneeHoffmann-La Roche Inc.
InventorsBernd Buttelmann, Thierry Godel
Life of this patent
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Abstract
The invention is concerned with basically-substituted imidazodiazepines of general formula I. These compounds can be used as anxiolytic and/or anticonvulsant and/or muscle relaxant and/or sedative-hypnotic active substances.
Claims6
Imidazodiazepinones of the formula ##STR10## wherein A and the two carbon atoms denoted by .alpha. and .beta. together signify ##STR11## Q signifies one of the residues ##STR12## R.sup.1 and R.sup.2 each signify 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 signify a 5- to 8-membered heterocycle optionally containing a further hetero atom or a fused benzene ring,
- R.sup.3 signifies hydrogen and R.sup.4 signifies lower alkyl or R.sup.3 and R.sup.4 together signify a di- or trimethylene group and
- R.sup.5 and R.sup.6 each signify hydrogen, halogen, trifluoromethyl, lower alkoxy or nitro,
- with the carbon atom denoted by .gamma. having the S-configuration when R.sup.3 is different from hydrogen,
- and pharmaceutically acceptable acid addition salts thereof.
3-(5-dipropylaminomethyl-oxazol-2-yl)-5-methyl-5,6-dihydro-4H-imida zo1,5-a!thieno2,3-f!diazepin-6-one.
A pharmaceutical composition comprising an effective amount for sedating a host of a compound of the formula:
- ##STR13## wherein A and the two carbon atoms denoted by .alpha. and .beta. together signify ##STR14## Q signifies one of the residues ##STR15## R.sup.1 and R.sup.2 each signify 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 signify a 5- to 8-membered heterocycle optionally containing a further hetero atom or a fused benzene ring,
- R.sup.3 signifies hydrogen and R.sup.4 signifies lower alkyl or R.sup.3 and R.sup.4 together signify a di- or trimethylene group and
- R.sup.5 and R.sup.6 each signify hydrogen, halogen, trifluoromethyl, lower alkoxy or nitro,
- with the carbon atom denoted by .gamma. having the S-configuration when R.sup.3 is different from hydrogen,
- and pharmaceutically acceptable acid addition salts thereof
- and a therapeutically inert carrier.
(S)-1-(5-Dipropylaminomethyl-oxaz ol-2-yl)-11,11a-dihydro-8H,10H-azeto1,2-a!imidazo5,1-c!thieno3,2-a!1,4! diazepin-8-one.
A method of sedating a host comprising administering an effective amount of a compound of the formula:
- ##STR16## wherein A and the two carbon atoms denoted by .alpha. and .beta. together signify ##STR17## Q signifies one of the residues ##STR18## R.sup.1 and R.sup.2 each signify 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 signify a 5- to 8-membered heterocycle optionally containing a further hetero atom or a fused benzene ring,
- R.sup.3 signifies hydrogen and R.sup.4 signifies lower alkyl or R.sup.3 and R.sup.4 together signify a di- or trimethylene group and
- R.sup.5 and R.sup.6 each signify hydrogen, halogen, trifluoromethyl, lower alkoxy or nitro,
- with the carbon atom denoted by .gamma. having the S-configuration when R.sup.3 is different from hydrogen,
- and pharmaceutically acceptable acid addition salts thereof.
Dependencies are inferred from the claim text.