Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1997-04-22
1999-03-23
Berch, Mark L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
544494, 544498, C07D48704, C07D48714, C07D49514, A61K 3155
Patent
active
058859861
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/EP95/04393, filed Nov. 08, 1995.
The present invention is concerned with imidazodiazepinones of the general formula ##STR4## wherein A and the two carbon atoms denoted by .alpha. and .beta. together signify one of the residues ##STR5## Q signifies one of the residues ##STR6## 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, alkoxy or nitro, R.sup.3 is different from hydrogen,
These compounds are novel and have valuable pharmacodynamic properties. They are therefore suitable for therapeutic purposes, especially for anxiolytic and/or anticonvulsant and/or muscle relaxant and/or sedative-hypnotic purposes.
Objects of the present invention are the mentioned compounds of formula I and salts thereof per se and as therapeutically active substances, their manufacture and their use for therapeutic purposes or for the production of corresponding medicaments as well as medicaments containing a compound of formula I or a salt thereof and the production of such medicaments.
The term "lower" denotes residues or compounds with a maximum of 7, preferably a maximum of 4, carbon atoms. The term "alkyl" denotes straight-chain or branched saturated hydrocarbon residues such as methyl, ethyl, n-propyl, iso-propyl, n-butyl, sec.-butyl, isobutyl and tert.-butyl. The term "alkoxy" denotes alkyl groups bonded via an oxygen atom, such as methoxy and ethoxy. The term "cycloalkyl" denotes saturated cyclic hydrocarbon residues such as e.g. cyclopropyl. The terms "alkenyl" and "alkynyl" denote straight-chain or branched hydrocarbon residues which contain a C--C double or, respectively, triple bond, such as allyl, but-2-enyl, 3-methyl-but-2-enyl, propargyl and the like. The term "aryl" denotes a phenyl residue optionally substituted by halogen, trifluoromethyl, lower alkyl or lower alkoxy. The term "halogen" embraces fluorine, chlorine, bromine and iodine. When R.sup.4 together signify a di- or trimethylene group and alkoxy or nitro, is different from hydrogen,
European Patent Application EP-A-197282 relates to oxadiazolyl imidazobenzodiazepine derivatives and to methods for preparing such compounds. These compounds are suitable for use in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics and nootropics. European Patent Application EP-A-519307 refers to tetracyclic imidazodiazepines useful for the prevention of epilepsy, anxiety, and related diseases. The compounds of the present invention are novel and have improved pharmacodynamic properties. They are therefore suitable for therapeutic purposes, especially for anxiolytic and/or anticonvulsant and/or muscle relaxant and/or sedative-hypnotic purposes.
Objects of the present invention are the mentioned compounds of formula I and salts thereof per se and as therapeutically active substances, their manufacture and their use for therapeutic purposes or for the production of corresponding medicaments as well as medicaments containing a compound of formula I or a salt thereof and the production of such medicaments.
The term "lower" denotes residues or compounds with a maximum of 7, preferably a maximum of 4, carbon atoms. The term "alkyl" denotes straight-chain or branched saturated hydrocarbon residues such as methyl, ethyl, n-propyl, iso-propyl, n-butyl, sec.-butyl, isobutyl and tert.-butyl. The term "alkoxy" denotes alkyl groups bonded via an oxygen atom, such as methoxy and ethoxy. The term "cycloalkyl" denotes saturated cyclic hydrocarbon residues such as e.g. cyclopropyl. The terms "alkenyl" and "alkynyl" denote straight-chain or branched hydrocarbon residues which contain a C--C double or, respectively, triple bond, such as allyl, bu
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Heterocycles vol. 39, No. 2, Dec. 31, 1994 pp. 693-720 Gereck et al (1994).
Nature 294, pp. 763-765 (1981) Mohler et al.
J. Neurochemistry 37, pp. 714-722 (1981) Mohler.
Buttelmann Bernd
Godel Thierry
Berch Mark L.
Hoffmann-La Roche Inc.
Johnston George W.
Tramaloni Dennis P.
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