Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-11-15
1997-11-18
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
544251, 544 60, 544115, 544234, 5142285, 5142332, 5142282, 514248, 514293, 546 82, 546 83, 546 84, C07D48704, A61K 31505
Patent
active
056888031
DESCRIPTION:
BRIEF SUMMARY
This is a 371 application of PCT/EP95/01856, filed May 16, 1995. The present invention is concerned with tricyclic dicarbonyl derivatives of the general formulae ##STR2## wherein R.sup.1 and R.sup.2 each independently signify hydrogen, lower alkyl, lower alkoxy, nitro, trifluoromethyl, amino, halogen, cyano or R.sup.3 R.sup.4 NS(O).sub.2 -- and R.sup.3 and R.sup.4 signify lower alkyl, and 6-membered heterocycle with 1-3N atoms optionally substituted by lower alkyl, hydroxy, amino or the group --CH.sub.2 NHCH.sub.3, a bicyclic heterocycle with 1-3N atoms or a group --NR.sup.5 R.sup.6 or --OR.sup.5 in which R.sup.5 and R.sup.6 can be the same or different and signify hydrogen, lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, amino-lower alkyl or lower alkylamino-lower alkyl, and --O--, Ia, Ib and II.
These compounds and salts are novel with the exception of been found that they possess valuable pharmaco-dynamic properties as non-competitive and/or AMPA/KA-R antagonists, so that they can be used as neuroprotectives, especially for the treatment or prevention of ischemia, hypoglycaemia, hypoxia, cerebral vascular spasms, spasticity, trauma, hemorrhagia, infections (viral, bacterial, amoebic, prional), epileptic seizures, autoimmune diseases, withdrawal symptoms, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, intoxications, olivopontocerebellar atrophy, spinal cord injuries, schizophrenia, depressions, anxiety states, dependence, pains, autism and mental retardation.
Objects of the present invention are the compounds defined earlier and pharmaceutically acceptable salts per se and as therapeutically active substances, a process for the manufacture of these novel compounds and salts, medicaments containing such a compound or a salt thereof, the production of such medicaments, the use of the compounds and salts defined earlier as neuroprotectives, especially in the control or prevention of ischemia, hypoglycaemia, hypoxia, cerebral vascular spasms, spasticity, trauma, hemorrhagia, infections (viral, bacterial, amoebic, prional), epileptic seizures, autoimmune diseases, withdrawal symptoms, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, intoxications, olivoponto-cerebellar atrophy, spinal cord injuries, schizophrenia, depressions, anxiety states, dependence, pains, autism and mental retardation, and the use of the compounds and salts defined earlier for the production of medicaments.
The term "lower" denotes compounds or groups with a maximum of 7, preferably a maximum of 4, carbon atoms.
The term "alkyl" denotes straight-chain or branched saturated hydrocarbon groups such as methyl, ethyl, propyl and the like.
The term "alkoxy" denotes alkyl groups in the sense of the foregoing definition which are bonded via an oxygen atom, such as methoxy and the like.
The term "halogen" signifies fluorine, chlorine, bromine and iodine.
The term "5- or 6-membered heterocycle" denotes cyclic saturated or unsaturated ring systems such as, for example, pyrrolyl, pyrrolidinyl, imidazolyl, pyrazolyl, pyrazolinyl, pyrazolidinyl, triazolyl, pyrimidinyl, piperazinyl, piperidinyl and the like, with the ring system being optionally substituted by lower alkyl, hydroxy, amino or a group --CH.sub.2 NHCH.sub.3.
The term "bicyclic heterocycle" denotes a ring system consisting of two rings which are condensed with one another, with one of the rings being a heterocycle and the second ring being especially a benzene ring, for example a quinoxalinyl group.
The term "pharmaceutically acceptable salts" embraces salts with inorganic and organic acids such as hydrochloric acid, hydrobromic acid, nitric acid, sulphuric acid, phosphoric acid, citric acid, formic acid, fumaric acid, maleic acid, acetic acid, succinic acid, tartaric acid, methanesulphonic acid, p-toluenesulphonic acid and the like as well as salts with inorganic bases such as sodium or potassium hydroxide. Such salts can be manufactured readily by any person skilled in the art havin
REFERENCES:
patent: 4472400 (1984-09-01), Tully et al.
patent: 4713383 (1987-12-01), Francis et al.
Buttelmann Bernd
Godel Thierry
Gross Laurence
Heitz Neidhart Marie-Paule
Riemer Claus
Ciambrone Coletti Ellen
Hoffmann-La Roche Inc.
Johnston George W.
Shah Mukund J.
Silverman Robert A.
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