Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-06-16
2000-08-22
Chang, Ceila
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514321, 514322, 546193, 546197, 546199, A61K 31445, C07D40114
Patent
active
061073105
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to novel heteroarylcarboxamide compounds which have affinity for 5-HT.sub.1A and/or .alpha..sub.1, and/or D.sub.2 -like (D.sub.2, D.sub.3 and D.sub.4 sub-types) receptors, to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.
The present invention provides compounds of formula I ##STR2## including enantiomers and pharmaceutically acceptable salts thereof in which --N.dbd.C(R")--N(R')--, --N(R')--C(R").dbd.C(R'")--, --C(R'").dbd.C(R")--N(R')--, --N(R')--N.dbd.C(R")--, --C(R").dbd.N--N(R')--, --N(R')--N.dbd.N--, --N.dbd.N--N(R')--, --N.dbd.C(R")--O--, --N.dbd.C(R")--S--, --O--C(R").dbd.N--, --S--C(R").dbd.N--, --O--N.dbd.C(R")--, --S--N.dbd.C(R")--, --C(R").dbd.N--O--, --C(R").dbd.N--S--, --S--C(R").dbd.C(R'")--, --C(R").dbd.C(R'")--S--, --O--C(R").dbd.C(R'")--, or --C(R").dbd.C(R'")--O--; containing 1 to 3 carbon atoms optionally substituted by one or more halo; carboxy; an alkanoyl group containing 1 to 6 carbon atoms; an alkoxycarbonyl group in which the alkoxy group contains 1 to 3 carbon atoms; formyl; cyano; or a carbamoyl group or carbamoylmethyl group each optionally N-substituted by one or two alkyl groups, which may be the same or different, each containing 1 to 3 carbon atoms; substituted by one or more halo; an alkoxy group containing 1 to 3 carbon atoms optionally substituted by one or more halo; halo; or an alkylthio group containing 1 to 3 carbon atoms optionally substituted by one or more halo; the substituents represented by R.sub.1 being the same or different when g is 2; group containing 1 to 3 carbon atoms; group containing 1 to 3 carbon atoms; substituted by one or more alkyl groups each containing 1 to 3 carbon atoms; ##STR3## in which V is a bond or an alkylene chain containing 1 to 3 carbon atoms optionally substituted by one or more alkyl groups each containing 1 to 3 carbon atoms; substituted by one or more alkyl groups each containing 1 to 3 carbon atoms; chain containing 1 to 4 carbon atoms provided that the total number of carbon atoms in X and X' amounts to 3 or 4; R.sub.5 is H or an alkyl group containing 1 to 3 carbon atoms; and
T represents the group CO.HET in which HET is 2-, 3- or 4-pyridyl, 2-, 4- or 5-pyrimidinyl, 2- or 3-thienyl, 2- or 3-furyl, 2-, 3- or 7-benzo[b]furanyl, 2,3-dihydro-7-benzo[b]furanyl, 2-, 3- or 7-benzo[b]thiophenyl, 2- or 3-piperidyl, 3-, 4- or 5-4- or 5-triazolyl, 5-tetrazolyl, 2-, 3- or 4-quinolinyl, 2- or 4-quinazolinyl, 3-, 4- or 5-isoxazolyl, 2-, 4- or 5-oxazolyl, 3-, 4- or 5-isothiazolyl or 2-, 4- or 5-thiazolyl each which may be optionally substituted by one or more substituents selected from a) halo, b) an alkyl group containing 1 to 3 carbon atoms optionally substituted by one or more halo, c) an alkoxy group containing 1 to 3 carbon atoms optionally substituted by one or more halo, d) an alkylthio group containing 1 to 3 carbon atoms optionally substituted by one or more halo, e) hydroxy, f) an acyloxy group containing 1 to 3 carbon atoms, g) hydroxymethyl, h) cyano, i) an alkanoyl group containing 1 to 6 carbon atoms, j) an alkoxycarbonyl group containing 2 to 6 carbon atoms, k) a carbamoyl group or carbamoylmethyl group each optionally N-substituted by one or two alkyl groups each containing 1 to 3 carbon atoms, I) a sulphamoyl or sulphamoylmethyl group each optionally N-substituted by one or two alkyl groups each containing 1 to 3 carbon atoms, m) a
REFERENCES:
patent: 5302599 (1994-04-01), Ennis
Rubini et al. "Synthesis of isosteric methylene oxy . . . " Tetrahedron v. 42, pp. 6039-6045, 1986.
Birch Alan Martin
Bradley Paul Anthony
Gill Julie Carolyn
Chang Ceila
Knoll Aktiengesellschaft
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