Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-01-05
1999-08-10
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
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Patent
active
059359730
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 .alpha..sub.2 and/or D.sub.2 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 pharmaceutically acceptable salts thereof in which
A is methylene or O;
B is methylene or O;
g is 0, 1, 2, 3 or 4;
R.sub.1 represents 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; 1) a sulphamoyl or sulphamoylmethyl group each optionally N-substituted by one or two alkyl groups each containing 1 to 3 carbon atoms; m) an alkylsulphonyloxy group containing 1 to 3 carbon atoms optionally substituted by one or more halo; n) a furyl group; o) an amino group optionally substituted by one or two alkyl groups each containing 1 to 3 carbon atoms; or two adjacent R.sub.1 groups together with the carbon atoms to which they are attached form a fused benz ring, the substituents represented by R.sub.1 being the same or different when g is 2, 3 or 4;
R.sub.2 is H, an alkyl group containing 1 to 3 carbon atoms optionally substituted by one or more halo, or an alkoxy group containing 1 to 3 carbon atoms optionally substituted by one or more halo;
R.sub.3 and R.sub.4, which are the same or different, are H, or an alkyl group containing 1 to 3 carbon atoms optionally substituted by one or more halo;
U is an alkylene chain containing 1 to 3 carbon atoms, optionally substituted by one or more alkyl groups each containing 1 to 3 carbon atoms;
Q represents a divalent group of formula IIa, IIb or IIc ##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;
V' is an alkylene chain containing 2 to 6 carbon atoms, optionally substituted by one or more alkyl groups each containing 1 to 3 carbon atoms;
X is an alkylene chain containing 0 to 2 carbon atoms and X' is an alkylene 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 5-triazolyl, 5-tetrazolyl, 2-, 3-, 4-, or 8-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 of 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 o
REFERENCES:
patent: 5314895 (1994-05-01), Desai et al.
Giardina et al., J. Med. Chem., vol. 28, No. 9, 1985, pp. 1354-1357.
Ennis et al., J. Med. Chem., vol. 35, No. 16, 1992, pp. 3058-3066.
Birch Alan Martin
Heal David John
Kerrigan Frank
Martin Keith Frank
Needham Patricia Lesley
Coleman Brenda
Knoll Aktiengesellschaft
Shah Mukund J.
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