Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1999-06-16
2000-10-24
Owens, Amelia
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514326, 546193, 546197, A01N 4340
Patent
active
061368253
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to novel heteroarylsulphonamide compounds which have affinity for 5-HT.sub.1A 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, and spasticity.
The present invention provides compounds of formula I ##STR2## including enantiomers and pharmaceutically acceptable salts thereof in which substituted by one or more halo; an alkoxy group containing 1 to 3 carbon atoms optionally substituted by one or more halo; halo; 6,7-methylenedioxy optionally C-substituted by one or two alkyl groups containing 1 to 3 carbon atoms; 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, 3 or 4; 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 the group (CH.sub.2)n in which n is 0, 1, 2 or 3, 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 E and E' amounts to 3 or 4; group containing 1 to 4 carbon atoms; and 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, 3-, 4- or 5-pyrazol, 1,2,3-triazol-4-yl, 1,2,3-triazol-5-yl, 1,2,4-triazol-2-yl, 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 of which may be optionally substituted by one or more substituents selected from a) halo, b) an alkyl group containing 1 to 4 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) an amino group optionally substituted by one or two alkyl groups each containing 1 to 5 carbon atoms, n) 1-pyrrolidinyl or 1-piperidinyl, o) nitro or p) acetamido.
In preferred compounds of formula I, A is --O--.
In preferred compounds of formula I, B is --O--.
In more preferred compounds of formula I, both A and B are --O--.
In preferred compounds of formula I, g is 0 or 1. When g is 1, R.sub.1 is preferably halo or an alkyl group containing 1 to 3 carbon atoms optionally substituted by one or more halo for example trifluoromethyl. In more preferred compounds of formula I, g is 1 and R.sub.1 is halo. Most preferably g is 1 and R.sub.1 is 7-chloro.
In preferred compounds of formula I, R.sub.2 is H.
In preferred compounds of formula I, R.sub.3 and R.sub.4 are both H.
In preferred compounds of formula I, U is
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patent: 5300523 (1994-04-01), Junge et al.
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patent: 5585392 (1996-12-01), Junge et al.
Birch Alan Martin
Wishart Neil
Knoll Aktiengesellschaft
Owens Amelia
LandOfFree
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