Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1996-06-05
1998-06-16
Grumbling, Matthew V.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514253, 514259, 514256, 514318, 514321, 514422, 548526, 546194, 546197, 540596, 544283, 544405, A61K 31445, A61K 31505, C07D40314, C07D40114
Patent
active
057671168
DESCRIPTION:
BRIEF SUMMARY
This is a national stage application filed under 35U.S.C. .oval-hollow.371 of PCT/EP94/02904, filed Sep. 1, 1994.
The present invention relates to novel therapeutic agents 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, 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. benzopyranyl)alkylamino!alkyl substituted 2-pyrimidinyl compounds which have vasoconstrictor activity. These compounds are claimed to be useful in treating conditions related to vasodilation.
The present invention provides compounds of formula I ##STR2## including pharmaceutically acceptable salts thereof in which A is methylene or --O--; 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 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; 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 and optionally substituted by one or more substituents selected from halo, an alkyl group containing 1 to 3 carbon atoms, an alkoxy group containing 1 to 3 carbon atoms, or a polyhalogenated alkyl group, for example proviso that T is not 2-pyrimidinyl when A is --O--.
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 0,1 or 2.
In preferred compounds of formula I, R.sub.1 represents halo (for example fluoro, chloro, or bromo), an alkyl group containing 1 to 3 carbon atoms, an alkoxy group containing 1 to 3 carbon atoms, hydroxy, or two adjacent R.sub.1 groups together with the carbon atoms to which they are attached form a fused benz ring. In more preferred compounds of formula I, R.sub.1 represents methoxy, fluoro, chloro, hydroxy, or two adjacent R.sub.1 groups together with the carbon atoms to which they are attached form a fused benz ring.
In preferred compounds of formula I, R.sub.2 is H or an alkyl group containing 1 to 3 carbon atoms. In more preferred compounds of fo
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Heal David John
Kerrigan Frank
Martin Keith Frank
Grumbling Matthew V.
Knoll Atkiengesellschaft
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