Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1989-12-26
1991-03-26
Shen, Cecilia
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514253, 544366, 544369, 544373, A61K 31495, C07D40306
Patent
active
050029487
ABSTRACT:
The present invention relates to novel piperazinylbutylindoles, -indazoles, the corresponding 2,3-dihydro derivatives and 2-indolones which have been found to have central serotonin activity with preference for the serotonin 5-HT.sub.lA receptor.
Compared to the anxiolytic drug buspirone, and other clinically investigated compounds such as ipsapirone and gepirone, most of the present compounds have lower efficacy at the 5-HT.sub.lA receptor which implies less side effects related to activation of the receptors.
The invention also includes acid addition salts, methods of preparation, pharmacetical compositions and method of treating CNS disorders occuring in anxiety, depression, aggression and in alcohol abuse, or in states of disease related to the cardiovascular, gastrointestinal and renal systems, by administering the aforementioned derivatives.
Separation and use of the stereo isomers of the 2,3-dihydro derivatives and 2-indolones are also part of this invention.
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Perregaard Jens
Stenberg John W.
H. Lundbeck A/S
Hueschen Gordon W.
Shen Cecilia
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