C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/223, 260/266
C07D 403/06 (2006.01) A61K 31/495 (2006.01) C07D 209/14 (2006.01) C07D 405/12 (2006.01) C07D 405/14 (2006.01)
Patent
CA 2006356
The present invention relates to novel piperazinylbutyldi- hydroindoles, piperazinylbutylindazoles, the corresponding 2,3-dihydro derivatives, and 2-indolones, having the following formula Image wherein the various symbols have the meanings set forth herein, which have been found to have central serotonin activity with preference for the serotonin 5-HT1A 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-HT1A receptor which implies less side effects related to activation of the receptors. The invention also includes acid addition salts and pharmaceutical compositions and their preparation for treating CNS disorders occurring 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 compounds. Separation and use of the stereo isomers of the 2,3-dihydro derivatives and 2-indolones are also part of this invention.
Perregaard Jens
Stenberg John Willie
H. Lundbeck A/s
Perley-Robertson Hill & Mcdougall Llp
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