Arylpiperidine derivatives

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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514258, 514278, 514317, 514323, 546183, 546201, 546 16, 546192, 546240, 546236, 544282, C07D23970, C07D22100, A61K 3144, A61K 31505

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active

052946193

ABSTRACT:
A series of novel N-alkyl or oxyalkyl arylpiperidine derivatives have been prepared, including their pharmaceutically acceptable acid addition salts, wherein the N-alkyl or oxyalkyl side chain is further substituted by certain aryl or heterocyclic ring groups. These particular compounds are useful in therapy as neuroleptic agents for the control of various psychotic disorders. Typical and preferred member compounds include 4-{{4-{2-[4-(2-methoxyphenyl)-1-piperidinyl]ethyl}phenyl}}thiazole-2-amine , 4-{{4-{4-[4-(2-methoxyphenyl)-1-piperidinyl]-n-butyl}phenyl}}thiazole-2-a mine, 3-{4-[4-(2-methoxyphenyl)-1-piperidinyl]-n-butyl}-1,8,8-trimethyl-3-azabic yclo[3.2.1]octane-2,4-dione, 5-{2-[4-(2-methoxyphenyl)-1-piperidinyl]ethyl}oxindole and 3-{2-[4-(1-naphthyl)-1-piperidinyl]ethyl}-2-methyl-4H-pyrido[1,2-a]pyrimid ine-4-one, respectively. Methods for preparing all these compounds from known starting materials are provided.

REFERENCES:
patent: 3573310 (1971-03-01), Van Dyke et al.
patent: 4623728 (1986-11-01), Sarges
Maryanoff et al., J. Org. Chem. 48(25) (1983) pp. 5074-5080 and 5080-M1 through 5080-M12.
Hacksell et al., J. Med. Chem., 24 1475-1482 (1981).
Rehse et al., Arc. Pharm. 312 670-681 (1979).

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