Antiserotonins, their preparation and pharmaceutical composition

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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514 63, 514221, 5142265, 514252, 514307, 514321, 514338, 544 49, 544229, 544249, 544363, 544368, 546 14, 546148, 546198, 5462711, A61K 31495, A61K 3155, A61K 31445, C07D23970, C07D40104, C07F 702

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active

055631444

ABSTRACT:
This invention relates to compounds having the formula R.sub.1 -(CH.sub.2).sub.n -Het wherein R.sub.1 is a residue having the formula (B), (C), (D); Het represents a radical phenyl-4 tetrahydro-1,2,3,6 pyridyl-1 whose phenyl cycle is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical; a radical phenyl-4 piperazinyl-1 whose phenyl cycle is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical; R.sub.3 is a hydrogen atom or a phenyl radical; R.sub.4 is a hydrogen or halogen atom or a residue Het; R.sub.5 is a carbonyl or sulfonyl radical; R.sub.6 is a radical Si(CH.sub.3).sub.2 or C(CH.sub.3).sub.2 ; n equals 1, 2, 3 or 4; excepting {[(phenyl-4 tetrahydro-1,2,3,6 pyridyl-1)-2 ethyl] amino}-3 benzisothiazol-1,2 dioxyde-1,1; their salts, their preparation and medicaments containing them.

REFERENCES:
patent: 4104387 (1978-08-01), Wade et al.
patent: 4132725 (1979-01-01), Barcza
Jean-Luc Malleron et al Journal of Medicinal Chemistry, vol. 34, No. 8, p. 2477 (1991).
Perregaard et al. J. Med. Chem. 1992, 35, 4813-4822.
Leysen et al, Molecular Pharmacology 21: 301-314.

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