- Heterocyclic derivatives, their preparation and medicinal products containing them
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Compounds are disclosed of formula: in which R1 represents a residue of formula STR1 X represents a hydrogen atom or an alkyl radical, Y represents a hydrogen atom or an alkyl or alkoxy radical, Z represents an alkyl radical, n is equal to 2 or 3, Het represents a substituted piperidino (substituted at the 4-position with a 1-indenylidene, 1-indenyl or 1-indanyl radical or with a chain --(CH2)m --R2 or =CH--R2), substituted 1,2,3,6-tetrahydro-1-pyridyl (substituted at the 4-position with a chain --(CH2)m --R2), m is equal to 1 or 2, and R2 represents an optionally substituted 2- or 3-indolyl radical, a 1- or 2-indanyl, 1- or 2-indenyl, an optionally substituted 1,2,3,4-tetrahydro-5H-pyrido[4,3-b]indol-2-yl radical, a 1,2,3,4-tetrahydro-3-quinolyl radical, an optionally substituted 1,2,3,4-tetrahydro-2-naphthyl radical or a 1-indolyl radical, their preparation and medicinal products containing them.
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- 3-(4-Piperidinylalkyl)indoles, Selective Inhibitors of Neuronal 5-Hydroxytryptamine Uptake
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A series 3-(4-piperidinylalkyl)indoles was synthesized and tested as uptake inhibitors of biogenic amines.Some of these compounds are potent and very selective in blocking the 5-hydroxytryptamine (5-HT) uptake, as evidenced by biochemical data and behavioral tests.A discussion on structure-activity relationships is given.The most interesting member of the series, indalpine, 3-indole (1), was selected for clinical studies.
- Gueremy, Claude,Audiau, Francois,Champseix, Alain,Uzan, Andre,Fur, Gerard Le,Rataud, Jean
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p. 1306 - 1310
(2007/10/02)
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