21585-16-0Relevant academic research and scientific papers
Tetrahydropyridin-4-yl indoles with a combination of affinity for dopamine-D2 receptors and serotonin reuptake sites
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Page/Page column 4, (2010/11/08)
The present invention relates to a group of novel tetrahydropyridin-4-yl indoles with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine-D2 receptors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said tetrahydropyridin-4-yl indoles. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The invention relates to novel tetrahydropyridin-4-yl indoles of the formula. and tautomers, stereoisomers, prodrugs, N-oxides, pharmacologically acceptable salts, hydrates and solvates thereof, wherein: R1 is hydrogen, halogen, alkyl(C1-3) or alkoxy(C1-3), CN or CF3, R2 is hydrogen or alkyl(C1-3), R3 is hydrogen or alkyl(C1-3), Z is hydrogen or alkyl(C1-3), alkoxy(C1-3) or alkylthio(C1-3), A is hydrogen or alkyl(C1-3), or A and Z together form a saturated or (partly) unsaturated 5- or 6-membered ring which may be substituted with halogen, alkyl (C1-3) or phenyl, in which ring Z represents carbon, sulfur of nitrogen.
4-(1H-INDOL-1-YL)-1-PIPERIDINYL DERIVATIVES
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, (2008/06/13)
The present invention concerns the compounds of formula STR1 the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dashed line designates an optional bond; R 1 and R 2 are each independently hydrogen, halogen, C. sub.1-6 alkyl or C. sub.1-6 alkyloxy; R 3 and R. sup.4 are each independently hydrogen, C 1-6 alkyl, phenyl or phenyl substituted with one, two or three substituents selected from halo, hydroxy, nitro, cyano, trifluoromethyl, C 1-6 alkyl, C 1-6 alkyloxy, C 1-6 alkylthio, mercapto, amino, mono-and di(C 1-6 alkyl)-amino, carboxyl, C 1-6 alkyloxycarbonyl and C 1-6 alkylcarbonyl; Alk is C 1-4 alkanediyl; D is a pyrimidinone, piperidone or a benzimidozolidinone; having antipsychotic activity; their preparation, compositions containing them and their use as a medicine.
Synthesis and in vitro evaluation of some new pyrimidines and related condensed ring systems as potential anticancer agents
Badawey, El-Sayed A. M.
, p. 229 - 233 (2007/10/03)
Several new pyrimidines 6-11, 18-20, furo-, thieno-, and pyrrolo[2,3-d]pyrimidines 3, 8, 12, triazolo[4,3-a]pyrimidines 14, 15, 16 and tetrazolo[1,5-a]pyrimidine 17 were prepared from the known intermediate 5-(2-hydroxyethyl)-6-methyl-2-thiouracil (2). Compound 7 (4-chloro-5-(2-chloroethyl)-2-methylthio-6-methyl-pyrimidine) exhibited weak antitumor activity in vitro.
