C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/238, 260/305
C07D 403/12 (2006.01) A61K 31/50 (2006.01) C07D 491/04 (2006.01) C07D 495/04 (2006.01) C07D 497/04 (2006.01)
Patent
CA 2021685
DIR 0447 ABSTRACT The present invention is concerned with compounds of formula 1: Image (1) wherein R1 is straight or branched alkyl having 1-4 C-atoms, halogen or cyano; n has the value 0-1; R2 is hydrogen, (1-6 C)alkyl, (3-6 C)alkenyl, (3-6 C)alkenyl, (3-6 C)cycloalkyl, (3-6 C)cycloalkyl- (1-4 C)alkyl, phenyl, phenyl-(1-3 C)alkyl, COOR6, COR6, CONR6R7 or SO2-R6, wherein R6 and R7 indepen- dently of each other are hydrogen, (1-6 C)alkyl, (3-6 C)cycloalkyl, phenyl or phenyl-(1-4 C)alkyl, wherein the benzene ring is optionally substituted with a methyl group or a halogen atom, with the proviso that R6 is not hydrogen when R2 is a group COOR6 or SO2R6; R3 is hydrogen, straight or branched (1-6 C)alkyl or a phenyl-(1-3 C)alkyl group optionally substituted in the benzene ring; and A is a group of formula 2 or 3 DIR 0447 Image DIR 0447 (2) (3) wherein one of the groups R8, R9, and R10 is hydrogen, (1-4 C)alkyl, (3-6 C)cycloalkyl, (3-4 C)alkenyl or (3-4 C)alkynyl and the two other groups, independent- ly of each other, are hydrogen or (1-4 C)alkyl, and the pharmacologically acceptable acid addition salts thereof, which are pharmaceutically useful as strong and selective antagonists of "neuronal" 5-hydroxy tryptamine (5-HT) receptors.
Derk Hamminga
Van Wijngaarden Ineke
Derk Hamminga
Duphar International Research B.v.
Fetherstonhaugh & Co.
Van Wijngaarden Ineke
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