5-ht2b receptor antagonists

Details 5-ht2b receptor antagonists 5-ht2b receptor antagonists

C - Chemistry, Metallurgy

07

D

C07D 277/40 (2006.01) A61K 31/425 (2006.01) A61P 1/00 (2006.01)

Patent

CA 2472763

The present invention concerns compounds of formula (I): wherein R1~ is selected from the group consisting of H, and optionally substituted C ~1-6 alkyl, C ~3-7 cycloalkyl, C ~3-7 cycloalkyl-C ~1-4 alkyl, and phenyl-C ~1-4 alkyl;R2~ and R3~ are either: (i) independently selected from H, R, R', SO~2R, C(=O)R, (CH~2)~nNR5~R6~, where n is from 1 to 4 and R5~ and R6~ are independently selected from H and R, where R is optionally substituted C ~1-4 alkyl group, and R' is an optionally substituted phenyl- C ~1-4 alkyl group, or (ii) together with the nitrogen atom to which they are attached, form an optionally substituted C ~5-7 heterocyclic group; R4~ is an optionally substituted C ~9-14 aryl group; their use as pharmaceuticals, in particular for treating conditions alleviated by antagonism of a 5-HT~2B receptor.

L'invention concerne des composés représentés par la formule (I) dans laquelle R1 est choisi dans le groupe H, et C 1-6 alkyl à substitution facultative, C 3-7 cycloalkyl, C 3-7 cycloalkyl-C 1-4 alkyl, et phenyl-C 1-4 alkyl; R2 et R3 sont: soit (i) indépendamment choisis parmi H, R, R', SO2R, C(=O)R, (CH2)nNR5R6, n étant compris entre 1 et 4 et R5 et R6 sont indépendamment choisis parmi H et R, R étant un groupe C 1-4 alkyl à substitution facultative, et R' est un groupe phenyl- C 1-4 alkyl à substitution facultative, soit (ii) ils forment ensemble avec l'atome d'azote auquel ils sont attachés, un groupe hétérocyclique C 5-7 à substitution facultative ; R4 est un groupe C 9-14 à substitution facultative ; leur utilisation en tant que produits pharmaceutiques, notamment dans le traitement de conditions soulagées par l'antagonisme d'un récepteur 5-HT 2B.

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