2-oxazolamines and their use as 5-ht2b receptor antagonists

Details 2-oxazolamines and their use as 5-ht2b receptor antagonists 2-oxazolamines and their use as 5-ht2b receptor antagonists

C - Chemistry, Metallurgy

07

D

C07D 263/48 (2006.01) A61K 31/421 (2006.01) A61K 31/422 (2006.01) A61P 1/00 (2006.01) C07D 413/04 (2006.01)

Patent

CA 2472762

The present invention relates to compounds of formula (I): wherein one of R1~and R4~ 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; and the other of R1~ and R4~ is an optionally substituted C~9-14 aryl group; 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, and R' is optionally substituted phenyl-C~1-4 alkyl, or (ii) together with the nitrogen atom to which they are attached, form an optionally substituted C~5-7 heterocyclic group; and their use as pharmaceuticals, in particular for treating conditions alleviated by the antagonism of a 5-HT~2B receptor.

La présente invention concerne les composés de la formule (I) où R1 ou R4 est sélectionné dans le groupe constitué de H et alkyle C1-6, cycloalkyle C3-7, cycloalkyle C3-7-alkyle C1-4, et phényle-alkyle C1-4 éventuellement substitués; l'autre R1 ou R4 respectivement restant représentant un groupe aryle C9-14 éventuellement substitué; R2 et R3 sont soit (i) indépendamment sélectionnés parmi H, R, R', SO2R, C(=O)R, (CH2)nNR5R6, où n vaut 1 à 4 et R5 et R6 sont indépendamment sélectionnés parmi H et R, R représentant alkyle C1-4 éventuellement substitué, et R' représentant phényle-C1-4 alkyle éventuellement substitué, soit (ii) ils forment, avec l'atome d'azote auquel ils sont liés, un groupe hétérocyclique C5-7 éventuellement substitué. L'invention concerne également leur utilisation comme produits pharmaceutiques, notamment pour traiter les états atténués par l'antagonisme d'un récepteur 5-HT2B.

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