Aryl-substituted acrylamides with leukotriene b4 (ltb-4)...

C - Chemistry – Metallurgy – 07 – D

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C07D 213/53 (2006.01) A61K 31/44 (2006.01) C07C 235/34 (2006.01) C07C 317/46 (2006.01) C07C 323/62 (2006.01) C07D 213/69 (2006.01) C07D 333/16 (2006.01) C07D 333/24 (2006.01)

Patent

CA 2265996

Disclosed are compounds of formula (I) wherein W is CH or N; R is (mono- or di- carbocyclic or heterocyclic aryl)-lower alkyl; R1 is hydrogen or lower alkyl; R2 and R3 are hydrogen, lower alkyl, lower alkoxy-lower alkyl or aryl-lower alkyl; or R2 and R3 joined together represent lower alkylene optionally interrupted by O, NH, N-lower alkyl or S so as to form a ring with the amide nitrogen; X is O, S, SO, SO2 or a direct bond; X1 is O, S, SO, SO2 or a direct bond; Y is a direct bond, lower alkylene or lower alkylidene; and Z is carboxyl, 5-tetrazolyl, hydroxymethyl or carboxyl derivatized in the form of a pharmaceutically acceptable ester; and pharmaceutically acceptable salts thereof; which are useful as LTB-4 antagonists.

L'invention concerne les composés présentant la formule (I). Dans cette dernière, W représente CH ou N; R est (aryle mono- ou di-carbocyclique ou hétérocyclique)-alkyle inférieur; R?1¿ est hydrogène ou alkyle inférieur; R?2¿ et R?3¿ sont hydrogène, alkyle inférieur, alcoxy inférieur-alkyle inférieur ou aryle-alkyle inférieur; ou R?2¿ et R?3¿ assemblés représentent de l'alkylène inférieur éventuellement interrompu par O, NH, N-alkyle inférieur ou S pour former une chaîne avec l'azote d'amide; X est O, S, SO, SO¿2? ou une liaison directe; X?1¿ est O, S, SO, SO¿2? ou une liaison directe; Y est une liaison directe, de l'alkylène inférieure ou de l'alkylidène inférieur, et Z est carboxyle, 5-tétrazolyle, hydroxyméthyle ou du carboxyle dérivé sous forme d'un ester pharmaceutiquement acceptable. L'invention traite aussi de sels pharmaceutiquement acceptables de ces derniers qui sont utiles comme antagonistes de la leucotriène B-4.

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