Substituted phenyl compounds

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 65/24 (2006.01) A61K 31/19 (2006.01) A61K 31/215 (2006.01) A61K 31/33 (2006.01) C07C 43/23 (2006.01) C07C 45/00 (2006.01) C07C 45/60 (2006.01) C07C 45/63 (2006.01) C07C 45/67 (2006.01) C07C 45/71 (2006.01) C07C 47/565 (2006.01) C07C 47/575 (2006.01) C07C 49/813 (2006.01) C07C 49/84 (2006.01) C07C 59/68 (2006.01) C07C 59/90 (2006.01) C07C 65/26 (2006.01) C07C 65/28 (2006.01) C07C 69/736 (2006.01) C07C 69/738 (2006.01) C07C 205/34 (2006.01) C07C 205/37 (2006.01) C07C 205/38 (2006.01) C07C 217/76 (2006.01

Patent

CA 2176363

Compounds of formula (I) are described wherein R1 is hydrogen, -(lower alkyl)q(CO2R6 or OH), -CN, -C(R7)=NOR8, NO2, -O(lower alkyl)R9, -CC-R10, - CR11=C(R12)(R13), -C(=O)CH2C(=O)CO2H, -CO(R14), alkylthio, alkylsulphinyl, alkylsulphonyl, carbamoyl, thiocarbamoyl, substituted carbamoyl, substituted thiocarbamoyl, sulphamoyl or an optionally substituted nitrogen-containing ring, m, n, o and p are independently zero or 1 and R2, R3, R4 and R5 are various groups; and physiologically acceptable salts, N-oxides and prodrugs thereof. The compounds have endothelin antagonist activity and are useful as pharmaceuticals.

L'invention concerne des composés de formule (I) dans laquelle R?1¿ représente hydrogène, -(alkyle inférieur)¿q?(CO¿2?R?6¿ ou OH), -CN, -C(R?7¿)=NOR?8¿, NO¿2?, -O(alkyle inférieur)R?9¿, -C?C-R?10¿, -CR?11¿=C(R?12¿)(R?13¿), -C(=O)CH¿2?C(=O)CO¿2?H, -CO(R?14¿), alkylthio, alkylsulfinyle, alkylsulfonyle, carbamoyle, thiocarbamoyle, carbamoyle substitué, thiocarbamoyle substitué, sulfamoyle ou un cycle contenant de l'azote facultativement substitué, m, n, o et p représentent indépendamment zéro ou 1 et R?2¿, R?3¿, R?4¿, et R?5¿ représentent différents groupes. L'invention porte également sur des sels physiologiquement acceptables, des N-oxydes et des promédicaments de ces derniers. Ces composés présentent une activité d'antagonistes de l'endothéline et sont utiles en tant que produits pharmaceutiques.

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