| abstract |
The present invention relates to therapeutic biaryl derivatives of formula (I), and pharmaceutically acceptable derivatives thereof; wherein R1 is a phenyl, naphthyl, pyridyl, thiazolyl, phenoxymethyl, or pyrimidyl group, optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C¿1-6?alkoxy, C1-6alkyl, nitro, cyano, hydroxymethyl, trifluoromethyl, -NR?6R6¿, and -NHSO¿2R?6, where each R6 is independently hydrogen or C¿1-4?alkyl; R?2¿ is hydrogen or C¿1-6?alkyl; X is oxygen, sulfur, -NH, or -NC1-4alkyl; R?3¿ is cyano, tetrazol-5-yl, or -CO¿2R?7 where R7 is hydrogen or C¿1-6?alkyl; R?4 and R5¿ are independently hydrogen, C¿1-6?alkyl, -CO2H, -CO2C1-6alkyl, cyano, tetrazol-5-yl, halogen, trifluoromethyl, or C1-6alkoxy, or, when R?4 and R5¿ are bonded to adjacent carbon atoms, R?4 and R5¿ may, together with the carbon atoms to which they are bonded, form a fused 5 or 6 membered ring optionally containing one or two nitrogen, oxygen, or sulfur atoms; and Y is N or CH, to processes for their preparation and their use in the treatment of diseases susceptible to amelioration by treatment with a beta-3 adrenoceptor agonist. |