| abstract |
Therapeutic derivatives of biaryl of the formula (1) and pharmaceutically acceptable derivatives thereof are described, wherein R 1 is a phenyl, naphthyl, pyridyl, thiazolyl, phenoxymethyl or pyrimidyl group, optionally substituted by one or more substituents selected from the group consisting in halogen, hydroxy, C1-6 alkoxy, C1-6 alkyl, nitro, cyano, hydroxymethyl, trifluoromethyl, -NR6R6 and ûNHSO2R6, where each R6 is independently hydrogen or C1-4 alkyl; R2 is hydrogen or C1-6 alkyl; X is oxygen, sulfur, -NH or -4N-C1-4 alkyl; R3 is cyano, tetrazol, -5-yl or ûCO2R7 where R7 is hydrogen or C1-6 alkyl; R4 and R5 are independently hydrogen, C1-6 alkyl, -CO2H, -CO2 C1-6 alkyl, cyano, tetrazol-5-yl, trifluoromethyl halogen or C1-6 alkoxy when R4 and R5 are attached to adjacent carbon atoms , R4 and R5 may, together with the carbon atoms to which they are attached, form a fused 5 or 6-membered ring that optionally contains one or two nitrogen, oxygen or sulfur atoms; and Y is N or CH, to processes for its preparation comprising A) deprotection of a compound of formula (2) B) Interconversion of another compound of formula (1); or C) Reaction of a compound of formula (2) with a compound of formula (4) followed by step (A) without purification of intermediate products: formulas (3) and (4); D) reaction of a compound of formula (5) with a compound of formula (6), its use in the treatment of diseases susceptible to improvement by the treatment of a beta-3-adrenoceptor agonist. |