Patent Number: 6,251,925

Title: Therapeutic biaryl derivatives

Abstract: The present invention relates to therapeutic biaryl derivatives of formula (I), and pharmaceutically acceptable derivatives thereof ##STR1## wherein R.sup.1 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.sub.1-6 alkoxy, C.sub.1-6 alkyl, nitro, cyano, hydroxymethyl, trifluoromethyl, --NR.sup.6 R.sup.6, and --NHSO.sub.2 R.sup.6, where each R.sup.6 is independently hydrogen or C.sub.1-4 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; X is oxygen, sulfur, --NH, or --NC.sub.1-4 alkyl; R.sup.3 is cyano, tetrazol-5-yl, or --CO.sub.2 R.sup.7 where R.sup.7 is hydrogen or C.sub.1-6 alkyl; R.sup.4 and R.sup.5 are independently hydrogen, C.sub.1-6 alkyl, --CO.sub.2 H, --CO.sub.2 C.sub.1-6 alkyl, cyano, tetrazol-5-yl, halogen, trifluoromethyl, or C.sub.1-6 alkoxy, or, when R.sup.4 and R.sup.5 are bonded to adjacent carbon atoms, R.sup.4 and R.sup.5 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 ameleoration by treatment with a beta-3 adrenoceptor agonist.

Inventors: Donaldson; Kelly Horne (Durham, NC), Shearer; Barry George (Apex, NC), Uehling; David Edward (Durham, NC)

Assignee: Glaxo Wellcome Inc.

International Classification: C07C 229/52 (20060101); C07C 217/14 (20060101); C07C 229/00 (20060101); C07C 217/00 (20060101); C07C 255/00 (20060101); C07C 255/58 (20060101); C07D 213/79 (20060101); C07D 213/00 (20060101); C07D 213/80 (20060101); C07D 307/00 (20060101); C07D 257/00 (20060101); C07D 257/04 (20060101); C07D 307/79 (20060101); C07C 229/52 (); C07C 213/79 (); C07C 213/88 (); A61K 031/44 (); A61K 031/19 ()

Expiration Date: 06/26/2018