New biphenylyl-substituted thioamide compounds, are integrin receptor antagonists useful e.g. for treating circulatory, inflammatory, osteolytic or ophthalmological diseases or microbial infections

摘要

Biphenylyl-substituted thioamide compounds (I) are new. Biphenyl derivatives of formula (I) and their stereoisomers, salts and solvates are new. A = NH2, C(=NH)NH2, NHC(=NH)NH2, C(=NH)NHA', Het or NH-Het; B' = OR or N(R)2; R = H, 3-14C cycloalkyl, 6-10C aryl or 7-14C aralkyl (optionally substituted by one or more R3 and optionally interrupted by O in the alkyl chain); R1, R'1, R''1, R2, R'2, R''2 = H, halo, NO2, NH2, NHR, N(R)2, OH, OR, COR, CO3R, SO2R or SR; R3 = halo, NO2, CF3, OH, OCF3, SCF3, OMe or OEt; Het = mono- or bicyclic heteroaryl containing 1-4 N (optionally substituted by one or more of A', NHA', N(A')2 and/or NH2); A' = 1-8C alkyl; X, Y = O or S, but not both O; Z' = CH2 or O; n = 1-4. An Independent claim is included for the preparation of (I).