New biphenylylethylamine derivatives useful as PPAR-gamma receptor modulators for treating e.g. dermatological, metabolic or immunological disorders or precancerous lesions

摘要

N-substituted N-(2-(1,1'-biphenyl-4-yl)-ethyl)-amine derivatives (I) are new. N-substituted N-(2-(1,1'-biphenyl-4-yl)-ethyl)-amine derivatives of formula (I) and their optical or geometric isomers and salts are new. R1 = phenyl (optionally substituted by R5), -C(R6)=CHR5, -(CH2)m-(CO)n-(X)p-(CH2)q-R5 or N-protected alpha-aminoacid residue containing a conventional amino-protecting group (e.g. 9-fluorenylmethylcarbamate, tert-butylcarbamate, benzyl or trifluoroacetyl); R2 = 5-(R8)-1,3,4-oxadiazol-2-yl, -CO-R9 or azole group of formula (a); R3 = H, halo, 1-12C alkyl, OH, 1-7C alkoxy, polyether group, NO2 or amino (optionally substituted by one or more of 1-12C alkyl, aryl, aralkyl, heteroaryl or heterocyclyl); R4 = 1-12C alkyl, aryl, aralkyl, heteroaryl, heterocyclyl or 9-fluorenylmethyl; R5 = H, 1-12C alkyl, aryl, aralkyl, heteroaryl, heterocyclyl or -(CO)s(Z)tR7; R6 = H or 1-12C alkyl; m, n, p, q, s, t = 0, 1 or 2; X = O, S or NR7; V = O or S; W = N or CR11; Y = N or C; Z = O, N or S; R7, R8 = H, 1-12C alkyl, aryl, aralkyl, heteroaryl or heterocyclyl; R9 = -O-(CH2)v-R10, OH, 1-7C alkoxy, aryl, aralkyl, heteroaryl, heterocyclyl or -NR'R''; R' = H, 1-12C alkyl, aryl, aralkyl, heteroaryl or heterocyclyl; R'' = H, 1-12C alkyl, aryl, aralkyl (optionally substituted by one or more halo), heteroaryl, heterocyclyl or -(CH2)v-R10; R10 = aryl, aralkyl, heteroaryl, heterocyclyl, -NHCOOR11 or -C-R11R12; v = 1-3; R11 = H, 1-12C alkyl, aryl, aralkyl, heteroaryl or heterocyclyl; R12 = H or 1-3C alkyl; A = -(CH2)z-(NR13)y-(CO)x-(D)w-; D = O, S, NR14 or CH2; x, y, z = 0 or 1; w = 0-6; R13, R14 = H or 1-12C alkyl.