| 摘要 |
Biphenyl compounds (I) are new. Biphenyl compounds of formula (I), their optical and geometric isomers and salts when R1 contains a carboxylic acid functional group, are new. R1 = CH2-CH(R6)-C(O)-R5 or a group of formula (i); R2, R3 = NO2 or amino (both optionally substituted by 1-6C alkyl), H, 1-6C alkyl, aryl, halo, OR7 or polyether; X = CH2-N(R8)-CO, N(R8)-CO-N(R9), N(R8)-CO-CH2 or N(R8)-CH2-CO; R4 = T, pyrrolyl, pyrazinyl, naphthyl, biphenyl, indolyl, indenyl, benzothienyl, benzofuryl, benzothiazolyl or quinolyl (all optionally substituted by at least one R11 and/or R12), (CH2)n-(CO)qR13, adamantyl, diphenylmethyl, diphenylethyl, diphenylpropyl, diphenylbutyl, cyclopropylmethyl, cyclopentylethyl, 2-benzimidazolyl-ethyl, cyclohexylmethyl, phenoxyphenyl, 9H-fluorenyl, benzyloxyphenyl, 4-heptyloxyphenyl, 4-(6-methyl-2-benzothiazolyl)phenyl or (CH2)n-O-R13; T = phenyl, benzyl, phenethyl, thienyl, furyl or pyridyl (all substituted by R10); R5 = OH or 1-9C alkoxy; R6 = 1-6C alkyl, OR14 or SR14; R7 = H, 1-6C alkyl, aryl or aralkyl; R8, R9 = H or 1-6C alkyl; R10 = S(O)mR15, (CH2)p-COR16 or O-R17; R11, R12 = H, CF3, 1-12C alkyl, 1-9C alkoxy, polyether, NO2, OH (optionally protected by acetyl or benzoyl), amino (optionally substituted by 1-12C alkyl, CONH-R24, acetyl or benzoyl), S(O)mR15, (CH2)p-COR16 or OR17; n = 1-9; q = 0 or 1; R13 = OR18, N(R19)(R20), aralkyl, aryl or heteroaryl; m, p = 0-2; R14 = 1-12C alkyl, CF3, aryl or aralkyl; R15 = 1-12C alkyl, aryl or aralkyl; R16 = 1-12C alkyl, OR21, N(R22)(R23), aryl or aralkyl; R17 = aryl or aralkyl; R18-R23 = H or 1-12C alkyl, or R19 + R20 and R22 + R23 = heterocyclyl, and R24 = phenyl, diphenylmethyl, diphenylpropyl, diphenylbutyl, biphenylyl, phenoxyphenyl, 9H-fluorenyl, 4-benzyloxyphenyl, 4-heptyloxyphenyl or 4-(6-methyl-2-benzothiazolyl)phenyl. Independent claims are also included for: (1) a composition (C) which comprises at least one (I) formulated into a carrier, and (2) a cosmetic composition which comprises at least one (I) formulated into a carrier.
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