| 摘要 |
Compounds of formula Iwherein n is 1, 2 or 3; R1 is H, C1-4alkyl, aryl, or aryl-C1-4alkyl; Y is C1-4alkylene, -CO-C1-4alkylene, -CO-C2-5alkenylene, -CO-NH-, -CO-C1-3alkylene-NH-, or -CO-O-; R2 is an aromatic or heteroaromatic residue, each being optionally substituted by CF3, halogen, OH, C1-4alkoxy, amino, mono- or di-C1-4alkyl substituted amino, phenyl, benzyl or C1-4alkyl optionally substituted by amino; R3is the side chain present on the Calpha of an alpha-amino acid; R4 is biphenylyl, benzyl, hydroxy-benzyl, alpha- or beta-naphthyl-methyl, 5,6,7,8-tetrahydro-beta-naphthyl-methyl or indolyl-methyl, each being optionally substituted on the ring by CF3, halogen, OH, C1-4alkoxy, amino, mono- or di-C1-4alkyl substituted amino, phenyl, benzyl or C1-4alkyl optionally substituted by amino; and X is -CN, -NR5R6 or -O-R8 wherein R5 is H, C1-6alkyl, aryl or aryl-C1-4alkyl; R6 is H or C1-6alkyl; and R8 is H, C1-4alkyl, aryl or aryl-C1-4alkyl; in free form or in salt form; which are useful in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1, -ICAM-2 or -ICAM-3 interactions.
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