| 摘要 |
The non-peptide methylene carbonylamino derivatives or pharmaceutically acceptable salts or esters thereof have the formula (I) wherein: X is -CO2H, -PO-3H, -SO2R5, -SO3H, -OPO-3H or -CO2R4; Y is -CO-, -SO2- or PO2-; R1 is aryl-alkenyl, aryl-alkynyl, alkenyl, alkynyl, cycloalkyl, aryl-fused cycloalkyl, cycloalkenyl, aryl, aralkyl, cycloalkyl-alkyl, cycloalkenyl-cycloalkyl, bi-aryl, alkoxy, alkenyloxy, alkynyloxy, aralkoxy, aryl-alkenyloxy, aryl-alkynyloxy, alkylamino, alkenylamino, alkynylamino, aryl-alkylamino, aryl-alkenylamino, aryl-alkynylamino, aryloxy, arylamino, N-alkylurea-alkyl, N-arylurea-alkyl, alkylcarbonylamino-alkyl, aminocarbonyl-alkyl, heterocyclyl, heterocyclyl-alkyl, heterocyclyl-amino, carboxyalkyl-aralkyl, oxocarbocyclyl-fused aryl or heterocyclylalkyl provided that R1 cannot be t-butoxy or benzyloxy; R2 is hydrogen, aryl, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl or aralkyl or R2 and R3 together with the atoms to which they are attached can form a heterocycle; R3 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aralkyl, aryl-alkenyl, aryl-alkynyl, hydroxy-alkyl, alkoxy-alkyl, aralkoxy-alkyl, amino-alkyl, (aryl-alkyloxycarbonylamino) alkyl, thio-alkyl, alkylsulphonyl-alkyl, (hydroxy-alkylthio) alkyl, thioalkoxy-alkyl, acylamino-alkyl, alkylsulphonylamino-alkyl, arylsulphonylamino-alkyl, morpholino-alkyl, thiomorpholino-alkyl, morpholinocarbonyl-alkyl, thiomorpholinocarbonyl-alkyl, [N-(alkyl, alkenyl or alkynyl)- or N,N-[dialkyl, dialkenyl, dialkynyl or (alkyl, alkenyl)-amino] carbonyl-alkyl, carboxy-alkyl, dialkylamino-acylaminoalkyl or amino acid side chains selected from arginine, asparagine, glutamine, S-methyl cysteine, methionine or corresponding sulphoxide or sulphone derivatives thereof, glycine, leucine, isoleucine, allo-isoleucine, tert-leucine, norleucine, phenylalanine, tyrosine, tryptophan, proline, alanine, ornithine, histidine, glutamine, valine, threonine, serine, aspartic acid, beta-cyanoalanine and allothreonine; R4 is aryl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aralkyl, hydrogen, heterocyclyl, heterocyclylcarbonyl, aminocarbonyl, amido, mono- or dialkylaminocarbonyl, mono- or diarylaminocarbonyl, alkylarylaminocarbonyl, diarylaminocarbonyl, mono- or diacylaminocarbonyl, aromatic or aliphatic acyl or optionally substituted alkyl; R5 is aralkyl, aryl-alkenyl, aryl-alkynyl, aryl, alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl and n is 0, 1 or 2; provided that when R1 is N-alkylurea alkyl or N-arylurea alkyl and Y is CO, R3 is not 3-indolylmethyl. A pharmaceutical composition thereof is useful for preventing, inhibiting or suppressing of cell adhesion.
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