Patent ID: 6376538
Filing Date: 2002-04-23
Classification: A61K,A61P,C07C,C07D,C07K

Abstract:
A cell adhesion inhibitory compound selected from a compound of the formula (I): and pharmaceutically acceptable derivatives of (I), wherein:X is selected from the group consisting of â€”CO2H, â€”POâˆ’3H, â€”SO2R5, â€”SO3H, â€”OPOâˆ’3H, and â€”CO2R4; wherein R5 is selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, aryl-substituted alkyl, and aryl-substituted alkenyl or alkynyl; Y is selected from the group consisting of â€”COâ€”, â€”SO2â€” and â€”PO2â€”; R1 is selected from the group consisting of alkenyl, alkynyl, cycloalkyl, aryl-fused cycloalkyl, cycloalkenyl, aryl, substituted aralkyl, aryl-substituted alkenyl or alkynyl, cycloalkyl-substituted alkyl, cycloalkenyl-substituted alkyl, biaryl, alkenyloxy, alkyloxy, aryloxy, aryl-substituted alkenyloxy or alkyloxy, alkylamino, alkenylamino or alkynylamino, aryl-substituted alkylamino, aryl-substituted alkenylamino or alkynylamino, aryloxy, arylamino, N-alkylurea-substituted C1-C4 alkyl, N-arylurea-substituted C1-C4 alkyl, aminocarbonyl-substituted alkyl, heterocyclyl, heterocyclyl-substituted alkyl, heterocycly-substituted amino, carboxylalkyl substituted aralkyl, oxocarbocyclyl-fused aryl and heterocyclylalkyl; R2 is selected from the group consisting of hydrogen, aryl, alkyl alkenyl or alkynyl, cycloalkyl, cycloalkenyl, aryl-substituted alkyl and, wherein R2 and R3 may be taken together with the atoms to which they are attached, to form a heterocycle; R3 is selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aralkyl, aryl-substituted alkenyl or alkynyl, cycloalkyl, cycloalkenyl, aralkyl, aryl-substituted alkenyl or alkynyl, hydroxy-substituted alkyl, alkoxy-substituted alkyl, arylkoxy-substituted alkyl, amino-substituted alkyl, (aryl-substituted alkyloxycarbonylamino)-substituted alkyl, thiol-substituted alkyl, alkylsulfonyl-substituted alkyl, (hydroxy-substituted alkylthio)-substituted alkyl, thioalkoxy-substituted alkyl, acylamino-substituted alkyl, alkylsulfonylamino-substituted alkyl, arylsulfonylamino-substituted alkyl, morpholino-alkyl, thiomorpholino-alkyl, morpholino carbonyl-substituted alkyl, thiomorpholinocarbonyl-substituted alkyl, (N-alkyl, alkenyl or alkynyl)- or N,N-(dialkyl, dialkenyl, dialkynyl)- or N,N-(alkyl,alkenyl)-aminocarbonyl-substituted alkyl, carboxyl-substituted alkyl, dialkylamino-substituted acylaminoalkyl and amino acid side chains selected from arginine, asparagine, glutamine, S-methyl cysteine, methionine and corresponding sulfoxide and sulfone derivatives thereof, glycine, leucine, isoleucine, allo-isoleucine, tert-leucine, norleucine, phenylalanine, tyrosine, tryptophan, proline, alanine, ornithine, histidine, glutamine, valine, threonine, serine, betacyanoalanine, and allothreonine; and wherein R2 and R3 may be taken together with the atoms to which they are attached, to form a heterocycle; R4 is selected from the group consisting of aryl, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl and aryl-substituted alkyl, hydrogen, heterocyclyl, heterocyclylcarbonyl, amido, mono- or dialkylaminocarbonyl, mono- or diarylaminocarbonyl, alkylarylaminocarbonyl, diarylaminocarbonyl, mono- or diacylaminocarbonyl, aromatic acyl, alkyl optionally substituted by stubstituents selected from the group consisting of amino, carboxy, hydroxy, mercapto, mono- or dialkylamino, mono- or diarylamino, alkylarylamino, diarylamino, mono- or diacylamino, alkoxy, alkenyloxy, aryloxy, thioalkoxy, thioalkenoxy, thioalkynoxy, thioaryloxy and heterocyclyl; and n is 0, 1, or 2; and at least one of R1-R5 includes a heterocyclic group.