Patent ID: 6426331
Filing Date: 2002-07-30
Classification: A61K,C07K

Abstract:
A compound of the formula: whereinR1 and R2 are each members independently selected from the group consisting of hydrogen, (C1-C2)alkyl, aryl, aryl(C1-C8)alkyl, (C1-C8)heteroalkyl and aryl(C1-C8)heteroalkyl, with the proviso that at least one of R1 and R2 is selected from the group consisting of aryl, aryl(C1-C8)alkyl and aryl(C1-C8)heteroalkyl; A1 is a member selected from the group consisting of L-&agr;-amino acids, D-&agr;-amino acids and radicals having the formula: â€ƒwherein one of R4 and R5 is a member selected from the group consisting of hydrogen, (C1-C8)alkyl and (C1-C8)heteroalkyl, and the other of R4 and R5 combines with R3 to form a 5-, 6-, 7- or 8-membered ring containing from one to three heteroatoms; A2 is a member selected from the group consisting of L-&agr;-amino acids, D-&agr;-amino acids and radicals having the formula: whereinR6 is selected from the group consisting of hydrogen and (C1-C4)alkyl; R7 and R8 are each members independently selected from the group consisting of hydrogen, (C1-C8)alkyl and (C1-C8)heteroalkyl, or can be combined with each other to form a 5-, 6-, 7- or 8-membered ring containing from zero to three heteroatoms; X is an unsubstituted (C1-C4) saturated or unsaturated alkyl linking group; Ar is an aryl group; and Y is a radical selected from the group consisting of: â€”B1â€”Z1 and â€”B2â€”(Z1)(Z2) â€ƒwherein B1 is a bond or a divalent linking group; B2 is a trivalent linking group; Z1 is a member selected from the group consisting of â€”CO2R9, â€”P(O)(OR9)(OR10), â€”P(O)(R9)(OR10), â€”S(O)2(OR9), â€”S(O)(OR9) and a carboxylic acid isostere; and Z2 is a member selected from the group consisting of â€”CO2R9, â€”NHR11, â€”P(O)(OR9)(OR10), â€”P(O)(R9)(OR10), â€”S(O)2(OR9), â€”S(O)(OR9) and a carboxylic acid isostere; â€ƒwherein R9 and R10 are each independently selected from the group consisting of H, (C1-C8)alkyl, aryl and (C1-C8)heteroalkyl; and R11 is (C1-C8)alkyl.