INTEGRIN RECEPTOR ANTAGONISTS

摘要

Integrin receptor antagonists of formula (I) are disclosed, wherein: X-X' is NR<1>-CH, NC(O)R<3>-CH, N=C, CR<1>=C, CHR<1>-CH, O-CH or S-CH; R<1> is H, C1-6alkyl, C3-7cycloalkyl-C0-6alkyl or ArC0-6alkyl; R<2> is (CH2)nCO2R; R<3> is H, C1-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl, or C3-6cycloalkyl-C0-6alkyl; R<4> is Y-U; R<5> and R<5'> are R' or together are =O; R is H, C1-6alkyl, benzyl or a carboxy protecting group; U is -NR<1>NR<1>C(O), =N-N=CH or -R<1>NN=CH; Y is W-(CR'2)q-Z-(CR'R')r-; W is R'R'''N-, R'R"NR'N-, R'R"NR'NCO-, R'2NR'NC(=NR')-, R'ONR'C(=NR')-, OH, (a), (b), (c), (d), (e), (f), (g), (h), (i), (j) or (k); R' is H, C1-6alkyl, C3-7-cycloalkyl-C0-4alkyl or Ar-C0-4alkyl; R" is R', -COR', CO2C1-6alkyl or CO2C0-4alkyl-Ar; R''' is R', -CF3, -SR', or -OR'; R is R', COR', CN, NO2, SO2R', CO2C1-6alkyl or CO2C0-4alkyl-Ar; Z is (CH2)t, Het, Ar or C3-7cycloalkyl; R is H, C1-4alkyl, OR<1>, SR<1>, C1-4alkyl, C1-4alkylsulfonyl, C1-4alkylsulfoxyl, -CN, N(R<1>)2, CH2N(R<1>)2, -NO2, -CF3, -CO2R<3>, -CON(R<1>)2, -COR<1>, -NR<1>C(O)R<1>, OH, F, Cl, Br, I or CF3S(O)r-; Q is NR<1>, S or O; and pharmaceutically acceptable salts thereof.