Integrin receptor antagonists

Antagonistes de recepteurs de l'integrine

Abstract

Compounds of the formula (I): wherein A1 is C or N; E is a five- or six-membered heteroaromatic or six-membered aromatic ring optionally substituted by R3 or R4; X1-X2- is CHR1-CH, CR1=CH, NR1-CH, S(O)u-CH or O-CH; X3 is CR5R5, NR5, S(O)u or O; R2 is -OR', -NR'R", -NR'SO2R"', -NR'OR',-OCR'2C(O)OR', -OCR'2OC(O)-R', -OCR'2C(O)NR'2, CF3 or -COCR'2R2'; R3, R4 and R7 are independently H, halo, -OR12, -SR12, -CN, -NR'R12, -NO2, -CF3, CF3S(O)r-, -CO2R', -CONR'2, R14-C0-6alkyl-, R14-C1-6oxoalky-, R14-C2-6alkenyl-, R14-C2-6alkynyl, R14-CO-6alkyloxy, R14-C0-6alkylamino- or R 14-C0-6alkyl-S(O)r-; R6 is W-(CR'2)q-Z-(CR'R10)r-U-(CR'2)S-V- or W'-(CR'2)q-U-(CR'2)s- U and V are absent or CO, CR'2, C(=CR15 2), S(O)n, O, NR15, CR15'OR15, CR'(OR")CR'2, CR'2CR'(OR"), C(O)CR'2, CR15 2C(O), CONR15, NR15CO, OC(O), C(O)O, C(S)O, OC(S), C(S)NR15, NR15C(S), SO2NR15, NR15SO2, N=N, NR15NR15, NR15CR15 2, NR15CR15 2, CR15 2O, OCR15 2, C.ident.C, CR15=CR15, Het, or Ar, provided that U and V are not simultaneously absent; and W and W' are a nitrogen-containing substituent, are integrin receptor antagonists.

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