VITRONECTIN RECEPTOR ANTAGONISTS

摘要

Compounds of formula (I) are disclosed which are inhibitors of the vitronectin receptor, 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 or benzyl; R<2> is (CH2)nCO2H; R<3> is H, C1-6alkyl, Ar-C0-6alkyl, Het-C0-6 alkyl, or C3-6cycloalkyl-C0-6alkyl; R<4> is W-U, Y-(CHR<5>)m-U or Z-C(O); R<5> and R<6> are independently chosen from H, C1-6alkyl, Ar-C0-6alkyl;, Het-C0-6alkyl and C3-6cycloalkyl-C0-6alkyl; m is 1 or 2; n is 1 or 2; U is NR<1>C(O), C(O)NR<1>, CH=CH, CC, CH2-CH2, O-CH2, CH2-O or CH2OCONR<1>; W is (a), (b) or (c); R<a> is H, OH, NO2, N(R<6>)2, CON(R<6>)2, CH2N(R<6>)2, or R<6>HN-C(=NH); Y is NH2, NHR<6>, N(R<6>)2, C(O)N(R<6>)2, OH, =N-OR<6>, (d), (e) or (f); Z is (g) or (h); R<d> is H, N(R<1>)2, C1-4alkyl, CON(R<1>)2, OH, OR<1>, or Ar-C0-4alkyl; R<e> is H, C1-4alkyl, 2- or 3-pyridinyl, 1-, 2- or 3-piperidinyl, or 2- or 4-pyrimidinyl; and pharmaceutically acceptable salts thereof.