ANTAGONIST OF VITRONECTIN RECEPTOR, PHARMACEUTICAL COMPOSITION CONTAINING THEREOF, PROCESS OF ITS PREPARATION AND USE

摘要

PCT No. PCT/US96/20327 Sec. 371 Date Jul. 27, 1999 Sec. 102(e) Date Jul. 27, 1999 PCT Filed Dec. 20, 1996 PCT Pub. No. WO97/24124 PCT Pub. Date Jul. 10, 1999Compounds of formula (I) are disclosed, wherein: A is a fibrinogen antagonist template; W is a linking moiety of the form -(CHRg)a-U-(CHRg)b-V-; Q1, Q2, Q3 and Q4 are independently N or C-Ry, provided that no more than one Q1, Q2, Q3 and Q4 is N; R' is H or C1-6alkyl, C3-7cycloalkyl-C0-6-alkyl or Ar-C0-6alkyl; Rg is H or C1-6alkyl, Het-C0-6alkyl, C3-7cycloalkyl-C0-6alkyl or Ar-C0-6alkyl; Rk is Rg, -C(O)Rg or -C(O)ORg Ri is H, C1-6alkyl, Het-C0-6alkyl, C3-7cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl-U'-C1-6alkyl, C3-7cycloalkyl-C0-6alkyl-U'-C1-6alkyl or Ar-C0-6alkyl-U'-C1-6alkyl; Ry is H, halo, -ORg, -SRg, -CN, -NRgRk, -NO2, -CF3, CF3S(O)r, -CO2Rg, -CORg or -CONRg2, or C1-6alkyl optionally substituted by halo, -ORg, -SRg, -CN, -NR8R'', -NO2, -CF3, R'S(O)3-, -CO2Rg, -CORg or -CONRg2; U and V are absent or CO, CRg2, C(=CRg2), S(O)c, O, NRg, CRgORg, CRg(ORk)CRg2, CRg7CRg(ORk), C(O)CRg2, CRg2C(O), CONRi, NRiCO, OC(O), C(O)O, OC(S), C(S)NRg, NR8C(S), S(O2NRg, NRgS(O)2N=N, NRgNRg, NRgCRg2, NRgCRg2, CRg2O, OCRg2, CRg=CRg, C=C, Ar or Het; a is 0, 1 or 2; c is 0, 1 or 2; r is 0, 1 or 2; and u is 0 or 1; or pharmaceutically acceptable salts thereof, which are vitronectin receptor antagonists useful in the treatment of osteoporosis.