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    VITRONECTIN RECEPTOR ANTAGONISTS
    25.
    发明公开
    VITRONECTIN RECEPTOR ANTAGONISTS 失效
    连素受体拮抗剂

    公开(公告)号：EP0957917A1

    公开(公告)日：1999-11-24

    申请号：EP97909979.0

    申请日：1997-10-01

    申请人： SMITHKLINE BEECHAM CORPORATION

    发明人： CALLAHAN, James, Francis ,  COUSINS, Russell, Donovan ,  KEENAN, Richard, McCullock ,  KWON, Chet ,  MILLER, William, Henry ,  UZINKAS, Irene, Nijole

    IPC分类号： C07D223 ,  A61K31 ,  A61K33 ,  A61K45 ,  A61P9 ,  A61P19 ,  A61P29 ,  A61P35 ,  A61P43 ,  C07D233 ,  C07D235 ,  C07D243 ,  C07D401 ,  C07D403 ,  C07D413 ,  C07D417 ,  C07D487

    CPC分类号： C07D223/16 ,  A61K31/55 ,  A61K33/24 ,  A61K45/06 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  Y02P20/55 ,  Y02P20/582 ,  A61K31/47 ,  A61K2300/00

    摘要： Benzodiazepine compounds (I) of formula (I'; R = H), and their salts, are new: R1 = 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl, 3-4C oxoalkenyl, 3-4C oxoalkynyl, 1-4C aminoalkyl, 3-4C aminoalkenyl, 3-4C aminoalkynyl, (all optionally substituted by one A and one or more R10 or R7), H or R7; A = 3-6C cycloalkyl, Het or Ar; R7 = COR8, COC(R')2R9, C(S)R8, S(O)mOR', S(O)mNR'R'', PO(OR'), PO(OR')2, NO2 or tetrazolyl; R8 = OR', NR'R'', NR'SO2R', NR'OR' or OC(R')2COOR'; R9 = OR', CN, S(O)rR', S(O)mN(R')2, COR', CON(R')2 or COOR'; R10 = 1-6C alkyl, 1-6C oxoalkyl, 2-6C alkenyl, 2-6C alkynyl, 1-6C alkyloxy, 1-6C alkylamino, S(O)r-(1-6C alkyl) (all optionally substituted by A), H, OH, NH2, S(O)rH, OR11, CN, NR'R11, NO2, CF3, S(O)rCF3, COOR' or CON(R')2; R11 = R', COR', CON(R')2, COOR', S(O)mR' or S(O)mN(R')2; R2 = a group of formula (a)-(i); W = (CHRg)a-U-(CHRg)b; U = bond, CO, C(Rg)2, C(=CRg2), S(O)k, O, NRg, CRgORg, CRg(ORk)C(Rg)2, C(Rg)2CRg(ORk), COC(Rg)2, C(Rg)2C(O), CONRi, NRiCO, OC(O), C(O)O, C(S)O, OC(S), C(S)NRg, NRgC(S), S(O)2NRg, NRgS(O)2, N=N, NRgNRg, NRgC(Rg)2, C(Rg)2NRg, C(Rg)2O, OC(Rg)2, CC or CRg=CRg; G = NRe, S or O; Rg = H, 1-6C alkyl (optionally substituted by Het, 3-7C cycloalkyl or Ar) or Het, 3-7C cycloalkyl or Ar; Rk = Rg, CORg or COORf; Ri = Rg or 1-6C alkyl (substituted by 1-3 halo, CN, N(Rg)2, ORg, SRg, COORg or CON(Rg)2); Rf = H, Ar, or 1-6C alkyl (optionally substituted by Ar); Re = Rg or (CH2)kCOORg; Rb, Rc = H, A, 1-6C alkyl (optionally substituted by A), halo, CF3, ORf, S(O)kRf, CORf, NO2, N(Rf)2, CON(Rf)2 or CH2N(Rf)2; or Rb+Rc complete a 5-6 membered aromatic or non-aromatic carbocyclic or heterocyclic ring (optionally mono- to tri- substituted by halo, CF3, 1-4C alkyl, ORf, S(O)kRf, CORf, COORf, OH, NO2, N(Rf)2, CON(Rf)2, CH2N(Rf)2 or methylenedioxy; Q = C-Ry, and one Q may also be N; R' = H, Ar, 3-6C cycloalkyl or 1-6C alkyl (optionally substituted by Ar or (3-6C cycloalkyl); R'' = R', COR' or COOR'; Ry = H, halo, ORg, SRg, CN, NRgRk, NO2, CF3, S(O)rCF3, COORg, CORg, CON(Rg)2 or 1-6C alkyl (optionally substituted by halo, ORg, SRg, CN, NRgR'', NO2, CF3, S(O)rR', COORg, CORg or CON(Rg)2); a, b, k, r, s = 0-2; m = 1 or 2; u, v = 0 or 1. Also defined is a variable R''' = H, A, 1-6C alkyl (optionally substituted by A), halo, CF3, ORf, S(O)kRf, CORf, NO2, N(Rf)2, CON(Rf)2 or CH2N(Rf)2 which is not shown in the formula. Also claimed is a composition comprising (I), a carrier, and optionally an antineoplastic agent or inhibitor of bone resorption. Intermediates (II) of formula (I'; R = 1-6C alkyl).