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    CHEMICAL COMPOUNDS
    5.
    发明公开
    CHEMICAL COMPOUNDS 审中-公开
    化学化合物

    公开(公告)号：EP1940394A2

    公开(公告)日：2008-07-09

    申请号：EP06850059.4

    申请日：2006-10-20

    申请人： SMITHKLINE BEECHAM CORPORATION

    发明人： CALLAHAN, James, Francis ,  KERNS, Jeffrey, K. ,  LIN, Xichen

    IPC分类号： A61K31/416

    CPC分类号： C07D231/56 ,  C07D401/04 ,  C07D401/14

    摘要： The invention is directed to novel indazole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I) where R1 and R2 are as defined below. These compounds are useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKKβ) activity, in particular in the treatment and prevention of disorders mediated by IKK2 mechanisms including inflammatory and tissue repair disorders. Such disorders include rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease).

    摘要翻译： 本发明涉及新型吲唑甲酰胺衍生物。 具体而言，本发明涉及根据式（I）的化合物，其中R 1和R 2如下所定义。 这些化合物可用于治疗与不适当的IKK2（也称为IKKβ）活性相关的病症，特别是用于治疗和预防由IKK2机制介导的病症，包括炎症和组织修复病症。 这些疾病包括类风湿性关节炎，哮喘和COPD（慢性阻塞性肺病）。

    VITRONECTIN RECEPTOR ANTAGONISTS
    9.
    发明授权
    VITRONECTIN RECEPTOR ANTAGONISTS 失效
    连素受体拮抗剂

    公开(公告)号：EP0957917B1

    公开(公告)日：2005-12-07

    申请号：EP97909979.3

    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： C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  C07D471/04 ,  A61K31/44 ,  A61K31/47 ,  A61K31/52 ,  A61K31/55 ,  A61K31/415 ,  A61K31/445 ,  A61K31/495 ,  C07D223/16 ,  C07D233/56 ,  C07D233/64 ,  C07D235/18 ,  C07D235/22 ,  C07D243/14

    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).