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    N-substituted tricyclic 3-aminopyrazoles as anti-mitotic tubulin polymerization inhibitors
    7.
    发明授权
    N-substituted tricyclic 3-aminopyrazoles as anti-mitotic tubulin polymerization inhibitors 有权
    N-取代的三环3-氨基吡唑作为抗有丝分裂的微管蛋白聚合抑制剂

    公开(公告)号：US07816390B2

    公开(公告)日：2010-10-19

    申请号：US12021535

    申请日：2008-01-29

    申请人： Robert A. Galemmo ,  Dana L. Johnson ,  Umar S. M. Maharoof ,  Jay M. Mei ,  Robert W. Tuman

    发明人： Robert A. Galemmo ,  Dana L. Johnson ,  Umar S. M. Maharoof ,  Jay M. Mei ,  Robert W. Tuman

    IPC分类号： A61K31/416 ,  C07D231/54

    CPC分类号： C07D231/54 ,  C07D401/12

    摘要： The invention is directed to compounds having the following structures: N-(3-ethoxyphenyl)-1,4-dihydro-6-ethoxy-7-(3-hydroxypropoxy)-1-methylindeno[1,2-c]pyrazole-3-amine; 3-[3-(3-Bromo-phenylamino)-6-ethoxy-1-methyl-1,4-dihydro-indeno[1,2-c]pyrazol-7-yloxy]-propan-1-ol; or 3-[3-(2-Chloro-pyridin-4-ylamino)-6-ethoxy-1-methyl-1,4-dihydro-indeno[1,2-c]pyrazol-7-yloxy]-propan-1-ol, and N-oxides, pharmaceutically acceptable salts, solvates, tautomers and stereochemical isomers thereof and the uses of such compounds as inhibitors of tubulin polymerization and for the treatment of solid tumors. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.

    摘要翻译： 本发明涉及具有以下结构的化合物：N-（3-乙氧基苯基）-1,4-二氢-6-乙氧基-7-（3-羟基丙氧基）-1-甲基茚并[1,2-c]吡唑-3 -胺; 3- [3-（3-溴 - 苯基氨基）-6-乙氧基-1-甲基-1,4-二氢 - 茚并[1,2-c]吡唑-7-基氧基] - 丙-1-醇; 或3- [3-（2-氯 - 吡啶-4-基氨基）-6-乙氧基-1-甲基-1,4-二氢 - 茚并[1,2-c]吡唑-7-基氧基] - 丙-1 - 醇和N-氧化物，其药学上可接受的盐，溶剂合物，互变异构体和立体化学异构体，以及这些化合物作为微管蛋白聚合抑制剂和用于治疗实体瘤的用途。 本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。

    N-SUBSTITUTED TRICYCLIC 3-AMINOPYRAZOLES AS ANTI-MITOTIC TUBULIN POLYMERIZATION INHIBITORS
    8.
    发明申请
    N-SUBSTITUTED TRICYCLIC 3-AMINOPYRAZOLES AS ANTI-MITOTIC TUBULIN POLYMERIZATION INHIBITORS 有权
    N-取代的三茂胺3-氨基吡唑作为抗菌霉素聚合抑制剂

    公开(公告)号：US20080227821A1

    公开(公告)日：2008-09-18

    申请号：US12021535

    申请日：2008-01-29

    申请人： Robert A. Galemmo ,  Dana L. Johnson ,  Umar S.M. Maharoof ,  Jay M. Mei ,  Robert W. Tuman

    发明人： Robert A. Galemmo ,  Dana L. Johnson ,  Umar S.M. Maharoof ,  Jay M. Mei ,  Robert W. Tuman

    IPC分类号： A61K31/4439 ,  C07D231/54 ,  A61K31/416 ,  A61P35/00 ,  C07D401/12

    CPC分类号： C07D231/54 ,  C07D401/12

    摘要： The invention is directed to compounds having the following structures: N-(3-ethoxyphenyl)-1,4-dihydro-6-ethoxy-7-(3-hydroxypropoxy)-1-methylindeno[1,2-c]pyrazole-3-amine; 3-[3-(3-Bromo-phenylamino)-6-ethoxy-1-methyl-1,4-dihydro-indeno[1,2-c]pyrazol-7-yloxy]-propan-1-ol; or 3-[3-(2-Chloro-pyridin-4-ylamino)-6-ethoxy-1-methyl-1,4-dihydro-indeno[1,2-c]pyrazol-7-yloxy]-propan-1-ol, and N-oxides, pharmaceutically acceptable salts, solvates, tautomers and stereochemical isomers thereof and the uses of such compounds as inhibitors of tubulin polymerization and for the treatment of solid tumors. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.

    摘要翻译： 本发明涉及具有以下结构的化合物：N-（3-乙氧基苯基）-1,4-二氢-6-乙氧基-7-（3-羟基丙氧基）-1-甲基茚并[1,2-c]吡唑-3 -胺; 3- [3-（3-溴 - 苯基氨基）-6-乙氧基-1-甲基-1,4-二氢 - 茚并[1,2-c]吡唑-7-基氧基] - 丙-1-醇; 或3- [3-（2-氯 - 吡啶-4-基氨基）-6-乙氧基-1-甲基-1,4-二氢 - 茚并[1,2-c]吡唑-7-基氧基] - 丙-1 - 醇和N-氧化物，其药学上可接受的盐，溶剂合物，互变异构体和立体化学异构体，以及这些化合物作为微管蛋白聚合抑制剂和用于治疗实体瘤的用途。 本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。