利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

13 条记录 (耗时 0.02 秒)

    1H-FURO[3,2-C] PYRAZOLE COMPOUNDS USEFUL AS KINASE INHIBITORS
    6.
    发明公开
    1H-FURO[3,2-C] PYRAZOLE COMPOUNDS USEFUL AS KINASE INHIBITORS 有权
    1H呋喃并[3,2-C]吡唑化合物，其适合用作激酶抑制剂的

    公开(公告)号：EP2051981A1

    公开(公告)日：2009-04-29

    申请号：EP07729539.2

    申请日：2007-05-25

    申请人： NERVIANO MEDICAL SCIENCES S.r.l.

    发明人： FANCELLI, Daniele ,  PULICI, Maurizio ,  MOLL, Jurgen ,  BANDIERA, Tiziano

    IPC分类号： C07D491/04 ,  A61K31/4162 ,  A61P35/00

    CPC分类号： C07D491/048

    摘要： Furo[3,2-c]pyrazole derivatives of formula (I) as defined in the description, and pharmaceutically acceptable salts thereof, wherein A is an aryl or heteroaryl ring, - NHZR5 is at the ortho position to the CONH linker; - R1 and R2 are the same or different and, independently from each other, represent a hydrogen atom, or an organic residue; R3 is a hydrogen or halogen atom or an organic group; R4 is a hydrogen or halogen atom or an organic group; Z is direct bond, >C=O, or -C(=O)NH-; - R5 is hydrogen or an optionally substituted organic group or isomers, tautomers, carriers, metabolites, prodrugs, and pharmaceutically acceptable salts thereof. A process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, in particular Aurora kinases activity or IGF-1R activity, like cancer.

    1H-THIENO[2,3-C]-PYRAZOLE COMPOUNDS USEFUL AS KINASE INHIBITORS
    7.
    发明公开
    1H-THIENO[2,3-C]-PYRAZOLE COMPOUNDS USEFUL AS KINASE INHIBITORS 有权
    -1H-噻吩并[2,3-C] -PYRAZOLVERBINDUNGEN适用作为激酶抑制剂的

    公开(公告)号：EP1904503A1

    公开(公告)日：2008-04-02

    申请号：EP06764123.3

    申请日：2006-07-10

    申请人： NERVIANO MEDICAL SCIENCES S.r.l.

    发明人： MOLL, Juergen ,  FANCELLI, Daniele ,  BANDIERA, Tiziano ,  QUARTIERI, Francesca ,  PULICI, Maurizio

    IPC分类号： C07D495/04 ,  A61K31/4162 ,  A61P35/00

    CPC分类号： C07D495/04

    摘要： There are provided thieno[2,3-c]pyrazole derivatives of formula (I), wherein A is an aryl or heteroaryl ring, on which the substituent -NHZR5 is at the ortho position to the CONH linker; R1 and R2 are the same or different and, independently from each other, represent a hydrogen atom or an organic group; R4 is a hydrogen or halogen atom or an organic group; Z is direct bond, >C=O, or -C(=O)NH-; R5 is hydrogen or an organic group; or isomers, tautomers, carriers, metabolites, prodrugs, and pharmaceutically acceptable salts thereof. A process for their preparation and pharmaceutical compositions comprising them are also disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

    USE OF A KINASE INHIBITOR FOR THE TREATMENT OF PARTICULAR RESISTANT TUMORS
    8.
    发明公开
    USE OF A KINASE INHIBITOR FOR THE TREATMENT OF PARTICULAR RESISTANT TUMORS 审中-公开
    应用激酶抑制剂治疗特定的抗性肿瘤

    公开(公告)号：EP2004180A2

    公开(公告)日：2008-12-24

    申请号：EP07727513.9

    申请日：2007-03-29

    申请人： Nerviano Medical Sciences S.r.l.

    发明人： FANCELLI, Daniele ,  ISACCHI, Antonella ,  MODUGNO, Michele ,  MOLL, Jurgen ,  RUSCONI, Luisa ,  SONCINI, Chiara ,  LUPI, Rosita

    IPC分类号： A61K31/4162 ,  A61P35/02

    CPC分类号： A61K31/4162 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377

    摘要： The invention provides low molecular weight compounds, namely tetrahydropyrrolo[3,4-c]pyrazoles, showing a high affinity for the ATP pocket of ABL tyrosine kinase. These compounds are thus ATP-competitive tyrosine kinase inhibitors displaying a significant inhibitory potency also, and in particular, towards BCR-ABL inhibitor-resistant T315I ABL mutants. The compounds of the invention find a useful application in the treatment of BCR-ABL inhibitor-resistant ABL-mediated diseases, such as Imatinib-resistant chronic myelogenous leukemia. Moreover, the invention provides a screening method for the identification of compounds capable of binding the ATP pocket of a kinase protein, in particular of the T315I mutant ABL kinase.

    摘要翻译： 本发明提供低分子量化合物，即四氢吡咯并[3,4-c]吡唑，其显示出对ABL酪氨酸激酶的ATP袋的高亲和力。 因此，这些化合物也是ATP竞争性酪氨酸激酶抑制剂，并且特别是对BCR-ABL抑制剂抗性T315I ABL突变体显示出显着的抑制效力。 本发明的化合物可用于治疗抗BCR-ABL抑制剂的ABL介导的疾病，例如耐伊马替尼的慢性粒细胞性白血病。 此外，本发明提供了用于鉴定能够结合激酶蛋白质的ATP袋，特别是T315I突变体ABL激酶的化合物的筛选方法。