USE OF INHIBITORS FOR THE TREATMENT OF RTK-HYPERFUNCTION-INDUCED DISORDERS, PARTICULARLY CANCER
    8.
    发明申请
    USE OF INHIBITORS FOR THE TREATMENT OF RTK-HYPERFUNCTION-INDUCED DISORDERS, PARTICULARLY CANCER 有权
    使用抑制剂治疗RTK超敏感性疾病,特别是癌症

    公开(公告)号:US20100184686A1

    公开(公告)日:2010-07-22

    申请号:US12689672

    申请日:2010-01-19

    摘要: The present invention concerns the use of inhibitors for the treatment and/or prophylaxis of diseases which are the consequence of increased receptor tyrosine kinase activity, particularly cancer. The use is particularly directed towards inhibition or lowering of the overexpression and/or altered activity of receptor tyrosine kinases (RTKs). In particular, this altered activity of receptor tyrosine kinase can be triggered by a mutation of FGFR-4, wherein this mutation is in particular a point mutation in the transmembrane domain of FGFR-4 and leads to an exchange of a hydrophobic amino acid for a hydrophilic amino acid. The invention further concerns the use of an inhibitor directed against FGFR-4, for the treatment and/or prophylaxis of cancer. Furthermore, the invention concerns a mutated FGFR-4, which leads to over-expression and/or altered activity in cells. Finally, the invention concerns a DNA and RNA sequence of a mutated FGFR-4 molecule. Finally, in addition the invention concerns a pharmaceutical composition, containing the inhibitor as described above and further a diagnostic and screening procedure.

    摘要翻译: 本发明涉及抑制剂用于治疗和/或预防由于受体酪氨酸激酶活性增加,特别是癌症引起的疾病的用途。 该用途特别涉及抑制或降低受体酪氨酸激酶(RTK)的过表达和/或改变的活性。 特别地,受体酪氨酸激酶的这种改变的活性可以由FGFR-4的突变引发,其中该突变特别是FGFR-4的跨膜结构域中的点突变,并导致疏水性氨基酸的交换 亲水氨基酸。 本发明还涉及使用针对FGFR-4的抑制剂来治疗和/或预防癌症。 此外,本发明涉及突变的FGFR-4,其导致细胞中过度表达和/或改变的活性。 最后,本发明涉及突变的FGFR-4分子的DNA和RNA序列。 最后,本发明还涉及包含如上所述的抑制剂的药物组合物,并进一步进行诊断和筛选程序。

    Use of inhibitors for the treatment of RTK-hyperfunction-induced disorders, particularly cancer
    9.
    发明授权
    Use of inhibitors for the treatment of RTK-hyperfunction-induced disorders, particularly cancer 有权
    使用抑制剂治疗RTK-超功能障碍,特别是癌症

    公开(公告)号:US07297774B2

    公开(公告)日:2007-11-20

    申请号:US10863880

    申请日:2004-06-08

    IPC分类号: C07K14/00 C12N15/11 C12P21/06

    摘要: The present invention concerns the use of inhibitors for the treatment and/or prophylaxis of diseases which are the consequence of increased receptor tyrosine kinase activity, particularly cancer. The use is particularly directed towards inhibition or lowering of the overexpression and/or altered activity of receptor tyrosine kinases (RTKs). In particular, this altered activity of receptor tyrosine kinase can be triggered by a mutation of FGFR-4, wherein this mutation is in particular a point mutation in the transmembrane domain of FGFR-4 and leads to an exchange of a hydrophobic amino acid for a hydrophilic amino acid. The invention further concerns the use of an inhibitor directed against FGFR-4, for the treatment and/or prophylaxis of cancer. Furthermore, the invention concerns a mutated FGFR-4, which leads to overexpression and/or altered activity in cells. Finally, the invention concerns a DNA and RNA sequence of a mutated FGFR-4 molecule. Finally, in addition the invention concerns a pharmaceutical composition, containing the inhibitor as described above and further a diagnostic and screening procedure.

    摘要翻译: 本发明涉及抑制剂用于治疗和/或预防由于受体酪氨酸激酶活性增加,特别是癌症引起的疾病的用途。 该用途特别涉及抑制或降低受体酪氨酸激酶(RTK)的过表达和/或改变的活性。 特别地,受体酪氨酸激酶的这种改变的活性可以由FGFR-4的突变引发,其中该突变特别是FGFR-4的跨膜结构域中的点突变,并导致疏水性氨基酸的交换 亲水氨基酸。 本发明还涉及使用针对FGFR-4的抑制剂来治疗和/或预防癌症。 此外,本发明涉及突变的FGFR-4,其导致细胞中的过表达和/或改变的活性。 最后,本发明涉及突变的FGFR-4分子的DNA和RNA序列。 最后,本发明还涉及包含如上所述的抑制剂的药物组合物,并进一步进行诊断和筛选程序。