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Treatment of platelet derived growth factor related disorders such as cancers using inhibitors of platelet derived growth receptor

机译:使用血小板衍生生长受体抑制剂治疗与血小板衍生生长因子相关的疾病,例如癌症

摘要

The present invention concerns compounds which can inhibit platelet derived growth factor receptor (PDGF-R) activity, preferably such compounds also inhibit the activity of other members of the PDGF-R super family and are selective for members of the PDGF-R super family. The PDGF-R super family includes PDGF-R and PDGF-R related kinases Flt, and KDR. The featured compounds are active on cell cultures to reduce the activity of the PDGF-R and preferably one or more PDGF-R related kinases. An example of a featured compound, A10 (see Figure 1A), and its ability to inhibit growth of tumor cells in vivo is described below. Using the present application as guide, other compounds able to inhibit PDGF-R and preferably Flt and/or KDR can be obtained. Such compounds are preferably used to treat patients suffering from cell proliferative disorders characterized by inappropriate PDGF-R activity.
机译:本发明涉及可以抑制血小板衍生的生长因子受体(PDGF-R)活性的化合物,优选地,此类化合物还抑制PDGF-R超家族的其他成员的活性并且对PDGF-R超家族的成员具有选择性。 PDGF-R超级家族包括PDGF-R和与PDGF-R相关的激酶Flt和KDR。所述特征化合物在细胞培养物中具有活性,以降低PDGF-R以及优选一种或多种PDGF-R相关激酶的活性。特色化合物A10(参见图1A)及其在体内抑制肿瘤细胞生长的能力的例子如下所述。使用本申请作为指导,可以获得能够抑制PDGF-R并且优选地抑制Flt和/或KDR的其他化合物。此类化合物优选用于治疗患有以PDGF-R活性不合适为特征的细胞增殖性疾病的患者。

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