The present invention concerns compounds which can inhibit platelet derived growth factor receptor (PDGF-R) activity, preferably such compounds also inhibit the activity 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 FIG. 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.
本发明涉及一类可以抑制血小板源性生长因子受体(PDGF-R)活性的化合物,最好这些化合物还可以抑制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超家族包括PDGF-R和PDGF-R相关激酶Flt和KDR。这些特色化合物在
细胞培养中对降低PDGF-R活性以及最好是一个或多个PDGF-R相关激酶的活性方面是活跃的。下面描述了一个特色化合物A10(见图1a)及其在体内抑制肿瘤细胞生长的能力。通过本申请作为指南,可以获得其他能够抑制PDGF-R,最好是Flt和/或KDR的化合物。这些化合物最好用于治疗患有细胞增殖异常的患者,其特征是PDGF-R活性异常。