Treatment of platelet derived growth factor related disorders such as cancers using inhibitors of platelet derived growth receptor
申请人:Sugen, Inc.
公开号:EP1000617A2
公开(公告)日:2000-05-17
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.
本发明涉及可抑制血小板衍生生长因子受体(PDGF-R)活性的化合物,最好此类化合物还能抑制 PDGF-R 超家族其他成员的活性,并对 PDGF-R 超家族成员具有选择性。PDGF-R 超家族包括 PDGF-R、PDGF-R 相关激酶 Flt 和 KDR。特色化合物对细胞培养物具有活性,可降低 PDGF-R,最好是一种或多种 PDGF-R 相关激酶的活性。下面将举例说明特色化合物 A10(见图 1A)及其抑制体内肿瘤细胞生长的能力。以本申请为指导,可以获得其他能够抑制 PDGF-R,最好是 Flt 和/或 KDR 的化合物。此类化合物最好用于治疗以不适当的 PDGF-R 活性为特征的细胞增殖性疾病患者。