申请人:FALLER Douglas V.
公开号:US20150283114A1
公开(公告)日:2015-10-08
The invention directed to compounds that are specific inhibitors of PKC delta, and methods and compositions for the treatment and prevent of cancers and other disorders. Compositions comprising compounds of the invention are used to treat cancers such as, for example, carcinoid and neuroendocrine tumors, malignant melanomas, pancreatic, gastrointestinal and lung cancers. Neuroendocrine tumor cell lines of pulmonary and gastrointestinal origin are surprisingly sensitive to PKC delta inhibition by the compounds of the invention. The invention is further directed to methods, compositions and kits containing compounds of the formulas (Ia), (Ib), (IIa), (IIb), (IIIa), (IIIb), (IVa), (IVb), and (V) as disclosed and described in FIGS.
11
and
12.
本发明涉及到特异性抑制PKC delta的化合物,以及用于治疗和预防癌症和其他疾病的方法和组合物。包含本发明化合物的组合物可用于治疗癌症,如类癌和神经内分泌肿瘤、恶性黑色素瘤、胰腺、胃肠和肺癌等。神经内分泌肿瘤细胞系源于肺和胃肠道对本发明化合物的PKC delta抑制作用具有惊人的敏感性。本发明还涉及到包含公式(Ia)、(Ib)、(IIa)、(IIb)、(IIIa)、(IIIb)、(IVa)、(IVb)和(V)的化合物的方法、组合物和试剂盒,如图11和12所述。