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Invention Application
WO2014047328A3 PKC DELTA INHIBITORS FOR USE AS THERAPEUTICS 审中-公开
PKC DELTA抑制剂用作治疗药物

PKC DELTA INHIBITORS FOR USE AS THERAPEUTICS
Abstract:
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 Figures 11 and 12.
Abstract(Chinese):

本发明涉及作为PKCδ特异性抑制剂的化合物，以及用于治疗和预防癌症和其它疾病的方法和组合物。 包含本发明化合物的组合物用于治疗癌症例如类癌和神经内分泌肿瘤，恶性黑素瘤，胰腺癌，胃肠癌和肺癌。 肺和胃肠道起源的神经内分泌肿瘤细胞系对本发明化合物对PKCδ抑制的惊人的敏感性。 本发明还涉及包含式（Ia），（Ib），（IIa），（IIb），（IIIa），（IIIb），（IVa），（IVb）和（IVb） V），如图11和12所示。

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