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    • 1. 发明申请
    • PROTEIN KINASE C INHIBITION AND NOVEL COMPOUND BALANOL
    • 蛋白激酶C抑制剂和新型化合物巴拉醇
    • WO1993003730A1
    • 1993-03-04
    • PCT/US1992007124
    • 1992-08-21
    • SPHINX PHARMACEUTICALS CORPORATIONHALLOCK, Yali, F.JANZEN, William, P.BALLAS, Lawrence, M.KULANTHIVEL, PalaniappanBOROS, Christie
    • SPHINX PHARMACEUTICALS CORPORATION
    • A61K31/55
    • C07D223/12
    • Balanol, which is derived from fungi of the genus Verticillium, especially the fungus Verticillium balanoides, is provided. Balanol, when substantially pure, is soluble in dimethyl sulfoxide, water, and methanol; insoluble in ethyl acetate and chloroform; gives a positive color reaction with polymolybdic acid, ninhydrin reagent, and ferric chloride; is negative with Dragendorff's reagent and Iodoplatinate spray; has an Rf value of approximately 0.58 with silica gel thin layer chromatography with n-butanol/acetic acid/water at a ratio of 4:1:1 respectively; and has a molecular weight of approximately 550. Compounds of the invention are useful for inhibiting protein kinase C and treating conditions related to, or affected by inhibition of protein kinase C, particularly cancer tumors, inflammatory disease, reperfusion injury, and cardiac dysfunctions related to reperfusion injury.
    • 提供了来源于轮枝孢属真菌的Balanol,特别是真菌(Verticillium balanoides)。 当基本上纯的时,巴拉醇可溶于二甲基亚砜,水和甲醇; 不溶于乙酸乙酯和氯仿; 与多钼酸,茚三酮试剂和氯化铁发生阳性显色反应; 对于Dragendorff的试剂和碘酸盐喷雾是阴性的; 分别使用正丁醇/乙酸/水分别为4:1:1的硅胶薄层色谱法,Rf值约为0.58。 并且具有约550的分子量。本发明的化合物可用于抑制蛋白激酶C并且治疗与蛋白激酶C的抑制有关或受其抑制,特别是癌症肿瘤,炎症性疾病,再灌注损伤和与下列疾病相关的心脏功能障碍 再灌注损伤。