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    • 8. 发明申请
    • Method of Cancer Treatment with Naphthol Analogs
    • 萘酚类似物治疗癌症的方法
    • US20100152140A1
    • 2010-06-17
    • US12529252
    • 2008-01-18
    • Ja Seok KooWilliam BornmannDavid Maxwell
    • Ja Seok KooWilliam BornmannDavid Maxwell
    • A61K31/66
    • A61K31/661
    • In one embodiment, the present invention relates to a method of treating a cancer characterized by overexpression of cyclic adenosine monophosphate response element-binding protein (CREB) or phosphorylated CREB (p-CREB) by administering to a patient suffering from the cancer a pharmaceutically-effective amount of a composition comprising a compound selected from the group consisting of 2-{1-[3-(Amidinothio)propyl]-1H-indol-3-yl}-3-(1-methylindol-3-yl)maleimide, naphthol analogs having the structure (I), wherein R1 is selected from the group consisting of —H, —F, —Cl, —Br, and —I; R2 is selected from the group consisting of —H, —F, —Cl, —Br, —I, —C1-6 alkyl, —C1-6alkenyl, and —C1-6 alkynyl; R3 is selected from the group consisting of —H and —NO2; and R4 is selected from the group consisting of —H, —C1-6 alkyl, —C1-6 alkenyl, —C1-6 alkynyl, —OC1-6 alkyl, —OC1-6 alkenyl, and —OC1-6 alkynyl; and salts and esters thereof.
    • 在一个实施方案中,本发明涉及一种治疗癌症的方法,其特征在于通过向患有癌症的患者施用药学上可接受的方法来过表达环腺苷一磷酸应答元件结合蛋白(CREB)或磷酸化CREB(p-CREB) 有效量的包含选自2- {1- [3-(脒基硫代)丙基] -1H-吲哚-3-基} -3-(1-甲基吲哚-3-基)马来酰亚胺的化合物的组合物, 具有结构(I)的萘酚类似物,其中R 1选自-H,-F,-Cl,-Br和-I; R 2选自-H,-F,-Cl,-Br,-I,-C 1-6烷基,-C 1-6烯基和-C 1-6炔基; R3选自-H和-NO 2; 并且R 4选自-H,-C 1-6烷基,-C 1-6烯基,-C 1-6炔基,-OC 1-6烷基,-OC 1-6链烯基和-OC 1-6苯基; 及其盐和酯。