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    • 41. 发明授权
    • Heterocyclic topoisomerase poisons
    • 杂环拓扑异构酶毒药
    • US06667302B2
    • 2003-12-23
    • US09869141
    • 2001-06-13
    • Edmond J. La VoieJung Sun KimLeroy Fong Liu
    • Edmond J. La VoieJung Sun KimLeroy Fong Liu
    • C07D40310
    • C07D403/14A61K31/4184A61K31/4192A61K31/517C07D235/20
    • The invention provides compounds of formula I: wherein R1 to R5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds, compositions, or salts to treat cancer. In embodiments, R4 and R5 taken together can be a 3, 4, or 5 membered saturated or unsaturated chain comprising members selected from the group consisting of non-peroxide oxygen, sulfur, N(X), and carbon, optionally substituted by oxo; wherein each X is independently absent or is H, 0, (C1-C4)alkyl, phenyl or benzyl; and wherein at least one of the chain members is an N—H group.
    • 本发明提供了式I化合物:其中R1至R5具有说明书中定义的任何值,以及化合物的药学上可接受的盐,包含该化合物的药物组合物,以及使用该化合物,组合物或盐的方法 治疗癌症。 在实施方案中,R 4和R 5一起可以是3,4或5元饱和或不饱和链,其包含选自非过氧化物氧,硫,N(X)和任选被氧代取代的碳的成员; 其中每个X独立地不存在或为H,O,(C 1 -C 4)烷基,苯基或苄基; 并且其中至少一个链成员是N-H基团。