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    • 37. 发明授权
    • Helquat derivatives, preparation thereof, and use thereof as medicaments
    • 葫芦巴衍生物,其制备及其用途作为药物
    • US09340543B2
    • 2016-05-17
    • US14655999
    • 2014-01-17
    • USTAV ORGANICKE CHEMIE A BIOCHEMIE AKADEMIE VED CR, V.V.I.
    • Filip TeplyMiroslav Hajek
    • C07D471/22C07D401/10C07D455/03A61K31/44A61P35/00
    • C07D471/22C07D401/10C07D455/03
    • The invention provides helquat derivatives of general formula I, wherein substituents R1 and R2 are independently selected from a group comprising H and C1 to C3 alkyl; up to three of S1,2, S1′,2′, S3,4 and S3′, 4′ are present, each of S1,2, S1′,2′, S3,4 and S3′,4′ independently represents a linker consisting of a bivalent hydrocarbon chain having 3-6 carbon atoms; one or two atoms selected from the carbon atoms with the descriptor 2, 4, 2′, and 4′ are substituted with a substituent R3 of general formula II or general formula III wherein R4 is substituted or unsubstituted aryl; T1 and T2 independently represent a bivalent hydrocarbon chain having 2-5 carbon atoms; and anions (X1)− and (X2)− independently represent anions of pharmaceutically acceptable salts.The helquat derivatives are useful as medicaments in the treatment of diseases related to increased cellular proliferation, such as oncologic diseases.
    • 本发明提供通式I的helquat衍生物,其中取代基R 1和R 2独立地选自H和C 1至C 3烷基; 存在S1,2,S1',2',S3,4和S3',4'中的三个,S1,2,S1',2',S3,4和S3',4'各自独立地表示 由具有3-6个碳原子的二价烃链组成的连接体; 一个或两个选自具有描述符2,4,2'和4'的碳原子的原子被通式II或通式III的取代基R3取代,其中R4是取代或未取代的芳基; T1和T2独立地表示具有2-5个碳原子的二价烃链; 而阴离子(X1) - 和(X2) - 独立地代表药学上可接受的盐的阴离子。 螺旋衍生物可用作治疗与增加的细胞增殖相关的疾病如药物疾病的药物。