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    • 10. 发明授权
    • Composition for treatment of tuberculosis
    • 用于治疗结核病的组合物
    • US09050295B2
    • 2015-06-09
    • US12808801
    • 2008-11-25
    • Martin FusseneggerWilfried WeberRonald Schoenmakers
    • Martin FusseneggerWilfried WeberRonald Schoenmakers
    • A61K31/17A61K31/4409A61K45/06
    • A61K31/17A61K31/4409A61K45/06A61K2300/00
    • The invention relates to a pharmaceutical composition comprising a compound preventing EthR from binding to the ethA promoter, for example a compound of formula 1 wherein R1 is optionally substituted phenyl or optionally substituted pyridyl; R2 (CH2)n wherein n is 1, 2, 3 or 4; R3 is CH3(CH2)m wherein m is 0, 1, 2 or 3; X1 is O, S, NH, N(CH3) or CH2; and X2 is O, S or NH; in particular 2-phenylethyl butyrate, and a thioamide or thiourea of formula 2 wherein R4 is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR7R8; or —NH—N═CH—R9; and substituents R5 to R9 have the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis.
    • 本发明涉及包含防止EthR与ethA启动子结合的化合物的药物组合物,例如式1的化合物,其中R 1是任选取代的苯基或任选取代的吡啶基; R2(CH2)n,其中n为1,2,3或4; R3是CH3(CH2)m,其中m是0,1,2或3; X 1是O,S,NH,N(CH 3)或CH 2; X2是O,S或NH; 特别是丁酸2-苯基乙酯和式2的硫代酰胺或硫脲,其中R 4是任选取代的苯基,任选取代的吡啶基,任选取代的吲哚基,-NR 7 R 8; 或-NH-N = CH-R 9; 并且取代基R 5至R 9具有在说明书中指出的含义,特别是乙二胺。 药物组合物可用于例如治疗多重耐药性结核病。