USE OF AVERMECTIN DERIVATIVE FOR INCREASING BIOAVAILABILITY AND EFFICACY OF MACROCYLIC LACTONES
    4.
    发明公开
    USE OF AVERMECTIN DERIVATIVE FOR INCREASING BIOAVAILABILITY AND EFFICACY OF MACROCYLIC LACTONES 审中-公开
    USING A除虫菌素衍生物对增强大环内酯类生物利用度与效果

    公开(公告)号:EP2768513A2

    公开(公告)日:2014-08-27

    申请号:EP12783158.4

    申请日:2012-10-18

    摘要: The present invention relates to the use of avermectin derivative as a drug for the treatment of parasitic infections. The avermectin derivative is represented by the formula (I) wherein: (i) R1 is chosen from the group constituted of —CH(CH3)2, —CH(CH3)CH2CH3, or cyclohexyle, (ii) X represents —CH2CH2—, or —CH═CH—, (iii) R2 is chosen from the group constituted of or —OH group, (iv) R3 is OH or NOH, (v) represents a single bond when R3 is OH, or a double bond when R3 is NOH, as an inhibitor of a membrane-bound protein which transports exogenous compounds out of target cells.

    摘要翻译: 本发明涉及使用阿维菌素衍生物作为用于寄生虫感染的治疗的药物。 除虫菌素衍生物由式(I)表示:其中:(ⅰ)R 1是选自下组构成-CH(CH 3)2的,-CH(CH 3)CH 2 CH 3,或cyclohexyls,(ⅱ)X -CH 2 CH 2 darstellt, 或-CH = CH-,(ⅲ)R 2是选自下组的构成或-OH基团,(ⅳ)R 3为OH或NOH,(v)代表单键当R 3是OH,或双键时R3 是NOH,作为其输送外源性化合物出来的靶细胞的膜结合蛋白的抑制剂。