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    Amide compounds as boosters of antivirals
    2.
    发明授权
    Amide compounds as boosters of antivirals 有权
    酰胺化合物作为抗病毒药物的助剂

    公开(公告)号：US08664391B2

    公开(公告)日：2014-03-04

    申请号：US13122817

    申请日：2009-10-07

    申请人： Tim Hugo Maria Jonckers ,  Wim Bert Griet Schepens ,  Geerwin Yvonne Paul Haché ,  Beate Sabine Hallenberger ,  Jennifer Chiyomi Sasaki ,  Judith Eva Baumeister ,  Gerben Albert Van 'T Klooster

    发明人： Tim Hugo Maria Jonckers ,  Wim Bert Griet Schepens ,  Geerwin Yvonne Paul Haché ,  Beate Sabine Hallenberger ,  Jennifer Chiyomi Sasaki ,  Judith Eva Baumeister ,  Gerben Albert Van 'T Klooster

    IPC分类号： C07D241/36

    CPC分类号： C07D417/12 ,  C07D277/24

    摘要： The present invention relates to compounds of formula (I) that have CYP450 inhibiting properties and are useful as boosting agents when used with HIV treatments. These compounds are represented by formula including the salts and stereoisomeric forms thereof, wherein R1 is 5-thiazolyl or 3-pyridinyl; R2 is iso-butyl, 2,2-dimethylpropyl; 2-hydroxy-2-methyl-propyl or cyclohexylmethyl; R3 is phenyl optionally substituted with one or more halogens, trifluoromethyl, C1-6-alkyl or C1-6-alkoxy wherein optionally two of said alkoxy groups are be linked to each other to form a 5 or 6-membered ring; heteroaryl; C3-7cycloalkyl optionally substituted with one or more halogens; C1-6alkyl optionally substituted with heteroaryl; —O—CH2— (heteroaryl). As boosting agents they are able to increase at least one of the pharmacokinetic variables of certain drugs when co-administered, or improve the bioavailability of certain drugs. Methods for the preparation of the compounds of the invention and pharmaceutical compositions comprising these compounds are also provided.

    摘要翻译： 本发明涉及具有CYP450抑制性质的式（I）化合物，并且当与HIV治疗一起使用时可用作增效剂。 这些化合物由下式表示，包括其盐和立体异构形式，其中R 1是5-噻唑基或3-吡啶基; R2是异丁基，2,2-二甲基丙基; 2-羟基-2-甲基 - 丙基或环己基甲基; R3是任选被一个或多个卤素，三氟甲基，C 1-6 - 烷基或C 1-6 - 烷氧基取代的苯基，其中任选地两个所述烷氧基彼此连接形成5或6元环; 杂芳基; 任选被一个或多个卤素取代的C 3-7环烷基; 任选被杂芳基取代的C 1-6烷基; -O-CH 2 - （杂芳基）。 作为增效剂，当共同施用时，它们能够增加某些药物的药代动力学变量中的至少一种，或提高某些药物的生物利用度。 还提供了制备本发明化合物的方法和包含这些化合物的药物组合物。