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6 条记录 (耗时 0.013 秒)

    SUBSTITUTED INDOLEPYRIDINIUM AS ANTI-INFECTIVE COMPOUNDS
    3.
    发明公开
    SUBSTITUTED INDOLEPYRIDINIUM AS ANTI-INFECTIVE COMPOUNDS 有权
    作为抗感染化合物的取代吲哚基铼

    公开(公告)号：EP1594870A1

    公开(公告)日：2005-11-16

    申请号：EP03811395.7

    申请日：2003-11-14

    申请人： Tibotec Pharmaceuticals Ltd.

    发明人： KESTELEYN, Bart, Rudolf, Romanie ,  VAN DE VREKEN, Wim ,  KINDERMANS, Natalie, Maria, Francisca ,  CANARD, Maxime, Francis, Jean-Marie, Ghislain ,  HERTOGS, Kurt ,  BETTENS, Eva ,  DE VROEY, Veronique, Corine, Paul ,  JOCHMANS, Dirk, Edward, Désiré ,  WIGERINCK, Piet Tom Bert Paul ,  TAHRI, Abdellah ,  WANG, Jing ,  SURLERAUX, Dominique Louis Nestor Ghislain

    IPC分类号： C07D471/00 ,  A61K31/437 ,  A61P31/12

    CPC分类号： C07D471/04

    摘要： The present invention concerns the compounds of formula (1) (R3)n P(I) N O R1 R2 their N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites, wherein n is 1, 2 or 3; R1 is H, CN, halo, aminoC(=O), C(=O)OH, C1-4-alkyloxyC(=O), C1-4alkylC(='O), mono- or di(C1-4alkyl)aminoC(=O), arylaminoC(=O), N-(aryl)-N-(C1-4alkyl)aminoC(=O), methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het1 or Het2; R2 is H, C1-10alkyl, C2-10allkenyl, C3-7cycloalkyl, wherein said C1-10alkyl,C2-10alkenyl and C3-7cycloalkyl may be optionally substituted; R3 is nitro, cyano, amino, halo, hydroxy,C1-4alkyloxy, hydroxyC(=O), aminoC(=O), C1-4alkyloxyC(=O), mono- or di(C1-4-alkyl)aminoC(=O), C1-4alkylC(=O), methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy methanimidamidyl or Het1; for use as a medicine. The invention further relates to a novel subgroup of the compounds of formula (I), and to compositions comprising compounds of formula (I).

    摘要翻译： 本发明涉及其N-氧化物，盐，立体异构体形式，外消旋混合物，前体药物，酯和代谢物的式（1）（R 3）n P（I）NR 1 R 2 R 2化合物，其中n是1,2或3; （= O），C（= O）OH，C 1-4烷氧基C（= O），C 1-4烷基C（= O），单或二（C 1-4烷基）氨基C （= O），芳基氨基C（= O），N-（芳基）-N-（C 1-4烷基）氨基C（= O），甲脒基，N-羟基甲脒基，单或二 或Het2; R2为H，C1-10烷基，C2-10链烯基，C3-7环烷基，其中所述C1-10烷基，C2-10链烯基和C3-7环烷基可以任选地被取代; R3是硝基，氰基，氨基，卤素，羟基，C1-4烷氧基，羟基C（= O），氨基C（= O），C1-4烷氧基C（= O），单 - 或二（C1-4-烷基） O），C 1-4烷基C（= O），甲脒基，单或二（C 1-4烷基）甲脒基，N-羟基甲脒基或Het 1; 用作药物。 本发明进一步涉及式（I）化合物的新亚组，并涉及包含式（I）化合物的组合物。

    SCREENING METHOD FOR COMPETITIVE HIV RT INHIBITORS
    5.
    发明公开
    SCREENING METHOD FOR COMPETITIVE HIV RT INHIBITORS 审中-公开
    筛选方法，竞争HIV逆转录酶抑制剂

    公开(公告)号：EP1853720A1

    公开(公告)日：2007-11-14

    申请号：EP06708055.6

    申请日：2006-02-06

    申请人： Tibotec Pharmaceuticals Ltd.

    发明人： JOCHMANS, Dirk, Edward, Désiré ,  WIGERINCK, Piet, Tom, Bert, Paul

    IPC分类号： C12Q1/48

    CPC分类号： C12Q1/48 ,  G01N2500/00

    摘要： A method for identifying a new class of nucleotide competitive RT inhibitors comprising: a) providing test compounds that are other than nucleoside triphosphates ; b) subjecting test compounds to a wild- type HIV virus replication test in cells; c) subjecting test compounds to a NNRTI resistant HIV virus replication test in cells; d) subjecting the test compounds to a kinetic reverse transcriptase enzymatic assay; and identifying the test compounds that are competitive towards the incorporated nucleotide in said assay; selecting the test compounds that are as well active in step b), are active in step c) and are identified as being competitive towards the incorporated nucleotide in step d).