7-oxo-pyridopyrimidines (II)
    8.
    发明授权
    7-oxo-pyridopyrimidines (II) 失效
    7-氧代 - 吡啶并嘧啶(II)

    公开(公告)号:US06518276B2

    公开(公告)日:2003-02-11

    申请号:US09943338

    申请日:2001-08-30

    IPC分类号: A61K31519

    CPC分类号: C07D471/04 C07D239/47

    摘要: The present invention provides compounds of the formula: wherein R1, R3, and Ar1 are those defined herein, and R2 is —CR′R″—Ra (where R′ and R″ are hydrogen, hydroxyalkyl or alkyl with at least one being alkyl or hydroxyalkyl and Ra is hydroxyalkyl), Rx—S—Ry— (where Rx is alkyl and Ry is alkylene), alkoxy-substituted alkyl, heterocyclylalkyl or C4-C5 cycloalkyl, wherein each of the hydroxy group present in R2 can be independently Ra—C(═O)—O, RaRbN—C(═O)—O, or Ra—S(O)2—O—, wherein Ra and Rb are independently hydrogen, alkyl, aryl, or aralkyl, and methods for preparation and uses thereof.

    摘要翻译: 本发明提供下式的化合物:其中R1,R3和Ar1是本文定义的,R2是-CR'R'-Ra(其中R'和R“是氢,羟基烷基或具有至少一个 (其中R x是烷基,R y是亚烷基),烷氧基取代的烷基,杂环基烷基或C 4 -C 5环烷基,其中R 2中存在的每个羟基可以是 独立地是R a -C(= O)-O,R a R b N-C(= O)-O或R a -S(O)2-O-,其中R a和R b独立地是氢,烷基,芳基或芳烷基, 用于其制备和使用。

    Nonnucleoside reverse transcriptase inhibitors
    9.
    发明授权
    Nonnucleoside reverse transcriptase inhibitors 失效
    非核苷逆转录酶抑制剂

    公开(公告)号:US07241794B2

    公开(公告)日:2007-07-10

    申请号:US10781373

    申请日:2004-02-18

    IPC分类号: A61K31/415 C07D231/18

    摘要: This invention relates to novel pyrazole derivatives of formula I wherein R1 to R4 are as defined in the summary and pharmaceutically acceptable salts and solvates thereof, methods to inhibit or modulate Human Immunodeficiency Virus (HIV) reverse transcriptase with compounds of formula I and pharmaceutical compositions containing of formula I admixed with at least one solvent, carrier or excipient. The compounds are useful for treating disorders in which HIV and genetically related viruses are implicated

    摘要翻译: 本发明涉及式I的新型吡唑衍生物,其中R 1至R 4如概述中所定义及其药学上可接受的盐和溶剂合物,用式I化合物抑制或调节人类免疫缺陷病毒(HIV)逆转录酶的方法和含有 式I与至少一种溶剂,载体或赋形剂混合。 该化合物可用于治疗涉及HIV和遗传相关病毒的疾病