申请人:JONES Lyn Howard
公开号:US20090215712A1
公开(公告)日:2009-08-27
This invention relates to pyrazole derivatives of formula (I)
or pharmaceutically acceptable salts, solvates or derivative thereofs, wherein R1 to R4 are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives.
The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodeficiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
本发明涉及式(I)的吡唆烷衍生物或其药学上可接受的盐、溶剂或衍生物,其中R1到R4在描述中定义,并涉及其制备方法、制备中使用的中间体、含有它们的组合物以及这些衍生物的用途。本发明化合物与酶反转录酶结合,并且是调节剂,特别是抑制剂。因此,本发明化合物在治疗多种疾病中有用,包括那些与反转录酶抑制有关的疾病。感兴趣的疾病包括由人类免疫缺陷病毒(HIV)和遗传相关的逆转录病毒引起的疾病,如获得性免疫缺陷综合症(AIDS)。