公开(公告)号：US07220772B2

公开(公告)日：2007-05-22

申请号：US10657033

申请日：2003-09-05

申请人： Paul John Edwards ,  Lyn Howard Jones ,  Charles Eric Mowbray ,  Paul Anthony Stupple ,  Isabelle Tran

发明人： Paul John Edwards ,  Lyn Howard Jones ,  Charles Eric Mowbray ,  Paul Anthony Stupple ,  Isabelle Tran

IPC分类号： A61K31/4152 ,  C07D231/18

CPC分类号： C07D231/18

摘要： This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereof, 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).

摘要翻译： 本发明涉及式（I）的吡唑衍生物或其药学上可接受的盐，溶剂合物或衍生物，其中R 1至R 4定义在说明书中， 用于制备它们，用于制备它们的中间体，含有它们的组合物和这些衍生物的用途。 本发明的化合物与酶逆转录酶结合，是调节剂，特别是其抑制剂。 因此，本发明的化合物可用于治疗各种病症，包括其中涉及逆转录酶的抑制的病症。 感兴趣的疾病包括由人类免疫缺陷病毒（HIV）引起的遗传相关逆转录病毒，如获得性免疫缺陷综合征（AIDS）。

公开(公告)号：US20050054707A1

公开(公告)日：2005-03-10

申请号：US10657033

申请日：2003-09-05

申请人： Paul Edwards ,  Lyn Jones ,  Charles Mowbray ,  Paul Stupple ,  Isabelle Tran

发明人： Paul Edwards ,  Lyn Jones ,  Charles Mowbray ,  Paul Stupple ,  Isabelle Tran

IPC分类号： A61K31/4152 ,  A61K31/416 ,  A61K31/4439 ,  C07D43/02

CPC分类号： C07D231/18

摘要： This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereof, 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 Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).

摘要翻译： 本发明涉及式（I）的吡唑衍生物或其药学上可接受的盐，溶剂合物或衍生物，其中R 1至R 4在说明书中定义，及其制备方法，其制备中使用的中间体 的含有它们的组合物和这种衍生物的用途。 本发明的化合物与酶逆转录酶结合，是调节剂，特别是其抑制剂。 因此，本发明的化合物可用于治疗各种病症，包括其中涉及逆转录酶的抑制的病症。 感兴趣的疾病包括由人免疫缺陷病毒（HIV）引起的遗传相关逆转录病毒，如获得性免疫缺陷综合征（AIDS）。