首页> 外国专利> 2-heteroaryl-5-substituted-1-,2, 4-triazolo 1,5a 1,3,5 triazine-7-amines and 7-heteroaryl-2-substituted-pyrazolo 1,5-a 1,3,5 triazine-4-amines their preparation and pharmaceutical compositions containing them

2-heteroaryl-5-substituted-1-,2, 4-triazolo 1,5a 1,3,5 triazine-7-amines and 7-heteroaryl-2-substituted-pyrazolo 1,5-a 1,3,5 triazine-4-amines their preparation and pharmaceutical compositions containing them

机译:2-杂芳基-5-取代的-1-,2,4-三唑[1,5a] [1,3,5]三嗪-7-胺和7-杂芳基-2-取代的吡唑并[1,5-a] [1,3,5]三嗪-4-胺及其制剂和含有它们的药物组合物

摘要

The invention concerns novel, pharmaceutically useful compounds of formula I in which Q is a 5-membered heteroaryl optionally bearing 1 or 2 substituents independently selected from (1-4C)alkyl and halogeno; R1 is hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl; R2 (when not as hereinbelow defined together with X) is hydrogen, (3-12C)cycloalkyl, (3-6C)alkenyl, phenyl(3-6C)alkenyl, tetrafluorophenyl, pentafluorophenyl, 5- or 6-membered heteroaryl, optionally substituted (1-6C)alkyl or optionally substituted phenyl; X is oxy, thio, sulphinyl, sulphonyl or an imino group of formula -NRa- in which Ra is hydrogen, (1-6C)alkyl or together with R2 and the adjacent nitrogen atom forms a 4 to 6-membered saturated heterocyclic ring; and A is N or CT in which T is hydrogen or (1-4C)alkyl; or a pharmaceutically acceptable salt thereof; processes for the manufacture of the compounds and pharmaceutical compositions containing them. The compounds are useful as adenosine antagonists. The invention further provides novel intermediates useful in the manufacture of the compounds of formula I. CHEM e
机译:本发明涉及式I的新的可药用化合物,其中Q是5元杂芳基,其任选地带有1或2个独立地选自(1-4C)烷基和卤代基的取代基; R 1为氢,(1-6C)烷基或(1-4C)烷酰基; R 2(当在下文中不与X一起定义时)是氢,(3-12C)环烷基,(3-6C)烯基,苯基(3-6C)烯基,四氟苯基,五氟苯基,5-或6-元杂芳基,任选取代的(1-6C)烷基或任选取代的苯基; X为氧基,硫代,亚磺酰基,磺酰基或式-NRa-的亚氨基,其中Ra为氢,(1-6C)烷基或与R2一起,且相邻的氮原子形成4至6元饱和杂环; A为N或CT,其中T为氢或(1-4C)烷基;或其药学上可接受的盐;化合物和包含它们的药物组合物的制备方法。该化合物可用作腺苷拮抗剂。本发明进一步提供了用于制备式I化合物的新型中间体。

著录项

  • 公开/公告号IL98316A

    专利类型

  • 公开/公告日1995-05-26

    原文格式PDF

  • 申请/专利权人 ZENECA LIMITED;

    申请/专利号IL19910098316

  • 发明设计人

    申请日1991-05-30

  • 分类号C07D484/04;A61K31/395;

  • 国家 IL

  • 入库时间 2022-08-22 04:19:09

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