[EN] 7-, 8-, and 10-SUBSTITUTED AMINO TRIAZOLO QUINAZOLINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITIONS AND THEIR USE<br/>[FR] DÉRIVÉS D'AMINO TRIAZOLO QUINAZOLINE À SUBSTITUTION EN POSITIONS 7, 8 ET 10 UTILISÉS EN TANT QU'ANTAGONISTES DU RÉCEPTEUR DE L'ADÉNOSINE, COMPOSITIONS PHARMACEUTIQUES ET LEUR UTILISATION
申请人:MERCK SHARP & DOHME
公开号:WO2020112706A1
公开(公告)日:2020-06-04
In its many embodiments, the present invention provides certain 7-, 8-, and 10-substituted amino triazolo quinazoline derivatives of Formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A, R1, R2, and R4 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutic agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and their use in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.
在其多种实施方式中,本发明提供了某些7-、8-和10-取代氨基三唑喹唑啉衍生物的化合物(I)的制备方法和用途,或其药学上可接受的盐,其中环A、R1、R2和R4如本文所定义,包括一种或多种这样的化合物的药物组合物(单独使用和与一种或多种其他治疗剂联合使用),以及其制备和用途的方法,单独使用和与其他治疗剂联合使用,作为A2a和/或A2b受体的拮抗剂,并且它们在治疗由腺苷A2a受体和/或腺苷A2b受体至少部分介导的各种疾病、症状或紊乱中的用途。