[EN] THIENO(3,2-d)PYRIMIDINES AND FURANO(3,2-d)PYRIMIDINES AND THEIR USE AS PURINERGIC RECEPTOR ANTAGONISTS<br/>[FR] THIENO(3,2-D)PYRIMIDINES ET FURANO(3,2-D)PYRIMIDINES ET LEUR UTILISATION EN TANT QU'ANTAGONISTES DES RECEPTEURS PURINERGIQUES
申请人:VERNALIS RES LTD
公开号:WO2002055524A1
公开(公告)日:2002-07-18
A compound of formula (I), wherein X is S or O; R1 is selected from H, alkyl, aryl, hydroxy, alkoxy, aryloxy, thioalkyl, thioaryl, halogen, CN, COR5, CO2R5, CONR6R7, CONR5NR6R7, NR6R7, NR5CONR6R7, NR5COR6, NR5CO2R8, and NR5SO2R8; R2 is selected from aryl attached via an unsaturated carbon atom; R3 is selected from H, alkyl, hydroxy, alkoxy, halogen, CN and NO2; R4 is selected from H, alkyl, aryl, hydroxy, alkoxy, aryloxy, thioalkyl, thioaryl, halogen, CN, NO2, COR5, CO2R5, CONR6R7, CONR5NR6R7, NR6R7, NR5CONR6R7, NR5COR6, NR5CO2R8 and NR5SO2R8; R5, R6 and R7 are independently selected from H, alkyl and aryl or where R6 and R7 are in an (NR6R7) group, R6 and R7 may be linked to form a heterocyclic group, or where R5, R6 and R7 are in a (CONR5NR6R7) group, R5 and R6 may be linked to form a heterocyclic group; and R8 is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, and the use thereof in therapy and in the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly A2A receptors, may be beneficial, particularly wherein said disorder is a movement disorder such a Parkinson's disease or said disorder is depression, cognitive or memory impairment, acute or chronic pain, ADHD or narcolepsy, or wherein said medicament is for neuroprotection in a subject.
化合物的
化学式为(I),其中X为S或O; R1选自H,烷基,芳基,羟基,烷氧基,芳氧基,
硫代烷基,
硫代芳基,卤素,CN,COR5,CO2R5,CONR6R7,CONR5NR6R7,NR6R7,NR5CONR6R7,NR5COR6,NR5CO2R8和NR5SO2R8; R2选自通过不饱和碳原子连接的芳基; R3选自H,烷基,羟基,烷氧基,卤素,CN和
NO2; R4选自H,烷基,芳基,羟基,烷氧基,芳氧基,
硫代烷基,
硫代芳基,卤素,CN, ,COR5,CO2R5,CONR6R7,CONR5NR6R7,NR6R7,NR5CONR6R7,NR5COR6,NR5CO2R8和NR5SO2R8; R5,R6和R7独立地选自H,烷基和芳基,或者当R6和R7在(NR6R7)基团中时,R6和R7可以连接形成杂环基团,或者当R5,R6和R7在(CONR5NR6R7)基团中时,R5和R6可以连接形成杂环基团; R8选自烷基和芳基,或其药学上可接受的盐或前药,以及其在治疗中的应用和用于治疗或预防阻断
嘌呤受体,特别是
腺苷受体,尤其是A2A受体可能有益的紊乱,特别是该紊乱是帕
金森病等运动障碍,或该紊乱是抑郁症,认知或记忆障碍,急性或慢性疼痛,ADHD或嗜睡症,或该药物是用于受试者的神经保护。