THIENO(3,2-D)PYRIMIDINES AND FURANO(3,2-D)PYRIMIDINES AND THEIR USE AS PURINERGIC RECEPTOR ANTAGONISTS

摘要

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, CO2R 5, 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 a nd 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, particular ly wherein said disorder is a movement disorder such a Parkinson's disease or said disorder is depression, cognitive or memory impairment, acute or chroni c pain, ADHD or narcolepsy, or wherein said medicament is for neuroprotection in a subject.