Purine derivatives as purinergic receptor antagonists

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C514S263230, C544S265000, C544S277000

Reexamination Certificate

active

07452894

ABSTRACT:
Use of a compound of formula (I) wherein R1is selected from alkyl, aryl, alkoxy, aryloxy, 0thioalkyl, thioaryl, CN, halo, NR5R6, NR4COR5, NR4CONR5R6, NR4CO2R7and NR4SO2R7; R2is selected from N, O or S-containing heteroaryl groups, wherein the heteroaryl group is attached via an unsaturated carbon atom which is adjacent to one or two N, O or S-heteroatom(s), other than ortho, ortho-disubstituted heteroaryl groups; R3is selected from H, alkyl, COR8, CONR9R10, CONR8NR9R10, CO2R11and SO2R11; R4, R5and R6are independently selected from H, alkyl and aryl or where R5and R6are in an (NR5R6) group then R5and R6may be linked to form a heterocyclic ring; R7is selected from alkyl and aryl; R8, R9and R10are independently selected from H, alkyl and aryl, or R9and R10may be linked to form a heterocyclic ring, or where R8, R9and R10are in a (CONR8NR9R10) group, R8and R9may be linked to form a heterocyclic group; and R11, is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, in the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly A2Areceptors, may be beneficial, particularly wherein said disorder is a movement disorder such as Parkinson's disease or said disorder is depression, cognitive or memory impairment, acute or chronic pain, ADHD or narcolepsy, or for neuroprotection in a subject; compounds of formula (I) for use in therapy; and novel compounds of formula (I) per se.

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