Pyrrolo [2,3-d] pyrimidine and their use as purinergic receptor antagonists

A method of treating a disorder in which blocking of adenosine A2A receptors is beneficial, wherein the disorder is selected from the group consisting of:

• acute and chronic pain;
• cerebral ischaemia;
• myocardial ischaemia;
• muscle ischaemia;
• retinal ischaemia-reperfusion injury;
• diabetic neuropathy;
• and depression;
• said method comprising administering to a subject in need of such treatment an effective dose of a compound of formula (I):
• wherein
• R1 is selected from the group consisting of alkyl, alkoxy, aryloxy, alkylthio, arylthio, aryl, halogen, CN, NR7R8, NR6COR7, NR6CONR7R8, NR6CO2R9, and NR6SO2R9;
• R2 is an aryl attached via an unsaturated ring carbon of said aryl group;
• R3 and R4 are independently selected from the group consisting of H, alkyl, halogen, alkoxy, alkylthio, CN, and NR7R8;
• R5 is selected from the group consisting of H, acyclic alkyl, COR6, CONR7R8, CONR6NR7R8, CO2R9, and SO2R9;
• R6, R7, and R8 are independently selected from the group consisting of H, alkyl, and aryl, or where R7 and R8 are in an NR7R8 group R7 and R8 may be linked to form a heterocyclic group, or where R6, R7, and R8 are in a (CONR6NR7R8) group, R6 and R7 may be linked to form a heterocyclic group;
• and
• R9 is selected from alkyl and aryl,
• or a pharmaceutically acceptable salt thereof.

A method of treatment of the symptoms and side effects of Parkinson's disease, comprising administering to a subject in need of such treatment an effective dose of a compound of formula (I):

• wherein
• R1 is selected from the group consisting of alkyl, alkoxy, aryloxy, alkylthio, arylthio, aryl, halogen, CN, NR7R8, NR6COR7, NR6CONR7R8, NR6CO2R9, and NR6SO2R9;
• R2 is an aryl attached via an unsaturated ring carbon of said aryl group;
• R3 and R4 are independently selected from the group consisting of H, alkyl, halogen, alkoxy, alkylthio, CN, and NR7R8;
• R5 is selected from the group consisting of H, acyclic alkyl, COR6, CONR7R8, CONR6NR7R8, CO2R9, and SO2R9;
• R6, R7, and R8 are independently selected from the group consisting of H, alkyl, and aryl, or where R7 and R8 are in an NR7R8 group R7 and R8 may be linked to form a heterocyclic group, or where R6, R7, and R8 are in a (CONR6NR7R8) group, R6 and R7 may be linked to form a heterocyclic group;
• and
• R9 is selected from alkyl and aryl,
• or a pharmaceutically acceptable salt thereof.