Thieno(3,2-d)pyrimidines and furano(3,2-d)pyrimidines and their use as purinergic receptor antagonists

US7384949B2 · kind B2 · utility

Assignee

• Vernalis Research Limited · GB

Inventors

• Roger John Gillespie · Wokingham, GB
• Joanne Lerpiniere · Wokingham, GB
• Claire Elizabeth Dawson · Wokingham, GB
• Suneel Gaur · Wokingham, GB
• Robert Mark Pratt · Wokingham, GB

Key dates

• Filing date: Jan 10, 2002
• Grant date: Jun 10, 2008
• Expiry date: Nov 18, 2022

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D495/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

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…