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

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United States of America Patent

SERIAL NO

12071577

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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A compound of formula (I), wherein X is S or O; R.sub.1 is selected from H, alkyl, aryl, hydroxy, alkoxy, aryloxy, thioalkyl, thioaryl, halogen, CN, COR.sub.5, CO.sub.2R.sub.5, CONR.sub.5R.sub.7, CONR.sub.5NR.sub.6R.sub.7, NR.sub.6R.sub.7, NR.sub.5CONR.sub.6R.sub.7, NR.sub.5COR.sub.6, NR.sub.5CO.sub.2R.sub.8, and NR.sub.5SO.sub.2R.sub.8; R.sub.2 is selected from aryl attached via an unsaturated carbon atom; R.sub.3 is selected from H, alkyl, hydroxy, alkoxy, halogen, CN and NO.sub.2; R.sub.3 is selected from H, alkyl, aryl, hydroxy, alkoxy, aryloxy, thioalkyl, thioaryl, halogen, CN, NO.sub.2, COR.sub.5, CO.sub.2R.sub.5, CONR.sub.6R.sub.7, CONR.sub.5NR.sub.6R.sub.7, NR.sub.6R.sub.7, NR.sub.5CONR.sub.6R.sub.7, NR.sub.5COR.sub.6, NR.sub.5CO.sub.2R.sub.8 and NR.sub.5SO.sub.2R.sub.8; R.sub.5, R.sub.6 and R.sub.7 are independently selected from H, alkyl and aryl or where R.sub.6 and R.sub.7 are in an (NR.sub.6R.sub.7) group, R.sub.6 and R.sub.7 may be linked to form a heterocyclic group, or where R.sub.5, R.sub.6 and R.sub.7 are in a (CONR.sub.5NR.sub.6R.sub.7) group, R.sub.5 and R.sub.6 may be linked to form a heterocyclic group; and R.sub.8 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 A.sub.2A 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.

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Patent Owner(s)

Patent OwnerAddress
VERNALIS RESEARCH LIMITEDNot Provided

International Classification(s)

Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Dawson, Claire Elizabeth Winnersh, GB 13 94
Gaur, Suneel Winnersh, GB 13 128
Gillespie, Roger John Oaksey, GB 39 563
Lerpiniere, Joanne Wokingham, GB 14 131
Pratt, Robert Mark Wokingham, GB 11 28

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