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

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United States of America Patent

PATENT NO 7384949
APP PUB NO 20040097524A1
SERIAL NO

10250938

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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.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.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.4 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 ##STR00001##

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Patent Owner(s)

Patent OwnerAddress
VERNALIS RESEARCH LIMITEDOAKDENE COURT 613 READING ROAD WINNERSH WOKINGHAM RG41 5UA

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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 Winnersh, GB 39 563
Lerpiniere, Joanne Winnersh, GB 14 131
Pratt, Robert Mark Winnersh, GB 11 28

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