Purine derivatives

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United States of America Patent

PATENT NO 6525032
APP PUB NO 20010020089A1
SERIAL NO

09789236

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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The present invention relates to compounds of the class of purin-2-ylcarboxamides, useful as anti-inflammatory agents, having the formula: ##STR1## and pharmaceutically acceptable salts and solvates thereof; wherein R.sup.1 is H, C.sub.1 -C .sub.6 alkyl or C.sub.3 -C.sub.7 cycloalkyl, each optionally substituted by 1 or 2 of hydroxyl, fluorenyl, or optionally substituted phenyl or naphthyl ; A is a bond or C.sub.1 -C.sub.6 alkylene; R.sup.2 is (i) H, C.sub.1 -C.sub.6 alkyl, or optionally substituted C.sub.3 -C.sub.7 cycloalkyl, phenyl, or naphthyl; or (ii) when A is C.sub.2 -C.sub.6 alkylene, --NR.sup.3 R.sup.3, --OR.sup.3, --COOR.sup.3, --OCOR.sup.4, --SO.sub.2 R.sup.4, --CN, --SO.sub.2 NR.sup.3 R.sup.4, --NR.sup.3 SO.sub.2 R.sup.4, --NR.sup.3 COR.sup.4 or --CONR.sup.3 R.sup.3 ; or (iii) a C-linked, 4 to 11 membered, mono or bicyclic heterocycle having either from 1 to 4 ring nitrogen atom(s) or 1 or 2 nitrogen and 1 oxygen or 1 sulphur ring atoms, said heterocycle being optionally C-substituted or N-substituted; or (iv) when A is C.sub.2 -C.sub.6 alkylene, optionally substituted N-linked azetidinyl, pyrrolidinyl, morpholinyl, tetrahydroisoquinolinyl, piperidinyl or piperazinyl; R.sup.7 is H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, phenyl, naphthyl, azetidin-3-yl, pyrrolidin-3-yl, piperidin-3-yl, piperidin-4-yl, or het; and R.sup.8 is H or C.sub.1 -C.sub.6 alkyl; and to intermediates used in processes for the preparation of, compositions containing, and uses as adenosine A2a receptor agonists of, compounds of formula (I).

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Patent Owner(s)

Patent OwnerAddress
PFIZER INC66 HUDSON BOULEVARD EAST ATTN LEGAL PATENT DEPARTMENT CHIEF IP COUNSEL NEW YORK NY 10001-2192

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Mantell, Simon John County of Kent, GB 18 130
Monaghan, Sandra Marina County of Kent, GB 10 100
Stephenson, Peter Thomas County of Kent, GB 14 172

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