Purine derivatives having phosphodiesterase IV inhibition activity

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United States of America Patent

PATENT NO 6319928
SERIAL NO

09418331

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Abstract

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A compound of the formula: ##STR1## wherein R.sub.2 is O or S; R.sub.3, R.sub.6a and R.sub.8 are the same or different and each represent a C.sub.1-8 alkyl which is unbranched or branched and unsubstituted or substituted with OH, alkoxy, CO.sub.2 H, .dbd.NOH, .dbd.NOCONH.sub.2, or .dbd.O; C.sub.3-8 cycloalkyl which is unsubstituted or substituted with OH, alkoxy, CO.sub.2 H, .dbd.NOH, .dbd.NOCONH.sub.2, or .dbd.O; C.sub.4-8 cycloalkylalkyl wherein the cycloalkyl portion is unsubstituted or substituted with OH, alkoxy, CO.sub.2 H, .dbd.NOH, .dbd.NOCONH.sub.2, or .dbd.O; aryl which is unsubstituted or substituted with Cl, NH.sub.2, alkylamino, dialkylamino, amido, C.sub.1 -C.sub.8 alkylamido, C.sub.1 -C.sub.3 dialkylamido, OH, alkoxy, HC.dbd.NOH, HC.dbd.NOCONH.sub.2, C.sub.1 -C.sub.3 alkyl, phenyl or benzyl; aralkyl (C.sub.1-4); heterocyclyl; heterocyclylalkyl (C.sub.1 -C.sub.4); and heteroaryl; R.sub.6b represents a H or R.sub.6a, or together R.sub.6b, N, and R.sub.6a make a 3 to 8 member ring containing at least one carbon, from one to three nitrogen atoms, from zero to two oxygen atoms, from zero to two sulfur atoms, said ring optionally substituted with alkoxy, CO.sub.2 H, CONH.sub.2, .dbd.NOH, .dbd.NOCONH.sub.2, .dbd.O; and where aryl is phenyl or naphthyl, the heterocyclyl is a 5, 6 or 7 membered ring including from one to three nitrogen atoms, and from zero to two oxygen atoms, from zero to two sulfur atoms, and can be substituted as in aryl on the carbons or nitrogens of that ring; or a pharmaceutically acceptable salt thereof, provided that when R.sub.3 is propyl, R.sub.8 is not cyclopentyl, noradamantyl, or dicyclopropylmethyl.

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Patent Owner(s)

Patent OwnerAddress
EURO-CELTIQUE S A2350 LUXEMBOURG

International Classification(s)

Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Cavalla, David J Cambridge, GB 22 161
Chasin, Mark Manalapan, NJ 116 12920
Gehrig, Andre Basel, CH 6 32
Hofer, Peter Liestal, CH 56 1088
Wintergerst, Peter Basel, CH 6 32

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