Heterocyclic compounds for inhibiting phosphodiesterase IV

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United States of America Patent

PATENT NO 5889014
SERIAL NO

08716902

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds have the formula: ##STR1## wherein: R.sub.1 and R.sub.2 may be the same or different and each is selected from the group consisting of hydrogen, saturated or unsaturated straight-chain or branched C.sub.1-12 alkyl groups, cycloalkyl and cycloalkyl-alkyl groups containing from 3 to 10 carbon atoms in the cycloalkyl moiety; R.sub.3 is hydrogen, halogen, or a saturated or unsaturated straight-chain or branched C.sub.1-12 alkyl group, a cycloalkyl and cycloalkyl-alkyl groups containing from 3 to 7 carbon atoms in the cycloalkyl moiety; R.sub.4 is a phenyl or benzyl or a 6-membered heteroaryl which may be unsubstituted or substituted with one or more halogen atoms, alkyl groups, nitro groups, hydroxyl groups, cyano groups, carboxyl groups, alkoxy group, alkoxycarbonyl, amido, carboxamido, substituted or unsubstituted amino groups, cycloalkyl and cycloalkyl-alkyl groups containing from 3 to 10 carbon atoms in the cycloalkyl moiety, aryl or aralkyl groups preferably containing from about 6 to about 10 carbon atoms, or heterocyclic groups containing nitrogen, oxygen or sulfur in the ring; said alkyl, cycloalkyl, cycloalkyl-alkyl, aryl, and arylalkyl groups being unsubstituted or substituted by halogen atoms, hydroxyl groups, cyano groups, carboxyl groups, alkoxy groups, alkoxycarbonyl, carboxamido or substituted or unsubstituted amino groups, or one or more lower alkyl groups having from 1 to 3 carbon atoms; Z is selected from the group consisting of --CH.sub.2 CO--, --NHCH.sub.2 --, --CH.sub.2 NH--, --CH.sub.2 CONH--, --CH.sub.2 NHCO--, --CH.sub.2 COCH.sub.2 --, --COCH.sub.2 --, --C(.dbd.NOC(.dbd.O)NHQ)--, and --C(.dbd.NQ)NH--; X.sub.1 and X.sub.2 may be the same or different and each is O or S; wherein Q is R.sub.4 or hydrogen except that when Z.dbd.C(.dbd.NOCONHQ)--, R.sub.4 is not benzyl and R.sub.1 and R.sub.2 are both not hydrogen.

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Patent Owner(s)

Patent OwnerAddress
EURO-CELTIQUE S A2350 LUXEMBOURG

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Cavalla, David John Cambridge, GB2 6 62
Chasin, Mark Manalapan, NJ 116 12920
Dolby, Lloyd J Eugene, OR 18 99

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