Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-12-03
1999-01-12
Davis, Zinna Northington
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514247, 514255, 514256, 514396, 544224, 544242, 544336, 546330, 546332, 5483351, 5483355, 5483361, C07D21302, C07D23706, A61K 3144, A61K 31415
Patent
active
058590340
ABSTRACT:
Tri-substituted phenyl derivatives having the general formula (I): ##STR1## In a preferred embodiment, Y is preferably an --XR.sup.a group, X is preferably --O--, Z is preferably an --XR.sup.5 group, R.sup.a is preferably hydrogen or an optionally substituted alkyl group, R.sup.1 is preferably an --NHC(--NCN)NHR.sup.13 or --NHC(.dbd.CHNO.sub.2)NHR.sup.13 group, R.sup.2, R.sup.3 and R.sup.4 are preferably hydrogen, R.sup.5 is preferably an optionally substituted alkyl, alkenyl, cycloalkyl, cycloalkenyl or heterocycloalkyl group, R.sup.12 is preferably hydrogen or a C.sub.1-3 alkyl group, R.sup.13 is preferably hydrogen, a C.sub.1-3 alkyl group, an optionally substituted phenyl group or an optionally substituted phenylC.sub.1-3 alkyl group, Ar.sup.1 is preferably an optionally substituted nitrogen containing heteroaryl group, and Ar is preferably a phenyl group. Compounds of the invention are potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of various diseases, such as asthma, which are associated with an unwanted inflammatory response or muscular spasm.
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Brown Julien Alistair
Warrellow Graham John
Celltech Therapeutics Limited
Davis Zinna Northington
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