Tri-substituted phenyl derivatives useful as PDE IV inhibitors

Details Tri-substituted phenyl derivatives useful as PDE IV inhibitors Tri-substituted phenyl derivatives useful as PDE IV inhibitors

1996-12-20

1998-08-25

Davis, Zinna Northington

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514277, 546334, 546339, 546336, C07D21302, A61K 3144

Patent

active

057983739

ABSTRACT:
Tri-substituted phenyl derivatives and pharmaceutical compositions containing them. In a preferred embodiment, the compounds have the general formula (2): ##STR1## wherein L is preferably --OR; R.sup.a is preferably an optionally substituted alkyl group; R is preferably an optionally substituted cycloalkyl group; R.sup.3 is preferably hydrogen; R.sup.4 is preferably hydrogen, --(CH.sub.2).sub.t --Ar or --(CH.sub.2).sub.t --Ar--(L.sup.1).sub.n --Ar'; R.sup.5 is preferably --(CH.sub.2).sub.t --Ar or --(CH.sub.2).sub.t ---Ar--(L.sup.1).sub.n --Ar'; R.sup.6 and R.sup.7 are preferably hydrogen, L.sup.1 is preferably a divalent linking group; Ar is preferably a monocyclic or bicyclic aryl or heteroaryl group; and Ar' is preferably Ar or an Ar containing 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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