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

1999-04-06

Rotman, Alan L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

514277, 546332, 546334, 546337, 546339, A61K 3144, C07D21344, C07D21356, C07D21361

Patent

active

058918965

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.sup.1 ; R.sup.a is preferably optionally substituted alkyl; R.sup.1 is preferably optionally substituted indanyl; R.sup.3 is preferably hydrogen, fluorine, hydroxy or an optionally substituted straight or branched chain alkyl group; R.sup.4 and R.sup.5 are preferably independently --(CH.sub.2).sub.t Ar, where t is zero or an integer 1, 2 or 3 wherein Ar is preferably optionally substituted monocyclic or bicyclic aryl or optionally substituted monocyclic or bicyclic heteroaryl; and R.sup.6 and R.sup.7 are preferably independently hydrogen, fluorine or optionally substituted alkyl. 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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