Trisubstituted phenyl derivatives and processes for their prepar

Details Trisubstituted phenyl derivatives and processes for their prepar Trisubstituted phenyl derivatives and processes for their prepar

1997-11-04

1999-02-02

Kight, John

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

514340, 514341, 514342, 514343, 514277, 5142278, 514255, 5142355, 514318, 546339, 546193, 544 586, 544360, 544124, A61K 3144, A61K 3142, C07D21324, C07D40106

Patent

active

058665935

ABSTRACT:
Compounds of the general formula (1) ##STR1## are described wherein Y is halogen or --OR.sup.1, where R.sup.1 is optionally substituted alkyl; X is --O--, --S-- or --N(R.sup.8)-, where R.sup.8 is hydrogen or alkyl; R.sup.2 is optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl; R.sup.3 is hydrogen, halogen or --OR.sup.9, where R.sup.9 is hydrogen or optionally substituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl, or formyl, carboxamido or thiocarboxamido; R.sup.4 is --(CH.sub.2).sub.n Ar, where Ar is monocyclic or bicyclic aryl optionally containing one or more heteroatoms selected from oxygen, sulfur and nitrogen atoms, wherein Ar is substituted by an optionally substituted C.sub.3-9 cycloaliphatic group optionally containing one or more heteroatoms selected from oxygen, sulphur or --N(R.sup.8)-, and n is zero or an integer 1, 2 or 3; R.sup.5 is --(CH.sub.2).sub.n Ar' where Ar' is monocyclic or bicyclic aryl optionally containing one or more heteroatoms selected from oxygen, sulfur or nitrogen atoms or is Ar; R.sup.6 is hydrogen or optionally substituted alkyl; and R.sup.7 is hydrogen or optionally substituted alkyl; or a salt, solvate or hydrate thereof. Compounds according to the invention are potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of diseases such as asthma where an unwanted inflammatory response or muscular spasm is present.

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