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US 5,665,737 AGranted
Substituted benzoxazoles
AssigneeEuro-Celtique S.A.
InventorsJohn David Cavalla, Lloyd J. Dolby, Peter Hofer, Mark Chasin
Life of this patent
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Abstract
Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition as compared to theophylline or rolipram, with improved selectivity with regard to, e.g., PDE III inhibition.
Claims24
A compound of the formula:
- ##STR8## wherein:
- X is O or S;
- R.sub.1 is selected from the group consisting of hydrogen, halogen, hydroxy, nitro, QZ.sub.2, OQZ.sub.2, OCOQZ.sub.2, NHQZ.sub.2 and NCOQZ.sub.2 ;
- R.sub.2 is selected from the group consisting of halogen, hydroxy, nitro, QZ.sub.2, OQZ.sub.2, OCOQZ.sub.2, NHQZ.sub.2 and NCOQZ.sub.2 wherein:
- Q is a straight-chain or branched alkylene, alkenylene or alkynylene group having from 1 to 12 carbon atoms;
- Z.sub.2 is pyridyl optionally substituted with one to three groups selected from halogen atoms, C.sub.1 -C.sub.6 alkyl groups, OH, OQH, NO.sub.2, NH.sub.2, CO.sub.2 QH, CON(QH).sub.2, OCOQH, and OCON(QH).sub.2 ;
- wherein at least one of R.sub.1 or R.sub.2 has a substituent with Z.sub.2 ;
- R.sub.3 is a six membered carbocyclic aryl substituted with 1-3 members of the group consisting of OH, O--(C.sub.1 -C.sub.6) alkyl, O(CO)(C.sub.1 -C.sub.6) alkyl, O--(C.sub.3 -C.sub.10) cycloalkyl, R.sub.5 or R.sub.6 ;
- Z.sub.1 is a linkage selected from the group consisting of --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH(CH.sub.3)-- and --C(CH.sub.3).sub.2 --;
- R.sub.4 is hydrogen or a halogen;
- R.sub.5 is hydrogen or C.sub.1 -C.sub.12 alkyl;
- and
- R.sub.6 is C.sub.1 -C.sub.4 alkyl.
10 more elements
A compound according to clam 1, wherein R.sub.3 is a substituted phenyl.
Dependencies are inferred from the claim text.