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US 5,399,790 AGranted
Non-steroid and non-prostanoid inhibitors of steroid and prostaglandin transforming enzymes
AssigneeThe Trustees of the University of Pennsylvania
InventorsTrevor M. Penning, Joseph W. Ricigliano
Life of this patent
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Abstract
Compounds such as 1-(4'-nitrophenyl)-2-propen-1-ol are disclosed which are non-steroidal mechanism-based inactivators of rat liver 3.alpha.-hydroxysteroid dehydrogenase. The corresponding ketones are time dependent inactivators of cyclooxygenase (PGH.sub.2 -synthase).
Claims9
A compound of the formula:
- ##STR16## where A is --C(O)-- or --CH(OH)--;
- R.sub.1 is selected from the groups consisting of CH.dbd.CH.sub.2, CH.dbd.CH--OMe, CH.dbd.CH--OEt, C.tbd.CH, C.tbd.C--OMe, and C.tbd.C--OEt;
- R.sub.2 is selected from the groups consisting of NO.sub.2, Z, CH.sub.2 Z, CHZ.sub.2, CZ.sub.3, COOH, NH.sub.2 and OH;
- R.sub.3 and R.sub.4 are independently selected from the groups consisting of H, NO.sub.2, Z, CH.sub.2 Z, CHZ.sub.2, CZ.sub.3, COOH, NH.sub.2 and OH;
- R.sub.5 is selected from the groups consisting of:
- ##STR17## and Z is a halogen atom, provided that, for compounds of formula (v), when R.sub.2 =NO.sub.2 and R.sub.3 and R.sub.4 =H, then A=--CH(OH)-- and R.sub.1 is other than C.tbd.CH.
3 more elements
Dependencies are inferred from the claim text.