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US 4,668,685 AGranted
Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans, which are analgesics or narcotic antagonists
AssigneeE.I. du Pont de Nemours and Company
InventorElie G. Shami
Life of this patent
Estimating the term…
Abstract
Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans are useful as analgesics or narcotic antagonists and provide enhanced bioavailability of 3-hydroxymorphinans from orally administered doses.
Claims30
A morphinan ester having the formula:
- ##STR34## or a pharmaceutically acceptable acid addition salt thereof, wherein:
- a is a single bond, or double bond;
- R is methyl, allyl, methylallyl, cyclopropylmethyl, or cyclobutylmethyl;
- R.sup.1 is H, or OH;
- R.sup.2 is H, OH, or =O;
- R.sup.3 and R.sup.4 are H, or taken together are --O- - -;
- R.sup.5 is t-butyl, or n-propyl;
- X at the 2-position is OR.sup.6, NHR.sup.6, or NR.sup.6 R.sup.7 ;
- Y at the 4-position is H or OR.sup.6 ;
- R.sup.6 is H, C.sub.1 -C.sub.4 alkyl, or COR.sup.8 ;
- R.sup.7 is C.sub.1 -C.sub.4 alkyl, or COR.sup.8 ;
- and
- R.sup.8 is H, or C.sub.1 -C.sub.4 alkyl.
10 more elements
Dependencies are inferred from the claim text.