Prodrug esters of diflunisal and related compounds
AssigneeMerck & Co., Inc.
InventorConrad P. Dorn
Life of this patent
Estimating the term…
Abstract
1-(Alkoxy or aroxy)carbonyloxyalkyl esters of diflunisal and related compounds are stable in aqueous medium and non-irritant to mucous membranes of mouth, throat, and stomach. Accordingly, they are useful Prodrugs of the analgesic and anti-inflammatory drug, diflunisal.
Claims6
A compound of structural formula (I):
- ##STR11## wherein:
- R is
- (a) C.sub.1-6 alkyl;
- or
- (b) C.sub.3-6 cycloalkyl;
- R.sup.1 is
- (a) hydrogen;
- (b) C.sub.1-6 alkyl;
- or
- (c) C.sub.3-6 cycloalkyl;
- R.sup.2 is
- (a) hydrogen;
- (b) C.sub.1-6 alkanoyl;
- (c) C.sub.1-6 alkoxycarbonyl;
- R.sup.3 is
- (a) hydrogen;
- or
- (b) C.sub.1-6 alkyl;
- and
- X is halo.
A pharmaceutical composition for treating and/or controlling inflammation, pain or fever in a mammal comprising a pharmaceutical carrier and an effective amount of a compound of formula:
- ##STR14## wherein:
- R is
- (a) C.sub.1-6 alkyl;
- or
- (b) C.sub.3-6 cycloalkyl;
- R.sup.1 is
- (a) hydrogen;
- (b) C.sub.1-6 alkyl;
- or
- (c) C.sub.3-6 cylcoalkyl;
- R.sup.2 is
- (a) hydrogen;
- (b) C.sub.1-6 alkanoyl;
- (c) C.sub.1-6 alkoxycarbonyl;
- R.sup.3 is
- (a) hydrogen;
- or
- (b) C.sub.1-6 alkyl;
- and
- X is halo.
A method of treating and/or controlling inflammation, pain and fever comprising the administration of a mammal in need of such treatment an effective amount of a compound of formula:
- ##STR15## wherein:
- R is
- (a) C.sub.1-6 alkyl;
- or
- (b) C.sub.3-6 cycloalkyl;
- R.sup.1 is
- (a) hydrogen;
- (b) C.sub.1-6 alkyl;
- or
- (c) C.sub.3-6 cycloalkyl;
- R.sup.2 is
- (a) hydrogen;
- (b) C.sub.1-6 alkanoyl;
- (c) C.sub.1-6 alkoxycarbonyl;
- R.sup.3 is
- (a) hydrogen;
- or
- (b) C.sub.1-6 alkyl;
- and
- X is halo.
Dependencies are inferred from the claim text.