Prodrugs
OwnerEdward A. Dennisinventor
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Abstract
The present invention provides prodrugs that serve as useful therapeutics for various disease states and conditions mediated by underlying specific hydrolytic enzyme activity. The prodrugs hereof (additionally) impart a physiologically bioactive component thus providing prodrug compounds that are capable of imparting dual effect systemically.
Claims25
A method of inactivating or inhibiting a phospholipase A enzyme, comprising administering to a subject susceptible to or experiencing a condition mediated by the activity of said enzyme an amount sufficient to inactivate or inhibit the activity of said enzyme of a pharmaceutically acceptable form of a compound of the formula:
- ##STR7## wherein R is oxygen or imino,
- each X independently is oxygen, sulfur or imino,
- A is a moiety recognized by a phospholipase A enzyme such that said enzyme hydrolyses the bond linking AX with C(0)Y,
- B. is a physiologically bioactive leaving group,
- Y is an alkylene or alkenylene or alkylene or alkenylene substituted with one or more lower alkyl groups.
A compound of the formula:
- ##STR8## wherein R is oxygen or imino,
- each X independently is oxygen, sulfur or imino,
- A is a moiety recognized by a phospholipase A enzyme such that said enzyme hydrolyses the bond linking AX with C(0)Y,
- B is a physiologically bioactive leaving group,
- Y is an alkylene or alkenylene or alkylene or alkenylene substituted with one or more lower alkyl groups.
Dependencies are inferred from the claim text.