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US 4,760,057 AGranted
(Acyloxyalkoxy)carbonyl derivatives as bioreversible prodrug moieties for primary and secondary amine functions in drugs
AssigneeMerck & Co., Inc.
InventorJose Alexander
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Abstract
This invention relates to novel (acyloxyalkoxy)carbonyl derivatives as bioreversible prodrug moieties for primary and secondary amine functions in drugs having a primary or secondary amine function thereon. Hydrolytic enzymes are used to trigger the regeneration of the parent amine drug of the carbamate prodrug moiety. The case also contains pharmaceutical composition, method of treatment and process claims.
Claims15
A compound of the formula:
- ##STR4## wherein RR'N represents an amino substituted primary or secondary amine pharmaceutical;
- R.sub.1 and R.sub.2 are selected from the group consisting of hydrogen, and substituted C.sub.1-6 alkyl or alkyl wherein the substituents are carboxy or C.sub.1-5 alkoxy carbonyl
- R.sub.3 is selected from the group consisting of
- C.sub.1-20 alkyl
- C.sub.2-20 alkenyl
- C.sub.2-5 alkynyl
- aryl
- C.sub.6-8 aralkyl
- C.sub.3-8 cycloalkyl
- C.sub.3-10 cycloalkenyl
- carboxy C.sub.2-20 alkyl
- carboxy C.sub.5-20 cycloalkyl
- halo (C.sub.2-20) alkyl.
10 more elements
Dependencies are inferred from the claim text.