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US 5,466,811 AGranted
Dioxolenylmethyl carbamates pro moieties for amine drugs
AssigneeMerck & Co., Inc.
InventorJose Alexander
Life of this patent
Estimating the term…
Abstract
This invention relates to a the use of new oxodioxolenylmethyl carbamates to produce bioreversible neutral prodrugs from primary and secondary amines.
Claims5
A prodrug moiety which comprises a derivatized 4-hydroxymethyl-2-oxo-1,3-dioxol-4-ene of Formula II:
- ##STR18## where R.sup.3 is hydrogen, straight or branched chain C.sub.1 to C.sub.6 alkyl, straight or branched chain C.sub.1 to C.sub.6 alkenyl, phenyl, substituted phenyl wherein the substitutents are fluoro, chloro, bromo, iodo, nitro, C1 to C6 carboxyalkyl, or C1 to C6 alkyloxy;
- R4 is hydrogen, straight or branchanged chain C.sub.1 to C.sub.6 alkyl, straight or branched chain C.sub.1 to C.sub.6 alkenyl, phenyl, substituted phenyl wherein the substitutents are fluoro, chloro, bromo, iodo, nitro, C1 to C6 carboxyalkyl, or C1 to C6 alkyloxy;
- R5 is hydrogen, straight or branchanged chain C.sub.1 to C.sub.6 alkyl, straight or branched chain C.sub.1 to C.sub.6 alkenyl, phenyl, substituted phenyl wherein the substitutents are fluoro, chloro, bromo, iodo, nitro, C1 to C6 carboxyalkyl, or C1 to C6 alkyloxy;
- and
- where Y is halo, p-nitro phenoxy, dinitrophenoxy, pentachlorophenoxy, or pentafluorophenoxy, pyridinium ion or 4-dimethyl amino pyridinium ion.
2 more elements
Dependencies are inferred from the claim text.