Polymeric nucleoside prodrugs
AssigneeReliable Biopharmaceutical Corporation
InventorsUmaShanker Sampath, Joseph Toce, Sourena Nadji
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Abstract
Disclosed are polymeric compounds which are useful as prodrugs, comprising a chain of monomeric nucleosides, nucleoside analogs or abasic nucleosides, wherein at least one of the nucleosides or nucleoside analogs or a heterocyclic derivative thereof is pharmaceutically active and the nucleosides, nucleoside analogs or abasic nucleosides are linked by a phosphodiester group, a phosphorothioate group or an H—, alkyl or alkenyl phosphonate group.
Claims21
A heteropolymeric compound comprising a chain of monomeric nucleosides, nucleoside analogs, abasic nucleosides, or heterocyclic derivatives thereof, wherein each of said nucleosides, nucleoside analogs, abasic nucleosides, or heterocyclic derivatives thereof is pharmaceutically active and said nucleosides, nucleoside analogs, abasic nucleosides or heterocyclic derivatives thereof are linked by a phosphodiester group comprising a 3′ or 5′ terminal moiety, phosphorothioate group, or H—, alkyl or alkenyl phosphonate group.
A heteropolymeric compound of general formula (I)
- wherein R1 is optionally present and if present is independently selected from the group consisting of a pharmaceutically active nucleoside, nucleoside analog or heterocyclic derivative thereof;
- R2 is present in the β or α face and is independently selected from the group consisting of hydrogen, O—R5, R5, N—R5R6, N3, X, or S—R5;
- wherein R5 and R6 are independently selected from the group consisting of hydrogen, C1-C35 alkyl, C2-35 alkenyl, C3-35 cycloalkyl, C1-35 alkoxy, C1-35 alkylamino, C2-35 ether, C2-35 thioether, aryl, C6-35 non-aromatic heterocyclic, or a heteroaryl;
- X is Cl, Br, F, or I;
- R3 is independently selected from the group consisting of O or S;
- wherein when R3 is S, R4 is O− and when R3 is O, R4 is selected from the group consisting of C1-5 alkyl, C1-5 alkenyl and O−;
- wherein said alkyl, alkenyl, cycloalkyl, alkoxy, alkenyloxy, aryl, non-aromatic heterocyclic or heteroaryl are optionally substituted with one or more substituents selected from the group consisting of halogen, hydroxy, amino, acyloxy and carboxy.
- n is an integer from 1-100;
- or a pharmaceutically acceptable salt thereof.
21-31. (canceled)
Dependencies are inferred from the claim text.