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US 2016/0354399 A1Published application
Substituted gemcitabine aryl amide analogs
AssigneeNucorion Pharmaceuticals, Inc.
InventorZucai Suo
Life of this patent
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Abstract
In accordance with the purpose(s) of the invention, as embodied and broadly described herein, the invention, in one aspect, relates to substituted gemcitabine aryl amide analogs, methods of making the same, pharmaceutical compositions comprising same, methods of treating viral disorders and disorders of uncontrolled cellular proliferation using same.
Claims31
-104. (canceled)
A composition comprising:
- a compound, or pharmaceutically acceptable salt, solvate, or polymorph thereof, having a structure of formula (I):
- wherein:
- R1a and R1e are independently selected from hydrogen, fluoro, chloro, bromo, iodo, methyl, methoxy, fluoromethyl, fluoromethoxy, difluoromethyl, difluoromethoxy, trifluoromethyl, trifluoromethoxy, ethyl, ethoxy, propyl, propoxy, butyl, butoxy, cyano, hydroxy, thiol, alkylthiol, optionally substituted benzyl, optionally substituted phenoxy, nitro, amino, monoalkylamino, and dialkylamino;
- R1b and R1d are independently selected from hydrogen, fluoro, chloro, bromo, iodo, methyl, methoxy, fluoromethyl, fluoromethoxy, difluoromethyl, difluoromethoxy, trifluoromethyl, trifluoromethoxy, ethyl, ethoxy, propyl, propoxy, butyl, butoxy, cyano, hydroxy, thiol, alkylthiol, optionally substituted phenyl, optionally substituted benzyl, optionally substituted phenoxy, nitro, amino, monoalkylamino, and dialkylamino;
- R1c is selected from hydrogen, fluoro, chloro, bromo, iodo, methyl, methoxy, fluoromethyl, fluoromethoxy, difluoromethyl, difluoromethoxy, trifluoromethyl, trifluoromethoxy, ethyl, ethoxy, propyl, propoxy, butyl, butoxy, cyano, hydroxy, thiol, alkylthiol, optionally substituted phenyl, optionally substituted benzyl, optionally substituted phenoxy, —C(O)R5, —C(O)OR5, —C(O)NHR5, —OC(O)R5, —NHC(O)R5, and —NHC(O)OR5;
- at least one of R1a, R1b, R1c, R1d, and R1e is not hydrogen;
- R5 is hydrogen, methyl, ethyl, propyl, butyl, pentyl, or hexyl;
- R2 is selected from hydrogen, C1-C4 alkyl, and amine protecting group;
- R3 is selected from hydrogen and hydroxyl protecting group;
- R4 is selected from hydrogen, C1-C8 alkyl, and hydroxyl protecting group;
- or R3 and R4 together comprise a divalent moiety having a structure represented by a formula:
- and
- each R6 is independently selected from methyl, ethyl, propyl, and butyl;
- and
- an additional therapeutic compound.
12 more elements
Dependencies are inferred from the claim text.