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US 2014/0213543 A1Published application
Nucleosides with antiviral and anticancer activity
AssigneeRegents of the University of Minnesota
InventorCarston R. Wagner
Life of this patent
Estimating the term…
Abstract
The invention provides a compound of formula (1), wherein R1-R6 and X have any of the values described, as well as pharmaceutical compositions comprising such compounds and therapeutic methods comprising the administration of such compounds.
Claims29
1-31. (canceled)
A compound of formula I:
- wherein:
- R1 is guanine, cytosine, thymine, 3-deazaadenine, or uracil, optionally substituted by 1, 2, or 3 U;
- wherein each U is independently halo, hydroxy, (C1-C6)alkyl, (C3-C6)cycloalkyl, (C1-C6)alkoxy, (C3-C6)cycloalkyloxy, (C1-C6)alkanoyl, (C1-C6)alkanoyloxy, trifluoromethyl, hydroxy(C1-C6)alkyl, —(CH2)1-4P(═O)(ORw)2, aryl, aryl(C1-C6)alkyl, or NRxRy;
- R2 is halo;
- R6 and R7 are independently H or (C1-C6)alkyl;
- R3 is hydroxy;
- R4 is hydrogen, (C1-C6)alkyl, (C3-C6)cycloalkyl, aryl, aryl(C1-C6)alkyl, or 2-cyanoethyl;
- R5 is an amino acid;
- X is oxy, thio, or methylene;
- each Rw is independently hydrogen or (C1-C6)alkyl;
- Rx and Ry are each independently hydrogen, (C1-C6)alkyl, (C3-C6)cycloalkyl, phenyl, benzyl, phenethyl, or (C1-C6)alkanoyl;
- or Rx and Ry together with the nitrogen to which they are attached are pyrrolidino, piperidino or morpholino;
- wherein any (C1-C6)alkyl of R1, R4-R7, Rw, Rx, and Ry is optionally substituted with one or more halo, hydroxy, (C1-C6)alkoxy, (C3-C6)cycloalkyloxy, (C1-C6)alkanoyl, (C1-C6)alkanoyloxy, trifluoromethyl, azido, cyano, oxo (═O), (C1-C6)alkyl, (C3-C6)cycloalkyl, (C3-C6)cycloalkyl(C1-C6)alkyl, (C1-C6)alkyl-S—(C1-C6)alkyl-, aryl, heteroaryl, alkyl(C1-C6)alkyl, or heteroary(C1-C6)alkyl, or NRajRak;
- wherein each Raj and Rak is independently hydrogen, (C1-C6)alkyl, (C3-C6)cycloalkyl, phenyl, benzyl, or phenethyl;
- and wherein any aryl or heteroaryl may optionally be substituted with one or more substituents selected from the group consisting of halo, hydroxy, (C1-C6)alkyl, (C3-C6)cycloalkyl, (C1-C6)alkoxy, (C3-C6)cycloalkyloxy, (C1-C6)alkanoyl, (C1-C6)alkanoyloxy, trifluoromethyl, trifluoromethoxy, nitro, cyano, and amino;
- or a pharmaceutically acceptable salt thereof.
13 more elements
Dependencies are inferred from the claim text.