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US 2012/0070411 A1Published application
Substituted nucleotide analogs
AssigneeAlios BioPharma, Inc.
InventorsLeonid Beigelman, Lawrence Blatt, Guangyi Wang, Vivek Kumar Rajwanshi, Natalia Dyatkina, David Bernard Smith
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Abstract
Disclosed herein are phosphoroamidate nucleotide analogs, methods of synthesizing phosphoroamidate nucleotide analogs and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with the phosphoroamidate nucleotide analogs.
Claims53
A compound of Formula (I) or a pharmaceutically acceptable salt thereof:
- wherein:
- B1 is an optionally substituted heterocyclic base or an optionally substituted heterocyclic base with one or more protected amino groups;
- R1 is an optionally substituted N-linked amino acid or an optionally substituted N-linked amino acid ester derivative;
- R2 is selected from the group consisting of an optionally substituted aryl, an optionally substituted heteroaryl and an optionally substituted heterocyclyl;
- R3a and R3b are independently selected from the group consisting of hydrogen, an optionally substituted C1-6 alkyl, an optionally substituted C2-6 alkenyl, an optionally substituted C2-6 alkynyl, an optionally substituted C1-6 haloalkyl and aryl(C1-6 alkyl), provided that at least one of R3a and R3b is not hydrogen;
- or R3a and R3b are taken together to form a group selected from the group consisting of an optionally substituted C3-6 cycloalkyl, an optionally substituted C3-6 cycloalkenyl, an optionally substituted C3-6 aryl and an optionally substituted C3-6 heteroaryl;
- R4 is hydrogen;
- R5 is selected from the group consisting of hydrogen, —OR9 and —OC(═O)R10;
- R6 is selected from the group consisting of hydrogen, halogen, —OR11 and —OC(═O)R12;
- or R5 and R6 are both oxygen atoms and linked together by a carbonyl group;
- R7 is selected from the group consisting of hydrogen, halogen, an optionally substituted C1-6 alkyl, —OR13 and —OC(═O)R14;
- R8 is hydrogen or an optionally substituted C1-6 alkyl;
- R9, R11 and R13 are independently selected from the group consisting of hydrogen and an optionally substituted C1-6 alkyl;
- and
- R10, R12 and R14 are independently selected from the group consisting of an optionally substituted C1-6 alkyl and an optionally substituted C3-6 cycloalkyl;
- provided a compound of Formula (I) cannot have a structure selected from the group consisting of:
13 more elements
Dependencies are inferred from the claim text.