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US 8,980,865 B2Granted
Substituted nucleotide analogs
AssigneeAlios BioPharma, Inc.
InventorsGuangyi Wang, Leonid Beigelman
Life of this patent
Estimating the term…
Abstract
Disclosed herein are phosphorothioate nucleotide analogs, such as thiophosphoroamidate prodrugs and thiophosphates (including α-thiomonophosphates, α-thiodiphosphates, and α-thiotriphosphates), methods of synthesizing phosphorothioate nucleotide analogs, such as thiophosphoramidate prodrugs, and thiophosphates and methods of treating viral infections, such as HCV, cancer, and/or parasitic diseases with the phosphorothioate nucleotide analogs, such as thiophosphoramidate prodrugs, and thiophosphates.
Claims24
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 a protected amino group;
- R1 is selected from the group consisting of O−, OH, an optionally substituted N-linked amino acid and an optionally substituted N-linked amino acid ester derivative;
- R2 is absent or selected from the group consisting of hydrogen, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted heterocyclyl and
- wherein R6, R7 and R8 are independently absent or hydrogen, and n is 0 or 1;
- provided that when R1 is O− or OH, then R2 is absent, hydrogen or
- R3 is selected from the group consisting of hydrogen, halogen, —OR9 and —OC(═O)R10;
- R4 is selected from the group consisting of halogen, —OR11 and —OC(═O)R12;
- or R3 and R4 are both oxygen atoms and linked together by a carbonyl group;
- R5 is selected from the group consisting of an optionally substituted C2-6 alkenyl, an optionally substituted C2-6 alkynyl and an optionally substituted C3-6 cycloalkyl;
- or R4 and R5 together form —(C1-6 alkyl)-O— or —O—(C1-6 alkyl)—;
- R9 and R11 are independently hydrogen or an optionally substituted C1-6 alkyl;
- and
- R10 and R12 are independently an optionally substituted C1-6 alkyl or an optionally substituted C3-6 cycloalkyl.
11 more elements
Dependencies are inferred from the claim text.