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US 2019/0055273 A1Published application
Acyclic antivirals
AssigneeAlios BioPharma, Inc.
InventorsLeonid BEIGELMAN, Guangyi WANG, Minghong ZHONG
Life of this patent
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Abstract
Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HBV and/or HDV and/or HIV infection with one or more nucleotide analogs
Claims86
A compound of Formula (I), or a pharmaceutically acceptable salt thereof, having the structure:
- wherein:
- B1 is an optionally substituted C-linked bicyclic heteroaryl containing 9 atoms in the rings and 3, 4 or 5 nitrogens or an optionally substituted C-linked bicyclic heterocyclyl containing 9 atoms in the rings and 3, 4 or 5 nitrogens;
- R1 and R2 are each independently selected from the group consisting of O−, —OH, an optionally substituted —O—C1-24 alkyl, an optionally substituted —O—C2-24 alkenyl, an optionally substituted —O—C2-24 alkynyl, an optionally substituted —O—C3-6 cycloalkyl, an optionally substituted —O—C3-6 cycloalkenyl, an optionally substituted —O-aryl, an optionally substituted —O-heteroaryl, an optionally substituted —O-aryl(C1-6 alkyl), an optionally substituted *—O—(CR4R5)p—O—C1-24 alkyl, an optionally substituted *—O—(CR6R7)q—O—C1-24 alkenyl,
- an optionally substituted N-linked amino acid and an optionally substituted N-linked amino acid ester derivative;
- or
- R1 is
- and R2 is O− or OH;
- or
- R1 and R2 are taken together to form a moiety selected from the group consisting of an optionally substituted
- and an optionally substituted
- wherein the phosphorus and the moiety form a six-membered to ten-membered ring system;
- R3a and R3b are each independently selected from the group consisting of hydrogen, halogen, an unsubstituted C1-4 alkyl, an unsubstituted C3-6 cycloalkyl, cyano, halogen(C1-4 alkyl), hydroxy(C1-4 alkyl), alkoxy(C1-4 alkyl), acyl(C1-4 alkyl) and cyano(C1-4 alkyl);
- or
- R3a and R3b are taken together with the carbon to which they are connected to form an optionally substituted C3-6 cycloalkyl;
- each R4, each R5, each R6 and each R7 are independently hydrogen, an optionally substituted C1-24 alkyl or alkoxy;
- R8, R9, R11 and R12 are each independently selected from the group consisting of hydrogen, an optionally substituted C1-24 alkyl and an optionally substituted aryl;
- R10 and R13 are each independently selected from the group consisting of hydrogen, an optionally substituted C1-24 alkyl, an optionally substituted aryl, an optionally substituted —O—C1-24 alkyl, an optionally substituted —O-aryl, an optionally substituted —O-heteroaryl and an optionally substituted —O-monocyclic heterocyclyl;
- R14 is selected from the group consisting of hydrogen, an optionally substituted C1-24 alkyl and an optionally substituted aryl;
- R15 and R16 are each independently selected from the group consisting of —C≡N, an optionally substituted C2-8 organylcarbonyl, an optionally substituted C2-8 alkoxycarbonyl and an optionally substituted C2-8 organylaminocarbonyl;
- R17 is selected from the group consisting of hydrogen, an optionally substituted C1-24-alkyl, an optionally substituted C2-24 alkenyl, an optionally substituted C2-24 alkynyl, an optionally substituted C3-6 cycloalkyl and an optionally substituted C3-6 cycloalkenyl;
- R19, R20 and R21 are each independently absent or hydrogen;
- m is 0 or 1;
- n is 1 or 2;
- p and q are each independently selected from the group consisting of 1, 2 and 3;
- r is 1 or 2;
- s is 0 or 1;
- Z1 is oxygen (O) or sulfur (S).
24 more elements
Dependencies are inferred from the claim text.