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US 11,447,512 B2Granted
Antiviral nucleoside reverse transcriptase inhibitor
AssigneeShenzhen TargetRx, Inc.
InventorsYihan Wang, Jiuyang Zhao
Life of this patent
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Abstract
An antiviral nucleoside reverse transcriptase inhibitor compound as shown in formula (I), and a pharmaceutically acceptable salt, a stereoisomer, a solvate, a hydrate, a crystal form or an isotopic derivative of the compound. A preparation method therefor, a pharmaceutical composition thereof, and a use thereof in the preparation of a drug for treating and/or preventing viral infectious diseases, such as human immunodeficiency virus (HIV) and hepatitis B virus (HBV).
Claims10
A compound of Formula (I),
- wherein,
- X is O;
- Y is S;
- m is selected from 0 to 5;
- A is selected from
- 1) optionally substituted C6-C11 aryl or optionally substituted C5-C11 heteroaryl;
- or
- 2) —(CH2)nCH3, wherein n is selected from 12 to 21;
- or
- 3) —C(═O)R1, —C(═O)OR1, —C(═O)N(R1)(R1), wherein each R1 is independently selected from H, optionally substituted C1-C6 alkyl, optionally substituted C1-C6 heteroalkyl, optionally substituted C3-C7 carbocyclyl, optionally substituted C3-C7 heterocyclyl, or two R1 groups together form optionally substituted C3-C7 carbocyclyl or optionally substituted C3-C7 heterocyclyl;
- V is selected from O or NH;
- B is H, or the following structure:
- wherein,
- R2 and R3 are each independently selected from H, optionally substituted C1-C6 alkyl or a side chain of a natural or a pharmaceutically acceptable amino acid, and if the side chain contains a carboxyl group, the carboxyl group may be optionally esterified to an alkyl or aryl ester or, R2 and R3, together with the carbon atom to which they are attached may form optionally substituted C3-C7 carbocyclyl or optionally substituted C3-C7 heterocyclyl;
- L is selected from —C(═O)—, —O(C═O)—, —NR4(C═O)—, —S(═O)p—, —NR4S(═O)p—, wherein each R4 is independently selected from H, optionally substituted C1-C6 acyl, optionally substituted C1-C6 alkyl, optionally substituted C3-C7 carbocyclyl, optionally substituted C3-C7 heterocyclyl, optionally substituted C6-C11 aryl or optionally substituted C5-C11 heteroaryl, p is selected from 1 or 2;
- Z is O;
- R5 is selected from optionally substituted C1-C6 alkyl, optionally substituted C1-C6 heteroalkyl, optionally substituted C1-C6 acyl, optionally substituted C2-C6 alkenyl, optionally substituted C2-C6 alkynyl, optionally substituted C3-C7 carbocyclyl, optionally substituted C3-C7 heterocyclyl, optionally substituted C6-C11 aryl, or optionally substituted C5-C11 heteroaryl, as valency permits;
- or a pharmaceutically acceptable salt, a stereoisomer, a solvate, a hydrate, a polymorph, or an isotopic variant thereof.
15 more elements
Dependencies are inferred from the claim text.