Substituted pyrrolo[1,2-c]pyrimidines as hepatitis B antiviral agents

Patent metadata

Field	Value
Publication number	US-11472808-B2
Application number	US-202016892464-A
Country	US
Kind code	B2
Filing date	Jun 4, 2020
Priority date	Jun 4, 2019
Publication date	Oct 18, 2022
Grant date	Oct 18, 2022

Abstract

The present invention discloses substituted pyrrolo[1,2-c]pyrimidines, such as the compoundwhich inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

First claim

What is claimed:

1. A compound selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or excipient in combination with a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

3. A method for treating a hepatitis B virus infection in a subject in need thereof, wherein the method comprises administering to the subject a therapeutically effective amount of at least one compound according to claim 1 , or a pharmaceutically acceptable salt thereof.

4. The method according to claim 3 , wherein the method further comprises administering to the subject at least one additional therapeutic agent selected from the group consisting of a hepatitis B virus polymerase inhibitor, an inducer of cellular viral ribonucleic acid sensor, interferon, a literature-described capsid assembly modulator, a reverse transcriptase inhibitor, a therapeutic vaccine, a toll-like receptor agonist, a viral entry inhibitor, and a viral maturation inhibitor.

5. The method of claim 4 , wherein the compound, or a pharmaceutically acceptable salt thereof, and the at least one additional therapeutic agent are co-administered.

6. The method of claim 4 , wherein the compound, or a pharmaceutically acceptable salt thereof, and the at least one additional therapeutic agent are co-formulated.

Assignees

• Enanta Pharm Inc

Inventors

• Qiu Yao-Ling
• Peng Xiaowen
• Li Wei
• Gao Xuri
• Kass Jorden
• Suh Byung-Chul
• Cao Hui
• Zhang Jiajun
• Or Yat Sun

Classifications

• C07D519/00 Primary

  Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00 · CPC title

• C07D487/04 Primary

  Ortho-condensed systems · CPC title

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title