Hepatitis B antiviral agents

Patent metadata

Field	Value
Publication number	US-10952978-B2
Application number	US-201816114842-A
Country	US
Kind code	B2
Filing date	Aug 28, 2018
Priority date	Aug 28, 2017
Publication date	Mar 23, 2021
Grant date	Mar 23, 2021

Abstract

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:

X-A-Y-L-R  (I)

which 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 represented by Formula (XVII), or a pharmaceutically acceptable salt thereof:

wherein R 21 , R 21 ′ and R 21 ″ are independently selected from hydrogen, fluorine, methyl, difluoromethyl, and trifluoromethyl; R 39 is hydroxyl; and R 40 is —[C(R 41 )(R 42 )] q —R 43 , wherein q is 2; R 41 is hydrogen, and R 42 is hydroxyl; or R 41 and R 42 of one C(R 41 )(R 42 ) group together form an oxo group; and R 43 is methyl.

2. A pharmaceutical composition, comprising a compound according to claim 1 and a pharmaceutically acceptable carrier or excipient.

3. A compound selected from the compounds set forth below or a pharmaceutically acceptable salt thereof:

Compound
Structure

108

109

136

137

180

181

182

183

273

274

331

338

339

340

345

4. The compound of claim 3 having the structure

5. The compound of claim 3 having the structure

6. The compound of claim 3 having the structure

7. The compound of claim 3 having the structure

8. The compound of claim 3 having the structure

9. The compound of claim 3 having the structure

10. The compound of claim 3 having the structure

11. The compound of claim 3 having the structure

12. The compound of claim 3 having the structure

13. The compound of claim 3 having the structure

14. A pharmaceutical composition, comprising a compound accor

Assignees

• Enanta Pharm Inc

Inventors

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

Classifications

• C07C2602/50

  Spiro compounds · CPC title

• C07C2602/44

  the bicyclo ring system containing eight carbon atoms · CPC title

• C07C2601/16

  the ring being unsaturated · CPC title

• C07C2601/14

  The ring being saturated · CPC title

• C07C2601/10

  the ring being unsaturated · CPC title