Hepatitis B capsid assembly modulators

Patent metadata

Field	Value
Publication number	US-11566001-B2
Application number	US-202117514578-A
Country	US
Kind code	B2
Filing date	Oct 29, 2021
Priority date	Jun 11, 2018
Publication date	Jan 31, 2023
Grant date	Jan 31, 2023

Abstract

Described herein are hepatitis B capsid assembly modulators and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of hepatitis B.

First claim

What is claimed is:

1. A compound of Formula (Ia), or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof:

wherein:
Ring A is aryl;
each R 11 is independently halogen;
n is 2 or 3;
R 12 is hydrogen;

is

R 13 is hydrogen, halogen, or C 1 -C 6 alkyl;
R 16 is hydrogen or C 1 -C 6 alkyl;
R 17 is cycloalkyl optionally substituted with one, two, or three R 7 ;
each R 7 is independently C 1 -C 6 alkyl optionally substituted with one, two, or three R 7a ;
each R 7a is independently halogen, —CN, —OH, —OR a , —NR b R c , —C(═O)R a , —C(═O)OR b , or —C(═O)NR b R c ;
each R a is independently C 1 -C 6 alkyl or C 1 -C 6 haloalkyl; and
each R b and R c are independently hydrogen, C 1 -C 6 alkyl, or C 1 -C 6 haloalkyl.

2. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:
Ring A is phenyl; n is 2 or 3; and each R 11 is independently fluorine.

3. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

is

4. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

is

5. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:
R 13 is halogen.

6. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:
R 16 is hydrogen.

7. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:
R 17 is cyclohexyl optionally substituted with one, two, or three R 7 .

8. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:
each R 7 is independently C 1 -C 6 alkyl optionally substituted with one R 7a .

9. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:
each R 7a is independently —C(═O)OR b .

10. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, and a pharmaceutically acceptable excipient.

11. A method of treating hepatitis B in a subject, comprising administering to the subject a compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof.

Assignees

• Venatorx Pharmaceuticals Inc

Inventors

• Burns Christopher J
• Coburn Glen
• Liu Bin
• Yao Jiangchao
• Benetatos Christopher
• Boyd Steven A
• Condon Stephen M
• Haimowitz Thomas

Classifications

• C07D471/04

  Ortho-condensed systems · CPC title

• C07D409/14

  containing three or more hetero rings · CPC title

• C07D417/12

  linked by a chain containing hetero atoms as chain links · CPC title

• A61P31/20 Primary

  for DNA viruses · CPC title

• C07D401/12

  linked by a chain containing hetero atoms as chain links · CPC title