Substituted benzofuran, benzopyrrole, benzothiophene, and structurally related complement inhibitors

Patent metadata

Field	Value
Publication number	US-11021458-B2
Application number	US-201916511642-A
Country	US
Kind code	B2
Filing date	Jul 15, 2019
Priority date	Apr 6, 2018
Publication date	Jun 1, 2021
Grant date	Jun 1, 2021

Abstract

Disclosed are compounds of formulae I and II, and pharmaceutically acceptable salts and prodrugs thereof, which are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising such a compound, and methods of using the compounds and compositions in the treatment or prevention of a disease or condition characterized by aberrant complement system activity.

First claim

What is claimed is:

1. A compound, or a pharmaceutically acceptable salt thereof, selected from the group consisting of:

2. The compound of claim 1 , wherein the compound is in the form of a hydrochloride salt.

3. The compound of claim 1 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

4. The compound of claim 3 , wherein the compound is in the form of a hydrochloride salt.

5. The compound of claim 1 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

6. The compound of claim 5 , wherein the compound is in the form of a hydrochloride salt.

7. The compound of claim 1 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

8. The compound of claim 7 , wherein the compound is in the form of a hydrochloride salt.

9. A pharmaceutical composition, comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

10. A pharmaceutical composition, comprising the compound of claim 3 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

11. A pharmaceutical composition, comprising the compound of claim 5 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

12. A pharmaceutical composition, comprising the compound of claim 7 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

Assignees

• Biocryst Pharm Inc

Inventors

• Kotian Pravin L
• Babu Yarlagadda S
• Zhang Weihe
• Lu peng-cheng
• Wu Minwan
• Lv Wei
• Nguyen Trung Xuan
• Dang zhao
• Chintareddy Venkat R
• Kumar V Satish
• Raman Krishnan

Classifications

• C07D239/70 Primary

  condensed with carbocyclic rings or ring systems · CPC title

• A61K9/50

  Microcapsules {having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals (A61K9/2081 takes precedence; particles with a single coating comprising drug A61K9/167)} · CPC title

• C07D235/08

  Radicals containing only hydrogen and carbon atoms · CPC title

• C07D401/04

  directly linked by a ring-member-to-ring-member bond · CPC title

• C07D495/04

  Ortho-condensed systems · CPC title