Prostaglandin E synthase inhibitors and methods for utilizing the same

Patent metadata

Field	Value
Publication number	US-12030877-B2
Application number	US-202117538442-A
Country	US
Kind code	B2
Filing date	Nov 30, 2021
Priority date	Jun 28, 2016
Publication date	Jul 9, 2024
Grant date	Jul 9, 2024

Abstract

Compounds and compositions are provided that can inhibit microsomal prostaglandin E synthase-1 (mPGES-1). The compounds and compositions can reduce inflammation in a subject, such as inflammation caused by an inflammation disorder or symptoms thereof. Pharmaceutical compositions comprising the compound are also provided. Furthermore, methods are provided for reducing inflammation and/or inhibiting mPGES-1. The methods can comprise administering an effective amount of the composition to a subject.

First claim

What is claimed is:

1. A compound of the formula:

or pharmaceutically acceptable salts thereof,
wherein R 1 is selected from the group consisting of H, an alkyl, an alkyl halide, an ether, and a carboxylic acid;
wherein R 2 is selected from the group consisting of an alkyne and an aromatic; and
wherein R 3 is selected from the group consisting of H, a carboxyl, a carboxylic acid, and an alkyl.

2. The compound of claim 1 , wherein R 1 is selected from the group consisting of: H,

3. The compound of claim 1 , wherein R 2 is selected from the group consisting of:

4. The compound of claim 1 , wherein R 3 is selected from the group consisting of:
H,

5. A compound having the formula selected from the group consisting of:

6. A pharmaceutical composition, comprising:
a first compound of the formula

 or pharmaceutically acceptable salts thereof,
wherein R 1 is selected from the group consisting of H, an alkyl, an alkyl halide, an ether, and a carboxylic acid,
wherein R 2 is selected from the group consisting of H, a halide, an alkyne, and an aromatic, and
wherein R 3 is selected from the group consisting of H, a carboxyl, a carboxylic acid, and an alkyl;

a pharmaceutically-acceptable carrier; and
a second compound or composition having mPGES-1 inhibition activity, having anti-inflammatory activity, being useful for treatment of an inflammation disorder, being useful for treatment of symptoms associated with inflammation and/or an inflammation disorder, or combinations thereof.

7. The pharmaceutical composition of claim 6 , wherein R 1 of the first compound is selected from the group consisting of: H

8. The pharmaceutical composition of claim 6 , wherein R 2 of the first compound is selected from the group consisting of: H,

9. The pharmaceutical composition of claim 6 , wherein R 3 of the first compound is selected from the group consisting of: H,

10. The pharmaceutical composition of claim 6 , wherein the formula of the first compound is selected from the group consisting of:

Assignees

• Univ Kentucky Res Found

Inventors

• Zhan Chang-Guo
• Zheng Fang
• Ding Kai
• Zhou Ziyuan

Classifications

• C07D417/04

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

• C07D403/06

  linked by a carbon chain containing only aliphatic carbon atoms · CPC title

• C07D277/34 Primary

  Oxygen atoms · CPC title

• C07D251/20

  with no nitrogen atoms directly attached to a ring carbon atom · CPC title

• C07D231/12

  with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms · CPC title