IP Library Granted Patent US 9,783,546
Granted Patent B2
US 9,783,546 · App. 15/327,685 · Granted Oct 10, 2017

Compounds

Inventors: Zehong Wan (Shanghai, CN); Xiaomin Zhang (Shanghai, CN); Jian Wang (Shanghai, CN)
Assignee: GlaxoSmithKline Intellectual Property Development Limited
C07D487/14
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Quick Facts
Patent No.
US 9,783,546
App. No.
15/327,685
Granted
Oct 10, 2017
Kind
B2
Abstract

The present invention relates to novel compounds that inhibit Lp-PLA 2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA 2 , for example atherosclerosis, Alzheimer's disease.

Claims (26)

1. A compound which is

or a salt thereof.

2. A compound which is

or a pharmaceutically acceptable salt thereof.

3. The compound according to claim 1 which is (R)-3-((3, 5-difluoro-4-((2-(trifluoromethyl) pyridin-4-yl) oxy) benzyl) oxy)-7, 8, 8a, 9-tetra hydropyrrolo[1′,2′:3 ,4]imidazo [1,2-c]pyrimidin-1(6H)-one

or a pharmaceutically acceptable salt thereof.

4. The compound according to claim 1 which is (R)-3-((3, 5-difluoro-4-((2-(trifluoromethyl) pyridin-4-yl) oxy) benzyl) oxy)-7, 8, 8a, 9-tetra hydropyrrolo[1′,2′:3,4]imidazo[1,2-c]pyrimidin-1(6H)-one

5. The compound according to claim 1 which is a pharmaceutically acceptable salt of (R)-3-((3, 5-difluoro-4-((2-(trifluoromethyl) pyridin-4-yl) oxy) benzyl) oxy)-7, 8, 8a, 9-tetra hydropyrrolo[1′,2′:3,4]imidazo[1,2-c]pynmidin-1(6H)-one

6. The compound according to claim 1 which is (S)-3-((3, 5-difluoro-4-((2-(trifluoromethyl) pyridin-4-yl) oxy) benzyl) oxy)-7, 8, 8a, 9-tetra hydropyrrolo[1′,2′:3 ,4]imidazo[1,2-c]pyrimidin-1(6H)-one

or a pharmaceutically acceptable salt thereof.

7. The compound according to claim 1 , which is (S)-3-((3, 5-difluoro-4-((2-(trifluoromethyl) pyridm-4-yl) oxy) benzyl) oxy)-7, 8, 8a, 9-tetra hydropyrrolo[1′,2′:3 ,4]imidazo[1,2-c]pyrimidin-1(6H)-one

8. The compound according to claim 1 , which is a pharmaceutically acceptable salt of (S)-3-((3, 5-difluoro-4-((2-(trifluoromethyl) pyridm-4-yl) oxy) benzyl) oxy)-7, 8, 8a, 9-tetra hydropyrrolo[1′,2′:3,4]imidazo[1,2-c]pyrimidin-1(6H)-one

9. A pharmaceutical composition comprising a compound having a structure of

or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.

10. The pharmaceutical composition according to claim 9 wherein the compound has the structure of

or a pharmaceutically acceptable salt thereof.

11. The pharmaceutical composition according to claim 9 wherein the compound has the structure of

or a pharmaceutically acceptable salt thereof.

12. A method for treating neurodegeneration disease in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a compound having a structure of

or a pharmaceutically acceptable salt thereof.

13. The method according to claim 12 , wherein the neurodegeneration disease is Alzheimer's disease.

14. The method according to claim 12 , wherein the compound has the structure of

or a pharmaceutically acceptable salt thereof.

15. The method according to claim 12 , wherein the compound has the structure of

or a pharmaceutically acceptable salt thereof.

16. The method according to claim 12 , wherein the subject is human.

Assignments (2)
CHANGE OF ADDRESS Recorded Oct 8, 2025
From: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
To: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
Reel/Frame 073032/0390 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 20, 2017
From: WAN, ZEHONG; WANG, JIAN; ZHANG, XIAOMIN
To: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
Reel/Frame 041024/0169 →
Priority Claims (1)
WO PCT/CN2014/000695 · Jul 22, 2014 · international
Continuity (1)
Related Publication 20170204108A1 · Jul 20, 2017