IP Library › Granted Patent US 12,209,145
Granted Patent B2
US 12,209,145 · App. 17/854,379 · Granted Jan 28, 2025

PCSK9 antagonist compounds

Inventors: Harold B. Wood (Westfield, NJ); Hubert B. Josien (Jersey City, NJ); Thomas Joseph Tucker (North Wales, PA); Angela Dawn Kerekes (Plainfield, NJ); Ling Tong (Warren, NJ); Abbas M. Walji (Lansdale, PA); Anilkumar G. Nair (Rahway, NJ); Fa-Xiang Ding (Staten Island, NJ); Elisabetta Bianchi (Rome, IT); Danila Branca (Pomezia, IT); Chengwei Wu (Ambler, PA); Yusheng Xiong (Plainsboro, NJ); Sookhee Nicole Ha (Warren, NJ); Jian Liu (Edison, NJ); Sobhana Babu Boga (Karnataka, IN)
Assignee: MERCK SHARP & DOHME LLC
C07K7/64A61P3/06A61K38/00
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Quick Facts
Patent No.
US 12,209,145
App. No.
17/854,379
Granted
Jan 28, 2025
Kind
B2
Abstract

Disclosed are compounds of Formula I, or a salt thereof: where A, B, D, X, R 1 , R 2 and R 8 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions.

Claims (34)

1. A compound selected from the group consisting of:

or any other pharmaceutically acceptable salt form thereof.

2. A composition comprising at least one compound of claim 1 , or any other pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.

3. A method of treating hypercholesterolemia, comprising administering to a patient in need thereof a therapeutically effective amount of a composition of claim 2 .

4. A method of treating hypercholesterolemia, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of claim 1 , or any other pharmaceutically acceptable salt thereof.

5. A compound selected from the group consisting of:

wherein A − is a pharmaceutically acceptable anion.

6. A composition comprising at least one compound of claim 5 and at least one pharmaceutically acceptable excipient.

7. A method of treating hypercholesterolemia, comprising administering to a patient in need thereof a therapeutically effective amount of a composition of claim 6 .

8. A method of treating hypercholesterolemia, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of claim 5 .

9. A compound having the structure:

10. A composition comprising the compound of claim 9 , and at least one pharmaceutically acceptable excipient.

11. A method of treating hypercholesterolemia, comprising administering to a patient in need thereof a therapeutically effective amount of a composition of claim 10 .

12. A compound having the structure:

wherein A − is a pharmaceutically acceptable anion.

13. A composition comprising the compound of claim 12 , and at least one pharmaceutically acceptable excipient.

14. A method of treating hypercholesterolemia, comprising administering to a patient in need thereof a therapeutically effective amount of a composition of claim 13 .

15. A compound of claim 12 , wherein the compound is:

16. A composition comprising the compound of claim 15 , and at least one pharmaceutically acceptable excipient.

17. A method of treating hypercholesterolemia, comprising administering to a patient in need thereof a therapeutically effective amount of a composition of claim 16 .

18. A compound having the structure:

wherein A − is a pharmaceutically acceptable anion.

19. A composition comprising the compound of claim 18 , and at least one pharmaceutically acceptable excipient.

20. A method of treating hypercholesterolemia, comprising administering to a patient in need thereof a therapeutically effective amount of a composition of claim 19 .

21. A compound of claim 18 , wherein the compound is:

22. A composition comprising the compound of claim 21 , and at least one pharmaceutically acceptable excipient.

23. A method of treating hypercholesterolemia, comprising administering to a patient in need thereof a therapeutically effective amount of a composition of claim 22 .

24. A compound having the structure:

wherein A − is a pharmaceutically acceptable anion.

25. A composition comprising the compound of claim 24 , and at least one pharmaceutically acceptable excipient.

26. A method of treating hypercholesterolemia, comprising administering to a patient in need thereof a therapeutically effective amount of a composition of claim 25 .

27. A compound of claim 24 , wherein the compound is:

28. A composition comprising the compound of claim 27 , and at least one pharmaceutically acceptable excipient.

29. A method of treating hypercholesterolemia, comprising administering to a patient in need thereof a therapeutically effective amount of a composition of claim 28 .

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 30, 2023
From: WOOD, HAROLD B.; JOSIEN, HUBERT B.; TUCKER, THOMAS JOSEPH; KEREKES, ANGELA DAWN; WU, CHENGWEI; HA, SOOKHEE NICOLE; NAIR, ANILKUMAR G.; DING, FA-XIANG; WALJI, ABBAS M.; TONG, LING; LIU, JIAN; BOGA, SOBHANA BABU; XIONG, YUSHENG
To: MERCK SHARP & DOHME CORP.
Reel/Frame 063174/0912 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 30, 2023
From: BIANCHI, ELISABETTA; BRANCA, DANILA
To: IRBM S.P.A.
Reel/Frame 063175/0224 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 30, 2023
From: IRBM S.P.A.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 063175/0381 →
MERGER Recorded Mar 30, 2023
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 063176/0072 →
Continuity (3)
Continuation 16446940 · Jun 20, 2019
Provisional Application 62687913 · Jun 21, 2018
Related Publication 20230159592A1 · May 25, 2023
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