IP Library Granted Patent US 11,912,690
Granted Patent B2
US 11,912,690 · App. 17/990,806 · Granted Feb 27, 2024

Acid addition salts of benzimidazole derivative

Inventors: Eun Sun Kim (Gangwon-do, KR); Min Kyoung Lee (Seoul, KR); Sung Ah Lee (Gyeonggi-do, KR); Kwang Do Choi (Gyeonggi-do, KR); Jae Sun Kim (Gyeonggi-do, KR); Hyung Chul Yoo (Gyeonggi-do, KR)
Assignee: HK INNO.N CORPORATION
C07D405/12C07D235/06
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Quick Facts
Patent No.
US 11,912,690
App. No.
17/990,806
Granted
Feb 27, 2024
Kind
B2
Abstract

The present invention relates to a pidolate salt and malate salt of a compound represented by a formula 1 with an excellent liquid-phase stability, solid-phase stability, water solubility, precipitation stability and hygroscopicity all together as a compound for preventing and treating diseases mediated by an acid pump antagonistic activity, as well as a method for preparing the same.

Claims (26)

1. A pidolate salt of a compound represented by Formula 1, prepared by a process comprising:

a) dissolving a compound represented by Formula 1 and pyroglutamic acid in an organic solvent, thereby creating a solution;

b) concentrating the solution under decompression to precipitate a solid, then adding a co-solvent and stirring; and

c) filtering out and drying the precipitated solid:

2. The method of 1 , wherein the organic solvent is added in a volume 5 to 20 times (volume/weight) compared to the amount of compound represented by Formula 1.

3. The method of claim 1 , wherein the organic solvent is methanol.

4. The method of claim 3 , wherein the methanol is added in a volume 5 to 20 times (volume/weight) compared to the amount of compound represented by Formula 1.

5. The method of claim 4 , wherein the methanol is added in a volume 10 times (volume/weight) compared to the amount of compound represented by Formula 1.

6. The method of claim 1 , wherein the co-solvent is a mixed solution of acetone and ethyl acetate.

7. The method of claim 6 , wherein the ratio of acetone to ethyl acetate is 1:4 (v/v).

8. The method of claim 6 , wherein the mixed solution of acetone and ethyl acetate is added in a volume 5 to 20 times (volume/weight) compared to the amount of compound represented by Formula 1.

9. The method of claim 8 , wherein the mixed solution of acetone and ethyl acetate is added in a volume 5 times (volume/weight) compared to the amount of compound represented by Formula 1.

10. The method of claim 1 , wherein the pyroglutamic acid is L-pyroglutamic acid.

11. A malate salt of a compound represented by Formula 1, prepared by a process comprising:

a) dissolving a compound represented by Formula 1 and malic acid in an organic solvent, thereby creating a solution;

b) concentrating the solution under decompression to precipitate a solid, then adding a co-solvent and stirring; and

c) filtering out and drying the precipitated solid:

12. The method of 11 , wherein the organic solvent is added in a volume 5 to 20 times (volume/weight) compared to the amount of compound represented by Formula 1.

13. The method of claim 11 , wherein the organic solvent is methanol.

14. The method of claim 13 , wherein the methanol is added in a volume 5 to 20 times (volume/weight) compared to the amount of compound represented by Formula 1.

15. The method of claim 14 , wherein the methanol is added in a volume 10 times (volume/weight) compared to the amount of compound represented by Formula 1.

16. The method of claim 11 , wherein the co-solvent is a mixed solution of acetone and ethyl acetate.

17. The method of claim 16 , wherein the ratio of acetone to ethyl acetate is 1:4 (v/v).

18. The method of claim 16 , wherein the mixed solution of acetone and ethyl acetate is added in a volume 5 to 20 times (volume/weight) compared to the amount of compound represented by Formula 1.

19. The method of claim 18 , wherein the mixed solution of acetone and ethyl acetate is added in a volume 5 times (volume/weight) compared to the amount of compound represented by Formula 1.

20. The method of claim 11 , wherein the malic acid is L-malic acid.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 21, 2024
From: KIM, EUN SUN; LEE, MIN KYOUNG; LEE, SUNG AH; CHOI, KWANG DO; KIM, JAE SUN; YOO, HYUNG CHUL
To: CJ HEALTHCARE CORPORATION
Reel/Frame 068353/0310 →
CHANGE OF NAME Recorded Aug 21, 2024
From: CJ HEALTHCARE CORPORATION
To: HK INNO.N CORPORATION
Reel/Frame 068734/0702 →
Priority Claims (1)
KR 10-2016-0120996 · Sep 21, 2016 · national
Continuity (2)
Continuation 16334427
Related Publication 20230192670A1 · Jun 22, 2023