IP Library › Granted Patent US 12,435,077
Granted Patent B2
US 12,435,077 · App. 17/909,834 · Granted Oct 7, 2025

Oxazolidinone compound and methods of use thereof as an antibacterial agent

Inventors: Brendan M. Crowley (Collegeville, PA); Philippe Nantermet (Lansdale, PA); David B. Olsen (Lansdale, PA); Takao Suzuki (Shanghai, CN); Lihu Yang (Edison, NJ); Lanying You (Shanghai, CN)
Assignee: Merck Sharp & Dohme LLC
C07D417/10A61K31/541A61K45/06A61P31/06
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Quick Facts
Patent No.
US 12,435,077
App. No.
17/909,834
Granted
Oct 7, 2025
Kind
B2
Abstract

The present invention relates to the oxazolidinone compound of Formula (I): and pharmaceutically acceptable salts thereof. The present invention also relates to compositions containing the compound of Formula (I). The invention also provides methods for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis by administering a therapeutically effective amount of Formula (I) and/or a pharmaceutically acceptable salt thereof, or a composition comprising such compound and/or salt.

Claims (25)

1. A compound of Formula I

or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition which comprises a therapeutically effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

3. A method for treating a bacterial infection which comprises administering to a subject in need of such treatment a therapeutically effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof.

4. A method for treating a bacterial infection which comprises administering to a subject in need of such treatment the pharmaceutical composition according to claim 2 .

5. The method of claim 3 , wherein the bacterial infection is due to Mycobacterium tuberculosis.

6. The method of claim 4 , wherein the bacterial infection is due to Mycobacterium tuberculosis.

7. The method of claim 3 , wherein the compound or the pharmaceutically acceptable salt thereof is administered orally, parenterally, or topically.

8. The method of claim 4 , wherein the pharmaceutical composition is administered orally, parenterally, or topically.

9. The method of claim 5 , wherein the Mycobacterium tuberculosis is a drug resistant mycobacterial strain.

10. The method of claim 6 , wherein the Mycobacterium tuberculosis is a drug resistant mycobacterial strain.

11. The method of claim 5 , further comprising the step of administering a second therapeutic agent for treating Mycobacterium tuberculosis.

12. The method of claim 11 , wherein the second therapeutic agent is selected from the group consisting of: ethambutol, pyrazinamide, isoniazid, levofloxacin, moxifloxacin, gatifloxacin, ofloxacin, kanamycin, amikacin, capreomycin, streptomycin, ethionamide, prothionamide, cycloserine, terididone, para-aminosalicylic acid, clofazimine, clarithromycin, amoxicillin-clavulanate, pretomanid, bedaquiline, GSK 3036656, gepotidacin, thiacetazone, meropenem-clavulanate, TBA-7371 a decaprenylphosphoryl-β-D-ribose 2′-oxidase (DprE1) Inhibitor, OPC-167832, Telacebec (Q203) and thioridazine.

13. A compound of Formula I

14. A pharmaceutical composition which comprises a therapeutically effective amount of the compound of claim 13 and a pharmaceutically acceptable carrier.

15. A method for treating a bacterial infection which comprises administering to a subject in need of such treatment a therapeutically effective amount of the compound of claim 13 .

16. A method for treating a bacterial infection which comprises administering to a subject in need of such treatment the pharmaceutical composition according to claim 14 .

17. The method of claim 15 , wherein the bacterial infection is due to Mycobacterium tuberculosis.

18. The method of claim 16 , wherein the bacterial infection is due to Mycobacterium tuberculosis.

19. The method of claim 15 , wherein the compound is administered orally, parenterally, or topically.

20. The method of claim 16 , wherein the pharmaceutical composition is administered orally, parenterally, or topically.

21. The method of claim 17 , wherein the Mycobacterium tuberculosis is a drug resistant mycobacterial strain.

22. The method of claim 18 , wherein the Mycobacterium tuberculosis is a drug resistant mycobacterial strain.

23. The method of claim 17 , further comprising the step of administering a second therapeutic agent for treating Mycobacterium tuberculosis.

24. The method of claim 23 , wherein the second therapeutic agent is selected from the group consisting of: ethambutol, pyrazinamide, isoniazid, levofloxacin, moxifloxacin, gatifloxacin, ofloxacin, kanamycin, amikacin, capreomycin, streptomycin, ethionamide, prothionamide, cycloserine, terididone, para-aminosalicylic acid, clofazimine, clarithromycin, amoxicillin-clavulanate, pretomanid, bedaquiline, GSK 3036656, gepotidacin, thiacetazone, meropenem-clavulanate, TBA-7371 a decaprenylphosphoryl-β-D-ribose 2′-oxidase (DprE1) Inhibitor, OPC-167832, Telacebec (Q203) and thioridazine.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 7, 2022
From: CROWLEY, BRENDAN M.; NANTERMET, PHILIPPE; OLSEN, DAVID B.; YANG, LIHU
To: MERCK SHARP & DOHME CORP.
Reel/Frame 061012/0474 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 7, 2022
From: SUZUKI, TAKAO; YOU, LANYING
To: WUXI APPTEC (SHANGHAI) CO. LTD.
Reel/Frame 061012/0775 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 7, 2022
From: WUXI APPTEC (SHANGHAI) CO. LTD.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 061013/0318 →
MERGER Recorded Sep 7, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061013/0398 →
Priority Claims (1)
WO PCT/CN2020/080359 · Mar 20, 2020 · international
Continuity (1)
Related Publication 20240208958A1 · Jun 27, 2024
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