IP Library Granted Patent US 10,624,893
Granted Patent B2
US 10,624,893 · App. 16/087,161 · Granted Apr 21, 2020

Antituberculosis agent

Inventors: Lluis Ballell Pages (Tres Cantos, ES); David Barros Aguirre (Tres Cantos, ES); Robert H. Bates (Tres Cantos, ES); Julia Castro Pichel (Tres Cantos, ES); Jorge Esquivias Provencio (Tres Cantos, ES); Kevin Pethe (Singapore, SG)
Assignee: GlaxoSmithKline Intellectual Property Development Limited
A61K31/513A61K45/06A61P31/06C07D401/06
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Quick Facts
Patent No.
US 10,624,893
App. No.
16/087,161
Granted
Apr 21, 2020
Kind
B2
Abstract

The present invention relates to the use in therapy of 6-((4-(2,3-dimethylphenoxy)piperidin-1-yl)methyl)pyrimidine-2,4(1H,3H)-dione or a pharmaceutically acceptable salt thereof, to pharmaceutically acceptable salts of 6-((4-(2,3-dimethylphenoxy)piperidin-1-yl)methyl)pyrimidine-2,4(1H,3H)-dione and to pharmaceutical formulations comprising 6-((4-(2,3-dimethylphenoxy)piperidin-1-yl)methyl)pyrimidine-2,4(1H,3H)-dione or a pharmaceutically acceptable salt thereof.

Claims (20)

1. A method for the treatment of a disease resulting from a mycobacterial infection in a human in need thereof, comprising administering to said human a therapeutically effective amount of 6-((4-(2,3-dimethylphenoxy)piperidin-1-yl)methyl)pyrimidine-2,4(1H,3H)-dione, or a pharmaceutically acceptable salt thereof.

2. A method for the treatment of a mycobacterial infection in a human in need thereof, the method comprising administering to said human a therapeutically effective amount of 6-((4-(2,3-dimethylphenoxy)piperidin-1-yl)methyl)pyrimidine-2,4(1H,3H)-dione, or a pharmaceutically acceptable salt thereof.

3. The method according to claim 1 , wherein the mycobacterial infection is a Mycobacterium tuberculosis infection.

4. The method according to claim 1 , wherein the disease is tuberculosis.

5. A salt of 6-((4-(2,3-dimethylphenoxy)piperidin-1-yl)methyl)pyrimidine-2,4(1H,3H)-dione.

6. A pharmaceutically acceptable salt of 6-((4-(2,3-dimethylphenoxy)piperidin-1-yl)methyl)pyrimidine-2,4(1H,3H)-dione.

7. The method according to claim 1 , further comprising administering a therapeutically effective amount of a second therapeutic agent.

8. The method according to claim 7 , wherein the second therapeutic agent is selected from the group consisting of isoniazid, rifampin, pyrazinamide, ethambutol, moxifloxacin, rifapentine, clofazimine, bedaquiline, nitroimidazo-oxazine PA-824, delamanid, OPC-167832, an oxazolidinone, EMB analogue SQ109, a benzothiazinone, a dinitrobenzamide, and an antiviral agent.

9. The method according to claim 8 , wherein the oxazolidinone is linezolid, tedizolid, radezolid, sutezolid, or posizolid.

10. The method according to claim 7 , wherein the second therapeutic agent is a therapeutic agent approved for or recommended for the treatment of tuberculosis.

11. A pharmaceutical composition comprising a) 6-((4-(2,3-dimethylphenoxy)piperidin-1-yl)methyl)pyrimidine-2,4(1H,3H)-dione, or a pharmaceutically acceptable salt thereof; and b) a pharmaceutically acceptable excipient.

12. The pharmaceutical composition according to claim 11 , further comprising a second therapeutic agent.

13. The pharmaceutical composition according to claim 12 , wherein the second therapeutic agent is selected from the group consisting of isoniazid, rifampin, pyrazinamide, ethambutol, moxifloxacin, rifapentine, clofazimine, bedaquiline, nitroimidazo-oxazine PA-824, delamanid, OPC-167832, an oxazolidinone, EMB analogue SQ109, a benzothiazinone, a dinitrobenzamide, and an antiviral agent.

14. A method of killing a mycobacterium and/or inhibiting the replication of a mycobacterium in a human infected with a mycobacterium , comprising contacting the mycobacterium or treating the human infected with the mycobacterium , with a therapeutically effective amount of 6-((4-(2,3-dimethylphenoxy)piperidin-1-yl)methyl)pyrimidine-2,4(1H,3H)-dione, or a pharmaceutically acceptable salt thereof.

15. The method according to claim 14 , wherein the mycobacterium is Mycobacterium tuberculosis.

16. The method according to claim 2 , wherein the mycobacterial infection is a Mycobacterium tuberculosis infection.

17. The method according to claim 8 , wherein the antiviral agent is an antiretroviral agent.

18. The pharmaceutical composition according to claim 13 , wherein the antiviral agent is an antiretroviral agent.

19. The pharmaceutical composition according to claim 13 , wherein the oxazolidinone is linezolid, tedizolid, radezolid, sutezolid, or posizolid.

20. The pharmaceutical composition according to claim 12 , wherein the second therapeutic agent is a therapeutic agent approved for or recommended for the treatment of tuberculosis.

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 Apr 11, 2019
From: BALLELL PAGES, LLUIS; BARROS AGUIRRE, DAVID; BATES, ROBERT H.; CASTRO PICHEL, JULIA; ESQUIVIAS PROVENCIO, JORGE; PETHE, KEVIN
To: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
Reel/Frame 048862/0666 →
Priority Claims (1)
EP 16382124 · Mar 22, 2016 · regional
Continuity (1)
Related Publication 20190091224A1 · Mar 28, 2019
Cited By (1)
US 12,433,889