IP Library Granted Patent US 11,224,596
Granted Patent B2
US 11,224,596 · App. 16/490,677 · Granted Jan 18, 2022

PZA and cytochrome bc1 inhibitor combination treatment

Inventors: Koenraad Jozef Lodewijk Marcel Andries (Beerse, BE); Anil Koul (Edegem, BE); Maria Cristina Villellas Arilla (Turnhout, BE)
Assignee: Janssen Sciences Ireland Unlimited Company
A61K31/4965A61K31/438A61K31/4545A61K31/47A61K31/498A61P31/06
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Quick Facts
Patent No.
US 11,224,596
App. No.
16/490,677
Granted
Jan 18, 2022
Kind
B2
Abstract

The present invention relates to novel combinations, which are useful in the treatment of tuberculosis.

Claims (28)

1. A combination consisting of the following active ingredients:

(i) PZA, or a pharmaceutically acceptable salt thereof; and

(ii) a cytochrome bc 1 inhibitor, or a pharmaceutically acceptable salt thereof.

2. The combination as claimed in claim 1 , wherein the cytochrome bc 1 inhibitor is Q203, or a pharmaceutically acceptable salt thereof.

3. The combination as claimed in claim 1 wherein the daily dose of PZA (or a pharmaceutically acceptable salt thereof) is 15 to 30 mg/kg (up to 2 g).

4. The combination as claimed in claim 1 wherein the daily dose of the cytochrome bc 1 inhibitor (or a pharmaceutically acceptable salt thereof) is 1.5 to 15 mg/kg (up to 1 g).

5. A pharmaceutical formulation comprising the combination as claimed in claim 1 , and a pharmaceutically acceptable excipient or diluent.

6. A method of treating a patient having a mycobacterial infection comprising administering an effective amount of the combination as claimed in claim 1 .

7. The method as claimed in claim 6 , wherein the mycobacterial infection is latent tuberculosis.

8. A process for preparing the pharmaceutical formulation as defined in claim 5 comprising bringing into association the active ingredients of the combination with one (or more) pharmaceutically acceptable excipient or carrier.

9. A combination comprising the following active ingredients:

(i) PZA, or a pharmaceutically acceptable salt thereof; and

(ii) a cytochrome bc 1 inhibitor, or a pharmaceutically acceptable salt thereof.

10. The method as claimed in claim 7 , wherein the cytochrome bc 1 inhibitor is Q203, or a pharmaceutically acceptable salt thereof.

11. The method as claimed in claim 7 , wherein the daily dose of PZA (or a pharmaceutically acceptable salt thereof) is 15 to 30 mg/kg (up to 2 g).

12. The method as claimed in claim 7 , wherein the daily dose of the cytochrome bc 1 inhibitor (or a pharmaceutically acceptable salt thereof) is 1.5 to 15 mg/kg (up to 1 g).

13. The method as claimed in claim 10 , wherein the daily dose of PZA (or a pharmaceutically acceptable salt thereof) is 15 to 30 mg/kg (up to 2 g).

14. The method as claimed in claim 10 , wherein the daily dose of the cytochrome bc 1 inhibitor (or a pharmaceutically acceptable salt thereof) is 1.5 to 15 mg/kg (up to 1 g).

15. The pharmaceutical formulation as claimed in claim 5 , wherein the cytochrome bc 1 inhibitor is Q203, or a pharmaceutically acceptable salt thereof.

16. The combination as claimed in claim 9 , further comprising additional antibacterial drugs.

17. The combination as claimed in claim 16 , wherein the additional antibacterial drugs are anti-tuberculosis drugs selected from:

agents known to interfere with the respiratory chain of Mycobacterium tuberculosis;

other antibacterial agents that may target the electron transport chain; and

other mycobacterial agents.

18. The combination as claimed in claim 16 wherein the additional antibacterial drugs is:

bedaquiline; and/or

clofazimine.

19. The combination as claimed in claim 16 , wherein the additional antibacterial drugs are selected from: direct inhibitors of the ATP synthase; inhibitors of ndh2; antibacterial agents that target the cytochrome bd oxidase; rifampicin (=rifampin); isoniazid; pyrazinamide; amikacin; ethionamide; ethambutol; streptomycin; para-aminosalicylic acid; cycloserine; capreomycin; kanamycin; thioacetazone; PA-824; delamanid; quinolones/fluoroquinolones; macrolides; rifamycins; rifabutin; rifapentin; delanamid and/or pretonamid.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 17, 2021
From: ANDRIES, KOENRAAD JOZEF LODEWIJK MARCEL; VILLELLAS ARILLA, MARIA CRISTINA; KOUL, ANIL
To: JANSSEN PHARMACEUTICA NV
Reel/Frame 058140/0563 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 17, 2021
From: JANSSEN PHARMACEUTICA NV
To: JANSSEN SCIENCES IRELAND UC
Reel/Frame 058140/0714 →
CHANGE OF NAME Recorded Nov 17, 2021
From: JANSSEN SCIENCES IRELAND UC
To: JANSSEN SCIENCES IRELAND UNLIMITED COMPANY
Reel/Frame 058173/0879 →
Priority Claims (1)
EP 17158607 · Mar 1, 2017 · regional
Continuity (1)
Related Publication 20200016154A1 · Jan 16, 2020