IP Library Granted Patent US 10,723,746
Granted Patent B2
US 10,723,746 · App. 14/894,400 · Granted Jul 28, 2020

Oxazolidinone-quinolone hybrid antibacterials for the parenteral treatment or prophylaxis of bacterial diseases

Inventors: Thomas Kapsner (Gröbenzell, DE); Axel Dalhoff (Wuppertal, DE); Thomas Gramatte (Dresden, DE)
Assignee: Morphochem Aktiengesellschaft Für Kombinatorische Chemie
C07F9/653A61K31/4375A61K31/4709A61P1/00A61P1/12A61P31/00A61P31/04
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 10,723,746
App. No.
14/894,400
Granted
Jul 28, 2020
Kind
B2
Abstract

The present invention relates to the use of oxazolidinone-quinolone hybrids for the parenteral (especially intravenous) treatment or prophylaxis of bacterial diseases. The present invention relates moreover to improved methods of administering oxazolidinone-quinolone hybrid antibacterials.

Claims (22)

1. A method for treating a bacterial infection caused by Clostridium difficile , comprising the step of administering to a patient in need thereof an oxazolidinone-quinolone hybrid at an infusion rate of from 0.4 to 3 mg/(kg body weight×hour), wherein the oxazolidinone-quinolone hybrid is 7-(4-{4-[(5S)-5-(acetylamino-methyl)-2-oxo-oxazolidin-3-yl]-2-fluoro-phenoxymethyl}-4-phosphonooxy-piperidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid:

or a salt thereof.

2. The method according to claim 1 wherein the oxazolidinone-quinolone hybrid is administered over a period of from 20 min to 24 h per day.

3. The method according to claim 1 wherein the oxazolidinone-quinolone hybrid is administered over a period of from 20 min to 5 h per day.

4. The method according to claim 1 wherein the oxazolidinone-quinolone hybrid is administered over a period of from 4 h to 12 h per day.

5. The method according to claim 1 wherein the infusion rate is from 0.4 to 1.5 mg/(kg body weight×h).

6. The method according to claim 1 wherein the infusion rate is from 0.4 to 0.75 mg/(kg body weight×h).

7. The method according to claim 1 , wherein the oxazolidinone-quinolone hybrid is the sodium salt of 7-(4-{4-[(5S)-5-(acetylamino-methyl)-2-oxo-oxazolidin-3-yl]-2-fluoro-phenoxymethyl}-4-phosphonooxy-piperidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid.

8. The method according to claim 1 , wherein the bacterial infection caused by Clostridium difficile is a gastro-intestinal infection caused by Clostridium difficile.

9. The method according to claim 8 , wherein the bacterial infection caused by Clostridium difficile is an intestinal disease caused by Clostridium difficile.

10. The method according to claim 9 , wherein the intestinal disease caused by Clostridium difficile is diarrhea, colitis, or pseudomembranous colitis.

11. The method according to claim 1 , wherein the bacterial infection caused by Clostridium difficile is ileus, toxic megacolon, fulminant colitis, colonic perforation or need for colectomy.

12. A method for treating a gastro-intestinal infection caused by Clostridium difficile , comprising the step of administering to a patient in need thereof an oxazolidinone-quinolone hybrid at an infusion rate of from 0.4 to 3 mg/(kg body weight×hour), wherein the oxazolidinone-quinolone hybrid is a sodium salt of 7-(4-{4-[(5S)-5-(acetylamino-methyl)-2-oxo-oxazolidin-3-yl]-2-fluoro-phenoxymethyl}-4-phosphonooxy-piperidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid:

or a salt thereof.

13. The method according to claim 12 wherein the oxazolidinone-quinolone hybrid is administered over a period of from 20 min to 24 h per day.

14. The method according to claim 12 wherein the oxazolidinone-quinolone hybrid is administered over a period of from 20 min to 5 h per day.

15. The method according to claim 12 wherein the oxazolidinone-quinolone hybrid is administered over a period of from 4 h to 12 h per day.

16. The method according to claim 12 wherein the infusion rate is from 0.4 to 1.5 mg/(kg body weight×hour).

17. The method according to claim 12 wherein the infusion rate is from 0.4 to 0.75 mg/(kg body weight×hour).

18. The method according to claim 12 , wherein the gastro-intestinal infection caused by Clostridium difficile is an intestinal disease caused by Clostridium difficile.

19. The method according to claim 18 , wherein the intestinal disease caused by Clostridium difficile is diarrhea, colitis, or pseudomembranous colitis.

20. The method according to claim 12 , wherein the gastro-intestinal infection caused by Clostridium difficile is ileus, toxic megacolon, fulminant colitis, colonic perforation or need for colectomy.

Assignments (2)
CHANGE OF NAME Recorded Jun 26, 2020
From: MORPHOCHEM AKTIENGESELLSCHAFT FÜR KOMBINATORISCHE CHEMIE
To: MORPHOCHEM GMBH
Reel/Frame 053066/0695 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 27, 2015
From: KAPSNER, THOMAS; DALHOFF, AXEL; GRAMATTE, THOMAS
To: MORPHOCHEM AKTIENGESELLSCHAFT FÜR KOMBINATORISCHE CHEMIE
Reel/Frame 037149/0165 →
Priority Claims (3)
EP 13002762 · May 28, 2013 · regional
EP 13005745 · Dec 10, 2013 · regional
EP 13005748 · Dec 10, 2013 · regional
Continuity (1)
Related Publication 20160130288A1 · May 12, 2016