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