Antibacterial agents for the treatment of gram positive infections
View Patent ↗The present invention relates to novel lipopeptide compounds, pharmaceutical compositions of these compounds and methods of using these compounds as antibacterial compounds. The compounds of the invention are particularly useful against a variety of bacteria, including resistant strains. The compounds are useful as antibacterial agents against Clostridium difficile.
1. A compound of Formula I
and pharmaceutically acceptable salts thereof, wherein:
R is
and v is an integer from 3 to 7.
2. A compound of Formula (II)
or a pharmaceutically acceptable salt thereof.
3. A pharmaceutical composition comprising a compound according to claim 2 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
4. A method of treating a bacterial infection comprising administering to a subject in need thereof a therapeutically-effective amount of the pharmaceutical composition according to claim 3 .
5. The method according to claim 4 , wherein the subject is a human, an animal, a cell culture, or a plant.
6. The method according to claim 5 , wherein the subject is a human.
7. The method according to claim 4 , wherein the bacterial infection is caused by a gram-positive bacteria.
8. The method according to claim 7 , wherein the bacteria is a Clostridium difficile strain.
9. The method according to claim 8 , wherein the Clostridium difficile strain is a Nap1 Clostridium difficile strain.
10. The method according to claim 7 , wherein the bacteria is an antibiotic resistant bacteria, wherein the antibiotic resistant bacteria is not resistant to the composition according to claim 3 .
11. The method according to claim 10 , wherein the antibiotic resistant bacteria is daptomycin resistant Staphylococcus aureus , daptomycin resistant Enterococcus faecium , daptomycin resistant Enterococcus faecalis , methicillin resistant Staphylococcus aureus , or a mixture of bacteria comprising at least one of the antibiotic resistant bacteria.
12. The method according to claim 10 , wherein the antibiotic-resistant bacteria is resistant to vancomycin, methicillin, glycopeptide antibiotics, penicillin or daptomycin.
13. The method according to claim 7 , wherein the bacterial infection is Clostridium Difficile Associated Disease (CDAD).
14. The method according to claim 13 , wherein the Clostridium Difficile Associated Disease arises from or is exacerbated by a Nap1 Clostridium difficile infection.
15. The compound according to claim 2 , wherein the compound is of the formula:
or a pharmaceutically acceptable salt thereof.