Bacitracin antibiotics
The invention concerns new Bacitracin compounds containing methylene-isoleucine.
1. A compound represented by the formula
wherein
at least one of R 1 , R 2 and R 3 is —CH═CH 2 , and
wherein
R 1 , R 2 and R 3 are independently —H, —CH 3 , or CH═CH 2 , and
salts and hydrates thereof.
2. A compound according to claim 1 , wherein one of R 1 , R 2 and R 3 is —CH 3 .
3. A compound according to claim 1 , wherein two of R 1 , R 2 and R 3 are —CH 3 .
4. A compound according to claim 1 , wherein R 1 is —CH═CH 2 .
5. A compound according to claim 1 , wherein R 2 is —CH═CH 2 .
6. A compound according to claim 1 , wherein R 3 is —CH═CH 2 .
7. A compound according to claim 1 , wherein R 1 and R 2 are —CH═CH 2 .
8. A compound according to claim 1 , wherein R 2 and R 3 are —CH═CH 2 .
9. A compound according to claim 1 , wherein R 1 and R 3 are —CH═CH 2 .
10. A compound according to claim 1 , wherein R 1 and R 2 and R 3 are —CH═CH 2 .
11. A composition comprising the compound of claim 1 and a second active pharmaceutical ingredient.
12. A pharmaceutical composition comprising the compound of claim 1 and one or more pharmaceutical excipients.
13. A pharmaceutical composition according to claim 12 , which has therapeutic effect.
14. A method of treating a human or animal having a bacterial infection, comprising administering to the human or animal a therapeutically effective amount a compound according to claim 1 to treat a bacterial infection.
15. Method for production of compounds according to claim 1 by substituting Isoleucine or Valine with 5-Methylene-Isoleucine during in vitro Bacitracin synthesis.