Antibiotic macrocycle compounds and methods of manufacture and use thereof
View Patent ↗The invention encompasses an active metabolite of the 18-membered macrocyclic antimicrobial agents, specifically, a metabolite of tiacumicin B and in certain embodiments, R-Tiacumicin B or and its related compounds. In particular, the invention encompasses a compound that acts as a potent antibiotic agent for the treatment of bacterial infections, specifically GI infections caused by toxin producing strains of Clostridium difficile ( C. difficile ) and Clostridium perfringens ( C. perfringens ).
1. An isolated compound of Formula II
in free form or in the form of its pharmaceutically acceptable salt.
2. The isolated compound of claim 1 , wherein the compound of Formula II is greater than 80% by weight stereomerically pure.
3. The isolated compound of claim 1 , wherein the compound of Formula II is an alkaline metal or tertiary alkyl ammonium salt.
4. The isolated compound of claim 1 , wherein the compound of Formula II is a Na + , K + , Mg 2+ , Ca 2+ , Zn 2+ salt.
5. The isolated compound of claim 1 , wherein the compound of Formula II is greater than 90% by weight stereomerically pure.
6. The isolated compound of claim 1 , wherein the compound of Formula II is greater than 95% by weight stereomerically pure.
7. The isolated compound of claim 1 , wherein the compound of Formula II is greater than 97% by weight stereomerically pure.
8. The isolated compound of claim 1 , wherein the compound of Formula II is substantially free of other diastereomers of the compound.