Polyacid glycopeptide derivatives
View Patent ↗Disclosed are derivatives of glycopeptides that are substituted at the C-terminus with a substituent that comprises two or more (e.g. 2, 3, 4, or 5) carboxy (CO 2 H) groups; and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial agents.
1. A compound of the formula:
wherein
R 17 is —CH(COOH)CH 2 COOH or —CH(COOH)CH 2 CH 2 COOH and stereoisomer thereof;
R 20 is 4-(4-chlorophenyl)benzyl or 4-(4-chlorobenzyloxy)benzyl;
or a pharmaceutically-acceptable salt.
2. The compound of claim 1 , wherein R 17 is —CH(COOH)CH 2 COOH.
3. The compound of claim 1 , wherein R 17 is —CH(COOH)CH 2 CH 2 COOH.
4. The compound of claim 1 , wherein R 20 is 4-(4-chloropbenyl)benzyl.
5. The compound of claim 1 , wherein R 20 is 4-(4-chlorobenzyloxy)benzyl.
6. A compound of the formula:
or a pharmaceutically-acceptable salt.
7. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of any one of 1 to 6 .
8. The pharmaceutical composition of claim 7 , wherein the composition further comprises a cyclodextrin.
9. The pharmaceutical composition of claim 8 , wherein the cyclodextrin is hydroxypropyl-β-cyclodextrin or sulfobutyl ether β-cyclodextrin.
10. A method of treating a bacterial disease in a mammal, the method comprising administering to the mammal a therapeutically effective amount of a compound of any one of claims 1 to 6 .