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|Title:||Polyacid glycopeptide derivatives|
|Abstract:||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.sub.2H) groups; and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial agents.|
|Inventor(s):||Linsell; Martin S. (San Mateo, CA), Judice; J. Kevin (El Granada, CA)|
|Assignee:||Theravance, Inc. (South San Francisco, CA)|
|Filing Date:||Mar 18, 2005|
|Claims:||1. A compound of the formula: ##STR00011## wherein R.sup.17 is --CH(COOH)CH.sub.2COOH or --CH(COOH)CH.sub.2CH.sub.2COOH and stereoisomer thereof; R.sup.20 is 4-(4-chlorophenyl)benzyl or 4-(4-chlorobenzyloxy)benzyl; or a pharmaceutically-acceptable salt. |
2. The compound of claim 1, wherein R.sup.17 is --CH(COOH)CH.sub.2COOH.
3. The compound of claim 1, wherein R.sup.17 is --CH(COOH)CH.sub.2CH.sub.2COOH.
4. The compound of claim 1, wherein R.sup.20 is 4-(4-chloropbenyl)benzyl.
5. The compound of claim 1, wherein R.sup.20 is 4-(4-chlorobenzyloxy)benzyl.
6. A compound of the formula: ##STR00012## 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-.beta.-cyclodextrin or sulfobutyl ether .beta.-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.