|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.2 H) 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:||Jun 25, 2004|
|Claims:||1. A compound of formula II: ##STR11## wherein R.sup.a is --CH.sub.2 CH.sub.2 --, --CH.sub.2 CH.sub.2 CH.sub.2 -- or --CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 --; R.sup.b and Z form an n-octyl, n-nonyl, n-decyl, n-undecyl or n-dodecyl group; or a pharmaceutically acceptable salt or stereoisomer thereof. |
2. The compound of claim 1, wherein R.sup.a is --CH.sub.2 CH.sub.2 --.
3. The compound of claim 2, wherein R.sup.b and Z form an n-decyl group.
4. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of any one of claims 1, 2 or 3.
5. The pharmaceutical composition of claim 4, wherein the composition further comprises a cyclodextrin.
6. The pharmaceutical composition of claim 5, wherein the cyclodextrin is hydroxypropyl-.beta.-cyclodextrin or sulfobutyl ether .beta.-cyclodextrin.
7. 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, 2 or 3.