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|Title:||Glycopeptide disulfide and thioester derivatives|
|Abstract:||Disclosed are disulfide and thioester derivatives of glycopeptides and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial agents.|
|Inventor(s):||Mu; YongQi (Los Altos, CA)|
|Assignee:||Theravance, Inc. (South San Francisco, CA)|
|Filing Date:||May 01, 2001|
|Claims:||1. A glycopeptide of formula II: ##STR10## |
wherein: R.sup.3 is --OH; R.sup.5 is hydrogen; R.sup.19 is hydrogen; R.sup.20 is --R.sup.a --S--(CO)--R.sup.h ; R.sup.a is alkylene, alkenylene, alkynylene, cycloalkylene, cycloalkenylene arylene, heteroarylene, heterocyclene, --C(O)-alkylene, --C(O)-alkenylene --C(O)-alkynylene, --C(O)-cycloalkylene, --C(O)-cycloallcenylene --C(O)-arylene, --C(O)-heteroarylene or heterocyclene; and R.sup.h is alkyl, alkenyl, alkynyl, cycloalkyl, cydoalkenyl, aryl, heteroaryl, or heterocyclic; or a pharmaceutically acceptable salt, stereoisonier, or prodrug thereof.
2. The glycopeptide of claim 1, wherein R.sup.a is alkylene, alkenylene, alkynylene, --C(O)-alkylene, --C(O)-alkenylene, or --C(O)-alkynylene, and R.sup.h is alkyl, alkenyl, or alkynyl.
3. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 1.
4. The pharmaceutical composition of claim 3, where the composition further comprises a cyclodextrin.
5. The glycopeptide of claim 1, wherein R.sup.a is alkylene.
6. The glycopeptide of claim 1, wherein R.sup.h is alkyl.
7. A method of treating a mammal having a bacterial disease, the method comprising administering to the mammal a therapeutically effective amount of a glycopeptide of claim 1, thereby effectively treating the bacterial disease.
8. A method of treating a mammal having a bacterial disease, the method comprising administering to the mammal a therapeutically effective amount of a pharmaceutical composition of claim 3, thereby effectively treating the bacterial disease.
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