Details for Patent: 7,157,554

Title:	Glycopeptide carboxy-saccharide derivatives
Abstract:	Disclosed are glycopeptide derivatives substituted at the C-terminus and/or the R-terminus with a substituent that comprises one or more saccharide groups and a carboxy group; and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial agents.
Inventor(s):	Linsell; Martin S. (San Mateo, CA), Fatheree; Paul R. (San Francisco, CA), Leadbetter; Michael R. (San Leandro, CA), Zhu; Yan (Foster City, CA), Judice; J. Kevin (El Granada, CA)
Assignee:	Theravance, Inc. (South San Francisco, CA)
Filing Date:	Mar 15, 2005
Application Number:	11/080,130
Claims:	1. A method of modifying a glycopeptide antibiotic to form a glycopeptide antibiotic derivative having reduced tissue accumulation when administered to a mammal, the method comprising forming a carboxy-saccharide derivative of the glycopeptide antibiotic that has a substituent comprising a dicarboxylic acid in which one of the carboxylic acid groups is coupled with a saccharide. 2. The method of claim 1, wherein the glycopeptide antibiotic is vancomycin or a derivative thereof. 3. The method of claim 1, wherein the glycopeptide antibiotic is chloroorienticin A or a derivative thereof. 4. The method of claim 1, wherein the glycopeptide antibiotic is teicoplanin or a derivative thereof. 5. The method of claim 1, wherein the substituent is a substituent of formula III: ##STR00012## wherein one of R.sup.g and R.sup.h is a saccharide, and the other of R.sup.g and R.sup.h is OH. 6. The method of claim 1, wherein the substituent is a substituent of formula IV: ##STR00013## wherein one of R.sup.m and R.sup.n is a saccharide, and the other is OH. 7. The method of claim 1, wherein the substituent is a substituent of formula (i): ##STR00014## 8. The method of claim 1, wherein the substituent is a substituent of formula (ii): ##STR00015## 9. The method of claim 1, wherein the substituent is a substituent of formula (iii): ##STR00016## 10. The method of claim 1, wherein the substituent is a substituent of formula (iv): ##STR00017## 11. A method of modifying a glycopeptide antibiotic to farm a glycopeptide antibiotic derivative having increased urinary clearance when administered to a mammal, the method comprising forming a carboxy-saccharide derivative of the glycopeptide antibiotic that has a substituent comprising a dicarboxylic acid in which one of the carboxylic acid groups is coupled with a saccharide. 12. The method of claim 11, wherein the glycopeptide antibiotic is vancomycin or a derivative thereof. 13. The method of claim 11, wherein the glycopeptide antibiotic is chloroorienticin A or a derivative thereof. 14. The method of claim 11, wherein the glycopeptide antibiotic is teicoplanin or a derivative thereof. 15. The method of claim 11, wherein the substituent is a substituent of formula III: ##STR00018## wherein one of R.sup.g and R.sup.h is a saccharide, and the other R.sup.g and R.sup.h is OH. 16. The method of claim 11, wherein the substituent is a substituent of formula IV: ##STR00019## wherein one of R.sup.m and R.sup.n is a saccharide, and the other is OH. 17. The method of claim 11, wherein the substituent is a substituent of formula (i): ##STR00020## 18. The method of claim 11, wherein the substituent is a substituent of formula (ii): ##STR00021## 19. The method of claim 11, wherein the substituent is a substituent of formula (iii): ##STR00022## 20. The method of claim 11, wherein the substituent is a substituent of formula (iv): ##STR00023##