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Generated: April 21, 2018

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Details for Patent: 7,265,086

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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:Oct 30, 2006
Application Number:11/589,614
Claims:1. A compound of the formula: ##STR00012## or a pharmaceutically acceptable salt or stereoisomer thereof; wherein R.sup.g and R.sup.20 are selected from: TABLE-US-00014 R.sup.g ##STR00013## ##STR00014## ##STR00015## ##STR00016## ##STR00017## ##STR00018## ##STR00019## ##STR00020## ##STR00021## ##STR00022## ##STR00023## ##STR00024## ##STR00025## ##STR00026## ##STR00027## ##STR00028## ##STR00029## ##STR00030## ##STR00031## ##STR00032## R.sup.20 --(CH.sub.2).sub.11CH.sub.3 --(CH.sub.2).sub.12CH.sub.3 --CH.sub.2CH.sub.2--NH--(CH.sub.2).sub.9CH.sub.3 --CH.sub.2CH.sub.2--NH--(CH.sub.2).sub.9CH.sub.3 --CH.sub.2CH.sub.2--S--(CH.sub.2).sub.9CH.sub.3 --CH.sub.2CH.sub.2--O--(CH.sub.2).sub.9CH.sub.3 ##STR00033## ##STR00034## ##STR00035## ##STR00036## ##STR00037## ##STR00038## ##STR00039## ##STR00040## ##STR00041## ##STR00042## --CH.sub.2CH.sub.2--NH--(CH.sub.2).sub.9CH.sub.3 --CH.sub.2CH.sub.2--S--(CH.sub.2).sub.9CH.sub.3 --CH.sub.2CH.sub.2--O--(CH.sub.2).sub.9CH.sub.3 ##STR00043##

2. The compound of claim 1, wherein R.sup.g is ##STR00044## and R.sup.20 is --CH.sub.2CH.sub.2--NH--(CH.sub.2).sub.9CH.sub.3.

3. The compound of claim 1, wherein R.sup.g is ##STR00045## and R.sup.20 is --CH.sub.2CH.sub.2--S--(CH.sub.2).sub.9CH.sub.3.

4. The compound of claim 1, wherein R.sup.g is ##STR00046## and R.sup.20 is ##STR00047##

5. The compound of claim 1, wherein R.sup.g is ##STR00048## and R.sup.20 is --CH.sub.2CH.sub.2--NH--(CH.sub.2).sub.9CH.sub.3.

6. The compound of claim 1, wherein R.sup.g is ##STR00049## and R.sup.20 is --CH.sub.2CH.sub.2--S--(CH.sub.2).sub.9CH.sub.3.

7. The compound of claim 1, wherein R.sup.g is ##STR00050## and R.sup.20 is ##STR00051##

8. A compound of the formula: ##STR00052## or a pharmaceutically acceptable salt or stereoisomer thereof; wherein R.sup.m and R.sup.20 are selected from: TABLE-US-00015 R.sup.m R.sup.20 ##STR00053## --CH.sub.2CH.sub.2--NH--(CH.sub.2).sub.9CH.sub.3 ##STR00054## --CH.sub.2CH.sub.2--O--(CH.sub.2).sub.9CH.sub.3 ##STR00055## --CH.sub.2CH.sub.2--S--(CH.sub.2).sub.9CH.sub.3 ##STR00056## ##STR00057## ##STR00058## ##STR00059## ##STR00060## ##STR00061## ##STR00062## ##STR00063## ##STR00064## ##STR00065## ##STR00066## ##STR00067## ##STR00068## ##STR00069##

9. The compound of claim 8, wherein R.sup.m is ##STR00070## and R.sup.20 --CH.sub.2CH.sub.2--NH--(CH.sub.2).sub.9CH.sub.3.

10. The compound of claim 8, wherein R.sup.m is ##STR00071## and R.sup.20 is --CH.sub.2CH.sub.2--S--(CH.sub.2).sub.9CH.sub.3.

11. The compound of claim 8, wherein R.sup.m is ##STR00072## and R.sup.20 is ##STR00073##

12. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of any one of claims 1 to 11.

13. 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 11.

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