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US 2002/0055464 A1Published application
Polyacid glycopeptide derivatives
AssigneeTheravance, Inc.
InventorsMartin S. Linsell, J. Kevin Judice
Life of this patent
Estimating the term…
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 (CO2H) groups; and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial agents.
Claims18
A glycopeptide substituted at the C-terminus with a substituent that comprises two or more carboxy groups;
- or a pharmaceutically acceptable salt, or stereoisomer, or prodrug thereof;
- provided the glycopeptide is not 1) teicoplanin A2 substituted at the C-terminus with a nitrogen-linked glutamic acid, 2) teicoplanin aglycon (TD) substituted at the C-terminus with a nitrogen-linked glutamic acid;
- or 3) a compound of formula II:
- 11
- a) wherein NR17 is nitrogen-linked aspartic acid;
- R18 is hydrogen;
- R19 is hydrogen;
- R20 is 2-(decylamino)ethyl;
- and R21 is hydrogen;
- b) wherein NR17 is nitrogen-linked aspartic acid;
- R18 is hydrogen;
- R19 is hydrogen;
- R20 is 2-(9-hydroxydecylamino)ethyl;
- and R21 is hydrogen;
- c) wherein R17 is 1,4-dicarboxybutyl;
- R18 is hydrogen;
- R19 is hydrogen;
- R20 is 2-(decylamino)ethyl;
- and R21 is hydrogen;
- d) wherein NR17 is nitrogen-linked aspartic acid;
- R18 is hydrogen;
- R19 is hydrogen;
- R20 is 2-(decylamino)ethyl;
- and R21 is —CH2—N-(D-glucamine);
- e) wherein R17 is nitrogen-linked aspartic acid;
- R18 is hydrogen;
- R19 is hydrogen;
- R20 is 2-[4-(4-chlorobenzyloxy)benzylamino]ethyl;
- and R21 is hydrogen;
- f) wherein NR17 is 5-(2-carboxypyrrolidin-1-ylcarbonyl)-5-(2-carboxy-3-phenylpropylamino)pentylamino;
- R18 is hydrogen;
- R19 is hydrogen;
- R20 is 2-(decylamino)ethyl;
- and R21 is hydrogen;
- g) wherein NR17 is nitrogen-linked aspartic acid;
- R18 is hydrogen;
- R19 is hydrogen;
- R20 is 2-(decylamino)ethyl;
- and R21 is —CH2—N—(N—CH3-D-glucamine);
- h) wherein NR17 is nitrogen-linked aspartic acid;
- R18 is hydrogen;
- R19 is hydrogen;
- R20 is 2-(decylamino)ethyl;
- and R21 is N-[2-(2-hydroxyethoxy)ethyl]-aminomethyl;
- or
- i) wherein NR17 is nitrogen-linked aspartic acid;
- R18 is hydrogen;
- R19 is hydrogen;
- R20 is 2-(4-isobutylbenzyl)ethyl;
- and R21 is N-[2-(2-hydroxyethoxy)ethyl]aminomethyl.
47 more elements
Dependencies are inferred from the claim text.