Desleucyl glycopeptide antibiotics and methods of making same

Details Desleucyl glycopeptide antibiotics and methods of making same Desleucyl glycopeptide antibiotics and methods of making same

A - Human Necessities

61

K

A61K 38/08 (2006.01) A61K 38/14 (2006.01) C07K 1/107 (2006.01) C07K 7/06 (2006.01) C07K 9/00 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2370782

Compounds that are analogs of glycopeptide antibiotics are disclosed. The compounds have the formula A1-A2-A3-A4-A5-A6-A7 wherein each of the groups A2 to A7 is a modified or unmodified .alpha.-amino acid residue, A1 is optional and, when present, is an organic group other than N-substituted leucine, and at least one of the groups A1 to A7 is linked via a glycosidic bond to one or more glycosidic groups each having one or more sugar residues, wherein at least one of said sugar residues is modified to bear at least one hydrophobic substituent. Methods of making these compounds, compositions including these compounds, and methods of using the compounds to treat infections in a host are also disclosed.

L'invention concerne des composés qui sont des analogues d'antibiotiques glycopeptidiques. Les composés sont représentés par la formule A¿1?-A¿2?-A¿3?-A¿4?-A¿5?-A¿6?-A¿7? dans laquelle chacun des groupes A¿2? à A¿7? est un résidu d'.alpha.-amino acide modifié ou non modifié, A¿1? est facultatif et, lorsqu'il est présent, est un groupe organique autre que la leucine N-substituée, et au moins un des groupes A¿1? à A¿7? est lié, par une liaison glygosidique, à au moins un groupe glycosidique comportant des résidus de sucre, un de ces derniers étant modifié de façon à comporter au moins un substituant hydrophobe. L'invention concerne également des procédés de préparation de ces composés, des compositions renfermant ces derniers, et des procédés d'utilisation de ces composés pour traiter des infections.

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