New macrolides with antibacterial activity

Details New macrolides with antibacterial activity New macrolides with antibacterial activity

C - Chemistry, Metallurgy

07

H

C07H 17/08 (2006.01) A61K 31/7048 (2006.01) A61P 31/04 (2006.01)

Patent

CA 2419296

The invention provides new macrolides antibiotics of formula (I) with improved biological properties and improved stability formula (I): wherein R1 is hydrogen, cyano, -S(L)mR2, -S(O)(L)mR2, or -S(O)2(L)mR2; L represents -(CH2)n- or -(CH2)nZ(CH2)n'-; m is 0 or 1; n is 1, 2, 3, or 4; n' is 0, 1, 2, 3, or 4; Z is O, S or NH; R2 is hydrogen, alkyl, heterocyclyl or aryl; which heterocyclyl and the aryl groups may be further substituted; * indicates a chiral center which is in the (R) or (S) form and pharmaceutically acceptable acid addition salts or in vivo cleavable esters thereof.

L'invention concerne de nouveaux antibiotiques macrolides selon la formule (I). Ces antibiotiques présentent des propriétés biologiques améliorées et une stabilité supérieure. Dans la formule (I), R?1¿ représente hydrogène, cyano, -S(L)¿m?R?2¿, -S(O)(L)¿m?R?2¿, ou -S(O)¿2?(L)¿m?R?2¿; L représente -(CH¿2?)¿n?- ou -(CH¿2?)¿n?Z(CH¿2?)¿n'?-; m représente 0 ou 1; n est 1, 2, 3, ou 4; n' est 0, 1, 2, 3, ou 4; Z représente O, S ou NH; R2 représente hydrogène, alkyle, hétérocyclyle ou aryle, lequel hétérocyclyle et les groupes aryle peuvent être davantage substitués; * représente un centre chiral qui se présente sous forme (R) ou (S) et des sels d'addition acides pharmaceutiquement acceptables ou des esters clivables in vivo de ces derniers.

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