Esters of carbapenems

Details Esters of carbapenems Esters of carbapenems

C - Chemistry, Metallurgy

07

D

C07D 477/14 (2006.01) A61K 31/415 (2006.01) A61K 31/695 (2006.01) C07D 477/08 (2006.01) C07F 7/10 (2006.01)

Patent

CA 2217885

A compound of general formula (I) in which R is (a); wherein R.alpha. is hydrogen, optionally substituted (C1-6)alkyl or optionally substituted aryl; R.beta. is hydrogen, optionally substituted (C1-6)alkyl or optionally substituted aryl; or R.alpha. and R.beta. together form an optionally substituted 5 or 6 membered heterocyclic ring with or without additional heteroatoms; R1 is (C1-6)alkyl which is unsubstituted or substituted by fluoro, a hydroxy group which is optionally protected by a readily removable hydroxy protecting group, or by an amino group which is optionally protected by a readily removable amino protecting group; R2 is hydrogen or methyl; and R3 is selected from the group consisting of (a) a group of formula (i) wherein R1 is hydrogen or (C1-6)alkyl, R2 is hydrogen, (C1-6)alkyl optionally substituted by halogen, (C1-6)alkenyl, (C1-6)alkoxycarbonyl, aryl, or heteroaryl, R3 is hydrogen, (C1-6)alkyl, or (C1-6)alkoxycarbonyl, and R4 is a pharmaceutically acceptable ester forming group, and (b) a group of formula CH(Ra)O.CO.Rb, wherein Ra is hydrogen, (C1-6)alkyl, (C3-7)cycloalkyl, methyl, or phenyl; and Rb is (C1-6)alkyl(C3-7)cycloalkyloxy or (C1-6)alkoxy(C1- 6)alkyl, is useful in the treatment of bacterial infections.

L'invention porte sur un composé s'avérant utile pour le traitement d'affections bactériennes de formule générale (I) dans laquelle R est (a) et où R?.alpha.¿ est hydrogène, C¿1-6? alkyle facultativement substitué ou aryle facultativement substitué; R?.beta.¿ est hydrogène, C¿1-6? alkyle facultativement substitué ou aryle facultativement substitué; R?.alpha.¿ et R?.beta.¿ forment ensemble un noyau hétérocyclique à 5 ou 6 éléments avec ou sans hétéroatomes additionnels, R?1¿ est C¿1-6? alkyle substitué ou non par fluoro, un groupe hydroxy facultativement protégé par un groupe protecteur hydroxy facilement retirable ou un groupe amino facultativement protégé par un groupe protecteur amino facilement retirable, R?2¿ est hydrogène ou méthyle et R?3¿ est sélectionné:(a) dans un groupe de formule (i) où R?1¿ est hydrogène ou C¿1-6? alkyle, R?1¿ est hydrogène, C¿1-6? alkyle facultativement substitué par halogène, C¿1-6? alcényle, C¿1-6? alkoxycarbonyle, aryle ou hétéroaryle, R?3¿ est hydrogène, C¿1-6? alkyle, C¿1-6? alkoxycarbonyle; et R?4¿ est un groupe ester pharmacocompatible, et (b): un groupe CH(R?a¿)O.CO.R?b¿ dans lequel R?a¿ est hydrogène, C¿1-6? alkyle, C¿3-7? cycloalkyle, méthyle ou phényle; et R?b¿ est C¿1-6? alkyle, C¿3-7? cycloalkyloxy ou C¿1-6? alkoxy C¿1-6? alkyle.

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