EP4338732A1 — Lefamulin and its derivatives for use in the treatment of tularemia

USPTO Abstract

A compound of formula (I)whereinn is 0 to 4;m is 0 or 1 with the proviso that the sulphur atom and R<sub>3</sub> are in vicinal position (if m = 0 then R<sub>3</sub> is in position 2', and if m = 1 then R<sub>3</sub> is on position 1');R is ethyl or vinyl;R<sub>1</sub> is hydrogen or (C<sub>1-6</sub>)alkyl,R<sub>2</sub> is hydrogen or- (C<sub>3-6</sub>)cycloalkyl, or- unsubstituted (C<sub>1-6</sub>)alkyl, or- (C<sub>1-6</sub>)alkyl substituted by one or more of- hydroxy; preferably one or two,- methoxy,- halogen, and- (C<sub>3-6</sub>)cycloalkyl, orR<sub>1</sub> and R<sub>2</sub> together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring containing at least 1 nitrogen atom or 1 nitrogen and 1 additional heteroatom e. g. selected from N or O, orR<sub>1</sub> is hydroxy and R<sub>2</sub> is formyl;R<sub>3</sub> is OH, OR<sub>4</sub>, a halogen atom, orR<sub>3</sub> is bound to 2' and represents -O-(CH<sub>2</sub>)<sub>p</sub>-O- with p is 2 or 3;R<sub>4</sub> is unsubstituted (C<sub>1-6</sub>)alkyl or (C<sub>3-6</sub>)cycloalkyl,or a pharmaceutically acceptable salt, solvate, prodrug or metabolite thereoffor the specific use in the treatment or prevention of a bacterial infection mediated by F. tularensis.