NOVEL 12-EPI-MUTILIN COMPOUNDS AND USES THEREOF
A compound of formula (I) wherein R 1 is wherein A is hydrogen atom or a (C 1-6 )alkyl, and wherein any Q is independently from each other a nitrogen atom or CH, wherein R 2 is the compound for use as a medicament and a pharmaceutical composition comprising the compound as well as a method of treatment or prevention a disease mediated by microbes making use thereof.
1 . A compound of formula (1)
wherein R 1 is
wherein A is a hydrogen atom or a (C 1-6) alkyl, and
wherein any Q is independently from each other a nitrogen atom or CH,
wherein R 2 is
2 . The compound according to claim 1 , wherein A is a (C 1-3 )alkyl selected from the group consisting of methyl, ethyl, 1-propyl, 2-propyl, and cyclopropyl.
3 . The compound according to claim 1 , wherein the compound is a compound of formula (II)
wherein A and Q are defined as in claim 1 .
4 . The compound according to claim 1 , wherein the compound is selected from the group consisting of compounds of formula (III), (IV) and (V)
5 . The compound according to claim 1 , wherein the compound is in the form of a salt and/or solvate.
6 .- 12 . (canceled)
13 . A pharmaceutical drug composition comprising a compound of claim 1 and at least one pharmaceutical excipient.
14 . The pharmaceutical drug composition according to claim 13 , further comprising an additional pharmaceutically active agent.
15 . A method of treatment or prevention of a disease mediated by bacteria, the method comprising a step of administering to a subject in need thereof a therapeutically effective amount of a compound of claim 1 .
16 . The compound according to claim 1 , wherein A is methyl.
17 . The compound according to claim 1 , wherein the compound is in the form of a dihydrochloride salt.
18 . The method according to claim 15 , wherein the disease is a bacterial infection.
19 . The method according to claim 15 , wherein the disease is mediated by Gram-positive bacteria selected from the group consisting of: staphylococci, streptococci, enterococci, clostridia, peptostreptococci, cutibacteria, Listeria monocytogenes, Eubacterium lentum, Finegoldia magna, Anaerococcus prevotii, Peptoniphilus assaccharolyticus , and combinations thereof.
20 . The method according to claim 15 , wherein the disease is mediated by bacteria selected from the group consisting of staphylococci, streptococci, and combinations thereof.
21 . The method according to claim 15 , wherein the disease is mediated by Gram-negative bacteria selected from the group consisting of: moraxella, haemophilus, chlamydiae, neisseriaceae, Mycoplasma spp., fusobacteria, Prevotella spp., Porphyromonas spp., legionella, spirochetes (bacteria selected from phylum of spirochaetes), Bacteroides fragilis, Acinetobacter lwoffii , and combinations thereof.
22 . The method according to claim 15 , wherein the disease is mediated by bacteria resistant to Lefamulin.
23 . The method according to claim 22 , wherein the bacteria has a Lefamulin resistance mediated by vga(A), Isa(E) or cfr.
24 . The method according to claim 15 , wherein the disease is selected from the group consisting of: a respiratory tract infection, an infection of skin and/or soft tissue, a systemic infection, a prosthetic joint infection, a sexually transmitted infection, acne, Lyme Disease, relapsing fever, and combinations thereof.