US 9,957,249 B2 · Saturated nitrogen and N-acylated heterocycles potentiating the activity of an active antibiotic against Mycobacteria

Abstract

The present invention concerns a compound of general formula (I): in which n=0 or 1, R1 represents an optionally substituted alkyl chain, in particular substituted alkyl chain, in particular substituted with fluorine, X is chosen from N and CH, and R2 is chosen from optionally substituted phenyl and benzyl, wherein the heterocycles having 6 vertices comprise one, two or three nitrogen atoms. The present invention also concerns the use of this compound as a medicament, in particular in the treatment of bacterial and mycobacterial infections such as tuberculosis in combination with an antibiotic that is active against bacteria and/or mycobacteria, said compound potentiating the activity of said antibiotic.

Claims20

Dependent claims

A compound of formula (I):

in which:
n is 0 or 1;
R1 is selected from the group consisting of —CH2CF3 and —CH2CH2CF3;
X is N or CH;
R2 is selected from the group consisting of phenyl, benzyl, phenyl substituted by linear or branched C1-C4 alkyl, benzyl substituted by linear or branched C1-C4 alkyl, phenyl substituted by linear or branched C1-C4 alkyl substituted by fluorine, benzyl substituted by linear or branched C1-C4 alkyl substituted by fluorine, phenyl substituted by one or more substituent selected from Cl, F, CF3, OCH3, and OH, and a six-membered heterocycle comprising one, two or three nitrogen atoms.

2 more elements

Dependencies are inferred from the claim text.

Facts

Application

14/653,669Filed 20 Dec 2013

Priority

FR 12 0354821 Dec 2012

Published

US 2015/0307471 A129 Oct 2015

Granted

1 May 2018

Term ends

Not estimatedThe source records don’t support an estimate.

Classification17 codes

C07D 401/04
Containing two hetero rings: directly linked by a ring-member-to-ring-member bond
A61K 31/40
Having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins: having five-membered rings with one nitrogen as the only ring hetero atom,…
A61K 31/451
Non condensed piperidines, e.g. piperocaine: having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine,…
A61K 31/4545
Containing further heterocyclic ring systems: containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine

Saturated nitrogen and N-acylated heterocycles potentiating the activity of an active antibiotic against Mycobacteria

Life of this patent

Saturated nitrogen and N-acylated heterocycles potentiating the activity of an active antibiotic against Mycobacteria

Life of this patent

Abstract

Claims20