Compounds

Patent metadata

Field	Value
Publication number	US-11969423-B2
Application number	US-201816639246-A
Country	US
Kind code	B2
Filing date	Aug 15, 2018
Priority date	Aug 16, 2017
Publication date	Apr 30, 2024
Grant date	Apr 30, 2024

Abstract

The invention relates to compounds of Formula (I) and their use in therapy, for example in the treatment of mycobacterial infections or in the treatment of diseases caused by mycobacterium, such as tuberculosis.

First claim

The invention claimed is:

1. A combination comprising:
a compound, wherein the compound is 4,4,4-trifluoro-1-(4-(2-(trifluoromethyl)pyridin-4-yl)piperidin-1-yl)butan-1-one having the following structure:

or a pharmaceutically acceptable salt thereof;
at least one anti-tuberculosis agent selected from isoniazid, rifampin, pyrazinamide, ethambutol, moxifloxacin, rifapentine, clofazimine, ethionamide, prothionamide, isoxyl, thiacetazone, rifabutin, a diarylquinoline, nitroimidazo-oxazine PA-824, delamanid (OPC-67683), an oxazolidinone, EMB analogue SQ109, OPC-167832, GSK3036656 (also known as GSK070), GSK2556286, GSK3211830, a benzothiazinone, an azaindole, a dinitrobenzamide, and a beta-lactam; and
at least one anti-viral agent selected from zidovudine, didanosine, lamivudine, zalcitabine, abacavir, stavudine, adefovir, adefovir dipivoxil, fozivudine, todoxil, emtricitabine, alovudine, amdoxovir, elvucitabine, nevirapine, delavirdine, efavirenz, loviride, immunocal, oltipraz, capravirine, lersivirine, GSK2248761, TMC-278, TMC-125, etravirine, saquinavir, ritonavir, indinavir, nelfinavir, amprenavir, fosamprenavir, brecanavir, darunavir, atazanavir, tipranavir, palinavir, lasinavir, enfuvirtide, T-20, T-1249, PRO-542, PRO-140, TNX-355, BMS-806, BMS-663068, BMS-626529, 5-Helix, raltegravir, elvitegravir, GSK1349572, GSK1265744, vicriviroc (Sch-C), Sch-D, TAK779, maraviroc, TAK449, didanosine, tenofovir, lopinavir, and darunavir.

2. The combination of claim 1 , wherein the composition is suitable for intravenous delivery.

3. The combination of claim 1 , wherein the composition is an inhalable formulation.

4. The combination of claim 1 , wherein the diarylquinoline comprises bedaquiline (TMC207) or TBAJ-587, the oxazolidinone comprises linezolid, tedizolid, radezolid, sutezolid (PNU-100480), posizolid (AZD-5847) or TBI-223, the benzothiazinone comprises BTZ043 or PBTZ169, the azaindole comprises TBA-7371, and the beta-lactam comprises meropenem, faropenem, ertapenem, tebipenem, or a beta-lactam combination.

Assignees

• Glaxosmithkline Ip Dev Ltd
• BioVersys AG

Inventors

• Porras De Francisco Esther
• Remuiñan-Blanco Modesto Jesús
• Bourotte Marilyne
• Deprez Benoit
• Willand Nicolas

Classifications

• A61K31/497 Primary

  containing further heterocyclic rings · CPC title

• A61K31/4545

  containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine · CPC title

• A61K31/501

  not condensed and containing further heterocyclic rings · CPC title

• A61K31/506

  not condensed and containing further heterocyclic rings · CPC title

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title