US 2020/0048187 A1 · LIPOPEPTIDE COMPOUNDS FOR THE TREATMENT OF PAIN DISORDERS

Lipopeptide compounds for the treatment of pain disorders

AssigneesInserm (Institut National De La Sante Et De La Recherche Medicale), Universite Paul Sabatier Toulouse III, Centre National de la Recherche Scientifique (CNRS), Centre Hospitalier Universitaire De Toulouse, Ecole Nationale Veterinaire De Toulouse

InventorsNicolas CENAC, Justine BERTRAND-MICHEL, Teresa PEREZ-BEREZO, Thierry DURAND, Jean-Marie GALANO, Julien PUJO, Eric OSWALD, Patricia MARTIN, Pauline LE FAOUDER, Alexandre GUY

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Abstract

The invention is based on the discovery of a new bacterial compound with analgesic properties which could be used as a new tool for the treatment of pain disorders such as visceral pain. Studying the mechanisms implicated in analgesic properties of the probiotic Escherichia coli strain Nissle 1917 (EcN), inventors characterized, the amino fatty acids produced by EcN, which display the Ecn analgesic properties. One of these compounds inhibits the hypersensitivity to colorectal distension induced by capsaicin, which is a very powerful nociceptive compound and acts via the GABA B receptor. Furthermore, inventors demonstrate that this compound is able to cross the cellular epithelial barrier (such as the intestinal epithelium). Thus, the invention relates to a lipopetide compound, derived from gamma-aminobutyric acid. The invention also relates to a lipopeptide compound according to the invention for the treatment of treating pain disorder, such as somatic pain and visceral pain.

Claims17

Dependent claims

A compound of Formula (I):

RC(O)-Xaa-Xbb-Y, Formula (I)
wherein
R is a C5-C19 linear or branched hydrocarbon chain,
Xaa is asparagine or an equivalent polar and non-charged amino acid selected from the group consisting of serine, threonine and glutamine,
Xbb is a gamma-aminobutyric acid, and
Y is —OH or NH2,
or a pharmaceutical acceptable salt thereof.

4 more elements

Dependencies are inferred from the claim text.

Facts

Application

16/607,772Filed 27 Apr 2018

Priority

EP 17305481.828 Apr 2017

Published

13 Feb 2020

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Classification5 codes

C07C 233/47
With the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom: having the carbon atom of…
C07C 237/22
Having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton: having nitrogen atoms of amino groups…
A61P 29/00
Non-central analgesic, antipyretic or antiinflammatory agents
C07C
Acyclic or carbocyclic compounds