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1. (WO2017060418) PROTECTED CARBOXYLIC ACID-BASED METABOLITES FOR THE TREATMENT OF MITOCHONDRIA-RELATED DISEASES

Pub. No.:    WO/2017/060418    International Application No.:    PCT/EP2016/073985
Publication Date: Fri Apr 14 01:59:59 CEST 2017 International Filing Date: Sat Oct 08 01:59:59 CEST 2016
IPC: C07D 317/34
C07D 323/00
C07C 69/38
C07C 235/80
A61K 31/225
A61P 9/00
A61P 35/00
Applicants: NEUROVIVE PHARMACEUTICAL AB
Inventors: MOSS, Steven
ELMÉR, Eskil
HANSSON, Magnus Joakim
EHINGER, Karl Henrik Johannes
KARLSSON, Karl Michael
PIEL, Sarah
Title: PROTECTED CARBOXYLIC ACID-BASED METABOLITES FOR THE TREATMENT OF MITOCHONDRIA-RELATED DISEASES
Abstract:
The present invention provides novel cell-permeable carboxylic acid-based metabolites and cell permeable precursors thereof aimed at increasing ATP-production in mitochondria and thus, for use in medicine. The main part of ATP produced and utilized in the eukaryotic cell originates from mitochondrial oxidative phosphorylation, a process to which high-energy electrons are provided by the Kreb's cycle. Not all Kreb's cycle intermediates are readily permeable to the cellular membrane, one of them being malonate. The provision of the novel cell permeable carboxylic acid- based metabolites is envisaged to allow passage over the cellular membrane and thus the cell permeable metabolite can be used to enhance mitochondrial ATP-output.