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1. (WO2018204358) APRAMYCIN DERIVATIVES

Pub. No.:    WO/2018/204358    International Application No.:    PCT/US2018/030447
Publication Date: Fri Nov 09 00:59:59 CET 2018 International Filing Date: Wed May 02 01:59:59 CEST 2018
IPC: A61K 31/7036
A61P 31/04
C07H 15/224
Applicants: WAYNE STATE UNIVERSITY
UNIVERSITAT ZURICH
Inventors: BOTTGER, Erik C.
HOBBIE, Sven N.
VASELLA, Andrea
CRICH, David
SONOUSI, Amr
KATO, Takayuki
QUIRKE, Jonathan
RAJASEKARAN, Parasuraman
SARPE, Vikram Ashok
Title: APRAMYCIN DERIVATIVES
Abstract:
The invention relates to derivatives of apramycin-based aminoglycoside antibacterial drugs modified in positions C5 and/or C6 and O5 and/or O6. The modifications impart favourable properties regarding increased selectivity and retention of activity in the presence of resistance determinants of the AAC(3) class. The invention further relates to said compounds for use in the therapy of bacterial infection by systemic administration, especially in instances where the infection is caused by a pathogen comprising a resistance determinant of the AAC(3) class, in particular AAC(3)-IV.