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1. (WO2018220365) ANTIBIOTIC RESISTANCE BREAKERS

Pub. No.:    WO/2018/220365    International Application No.:    PCT/GB2018/051468
Publication Date: Fri Dec 07 00:59:59 CET 2018 International Filing Date: Thu May 31 01:59:59 CEST 2018
IPC: C07D 498/06
A61P 31/04
A61K 31/4375
Applicants: KING'S COLLEGE LONDON
THE SECRETARY OF STATE FOR HEALTH
Inventors: RAHMAN, Khondaker Mirazur
JAMSHIDI, Shirin
LAWS, Mark Benjamin
NAHAR, Kazi
SUTTON, John Mark
HIND, Charlotte
Title: ANTIBIOTIC RESISTANCE BREAKERS
Abstract:
The invention relates to antibiotic compounds of formula (A1) and pharmaceutically acceptable salts, solvates, tautomers and combinations thereof, wherein X and L are optional linkers and one of RA or R1 comprises Ar1, wherein Ar1 is an antibiotic resistance breaker moiety which comprises an optionally substituted C6-10 aryl, C7-13 aralkyl, C5-10 heteroaryl, C6-13 heteroaralkyl, C5-10 heterocyclyl, C6-13 heterocyclalkyl, C3-10 carbocyclyl, C4-13 carbocyclalkyl, -C(=NR')-NR'R'' or –CH2- CH=CH2 group; wherein after administration of the compound to a bacterial infection this moiety reduces or prevents efflux. The invention also discloses pharmaceutical compositions comprising compounds of formula (A1) and the use of such compounds as medicaments, in particular, to treat bacterial infections, such as drug-resistant bacterial infections.