公开(公告)号：US20190127313A1

公开(公告)日：2019-05-02

申请号：US16094617

申请日：2017-04-21

Applicant: THE UNIVERSITY OF WARWICK

Inventor： Gregory Leonard CHALLIS ,  Daniel John GRIFFITHS ,  Joleen Solange Liesbet MASSCHELEIN

IPC: C07C69/732 ,  C12P7/64 ,  C07C69/738 ,  C07C235/28 ,  A61K31/232 ,  C12P13/02

Abstract: The invention provides novel compounds of formula (I) and their pharmaceutically acceptable salts, metabolites, isomers (e.g. stereoisomers) and prodrugs. Such compounds are effective in the treatment of infections caused by Gram-negative bacteria such as Acinetobacter baumannii. In formula (I), X is O, NR (where R is either H or C1-3 alkyl, e.g. CH3), or CH2; R3 is H, F, CI, Br, I, or CH3; R4 is H, or OH; R5 and R6 are independently selected from H and OH, or R5 and R6 together are ═O; R7 is H, F, CI, Br, I, or CH3; R8 is H, OH, or —OC(O)NR′2 (where each R′ is independently H or C1-3 alkyl, e.g. CH3), preferably R8 is H, OH or —OC(O)NH2; R9 is a 5- or 6-membered, saturated or unsaturated, carbocyclic ring optionally substituted by one or more substituents, or R9 is an optionally substituted straight-chained or branched C1-6 alkyl group (e.g. C1-3 alkyl group); R10 is a straight-chained or branched C1-8 alkyl group (e.g. C1-6 alkyl group), a C4-6 cycloalkyl group, or an optionally substituted aryl or heteroaryl group; and each --- independently represents an optional bond (i.e. each of C2-C3, C4-C5, C6-C7, C8-C9, C10-C11 and C18-C19 are independently either C—C (single) or C═C (double) bonds).