公开(公告)号：US20240140991A1

公开(公告)日：2024-05-02

申请号：US18263335

申请日：2021-11-30

Applicant: THE QUEEN'S UNIVERSITY OF BELFAST ,  UNIVERSITEIT LEIDEN

Inventor： Stephen COCHRANE ,  Ross BALLANTINE ,  Nathaniel MARTIN ,  Karol AL AYED ,  Michael HOEKSTRA ,  Sofia Denise Zamarbide LOSADA

IPC: C07K7/64 ,  A61P31/04 ,  C07K7/08

CPC classification number: C07K7/64 ,  A61P31/04 ,  C07K7/08 ,  A61K38/00

Abstract: A compound of formula (I) or formula (II) including tautomeric or stereochemically isomeric forms thereof, wherein: R1 represents C1-20 alkyl, C2-20 alkenyl, C6-20 aryl, or C4-20 heterocyclyl, each optionally substituted with one or more Y groups, R2a to R2l each independently represents H, C1-10 alkyl, C2-10 alkenyl, C6-12 aryl, or C4-12 heterocyclyl, each optionally substituted with one or more Y groups, R3 represents H, C1-10 alkyl, C2-10 alkenyl, C6-12 aryl, or C4-12 heterocyclyl, each optionally substituted with one or more Y groups, X represents NH, S or O, each Y independently represents cyano, halogen, N3, —C(O)RZ, —C(0)0Rz, —0C(0)Rz, —C(0)NHZ, —NHC(O)Rz, —NHC(0)NHRZ, —NHC(NH)NHRZ, —NCH(0)0Rz, -0C(0)NHRz, -0S(0)2RZ, —S(0)2NHRZ, —NHS(0)2RZ, —SRZ, —NRZZ or —ORz and each Rz independently represents H, C1-10 alkyl, C2-10 alkenyl, C6-10 aryl, or C4-10 heterocyclyl; or an N-oxide thereof or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof; and wherein formula (I) excludes laterocidine, wherein formula (I) excludes relacidine A, and wherein formula (I) excludes relacidine B. A pharmaceutical composition comprising the compound. The compounds and pharmaceutical compositions are useful as antibiotics.