[EN] BACTERIAL TOPOISOMERASE INHIBITORS [FR] INHIBITEURS DE TOPOISOMÉRASE BACTÉRIENNE
摘要:
Disclosed are bacterial topoisomerase inhibitors with antibacterial activity, including against fluoroquinolone-resistant Staphylococcus aureus, comprising structural domains: a) a left-hand side (LHS) usually comprising a fused bicyclic or tricyclic ring system, b) a linker domain, and c) a right-hand side (RHS) comprising an aromatic or heteroaromatic ring, wherein the novel topoisomerase inhibitors do not contain a secondary amine at the start of the RHS, which is the enzyme-binding moiety.
[EN] DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE [FR] DÉGRADATION DE LA TYROSINE KINASE DE BRUTON (BTK) PAR CONJUGAISON D'INHIBITEURS DE BTK AVEC UN LIGAND DE LIGASE E3 ET MÉTHODES D'UTILISATION
摘要:
Disclosed herein are novel bifunctional compounds formed by conjugating BTK inhibitor moieties with E3 ligase Ligand moieties, which function to recruit targeted proteins to E3 ubiquitin ligase for degradation, and methods of preparation and uses thereof.