Chemical joint

Heterobifunctional chemical linkers useful in protein degrading agents and other pharmaceutical chemistry uses are provided. The isobifunctional joint comprises an alkyne-piperidine joint and an alkane-piperidine joint; an alkane-piperazine linker; an alkylamino PEGylation linker; a dipiperazine lin...

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Main Authors WILKE KLAUS, DEOKAR RAJENDRA C, SINHA SAURABH, SINGH RAVINDRA VIR, PRASAD, DILIP, GUCHAI, PERRY, S, AKULA VENKATA GANESH, MADI SAMIR
Format Patent
LanguageChinese
English
Published 02.08.2024
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Summary:Heterobifunctional chemical linkers useful in protein degrading agents and other pharmaceutical chemistry uses are provided. The isobifunctional joint comprises an alkyne-piperidine joint and an alkane-piperidine joint; an alkane-piperazine linker; an alkylamino PEGylation linker; a dipiperazine linker; a piperazine-pyridine/pyrimidine-alkyne linker; a pyridine-PEG-piperazine joint and a pyrimidine-piperazine-PEG joint are adopted as the main components. Also provided are combinations of the provided linkers with ligands that target degradation pathways, such as E3 ubiquitin ligases. 提供了可用于蛋白质降解剂和其它药物化学用途的异双功能化学接头。该异双功能接头包括炔烃-哌啶和烷烃-哌啶接头；烷烃-哌嗪接头；烷氨基PEG化接头；二哌嗪接头；哌嗪-吡啶/嘧啶-炔烃接头；吡啶-PEG-哌嗪接头和嘧啶-哌嗪-PEG接头。还提供了所提供的接头与靶向降解途径(如E3泛素连接酶)的配体的组合。
Bibliography:Application Number: CN20228084778