BIFUNCTIONAL CHIMERIC HETEROCYCLIC COMPOUND AND USE THEREOF AS ANDROGEN RECEPTOR DEGRADER

A compound as shown in formula I, or an optical isomer thereof, a solvate thereof, a pharmaceutically acceptable salt thereof, a prodrug thereof, a tautomer thereof, a mesomer thereof, a racemate thereof, an enantiomer thereof, a diastereomer thereof, a mixture form thereof, a metabolite thereof, a...

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Hauptverfasser: DUAN, Jingyi, FU, Yiwei, ZHANG, Shaohua, DU, Wu, GUAN, Yikai, WEN, Kun, QIN, Dekun, CHEN, Muyang, LIU, Shijuan, LI, Haibo, HE, Jinyun, LI, Xinhai, LV, Haibin, CHEN, Song, LI, Yu, TU, Zhilin
Format: Patent
Sprache:eng ; fre ; ger
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Zusammenfassung:A compound as shown in formula I, or an optical isomer thereof, a solvate thereof, a pharmaceutically acceptable salt thereof, a prodrug thereof, a tautomer thereof, a mesomer thereof, a racemate thereof, an enantiomer thereof, a diastereomer thereof, a mixture form thereof, a metabolite thereof, a metabolic precursor thereof, or an isotope substitute form thereof. TB is a target recognition/binding portion, L is a linking portion, and U is a ubiquitin protease recognition/binding portion, the three portions being connected by means of chemical bonds. The compound can significantly down-regulate mutated androgen receptor (AR) proteins, and has good inhibitory activity on prostate cancer cell lines. The compound of formula I can be used for preparation of a protein degradation targeted chimera for targeted regulation of androgen receptors, and a drug for treating diseases correlated with regulation by androgen receptors, and has particularly good application prospects in drugs for treating prostate cancers and breast cancers.