BIFUNCTIONAL CHIMERIC HETEROCYCLIC COMPOUND AND USE THEREOF AS ANDROGEN RECEPTOR DEGRADER

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United States of America

APP PUB NO 20250051347A1
SERIAL NO

18293289

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Abstract

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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.

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Patent Owner(s)

  • HINOVA PHARMACEUTICALS INC.

International Classification(s)

Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Chen, Muyang Chengdu, CN 1 0
Chen, Song Chengdu, CN 164 1006
Du, Wu Chengdu, CN 29 43
Duan, Jingyi Chengdu, CN 3 1
Fu, Yiwei Chengdu, CN 5 2
Guan, Yikai Chengdu, CN 1 0
He, Jinyun Chengdu, CN 5 0
Li, Haibo Chengdu, CN 146 844
Li, Xinghai Chengdu, CN 47 254
Li, Yu Chengdu, CN 376 3295
Liu, Shijuan Chengdu, CN 1 0
Lv, Haibin Chengdu, CN 7 8
Qin, Dekun Chengdu, CN 7 8
Tu, Zhilin Chengdu, CN 6 9
Wen, Kun Chengdu, CN 8 0
Zhang, Shaohua Chengdu, CN 42 169

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