Title:
A CLASS OF BIFUNCTIONAL CHIMERIC HETEROCYCLIC COMPOUNDS FOR TARGETED DEGRADATION OF ANDROGEN RECEPTORS AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2020/211822
Kind Code:
A1
Abstract:
The present invention relates to a class of bifunctional chimeric heterocyclic compounds for targeted degradation of androgen receptors and use thereof, and specifically provides a compound shown in formula (I), or an isotopic compound thereof, or an optical isomer thereof, or a tautomer thereof, or a pharmacologically acceptable salt thereof, or a prodrug thereof, or a solvate thereof, wherein ARB is an androgen receptor recognition/binding part, L is a link part, and U is a ubiquitin protease recognition/binding part; and the three parts are connected by means of chemical bonds. The compound can perform targeted degradation on androgen receptors in prostate cancer cells, and suppress proliferation of the prostate cancer cells, and also show good metabolic stability and pharmacokinetic properties. The compound has good application prospect in preparation of targeted chimeras for protein degradation of androgen receptors and in the preparation of drugs for treating related diseases regulated by the androgen receptors.
Inventors:
DU WU (CN)
WEN KUN (CN)
FU YIWEI (CN)
LV HAIBIN (CN)
HE JINYUN (CN)
QIN DEKUN (CN)
LI YU (CN)
DUAN JINGYI (CN)
LI YONG (CN)
AI CHAOWU (CN)
TU ZHILIN (CN)
CHEN YUANWEI (CN)
LI XINGHAI (CN)
WEN KUN (CN)
FU YIWEI (CN)
LV HAIBIN (CN)
HE JINYUN (CN)
QIN DEKUN (CN)
LI YU (CN)
DUAN JINGYI (CN)
LI YONG (CN)
AI CHAOWU (CN)
TU ZHILIN (CN)
CHEN YUANWEI (CN)
LI XINGHAI (CN)
Application Number:
PCT/CN2020/085201
Publication Date:
October 22, 2020
Filing Date:
April 16, 2020
Export Citation:
Assignee:
HINOVA PHARMACEUTICALS INC (CN)
International Classes:
C07D403/12; A61K31/4439; A61P35/00; C07D239/42; C07D401/14; C07D411/12
Domestic Patent References:
| WO2018071606A1 | 2018-04-19 | |||
| WO2019023553A1 | 2019-01-31 | |||
| WO2012145361A1 | 2012-10-26 |
Foreign References:
| CN107428734A | 2017-12-01 | |||
| CN108137507A | 2018-06-08 | |||
| US20180099940A1 | 2018-04-12 | |||
| US20170327469A1 | 2017-11-16 |
Other References:
See also references of EP 3957633A4
Attorney, Agent or Firm:
GAOYUNG INTELLECTUAL PROPERTY AGENCY (GENERAL PARTNERSHIP) (CN)
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