PEPTIDOMIMETIC STAT PROTEIN DEGRADER, COMPOSITION AND USE THEREOF

Title:

PEPTIDOMIMETIC STAT PROTEIN DEGRADER, COMPOSITION AND USE THEREOF

Document Type and Number:

WIPO Patent Application WO/2023/226950

Kind Code:

A1

Abstract:

The present invention relates to a peptidomimetic STAT protein degrader, a composition and a use thereof. Disclosed are a structure represented by general formula (I), or a stereoisomer thereof, or a stereoisomer mixture thereof or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a use thereof as a STAT protein degrader. The inventor of the present invention has confirmed through experiments that the compound of the present invention can degrade a transcription factor STAT3. The compound of the present invention has obvious proliferation inhibitory activity on MOLM16 and SU-DHL-1 tumor cells. The compound of the present invention has good pharmacokinetic properties. In addition, the compound of the present invention has remarkable anti-tumor efficacy in vivo.

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Inventors:

WU YIZHE (CN)
ZHOU XINGLU (CN)
ZHU JIANRONG (CN)
LIU XINGGUO (CN)
HU MIAO (CN)

Application Number:

PCT/CN2023/095625

Publication Date:

November 30, 2023

Filing Date:

May 22, 2023

Export Citation:

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Assignee:

HANGZHOU HEALZEN THERAPEUTICS CO LTD (CN)

International Classes:

C07K5/117; A61K38/07; A61K38/08; A61P35/00; A61P37/04; C07K7/06

Domestic Patent References:

WO2021195481A1	2021-09-30
WO2020205467A1	2020-10-08

Foreign References:

CN114269763A	2022-04-01
CN102317290A	2012-01-11

Other References:

HAIBIN ZHOU, LONGCHUAN BAI, RENQI XU, YUJUN ZHAO, JIANYONG CHEN, DONNA MCEACHERN, KRISHNAPRIYA CHINNASWAMY, BO WEN, LIPENG DAI, PR: "Structure-Based Discovery of SD-36 as a Potent, Selective, and Efficacious PROTAC Degrader of STAT3 Protein", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 62, no. 24, 26 December 2019 (2019-12-26), US , pages 11280 - 11300, XP055701449, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.9b01530

Attorney, Agent or Firm:

HANGZHOU ZHIXIAN PATENT AGENCY (CN)

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