COMPOUNDS FOR SIMULTANEOUSLY INDUCING DEGRADATION OF EGFR AND PARP PROTEINS, PREPARATION METHOD THEREFOR AND USE THEREOF

Title:

COMPOUNDS FOR SIMULTANEOUSLY INDUCING DEGRADATION OF EGFR AND PARP PROTEINS, PREPARATION METHOD THEREFOR AND USE THEREOF

Document Type and Number:

WIPO Patent Application WO/2022/166570

Kind Code:

A1

Abstract:

A series of new-type dual-targeting degradation compounds, which have two independent inhibitor units and an E3 ligase ligand, or a pharmaceutically acceptable salt, hydrate, stereoisomer or prodrug thereof, a preparation method therefor and the use thereof in the preparation of a drug for treating or preventing tumors. The compounds can simultaneously and effectively induce E3 ligase-dependent degradation of EGFR and PARP in pancreatic cancer cell lines and 1299 cells, effectively inhibit the growth of cancer cells, solve the target diversity of advanced cancers in terms of tumor heterogeneity and the reversal of chemotherapy drug resistance, and provide a new form of treatment for treating EGFR- and PARP-mediated tumors and/or other diseases.

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Inventors:

LI HUA (CN)
CHEN LIXIA (CN)
ZHOU YIRONG (CN)
HUO JUNFENG (CN)
LIU YANG (CN)
GU XIAOXIA (CN)
ZHANG WENBO (CN)

Application Number:

PCT/CN2022/072346

Publication Date:

August 11, 2022

Filing Date:

January 17, 2022

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Assignee:

UNIV SHENYANG PHARMACEUTICAL (CN)

International Classes:

C07D417/14; A61K31/517; A61P35/00; C07D401/14; C07D403/14

Foreign References:

CN112939965A	2021-06-11
CN110753693A	2020-02-04
CN111606969A	2020-09-01

Other References:

ZHENG MENGZHU, ET AL: "Rational Design and Synthesis of Novel Dual PROTACs for Simultaneous Degradation of EGFR and PARP", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 64, no. 11, 10 June 2021 (2021-06-10), US , pages 7839 - 7852, XP055955727, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.1c00649
SCHMITT JULIE ET AL: "Design and Synthesis of a Trifunctional Molecular System “Programmed” to Block Epidermal Growth Factor Receptor Tyrosine Kinase, Induce High Levels of DNA Damage, and Inhibit the DNA Repair Enzyme (Poly(ADP-ribose) Polymerase) in Prostate Cancer Cells", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 63, no. 11, 11 June 2020 (2020-06-11), US , pages 5752 - 5762, XP055955744, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.9b02008

Attorney, Agent or Firm:

SHENYANG DONGDA INTELLECTUAL PROPERTY AGENCY CO., LTD (CN)

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