IP Library › Granted Patent US 11,059,811
Granted Patent B2
US 11,059,811 · App. 16/935,407 · Granted Jul 13, 2021

Benzofuran derivative, preparation method thereof and use thereof in medicine

Inventors: Biao Lu (Shanghai, CN); Xiaodong Shen (Shanghai, CN); Mingxun He (Shanghai, CN); Dong Liu (Shanghai, CN); Minsheng Zhang (Shanghai, CN)
Assignees: Jiangsu Hengrui Medicine Co., Ltd.; Shanghai Hengrui Pharmaceutical Co., Ltd.
C07D405/14A61K31/4433A61K31/4545A61K31/496A61K31/5377A61P35/00C07D405/12C07D409/14
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Quick Facts
Patent No.
US 11,059,811
App. No.
16/935,407
Granted
Jul 13, 2021
Kind
B2
Abstract

A benzofuran derivative, a preparation method thereof and a use thereof in medicine are described. In particular, a benzofuran derivative as shown by general formula (I), the preparation method thereof, a pharmaceutical composition containing the derivative, and uses thereof as an EZH2 inhibitor and in the prevention and/or treatment of diseases such as tumours and cancers, etc., and in particular, uses thereof in the prevention and/or treatment of non-Hodgkin's lymphoma, diffuse large B-cell lymphoma, follicular lymphoma and synovial sarcoma, are described.

Claims (4)

1. A method for inhibiting EZH2 in a patient in need of thereof, comprising administering to the patient a compound 2 or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising a therapeutically effective amount of the compound 2 or a pharmaceutically acceptable salt thereof

2. A method for treating a tumor or cancer, wherein the tumor or cancer is associated with EZH2 overexpression, comprising administering to a patient in need of thereof a compound 2 or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising a therapeutically effective amount of the compound 2 or a pharmaceutically acceptable salt thereof

3. The method according to claim 2 , wherein the tumor and cancer are selected from the group consisting of lymphoma, leukemia, breast cancer, lung cancer, prostate cancer, ovarian cancer, liver cancer, melanoma, rhabdomyosarcoma, synovial sarcoma, mesothelioma, cervical cancer, colon cancer, rectal cancer, stomach cancer, pancreatic cancer, brain cancer, skin cancer, oral cancer, bone cancer, kidney cancer, bladder cancer, fallopian tube tumor, ovarian tumor, peritoneal tumor, glioma, glioblastoma, head and neck cancer, and myeloma.

4. The method according to claim 3 , wherein the leukemia is chronic myeloid leukemia, acute myeloid leukemia, or mixed lineage leukemia; and the lymphoma is non-Hodgkin's lymphoma, diffuse large B-cell lymphoma, or follicular lymphoma.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 17, 2026
From: SHANGHAI HENGRUI PHARMACEUTICAL CO., LTD.
To: JIANGSU HENGRUI MEDICINE CO., LTD.
Reel/Frame 074190/0860 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 22, 2020
From: LU, BIAO; SHEN, XIAODONG; HE, MINGXUN; LIU, DONG; ZHANG, MINSHENG
To: JIANGSU HENGRUI MEDICINE CO., LTD.; SHANGHAI HENGRUI PHARMACEUTICAL CO., LTD.
Reel/Frame 053283/0704 →
Priority Claims (1)
CN 201510800975.7 · Nov 19, 2015 · national
Continuity (2)
Continuation 15775958
Related Publication 20200354349A1 · Nov 12, 2020
Cited By (1)
US 51,039