Title:
BRD4 INHIBITOR, PREPARATION METHOD AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2020/020308
Kind Code:
A1
Abstract:
Provided are a compound as depicted in formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof; Experimental results show that the compound provided has a good inhibitory effect on the proliferation of human prostate cancer cells CWR22RV1 and breast cancer cells; and combined use of the compound with an androgen receptor inhibitor HC-1119 significantly enhances the inhibitory effect on prostate cancer cells, and the inhibitory effect increases with increased concentration. The compound provided by the present specification can not only be used independently to prepare an antineoplastic agent, but can also be used in combination with other agents having antineoplastic effects, such as an androgen receptor inhibitor, or other targeting drugs etc., to prepare an antineoplastic agent having stronger therapeutic effects, especially an agent for treating prostate cancer and breast cancer.
Inventors:
FAN LEI (CN)
WANG FEI (CN)
WU XIAOQUAN (CN)
XU KEXIN (CN)
CHEN KE (CN)
LUO TONGCHUAN (CN)
ZHANG SHAOHUA (CN)
HUO YONGXU (CN)
TU ZHILIN (CN)
LI XINGHAI (CN)
CHEN YUANWEI (CN)
WANG FEI (CN)
WU XIAOQUAN (CN)
XU KEXIN (CN)
CHEN KE (CN)
LUO TONGCHUAN (CN)
ZHANG SHAOHUA (CN)
HUO YONGXU (CN)
TU ZHILIN (CN)
LI XINGHAI (CN)
CHEN YUANWEI (CN)
Application Number:
PCT/CN2019/097776
Publication Date:
January 30, 2020
Filing Date:
July 25, 2019
Export Citation:
Assignee:
HINOVA PHARMACEUTICALS INC (CN)
International Classes:
C07D471/04; A61K31/407; A61P31/18; A61P35/00; C07D487/04
Domestic Patent References:
| WO2015081203A1 | 2015-06-04 | |||
| WO2018130174A1 | 2018-07-19 |
Foreign References:
| CN104136435A | 2014-11-05 | |||
| CN106986872A | 2017-07-28 | |||
| CN106414442A | 2017-02-15 | |||
| CN105518007A | 2016-04-20 | |||
| CN107207493A | 2017-09-26 |
Other References:
MOL. CELL, vol. 19, 2005, pages 523 - 534
DEVAIAH ET AL., RROC. NAT. ACAD. SCI., USA, vol. 109, 2012, pages 6927 - 6932
CHEN CHONG ET AL.: "The effect of BRD4 inhibitor GSK525762A on the proliferation and apoptosis of acute B lymphocytic leukemia cells and its possible mechanism", NATIONAL LYMPHATIC TUMOR DIAGNOSIS AND TREATMENT PROGRESS SEMINAR, 2014
NI PING ET AL.: "Journal of Nanjing Medical University", 2015, article "The inhibitory effect of BRD4 inhibitor JQ 1 on the growth of non-small cell lung cancer"
See also references of EP 3831828A4
DEVAIAH ET AL., RROC. NAT. ACAD. SCI., USA, vol. 109, 2012, pages 6927 - 6932
CHEN CHONG ET AL.: "The effect of BRD4 inhibitor GSK525762A on the proliferation and apoptosis of acute B lymphocytic leukemia cells and its possible mechanism", NATIONAL LYMPHATIC TUMOR DIAGNOSIS AND TREATMENT PROGRESS SEMINAR, 2014
NI PING ET AL.: "Journal of Nanjing Medical University", 2015, article "The inhibitory effect of BRD4 inhibitor JQ 1 on the growth of non-small cell lung cancer"
See also references of EP 3831828A4
Attorney, Agent or Firm:
GAOYUNG INTELLECTUAL PROPERTY AGENCY (GENERAL PARTNERSHIP) (CN)
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