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Title:
AKR1C3 INHIBITOR OR PHARMACEUTICALLY ACCEPTABLE SALT OF SAME, PREPARATION METHOD FOR SAME, AND USES THEREOF
Document Type and Number:
WIPO Patent Application WO/2021/042411
Kind Code:
A1
Abstract:
Disclosed are an AKR1C3 inhibitor or a pharmaceutically acceptable salt of same, a preparation method for same, and uses thereof. A structural optimization is performed with a nonsteroidal anti-inflammatory medicament, flurbiprofen, serving as a lead compound. Disclosed are the biphenyl AKR1C3 inhibitor as represented by formula (I) and the preparation method therefor. As proven in target activity tests, the compound of the present invention is provided with an activity for significantly inhibiting AKR1C3, can be further developed into a medicament for treating or preventing diseases by inhibiting aldehyde ketone reductase AKR1C3, and lays a molecular foundation for studies on mechanisms related to tumor resistance.

Inventors:
SUN HAOPENG (CN)
HE SIYU (CN)
LIU YANG (CN)
GUO QINGLONG (CN)
FENG FENG (CN)
ZHAO LI (CN)
Application Number:
PCT/CN2019/105880
Publication Date:
March 11, 2021
Filing Date:
September 16, 2019
Export Citation:
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Assignee:
UNIV CHINA PHARMA (CN)
International Classes:
C07C59/64; A61K31/192; A61K31/277; A61K31/4406; A61K31/4409; A61K31/47; A61P35/00; C07C51/353; C07C51/363; C07C51/367; C07C57/58; C07C59/52; C07C63/72; C07C201/12; C07C205/56; C07C253/30; C07C255/57; C07C319/20; C07C323/62; C07D213/55; C07D215/12; C07D215/14
Domestic Patent References:
WO2008112249A12008-09-18
Foreign References:
US20070232589A12007-10-04
CN102844290A2012-12-26
Other References:
OSCAR SASSO ET AL.: "Multitarget fatty acid amide hydrolase/cyclooxygenase blockade suppresses intestinal inflammation and protects against nonsteroidal anti-inflammatory drug-dependent gastrointestinal damage", THE FASEB JOURNAL • RESEARCH COMMUNICATION, vol. 29, 30 June 2015 (2015-06-30), XP055788994
NITLIKAR, LAXMIKANT H: "Synthesis of some new flurbiprofen analogues as anti-inflammatory agents", INDIA ANTI-INFLAMMATORY & ANTI-ALLERGY AGENTS IN MEDICINAL CHEMISTRY, vol. 13, no. 2, 31 December 2014 (2014-12-31), pages 128 - 138, XP009526568, ISSN: 1871-5230, DOI: 10.2174/1871523012666131224110834
ILARIA PERETTO : "Synthesis and Biological Activity of Flurbiprofen Analogues as Selective Inhibitors of beta-Amyloid1-42 Secretion", JOURNAL OF MEDICINAL CHEMISTRY, vol. 48, no. 18, 8 June 2006 (2006-06-08), pages 5705 - 5720, XP002508517
Attorney, Agent or Firm:
NANJING SUGAO PATENT AND TRADEMARK FIRM (ORDINARY PARTNERSHIP) (CN)
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