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Title:
COMPOUND FOR TARGETED DEGRADATION OF BTK AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2019/127008
Kind Code:
A1
Abstract:
Provided in the present invention is a compound, which is a compound of X-Y-Z formula I or a stereoisomer, geometric isomer, tautomer, oxynitride, hydrate, solvate, metabolite, pharmaceutically acceptable salt or prodrug thereof. The compound has a potent degradation activity on wild-type BTK and a good degradation activity on BTK of C481S or C481A mutated BTKs (DC 50<30nM), with no inhibition or degradation activity on other targets such as EGFR, ITK, TEC, etc., and thus has an effect of specifically targeted degradation of BTK protein.

Inventors:
RAO, Yu (QINGHUAYUAN, HAIDIAN DISTRICT, Beijing 4, 100084, CN)
LIU, Wanli (QINGHUAYUAN, HAIDIAN DISTRICT, Beijing 4, 100084, CN)
SUN, Yonghui (QINGHUAYUAN, HAIDIAN DISTRICT, Beijing 4, 100084, CN)
Application Number:
CN2017/118595
Publication Date:
July 04, 2019
Filing Date:
December 26, 2017
Export Citation:
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Assignee:
TSINGHUA UNIVERSITY (QINGHUAYUAN, HAIDIAN DISTRICT, Beijing 4, 100084, CN)
International Classes:
C07D487/04; A61K31/519; A61P35/00; A61P35/02
Domestic Patent References:
WO2017040617A12017-03-09
WO2016174183A12016-11-03
WO2016106381A12016-06-30
Foreign References:
US20120108612A12012-05-03
CN107406454A2017-11-28
Attorney, Agent or Firm:
TSINGYIHUA INTELLECTUAL PROPERTY LLC (Room 301 Trade Building, Zhaolanyuan Tsinghua University, Qinghuayuan, Haidian District, Beijing 4, 100084, CN)
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