Title:
PROTEIN DEGRADATION TARGETING COMPOUND, ANTI-TUMOR APPLICATION, INTERMEDIATE THEREOF AND USE OF INTERMEDIATE
Document Type and Number:
WIPO Patent Application WO/2019/196812
Kind Code:
A1
Abstract:
The present disclosure relates to a compound of formula (I), an anti-tumor use thereof, intermediate compounds thereof of formula (III) and formula (IV), and a use thereof. The compound of formula (I) has a degrading effect on a specific target protein, and is mainly composed of three parts: the first part is Small Molecules Binding Protein (SMBP); the second part is a linker unit (LIN); and the third part is a Ubiquitin Ligase Binding Moiety (LUM), wherein SMBP and LIN are covalently bound, and LIN is covalently bound to ULM. The compounds designed and synthesized by the present disclosure have a wide pharmacological activities, have a function of degrading specific proteins and/or inhibiting activities, and can be used for the treatment of associated tumor.
Inventors:
YANG XIAOBAO (CN)
JIANG BIAO (CN)
SUN RENHONG (CN)
REN CHAOWEI (CN)
SUN NING (CN)
KONG YING (CN)
LI YAN (CN)
CHEN JINJU (CN)
YIN QIANQIAN (CN)
SONG XIAOLING (CN)
ZHAO QUANJU (CN)
QIU XING (CN)
JIANG BIAO (CN)
SUN RENHONG (CN)
REN CHAOWEI (CN)
SUN NING (CN)
KONG YING (CN)
LI YAN (CN)
CHEN JINJU (CN)
YIN QIANQIAN (CN)
SONG XIAOLING (CN)
ZHAO QUANJU (CN)
QIU XING (CN)
Application Number:
PCT/CN2019/081840
Publication Date:
October 17, 2019
Filing Date:
April 09, 2019
Export Citation:
Assignee:
UNIV SHANGHAI TECH (CN)
International Classes:
C07D401/14; A61K31/519; A61P35/00; C07D401/04
Domestic Patent References:
| WO2016197032A1 | 2016-12-08 | |||
| WO2017079267A1 | 2017-05-11 |
Foreign References:
| US20180099940A1 | 2018-04-12 | |||
| CN103787802A | 2014-05-14 | |||
| CN106458993A | 2017-02-22 | |||
| CN103396397A | 2013-11-20 |
Other References:
LI, YIMING ET AL.: "A Highly Efficient Cu-Catalyzed S-Transfer Reaction: From Amine to Sulfide", ORGANIC LETTERS, vol. 16, 6 May 2014 (2014-05-06), pages 2692 - 2695, XP055642038, DOI: 10.1021/ol5009747
See also references of EP 3778590A4
See also references of EP 3778590A4
Attorney, Agent or Firm:
SYNCLAW ATTORNEYS (CN)
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