Title:
BIFUNCTIONAL COMPOUND, PREPARATION METHOD THEREFOR, AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2021/180160
Kind Code:
A1
Abstract:
The present invention relates to a bifunctional compound, a preparation method therefor, and a use thereof, wherein the bifunctional compound comprises an E3 ubiquitin ligase-binding moiety; a target protein-binding moiety that binds to an androgen receptor; and a linking moiety that links the E3 ubiquitin ligase-binding moiety and the target protein-binding moiety. The bifunctional compound of the present application allows the androgen receptor to be positioned adjacent to the ubiquitin ligase, so as to achieve the degradation or inhibition of the androgen receptor.
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Inventors:
TONG YOUZHI (US)
Application Number:
PCT/CN2021/080167
Publication Date:
September 16, 2021
Filing Date:
March 11, 2021
Export Citation:
Assignee:
SUZHOU KINTOR PHARMACEUTICALS INC (CN)
International Classes:
A61K31/513; C07D233/86; A61K31/519; A61K45/06; A61K47/55; A61K47/62; A61K47/66; A61P11/06; A61P35/00; A61P37/02; C07D401/04; C07D471/10; C07D491/107
Domestic Patent References:
| WO2020142228A1 | 2020-07-09 | |||
| WO2017176708A1 | 2017-10-12 | |||
| WO2019023553A1 | 2019-01-31 | |||
| WO2019148055A9 | 2019-09-26 | |||
| WO2016197114A1 | 2016-12-08 |
Foreign References:
| CN110903345A | 2020-03-24 | |||
| CN110506039A | 2019-11-26 | |||
| CN107428734A | 2017-12-01 | |||
| CN106458993A | 2017-02-22 | |||
| CN108136044A | 2018-06-08 | |||
| CN108137507A | 2018-06-08 | |||
| CN110612297A | 2019-12-24 | |||
| CN110545853A | 2019-12-06 | |||
| US20170281784A1 | 2017-10-05 | |||
| CN202010165789A | 2020-03-11 | |||
| CN202011593015A | 2020-12-29 | |||
| CN202110246427A | 2021-03-05 |
Other References:
XIN HAN ET AL.: "Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer", JOURNAL OF MEDICINAL CHEMISTRY, vol. 62, no. 2, 10 January 2019 (2019-01-10), XP055658551, DOI: 10.1021/acs.jmedchem.8b01631
CAS , no. 13311-84-7
J. MED. CHEM., vol. 62, no. 2, 2019, pages 941 - 964
CAS , no. 13311-84-7
J. MED. CHEM., vol. 62, no. 2, 2019, pages 941 - 964
Attorney, Agent or Firm:
UNITALEN ATTORNEYS AT LAW (CN)
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