Title:
TARGETING CHIMERIC COMPOUND, PHARMACEUTICAL COMPOSITION COMPRISING SAME, PREPARATION METHOD THEREFOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/161166
Kind Code:
A1
Abstract:
A targeting chimeric compound, a pharmaceutical composition comprising same, a preparation method therefor and use thereof. The targeting chimeric compound is as represented by general formula (I), and each substituent in the general formula (I) is the same as defined in the description. Compared with fulvestrant in the prior art, the targeting chimeric compound has comparable or even better proliferative inhibitory activity on estrogen receptor α in mutant drug-resistant cells, and thus is expected to show a comparable or even better therapeutic effect on therapy.
Inventors:
WU LIANG (CN)
DENG YIJUN (CN)
DENG YIJUN (CN)
Application Number:
PCT/CN2022/071534
Publication Date:
August 04, 2022
Filing Date:
January 12, 2022
Export Citation:
Assignee:
JIANGSU YAHONG MEDITECH CO LTD (CN)
ASIERIS PHARMACEUTICALS SHANGHAI CO LTD (CN)
ASIERIS PHARMACEUTICALS SHANGHAI CO LTD (CN)
International Classes:
C07D417/14; A61K31/381; A61K31/427; A61P5/30; A61P35/00; C07D409/12; C07D409/14
Foreign References:
| CN110612297A | 2019-12-24 | |||
| CN105452244A | 2016-03-30 | |||
| CN112041307A | 2020-12-04 | |||
| CN1753676A | 2006-03-29 | |||
| US20160045607A1 | 2016-02-18 | |||
| CN110291087A | 2019-09-27 |
Other References:
RICHARDSON, T.I. FRANK, S.A. WANG, M. CLARKE, C.A. JONES, S.A. YING, B.P. KOHLMAN, D.T. WALLACE, O.B. SHEPHERD, T.: "Structure-activity relationships of SERMs optimized for uterine antagonism and ovarian safety", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ELSEVIER, AMSTERDAM NL, vol. 17, no. 13, 1 July 2007 (2007-07-01), Amsterdam NL , pages 3544 - 3549, XP022114536, ISSN: 0960-894X, DOI: 10.1016/j.bmcl.2007.04.044
GHEREZGHIHER, T. B. ET AL.,: "The naphthol selective estrogen receptor modulator (SERM), LY2066948, is oxidized to an o-quinone analogous to the naphthol equine estrogen, equilenin,", CHEMICO-BIOLOGICAL INTERACTIONS, vol. 196, 28 January 2012 (2012-01-28), XP028478732, DOI: 10.1016/j.cbi.2012.01.004
ROBERTS BRETT L., MA ZHI-XIONG, GAO ANG, LEISTEN ERIC D., YIN DAN, XU WEI, TANG WEIPING: "Two-Stage Strategy for Development of Proteolysis Targeting Chimeras and its Application for Estrogen Receptor Degraders", ACS CHEMICAL BIOLOGY, vol. 15, no. 6, 19 June 2020 (2020-06-19), pages 1487 - 1496, XP055953688, ISSN: 1554-8929, DOI: 10.1021/acschembio.0c00140
JIANTAO HU, BIAO HU, MINGLIANG WANG, FUMING XU, BUKEYAN MIAO, CHAO-YIE YANG, MI WANG, ZHAOMIN LIU, DANIEL F. HAYES, KRISHNAPRIYA C: "Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER)", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 62, no. 3, 14 February 2019 (2019-02-14), US , pages 1420 - 1442, XP055672912, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.8b01572
GHEREZGHIHER, T. B. ET AL.,: "The naphthol selective estrogen receptor modulator (SERM), LY2066948, is oxidized to an o-quinone analogous to the naphthol equine estrogen, equilenin,", CHEMICO-BIOLOGICAL INTERACTIONS, vol. 196, 28 January 2012 (2012-01-28), XP028478732, DOI: 10.1016/j.cbi.2012.01.004
ROBERTS BRETT L., MA ZHI-XIONG, GAO ANG, LEISTEN ERIC D., YIN DAN, XU WEI, TANG WEIPING: "Two-Stage Strategy for Development of Proteolysis Targeting Chimeras and its Application for Estrogen Receptor Degraders", ACS CHEMICAL BIOLOGY, vol. 15, no. 6, 19 June 2020 (2020-06-19), pages 1487 - 1496, XP055953688, ISSN: 1554-8929, DOI: 10.1021/acschembio.0c00140
JIANTAO HU, BIAO HU, MINGLIANG WANG, FUMING XU, BUKEYAN MIAO, CHAO-YIE YANG, MI WANG, ZHAOMIN LIU, DANIEL F. HAYES, KRISHNAPRIYA C: "Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER)", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 62, no. 3, 14 February 2019 (2019-02-14), US , pages 1420 - 1442, XP055672912, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.8b01572
Attorney, Agent or Firm:
GE CHENG & CO., LTD (CN)
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