Title:
BENZOTHIOPHENE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/109461
Kind Code:
A1
Abstract:
Disclosed in the present invention are a benzothiophene derivative, a preparation method therefor, and a use thereof. The structure of the benzothiophene derivative is as shown in general formula I, and the definition of each substituent is as described in the description and the claims. The benzothiophene derivative of the present invention is used as a selective estrogen receptor antagonist/degradation agent for treating estrogen receptor positive diseases.
Inventors:
YANG YUSHE (CN)
LU ZHENGYU (CN)
ZHANG DAN (CN)
CAO YANGZHI (CN)
LU ZHENGYU (CN)
ZHANG DAN (CN)
CAO YANGZHI (CN)
Application Number:
PCT/CN2022/134097
Publication Date:
June 22, 2023
Filing Date:
November 24, 2022
Export Citation:
Assignee:
SHANGHAI INST MATERIA MEDICA CAS (CN)
International Classes:
A61K31/381; C07D409/12; A61P35/00; C07D333/64
Foreign References:
| CN107406424A | 2017-11-28 | |||
| CN112839646A | 2021-05-25 | |||
| CN105008343A | 2015-10-28 |
Other References:
PARMENTIER MICHAEL, WAGNER MONA, WICKENDICK REGINA, BAENZIGER MARKUS, LANGLOIS AUDREY, GALLOU FABRICE: "A General Kilogram Scale Protocol for Suzuki–Miyaura Cross-Coupling in Water with TPGS-750-M Surfactant", ORGANIC PROCESS RESEARCH & DEVELOPMENT, AMERICAN CHEMICAL SOCIETY, US, vol. 24, no. 8, 21 August 2020 (2020-08-21), US , pages 1536 - 1542, XP093073193, ISSN: 1083-6160, DOI: 10.1021/acs.oprd.0c00281
BAENZIGER MARKUS, BAIERL MARCEL, DEVANATHAN KRISHNASWAMY, ESWARAN SUMESH, FU PENG, GSCHWEND BJOERN, HALLER MICHAEL, KASINATHAN GOP: "Synthesis Development of the Selective Estrogen Receptor Degrader (SERD) LSZ102 from a Suzuki Coupling to a C–H Activation Strategy", ORGANIC PROCESS RESEARCH & DEVELOPMENT, AMERICAN CHEMICAL SOCIETY, US, vol. 24, no. 8, 21 August 2020 (2020-08-21), US , pages 1405 - 1419, XP093073195, ISSN: 1083-6160, DOI: 10.1021/acs.oprd.0c00076
TRIA GEORGE S. ET AL.: "Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer", JOURNAL OF MEDICINAL CHEMISTRY, vol. 61, no. 7, 22 March 2018 (2018-03-22), pages 2837 - 2864, XP055564421, DOI: 10.1021/acs.jmedchem.7b01682
BAENZIGER MARKUS, BAIERL MARCEL, DEVANATHAN KRISHNASWAMY, ESWARAN SUMESH, FU PENG, GSCHWEND BJOERN, HALLER MICHAEL, KASINATHAN GOP: "Synthesis Development of the Selective Estrogen Receptor Degrader (SERD) LSZ102 from a Suzuki Coupling to a C–H Activation Strategy", ORGANIC PROCESS RESEARCH & DEVELOPMENT, AMERICAN CHEMICAL SOCIETY, US, vol. 24, no. 8, 21 August 2020 (2020-08-21), US , pages 1405 - 1419, XP093073195, ISSN: 1083-6160, DOI: 10.1021/acs.oprd.0c00076
TRIA GEORGE S. ET AL.: "Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer", JOURNAL OF MEDICINAL CHEMISTRY, vol. 61, no. 7, 22 March 2018 (2018-03-22), pages 2837 - 2864, XP055564421, DOI: 10.1021/acs.jmedchem.7b01682
Attorney, Agent or Firm:
XU&PARTNERS, LLC. (CN)
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