2-benzoylindole compounds and uses thereof

CN117285455BActive Publication Date: 2026-07-21JIANGSU SKYRUN PHARMA CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
JIANGSU SKYRUN PHARMA CO LTD
Filing Date
2022-06-17
Publication Date
2026-07-21

AI Technical Summary

Technical Problem

Existing selective estrogen receptor downregulators (SERDs) suffer from low bioavailability and drug resistance in the treatment of estrogen receptor (ER) positive breast cancer, necessitating the development of more selective oral drugs with superior pharmacokinetic properties.

Method used

A class of 2-benzoylindole compounds is provided as selective estrogen receptor downregulators (SERDs). Through the design of compounds with specific structures, they can bind to the estrogen receptor (ER) and reduce its expression. They can be prepared in pharmaceutically acceptable forms such as salts, prodrugs, crystal forms, and stereoisomers for the preparation of drugs to treat estrogen receptor-positive mediated diseases.

Benefits of technology

It achieves effective treatment of estrogen receptor-positive mediated diseases such as breast cancer, with better efficacy, fewer side effects and superior pharmacokinetic properties. It is suitable for oral administration and is applicable to the prevention and treatment of diseases such as abnormal cell proliferation and cancer metastasis related to estrogen receptors.

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Abstract

The application discloses a 2-benzoylindole compound shown in a formula I and application of the 2-benzoylindole compound. The 2-benzoylindole compound can be used as a selective estrogen receptor downregulator (SERD) and is used for preparing a medicine for preventing and / or treating diseases mediated or dependent on an estrogen receptor in a living body.
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