Benzothia(d)azepine compounds and their use as bile acid modulators
By developing benzothiazazazetacycloheptatriene and its derivatives, the shortcomings of existing bile acid modulators in terms of efficacy and selectivity have been overcome, achieving effective inhibition of ASBT and LBAT and providing better therapeutic effects.
CN116157389BActive Publication Date: 2026-02-10ALBIREO
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Patent Information
- Application Number
- CN202180057747.9
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- Priority Date
- 2020-08-03
- Filing Date
- 2021-08-03
- Publication Date
- 2026-02-10
- Estimated Expiration
- 2041-08-03
AI Technical Summary
Technical Problem
Existing bile acid modulators are inadequate in terms of efficacy, selectivity, and bioavailability, and cannot effectively inhibit apical sodium-dependent bile acid transporter (ASBT) and hepatic bile acid transporter (LBAT), thus failing to effectively treat related diseases.
Method used
A class of benzothiazazepine heptadiene and benzothiazazepine heptadiene derivatives were developed as inhibitors of ASBT and LBAT for the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases.
Benefits of technology
These compounds exhibit potent inhibitory effects, significantly reducing symptoms of bile acid cycle-related diseases and providing better treatment options.
✦ Generated by Eureka AI based on patent content.
Abstract
The present invention relates to certain 1,5-benzothiazepine and 1,2,5-benzothiadiazepine derivatives as defined herein. These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and / or liver bile acid transporter (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds, and to the use of these compounds in the treatment of cardiovascular diseases, disorders of fatty acid metabolism and glucose utilization, gastrointestinal diseases and liver diseases.
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