Quaternary ammonium salt locally-acting sphingosine 1-phosphate receptor subtype 1 agonist
By developing a locally acting quaternary ammonium salt S1PR1 modulator, the problems of bradycardia and systemic distribution of existing S1PR1 agonists have been solved, achieving effective treatment of inflammatory bowel disease and reducing the risk of infection.
CN122301787APending Publication Date: 2026-06-30NANJING ETERNAL INSTITUTE OF PHARMACEUTICAL RESEARCH CO LTD
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Patent Information
- Application Number
- CN202411983771.7
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2024-12-31
- Publication Date
- 2026-06-30
AI Technical Summary
Technical Problem
Existing S1PR1 agonists pose risks of bradycardia and infection due to systemic distribution, and since they are administered orally, they cannot effectively act locally on the site of inflammatory bowel disease.
Method used
Develop a quaternary ammonium salt compound designed as a locally acting S1PR1 modulator to avoid systemic distribution and reduce the risk of infection caused by systemic immunosuppression through local administration.
Benefits of technology
This compound exhibits good agonistic activity against sphingosine 1-phosphate receptor subtype 1, which can effectively improve inflammatory damage in ulcerative colitis, increase body weight and colon length in mice, and reduce the risk of infection.
✦ Generated by Eureka AI based on patent content.
Abstract
The invention belongs to the field of inflammatory bowel diseases, and relates to a sphingosine 1-phosphate receptor subtype 1 agonist with a quaternary ammonium salt local effect. The compound, the stereoisomer and the pharmaceutically acceptable salt of the compound are S1PR1 agonists for local action, and the compound has good agonistic activity of sphingosine 1 phosphate receptor subtype 1, is almost not absorbed by oral administration, is low in oral bioavailability, still has good in-vivo ulcerative colitis resistance activity, and can be used for preparing medicines for treating ulcerative colitis. Inflammation damage of intestinal tracts of mice with ulcerative colitis can be improved, the weight of the mice is increased, and the colon length of the mice is increased Therefore, the compound can reduce the infection risk caused by systemic immunosuppression while keeping the in-vivo ulcerative colitis resisting activity. The structural formula of the sphingosine 1-phosphate receptor subtype 1 agonist is as shown in formula I in the specification.
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