Triazole oxadiazoles derivatives

By developing selective S1P1/Edg1 receptor agonists, we have solved the problems of insufficient immunosuppressive activity and poor high-dose tolerance of existing S1P1 agonists in the treatment of multiple sclerosis, achieving higher efficacy and safety, combined with Immunomodulators to enhance therapeutic effects.

CN101918395AInactive Publication Date: 2010-12-15MERCK SERONO SA
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Patent Information

Application Number
CN200880125323.6
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Priority Date
2008-02-20
Filing Date
2008-12-17
Publication Date
2010-12-15
Estimated Expiration
Not applicable · inactive patent

AI Technical Summary

Technical Problem

Existing S1P1 agonists have problems with insufficient immunosuppressive activity and poor high-dose tolerance when treating multiple sclerosis. They also lack selectivity, affecting efficacy and safety.

Method used

Developed a selective S1P1/Edg1 receptor agonist that exhibits excellent selectivity compared to the S1P3/Edg3 receptor, combined with an immunomodulator to improve the therapeutic window of lymphocyte sequestering agents and enhance high-dose tolerance of the drug sex.

Benefits of technology

As a selective S1P1 agonist, the compound significantly improves the efficacy of treating multiple sclerosis, expands the therapeutic window, enhances drug tolerance, and can be used in combination with other active compounds to improve vascular function and immune regulation.

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Abstract

The invention relates to compounds of formula (I), wherein R1, R2, Ra, Rb, X have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
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