Activating agent for peroxisome proliferator activated receptor

By designing new PPARδ activator compounds, we solve the problem of insufficient activity of existing PPARδ activators, achieve significant PPARδ transcriptional activation effects, and provide new drug candidates for the treatment of various metabolic and lipid-related diseases.

CN102643248AInactive Publication Date: 2012-08-22NIPPON CHEMIPHAR CO LTD
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Patent Information

Application Number
CN201210028609.0
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Priority Date
2006-04-18
Filing Date
2007-04-18
Publication Date
2012-08-22
Estimated Expiration
Not applicable · inactive patent

AI Technical Summary

Technical Problem

Existing PPARδ activator compounds have deficiencies in structure and activity. In particular, the activity of phenylpropionic acid-type compounds is 30 times weaker than that of phenoxyacetic acid-type compounds, and the efficacy of phenylglycine-type compounds has not been fully explored.

Method used

A new type of compounds of general formulas (I), (II) and (III) was developed as an activator of PPARδ. Through specific molecular structure design, it significantly improved the transcriptional activation effect of PPARδ and became a powerful PPARδ agonist.

Benefits of technology

These compounds exhibit excellent PPARδ activating effects, surpassing the effects of traditional compounds, and have potential application value in the treatment and prevention of lipid abnormalities, metabolic syndrome, obesity, atherosclerosis, diabetes and other diseases.

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Abstract

A compound represented by the following general formula (II) or a salt thereof is used as an activator of PPAR'. wherein G a is O, CH 2 or the like; A a is thiazole, oxazole, or thiophene, which can have a substituent such as C 1-8 alkyl, C 1-8 alkoxy, halogen, C 1-8 alkyl substituted with halogen or the like; B a is a C 1-8 alkylene or C 2-8 alkenylene chain; and each of R 1a and R 2a independently is hydrogen, C 1-8 alkyl, C 1-8 alkoxy, halogen, C 1-8 alkyl substituted with halogen or the like.
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