445490-33-5

Upstream product

• 1215-59-4 5-benzyloxy-1H-indole 
• 96-32-2 bromoacetic acid methyl ester 

Downstream Products

• 600167-63-3 C₂₃H₁₉F₃N₂O₂S₂ 
• 779202-86-7 {5-[5-(4-Trifluoromethyl-phenyl)-isoxazol-3-ylmethoxy]-indol-1-yl}-acetic acid methyl ester 
• 600167-59-7 {5-[4-methyl-2-(4-trifluoromethyl-phenyl)-thiazol-5-ylmethoxy]-indol-1-yl}-acetic acid methyl ester 

Relevant academic research and scientific papers

Synthesis and SAR of selective benzothiophene, benzofuran, and indole-based peroxisome proliferator-activated receptor δ agonists

Recent literature has suggested the benefit of selective PPARδ agonists for the treatment of atherosclerosis and other disease states associated with the metabolic syndrome. Herein we report the synthesis and structure-activity relationships of a series of novel and selective PPARδ agonists. Our search began with identification of a novel benzothiophene template which was modified by the addition of various thiazolyl, isoxazolyl, and benzyloxy-benzyl moieties. Further elucidation of the SAR led to the identification of benzofuran and indole based templates. During the course of our research, we discovered three new chemical templates with varying degrees of affinity and potency for PPARδ versus the PPARα and PPARγ subtypes.

ISOXAZOLE DERIVATIVE HAVING AGONISTIC ACTIVITY AGAINST PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR

A compound of formula (I) : (wherein R1-R10 are each independently hydrogen, halogen, optionally substituted lower alkyl or the like, X1 is -O-, -S-, -NR11- (wherein R11 is hydrogen, lower alkyl or the like), -CR12R13CO-, -(CR12R13)mO-, -O(CR12R13)m- (wherein R12 and R13 are each independently hydrogen or lower alkyl and m is a integer between 1 and 3) or the like, X2 is a bond, -O-, -S-, -NR14- (wherein R14 is hydrogen, lower alkyl or the like, R14 and R6 can be taken together with the neighboring atom to form a ring) or -CR15R16-(wherein R15 and R16 are each independently hydrogen or lower alkyl, R15 and R6 or R10 can be taken together with the neighboring carbon atom to form a ring, R16 and R9 can be joined together to form a bond), X3 is COOR17, C( = NR17)NR18OR19 or the like), a pharmaceutically acceptable salt or a solvate thereof.

Compounds that modulate PPAR activity and methods of preparation

This invention relates to compounds that alter PPAR activity. The invention also relates to pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing dyslipidemia, hypercholesterolemia, obesity, hyperglycemia, atherosclerosis, hypertriglyceridemia and hyperinsulinemia in a mammal. The present invention also relates to methods for making the disclosed compounds.