1430231-75-6

Upstream product

• 805250-17-3 (6-hydroxy-2,3-dihydro-benzofuran-3-yl)-acetic acid methyl ester 
• 1000414-38-9 methyl ((3S)-6-hydroxy-2,3-dihydro-1-benzofuran-3-yl)acetate 
• 1430232-67-9 2,6-dimethyl-4-(3-(methylsulfonyl)propoxy)-3'-vinylbiphenyl 
• 1000413-84-2 2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)-[1,1'-biphenyl]-3-carbaldehyde 
• 1430232-70-4 (S)-2-(6-hydroxy-5-iodo-2,3-dihydrobenzofuran-3-yl)acetic acid methyl ester 

Relevant academic research and scientific papers

Benzocarbazoles dioxane derivatives, its preparation process and its use in medicine

The invention relates to a benzodioxane derivative, a preparation method thereof and application of the derivative in medicines. Specifically, the invention relates to a novel benzodioxane derivative shown as a formula (I), medial salt thereof or a medicine composition containing the derivative, and a preparation method of the derivative. The invention further relates to a use of the benzodioxane derivative and the medial salt thereof or the medicine composition containing the derivative in preparing therapeutic agent, especially GPR 40 agonist, and a drug for treating the diseases such as diabetes, metabolic disorders and the like, wherein each substituent group in the formula (I) is as defined in the description.

Discovery of novel orally bioavailable GPR40 agonists

The GPR40 (FFA1) has emerged as an attractive target for a novel insulin secretagogue with glucose dependency. A series of novel orally bioavailable GPR40 agonists was discovered. SAR study and structural optimization led to identification of compounds 28a and 30a as potent GPR40 agonists with superior physiochemical properties and robust in vivo efficacy in rhesus monkeys.