629659-06-9

Upstream product

• 85660-66-8 ethyl 1,2,3,6-tetrahydroazepino[4,5-b]indole-5-carboxylate 
• 403-43-0 4-fluorobenzoyl chloride 

Downstream Products

• 629662-66-4 10-bromo-3-(4-fluorobenzoyl)-1,2,3,6-tetrahydroazepino[4,5-b]indole-5-carboxylic acid ethyl ester 
• 629663-94-1 ethyl 3-(4-fluorobenzoyl)-6-methyl-1,2,3,6-tetrahydroazepino[4,5-b]indole-5-carboxylate 
• 629663-78-1 3-(4-fluorobenzoyl)-1-oxo-1,2,3,6-tetrahydroazepino[4,5-b]indole-5-carboxylic acid ethyl ester 

Relevant academic research and scientific papers

Discovery of XL335 (WAY-362450), a highly potent, selective, and orally active agonist of the farnesoid X receptor (FXR)

Azepino[4,5-b]indoles have been identified as potent agonists of the farnesoid X receptor (FXR). In vitro and in vivo optimization has led to the discovery of 6m (XL335, WAY-362450) as a potent, selective, and orally bioavailable FXR agonist (EC50 = 4 nM, Eff = 149%). Oral administration of 6m to LDLR-/- mice results in lowering of cholesterol and triglycerides. Chronic administration in an atherosclerosis model results in significant reduction in aortic arch lesions.

AZEPINOINDOLE AND PYRIDOINDOLE DERIVATIVES AS PHARMACEUTICAL AGENTS

The present invention is directed to compounds of formula (I) and formula (II): formula (I) and (II), wherein R1-R8, A and n are as described in the description. These compounds are used in pharmaceutical compositions and methods for modulating the activity of orphan nuclear receptors.