751468-47-0

Usage

InChI:InChI=1/C11H15FN2/c12-10-2-4-11(5-3-10)14-8-1-6-13-7-9-14/h2-5,13H,1,6-9H2

Upstream product

• 263409-95-6 4-(4-fluorophenyl)-1,4-diazepane-1-carboxylic acid tert-butyl ester 
• 112275-50-0 tert-butyl 1,4-diazepine-1-carboxylate 

Downstream Products

• 868064-37-3 (Z)-2-cyano-3-[4-(4-fluorophenyl)-1,4-diazepan-1-yl]but-2-enethioamide 

Relevant academic research and scientific papers

Discovery and structure-activity relationship of thienopyridine derivatives as bone anabolic agents

A cell-based assay was performed for the discovery of novel bone anabolic agents. Alkaline phosphatase (ALPase) activity of ST2 cells was utilized as an indicator of osteoblastic differentiation, and thienopyridine derivative 1 was identified as a hit compound. 3-Aminothieno[2,3-b]pyridine-2-carboxamide was confirmed to be a necessary core structure for the enhancement of ALPase activity, and then optimization of the C4-substituent on the thienopyridine ring was carried out. Introduction of cyclic amino groups to the C4-position of the thienopyridine ring improved the activity. Especially, N-phenyl-homopiperazine derivatives were found to be strong enhancers of ALPase among this new series. Furthermore, 3-amino-4-(4-phenyl-1,4-diazepan-1-yl)thieno[2,3-b]pyridine-2- carboxamide (15k) was orally administered to ovariectomized (OVX) rats over 6 weeks for evaluating the effects on areal bone mineral density (aBMD), and statistically significant improvements in aBMD were observed from the dosage of 10 mg/kg/day.

THIENOPYRIDINE DERIVATIVES

The present invention provides a compound promoting osteogenesis. The present invention provides a compound having the following general formula (I) wherein R 1 is H or alkyl, R 2 is R a S-, R a O-, R a NH-, R a (R b )N- or cyclic amino, and R a and R b are alkyl which may be substituted, cycloalkyl which may be substituted, or the like, or a pharmacologically acceptable salt thereof.

DIAZEPAN-1-YL-SULFONYL DERIVATIVES FOR THE TREATMENT OF METABOLIC SYNDROME

Compounds of formula (I): wherein variable groups are defined within; their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are described.