868066-58-4

Upstream product

• 868066-56-2 benzyl 4-{4-[2-(dimethylamino)-2-oxoethyl]phenyl}-1,4-diazepane-1-carboxylate 
• 19715-80-1 2-(4-bromophenyl)-N,N-dimethyl acetamide 
• 112275-50-0 tert-butyl 1,4-diazepine-1-carboxylate 

Downstream Products

• 868066-60-8 2-{4-[4-(3-cyano-2-thioxo-1,2-dihydropyridin-4-yl)-1,4-diazepan-1-yl]phenyl}-N,N-dimethylacetamide 
• 868066-54-0 3-amino-4-(4-(4-(2-(dimethylamino)-2-oxoethyl)phenyl)-1,4-diazepan-1-yl)thieno[2,3-b]pyridine-2-carboxamide 

Relevant academic research and scientific papers

BICYCLIC PYRIDINE COMPOSITIONS AND METHODS OF USING THE SAME FOR CANCER THERAPY

Disclosed herein are bicyclic pyridines, such as thienopyridine, pyrrolopyridine, furopyridine compounds, and methods for treating cancers. The method may comprise administering a therapeutically effective amount of any of the compositions described herei

QUINOLINE-BASED COMPOUNDS AND METHODS OF INHIBITING CDK8/19

Disclosed herein are quinoline-based compounds and method for inhibiting CDK8 or CDK19 for the intervention in diseases, disorders, and conditions. The quinoline-based composition comprise substituents at quinoline ring positions 4 and 6, wherein the substituent at position 4 is selected from a substituted or unsubstituted arylalkylamine or a substituted or unsubstituted arylhetrocyclylamine. Pharmaceutical compositions comprising the substituted qunioline compositions, methods of inhibiting CDK8 or CDK19, and methods of treating CDK8/19-associated diseases, disorders, or conditions are also disclosed.

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.