220220-06-4

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 7379-35-3 4-chlorpyridine hydrochloride 
• 350-46-9 4-Fluoronitrobenzene 
• 194853-82-2 1-(pyridin-4-yl)-1,4-diazepane 

Downstream Products

• 714249-12-4 ethyl ({[(7-cyano-2-naphthyl)methyl]{4-[4-(pyridin-4-yl)-1,4-diazepan-1-yl]phenyl}amino}sulfonyl)acetate 
• 220220-31-5 7-[({4-[4-(pyridin-4-yl)-1,4-diazepan-1-yl]phenyl}amino)methyl]-2-naphthonitrile 

Relevant academic research and scientific papers

Synthesis and biological activity of novel 1,4-diazepane derivatives as factor Xa inhibitor with potent anticoagulant and antithrombotic activity

Factor Xa (fXa) is a serine protease involved in the coagulation cascade, which has received great interest as a potential target for the development of new antithrombotic drugs. Herein we report a novel series of fXa inhibitors in which the 1,4-diazepane moiety was designed to interact with the S4 aryl-binding domain of the fXa active site. Compound 13 (YM-96765) showed potent fXa inhibitory activity (IC50=6.8nM) and effective antithrombotic activity without prolonging bleeding time.

Hexahydro-1,4-diazepine derivatives or salts thereof

Hexahydro-1,4-diazepine derivatives represented by general formula (I); pharmaceutically acceptable salts thereof; and drugs containing the same as the active ingredient, such as activated blood coagulation factor X inhibitor, wherein A: phenylene, pyridylene, or the like; B: a 5- or 6-membered aryl or heteroaryl ring; X: —CO—, —CONH—, —CSNH—, —SO2—, —SO2NH—, or the like; Y: a bond or alkylene; R1: hydrogen, alkyl, —Y—(hetero) aryl, or the like; R2: hydrogen, alkoxy, —COOH, or the like; R3: amidino or a group capable of being converted into amidino; and R4, R5: each independently hydrogen or lower alkyl.