220220-41-7

Upstream product

• 2208-07-3 ethyl acetimidate hydrochloride 
• 286430-94-2 ethyl ({({7-[amino(imino)methyl]-2-naphthyl}methyl)[4-(1,4-diazepan-1-yl)phenyl]amino}sulfonyl)acetate 
• 286430-88-4 tert-butyl 4-(4-{[(7-cyano-2-napthyl)methyl][(2-ethoxy-2-oxoethyl)sulfonyl]amino}phenyl)-1,4-diazepane-1-carboxylate 
• 220220-32-6 tert-butyl 4-(4-{[(7-cyano-2-naphthyl)methyl]amino}phenyl)-1,4-diazepane-1-carboxylate 
• 220220-23-5 tert-butyl 4-(4-nitrophenyl)-1,4-diazepane-1-carboxylate 
• 350-46-9 4-Fluoronitrobenzene 

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.