618359-57-2

Upstream product

• 234108-42-0 3-oxo-4-prop-2-ynylpiperazine-1-carboxylic acid benzyl ester 
• 78818-15-2 4-benzyloxycarbonylpiperazin-2-one 

Downstream Products

• 618359-56-1 1-(1-benzenesulfonyl-4-chloro-1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-4-(6-chlorobenzo[b]thiophene-2-sulfonyl)-piperazin-2-one 
• 234108-76-0 4-(1-benzenesylfonyl-4-chloro-1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-3-oxo-piperazine-1-carboxylic acid benzyl ester 
• 234108-77-1 1-(1-benzenesulfonyl-4-chloro-1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one 
• 234108-75-9 4-(4-chloro-1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-3-oxo-piperazine-1-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand

The discovery and SAR of ketopiperazino methylazaindole factor Xa inhibitors are described. Structure-activity data suggesting that this class of inhibitors does not bind in the canonical mode were confirmed by an X-ray crystal structure showing the neutral haloaromatic bound in the S1 subsite. The most potent azaindole, 33 (RPR209685), is selective against related serine proteases and attains higher levels of exposure upon oral dosing than comparable benzamidines and benzamidine isosteres. Compound 33 was efficacious in the canine AV model of thrombosis.

Substituted oxoazaheterocyclyl compounds

This invention is directed to oxoazaheterocycyl compounds which inhibit Factor Xa, to oxoazaheterocycyl compounds which inhibit both Factor Xa and Factor IIa, to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds, to a method of directly inhibiting Factor Xa and to a method of simultaneously directly inhibiting Factor Xa and Factor IIa..