221136-76-1

Upstream product

• 221136-66-9 3-bromo-1-(ethoxycarbonylmethyl)-6-methylpyrazinone 
• 221136-61-4 Ethyl (3-hydroxy-6-methyl-2-oxo-2H-pyrazin-1-yl)-acetate 
• 221136-54-5 [[1,2-dioxo-2-[(2-oxopropyl)amino]ethyl]amino]acetic acid ethyl ester 
• 221136-49-8 [[2-[(2-hydroxypropyl)amino]-1,2-dioxoethyl]amino]acetic acid ethyl ester 
• 55601-21-3 2,2-difluoro-2-phenylethylamine 

Downstream Products

• 454483-97-7 3-(2,2-difluoro-2-(phenyl)ethylamino)-6-methylpyrazin-(1H)-2-one-1-acetic acid 

Relevant academic research and scientific papers

Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino} carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif

We have identified RWJ -671818 (8) as a, novel, low molecular weight, orally active inhibitor of human a-thrombin (Ki = 1.3 nM) that is potentially useful for the acute and chronic treatment of venous and, arterial thrombosis. In a rat deep ven

N-[2-[[(DIAMINOMETHYLENE)AMINO]OXY]ETHYL]-3-[(2,2-DIFLUORO-2-PHENYLETHYL)AMINO]-6-METHYL-2-OXO-1(2H)-PYRAZINEACETAMIDE

The present invention is directed to N-[2-[[(diaminomethylene)amino]oxy]ethyl]-3-[(2,2-difluoro-2-phenylethyl)amino]-6-methyl-2-oxo-1(2H)-pyrazineacetamide, pharmaceutical compositions containing said compound and methods of treatment comprising inhibiting a serine protease using said compound. The present invention is further directed to a process for the preparation of the N-[2-[[(diaminomethylene)amino]oxy]ethyl]-3-[(2,2-difluoro-2-phenylethyl)amino]-6-methyl-2-oxo-1(2H)-pyrazineacetamide as a free base. The present invention is further directed to a process for the preparation of pharmaceutically acceptable salts of N-[2-[[(aminoiminomethyl)amino]oxy]ethyl]-3-[(2,2-difluoro-2-phenylethyl)amino]-6-methyl-2-oxo-1(2H)-pyrazineacetamide.

Cyclic oxyguanidine pyrazinones as protease inhibitors

Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable

Pyrazinone thrombin inhibitors

Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: for example: