960404-26-6Relevant 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
Lu, Tianbao,Markotan, Thomas,Ballentine, Shelley K.,Giardino, Edward C.,Spurlino, John,Brown, Kathryn,Maryanoff, Bruce E.,Tomczuk, Bruce E.,Damiano, Bruce P.,Shukla, Umesh,End, David,Andrade-Gordon, Patricia,Bone, Roger F.,Player, Mark R.
experimental part, p. 1843 - 1856 (2010/08/06)
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
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Page/Page column 45-46, (2010/11/29)
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.
