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

• Main Authors: HUMORA, MICHAEL, QIAN, YUN, PATEL, MITUL, N, LIU, FUQIANG, REYES, MAYRA, B, ZHANG, XINI, SORGI, KIRK, NILSEN, CHRISTOPHER, N
• Format: Patent
• Language: English; French
• Published: 06.11.2008
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

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. La présente invention concerne le N-[2-[[(diaminométhylène)amino]oxy]éthyl]-3-[(2,2-difluoro-2-phényléthyl)amino]-6-méthyl-2-oxo-1(2H)-pyrazineacétamide, les compositions pharmaceutiques le contenant et les méthodes de traitement comprenant l'inhibition d'une sérine protéase par l'emploi dudit composé. La présente invention concerne également un procédé de synthèse du N-[2-[[(diaminométhylène)amino]oxy]éthyl]-3-[(2,2-difluoro-2-phényléthyl)amino]-6-méthyl-2-oxo-1(2H)-pyrazineacétamide sous forme de base libre. La présente invention concerne en outre un procédé de synthèse de sels de qualité pharmaceutique du N-[2-[[(diaminométhylène)amino]oxy]éthyl]-3-[(2,2-difluoro-2-phényléthyl)amino]-6-méthyl-2-oxo-1(2H)-pyrazineacétamide.