N-[2-[[(DIAMINOMETHYLENE)AMINO]OXY]ETHYL]-3-[(2,2-DIFLUORO-2-PHENYLETHYL)AMINO]-6-METHYL-2-OXO-1(2H)-PYRAZINEACETAMIDE
    13.
    发明申请
    N-[2-[[(DIAMINOMETHYLENE)AMINO]OXY]ETHYL]-3-[(2,2-DIFLUORO-2-PHENYLETHYL)AMINO]-6-METHYL-2-OXO-1(2H)-PYRAZINEACETAMIDE 审中-公开
    N- [2 - [[(二氨基乙烯基)氨基]氧基]乙基] -3 - [(2,2-二氟-2-苯基)氨基] -6-甲基-2-氧代-1(2H) - 吡嗪胺

    公开(公告)号:US20080021044A1

    公开(公告)日:2008-01-24

    申请号:US11751155

    申请日:2007-05-21

    CPC classification number: C07D241/20

    Abstract: The present invention is directed to N-[2-[[(diaminomethylene)amino]oxy]ethyl]-3-[(2,2-difluoro-2-phenylethyl)amino]-6-methyl-s-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.

    Abstract translation: 本发明涉及N- [2 - [[(二氨基亚甲基)氨基]氧基]乙基] -3 - [(2,2-二氟-2-苯基乙基)氨基] -6-甲基-3-氧代-1( 2H) - 吡嗪乙酰胺,含有所述化合物的药物组合物和治疗方法,包括使用所述化合物抑制丝氨酸蛋白酶。 本发明进一步涉及制备N- [2 - [[(二氨基亚甲基)氨基]氧基]乙基] -3 - [(2,2-二氟-2-苯乙基)氨基] -6- 甲基-2-氧代-1(2H) - 吡嗪乙酰胺,为游离碱。 本发明进一步涉及制备N- [2 - [[(氨基亚氨基甲基)氨基]氧基]乙基] -3 - [(2,2-二氟-2-苯基乙基)氨基] -6-甲基-2-氧代-1(2H) - 吡嗪乙酰胺。

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