发明名称 Azetidin-2-one derivatives as serine protease inhibitors
摘要 The present invention relates to new 3-guanidinoalkyl-2-azetidinones of the formula <IMAGE> wherein: U and W can be the same or different and are selected from the group consisting of hydrogen and an amino protecting group; n is 1 to 3; X is a member selected from the group consisting of hydrogen, trialkylsilyl, arylsulfonyl, amino substituted arylsulfonyl, alkylsulfonyl, arylaminocarbonyl, alkylcarbonyl and arylcarbonyl; and Y is a member selected from the group consisting of hydrogen, arylalkenyl, arylalkyl, formyl, carboxy, alkoxycarbonyl, acyloxy, arylthio, arylsulfinyl, arylsulfonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, arylaminocarbonyl, the radical <IMAGE> in which R is hydrogen, alkyl or arylalkyl, and the radical <IMAGE> in which m is 1 to 3 and R' is hydrogen or -CO2R'' wherein R'' is hydrogen, alkyl or arylalkyl. The novel azetidinones of the present invention exhibit anti-thrombin and anti-trypsin activities and are thus useful in controlling blood coagulation and treating pancreatitis.
申请公布号 US5250677(A) 申请公布日期 1993.10.05
申请号 US19920957233 申请日期 1992.10.06
申请人 BRISTOL-MYERS SQUIBB COMPANY 发明人 HAN, WILLIAM T.
分类号 C07D205/09;C07D205/095;(IPC1-7):C07D205/08;C07D247/00;A61K31/395 主分类号 C07D205/09
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