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公开(公告)号:US4927959A
公开(公告)日:1990-05-22
申请号:US239663
申请日:1988-09-02
申请人: Shinichi Shimada , Noboru Kawaguchi , Tadayoshi Koyama , Akinori Wakaiki , Keiji Hayashi , Yasuyoshi Takeshita , Masamichi Nakakoshi , Gosei Kawanishi
发明人: Shinichi Shimada , Noboru Kawaguchi , Tadayoshi Koyama , Akinori Wakaiki , Keiji Hayashi , Yasuyoshi Takeshita , Masamichi Nakakoshi , Gosei Kawanishi
IPC分类号: A61K31/225 , A61P25/02 , A61P43/00 , C07C69/353 , C07C219/06 , C07C219/08
CPC分类号: C07C219/06 , C07C219/08
摘要: Novel alprenolol derivatives represented by the formula: ##STR1## wherein R is ##STR2## and hydrochlorides thereof are disclosed.
摘要翻译: 公开了由下式表示的新型阿普洛尔衍生物:其中R为
+ TR 及其盐酸盐。 -
公开(公告)号:US5116985A
公开(公告)日:1992-05-26
申请号:US630064
申请日:1990-12-19
申请人: Yasuyoshi Takeshita , Hiroshi Nakamura , Susumu Ishiguro , Noboru Kwaguchi , Shin'ichi Shimada , Tadayoshi Koyama , Motohide Seya , Noriko Abe , Shin Nomoto
发明人: Yasuyoshi Takeshita , Hiroshi Nakamura , Susumu Ishiguro , Noboru Kwaguchi , Shin'ichi Shimada , Tadayoshi Koyama , Motohide Seya , Noriko Abe , Shin Nomoto
IPC分类号: C07D217/02 , C07D217/16 , C07D217/24 , C07D217/26
CPC分类号: C07D217/24 , C07D217/02 , C07D217/16 , C07D217/26
摘要: The invention provides novel compounds and salts thereof, have the structure ##STR1## wherein R.sub.1 is a guianidinobenzoyloxy group and R.sub.2 is a hydrogen atom, a hydroxy, cyano, --COR.sub.3 (wherein R.sub.3 is an amino or lower alkyl group) or --COOR.sub.4 group [wherein R.sub.4 is a hydrogen atom, lower alkyl, phenyl, benzyl or --CH.sub.2 CONR.sub.5 R.sub.6 group (wherein R.sub.5 and R.sub.6 are the same or different and selected from a hydrogen atom and lower alkyl groups)], and wherein R.sub.1 is a hydroxy group and wherein R.sub.2 is a --COR.sub.3 (wherein R.sub.3 is an amino or lower alkyl group) or --COOR.sub.4 group [wherein R.sub.4 is a (C.sub.1, C.sub.3 or C.sub.4) alkyl, phenyl, benzyl or --CH.sub.2 CONR.sub.5 R.sub.6 group (wherein R.sub.5 and R.sub.6 are the same or different and selected from a hydrogen atom and lower alkyl groups)]. The compounds, wherein R.sub.1 is a guanidinobenzoyloxy group, are useful protease inhibitors as anti-trypsin agents.
摘要翻译: 本发明提供了新颖的化合物及其盐,其结构为:其中R1是一个胍基苯甲酰氧基,R2是氢原子,羟基,氰基,-COR3(其中R3是氨基或低级烷基)或-COOR4基团 [其中R4是氢原子,低级烷基,苯基,苄基或-CH2CONR5R6基团(其中R5和R6相同或不同并且选自氢原子和低级烷基)],其中R1是羟基,其中 R2是-COR3(其中R3是氨基或低级烷基)或-COOR4基[其中R4是(C1,C3或C4)烷基,苯基,苄基或-CH2CONR5R6基团(其中R5和R6是相同的或 不同且选自氢原子和低级烷基)]。 其中R1是胍基苯甲酰氧基的化合物是有用的蛋白酶抑制剂作为抗胰蛋白酶剂。
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