发明授权
US06403633B2 Heteroaryl amidines, methylamidines and guanidines, and use thereof as protease inhibitors
失效
杂芳基脒,甲脒和胍,以及其作为蛋白酶抑制剂的用途
- 专利标题: Heteroaryl amidines, methylamidines and guanidines, and use thereof as protease inhibitors
- 专利标题(中): 杂芳基脒,甲脒和胍,以及其作为蛋白酶抑制剂的用途
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申请号: US09828783申请日: 2001-04-10
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公开(公告)号: US06403633B2公开(公告)日: 2002-06-11
- 发明人: Carl R. Illig , Nalin L. Subasinghe , James B. Hoffman , Kenneth J. Wilson , M. Jonathan Rudolph , Juan José Marugán
- 申请人: Carl R. Illig , Nalin L. Subasinghe , James B. Hoffman , Kenneth J. Wilson , M. Jonathan Rudolph , Juan José Marugán
- 主分类号: A61K3138
- IPC分类号: A61K3138
摘要:
The present invention is directed to compounds of Formula I: wherein X is O, S or NR7 and R1-R7, Y and Z are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, plasmin and urokinase. Certain of the compounds exhibit direct, selective inhibition of urokinase, or are intermediates useful for forming compounds having such activity.
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