发明授权
US5741819A Arylsulfonylaminobenzene derivatives and the use thereof as factor Xa
inhibitors
失效
芳基磺酰氨基苯衍生物及其作为因子Xa抑制剂的用途
- 专利标题: Arylsulfonylaminobenzene derivatives and the use thereof as factor Xa inhibitors
- 专利标题(中): 芳基磺酰氨基苯衍生物及其作为因子Xa抑制剂的用途
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申请号: US488196申请日: 1995-06-07
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公开(公告)号: US5741819A公开(公告)日: 1998-04-21
- 发明人: Carl R. Illig , Richard M. Soll , Joseph M. Salvino , Bruce E. Tomczuk , Tianbao Lu , Nalin L. Subasinghe
- 申请人: Carl R. Illig , Richard M. Soll , Joseph M. Salvino , Bruce E. Tomczuk , Tianbao Lu , Nalin L. Subasinghe
- 申请人地址: PA Exton
- 专利权人: 3-Dimensional Pharmaceuticals, Inc.
- 当前专利权人: 3-Dimensional Pharmaceuticals, Inc.
- 当前专利权人地址: PA Exton
- 主分类号: A61K31/18
- IPC分类号: A61K31/18 ; A61K31/195 ; A61K31/245 ; A61K31/27 ; A61K31/435 ; A61K31/44 ; A61P25/00 ; A61P29/00 ; A61P35/00 ; C07C311/21 ; C07C311/44 ; C07D213/40 ; C07D453/02 ; A61K31/24
摘要:
The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds of structure: ##STR1## or pharmaceutically acceptable salts thereof; wherein R.sup.1 is alkyl, substituted alkyl, cycloalkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl; R.sup.2 is one of hydrogen, alkyl, cycloalkyl or aryl; R.sup.3 is one of hydrogen, hydroxy or alkoxy; R.sup.4 is one of --NH.sub.2, phenyl or pyridyl, wherein said phenyl and said pyridyl are optionally substituted with one or two of halogen, hydroxy, hydroxyalkyl, alkoxy, amino, monoalkylamino, dialkylamino, aminoalkyl, monoalkylaminoalkyl and/or dialkylaminoalkyl; X is one of --CH.sub.2 -- or --C(O)--; and n is from zero to eleven; provided that when R.sup.4 is --NH.sub.2, then R.sup.3 is hydrogen and n is other than zero; and also provided that when R.sup.3 is hydroxy or alkoxy, then R.sup.4 is other than --NH.sub.2, and n is other than zero.