发明授权
- 专利标题: Derivatives of p-guanidinobenzoic acid and pharmaceutical agents containing them as an active ingredient
- 专利标题(中): 对胍基苯甲酸的衍生物和含有它们作为活性成分的药剂
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申请号: US70683申请日: 1993-06-02
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公开(公告)号: US5376655A公开(公告)日: 1994-12-27
- 发明人: Katsuhiro Imaki , Yoshinobu Arai , Hiroyuki Ohno
- 申请人: Katsuhiro Imaki , Yoshinobu Arai , Hiroyuki Ohno
- 申请人地址: JPX Osaka
- 专利权人: Ono Pharmaceutical Co., Ltd.
- 当前专利权人: Ono Pharmaceutical Co., Ltd.
- 当前专利权人地址: JPX Osaka
- 优先权: JPX60-252066 19851112; JPX60-252067 19851112; JPX61-192117 19860819
- 主分类号: C07C279/18
- IPC分类号: C07C279/18 ; C07C309/65 ; C07C309/66 ; C07C311/08 ; C07C311/29 ; C07C311/46 ; C07C329/10 ; C07D213/65 ; C07D213/75 ; C07D277/04 ; C07D277/22 ; C07D295/26 ; A61K31/535 ; A61K31/21 ; A61K31/44 ; C07C327/16
摘要:
A derivative of p-guanidinobenzoic acid of the general formula (IA): ##STR1## wherein Y represents an oxygen atom or a sulfur atom and (a) when Y is an oxygen atom, (R.sup.1).sub.m is selected from the group consisting of: 5-(4-guanidinobenzoyloxy)-3-methoxymethyl, 3,5-dicarboxy, 3,5-bis(isopropoxycarbonyl), 3,5-bistrifluoromethyl, 3-acetyl, 3,5-bis(N-ethylcarbamoyl), and 3,5-bis(N-propylcarbamoyl);(b) when Y is a sulfur atom, (R.sup.1).sub.m is selected from the group consisting of: 2-methyl, 3-methyl, 4-fluoro, 2-chloro, 3-chloro, 2,5-dichloro 2,6-dichloro, 3,4-dichloro, 2-bromo, 2-methoxycarbonyl, and 4-(N,N-diethylaminosulfonyl);or an acid addition salt of said derivative. A method for the treatment or prevention of diseases induced by abnormal enhancing of degradation of proteins by the action of elastase in mammals subject to or suffering therefrom, including the step of administering an effective amount of a p-guanidinobenzoic acid as described herein, is also disclosed.
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