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1.发明公开Guanidinobenzoic ester derivative, a process for preparing same and pharmaceutical compositions containing same 失效Guanidinobenzoesäureesterderivate，其制备方法以及含有它们的药物组合物的方法。
公开(公告)号：EP0229370A1
公开(公告)日：1987-07-22
申请号：EP86117885.3
申请日：1986-12-22
申请人： Eisai Co., Ltd.
发明人： Souda, Shigeru , Shimomura, Naoyuki , Ueda, Norihiro , Miyazawa, Shuhei , Yamanaka, Takashi , Miyamoto, Kaname , Hishinuma, Ieharu , Nagakawa, Junichi , Nagaoka, Naoko , Kawashima, Hidetoshi , Kawata, Tsutomu , Nagaoka, Junsaku , Wakabayashi, Tsuneo
IPC分类号： C07C149/437 , C07D207/404 , C07D209/48 , C07D263/44 , A61K31/245 , A61K31/40 , A61K31/42
CPC分类号： C07D207/404 , C07C323/20 , C07D209/48 , C07D263/44
摘要： A guanidinobenzoic ester derivative having the formula
wherein X represents a group of the formula:
in which Y is a group of the formula:
-(CH₂) m -, m being an integer of 2 or 3,
or a group of the formula:
-OR
in which R is a hydrogen atom or a lower alkyl group, and n represents an integer of l to 5,
which is effective to inhibit enzymes such as trypsin, plasmin and thrombin and useful for treatment of the pancreatitis and hemorrhagic disease and thrombosis is disclosed as well as a process for preparing same and a pharmaceutical composition containing same.-
公开(公告)号：EP0568833B1
公开(公告)日：2000-07-12
申请号：EP93105829.1
申请日：1993-04-08
申请人： Eisai Co., Ltd.
发明人： Kato, Hiroyuki , Yoshitake, Shinji , Suzuki, Suguru , Suzuki, Noboru , Seto, Toshio , Nagaoka, Naoko , Mizui, Yoshiharu
CPC分类号： C07K14/8128 , A61K38/00
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3.发明授权Guanidinobenzoic ester derivative, a process for preparing same and pharmaceutical compositions containing same 失效胍基苯甲酸衍生物，其制备方法和含有其的药物组合物
公开(公告)号：EP0229370B1
公开(公告)日：1989-04-19
申请号：EP86117885.3
申请日：1986-12-22
申请人： Eisai Co., Ltd.
发明人： Souda, Shigeru , Shimomura, Naoyuki , Ueda, Norihiro , Miyazawa, Shuhei , Yamanaka, Takashi , Miyamoto, Kaname , Hishinuma, Ieharu , Nagakawa, Junichi , Nagaoka, Naoko , Kawashima, Hidetoshi , Kawata, Tsutomu , Nagaoka, Junsaku , Wakabayashi, Tsuneo
IPC分类号： C07C149/437 , C07D207/404 , C07D209/48 , C07D263/44 , A61K31/245 , A61K31/40 , A61K31/42
CPC分类号： C07D207/404 , C07C323/20 , C07D209/48 , C07D263/44
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公开(公告)号：EP0568833A1
公开(公告)日：1993-11-10
申请号：EP93105829.1
申请日：1993-04-08
申请人： Eisai Co., Ltd.
发明人： Kato, Hiroyuki , Yoshitake, Shinji , Suzuki, Suguru , Suzuki, Noboru , Seto, Toshio , Nagaoka, Naoko , Mizui, Yoshiharu
CPC分类号： C07K14/8128 , A61K38/00
摘要： A novel human antithrombin III (AT III) mutant having a high antithrombin activity in the absence of heparin and effective in the treatment of thrombotic disorders as an anticoagulant, which is obtained by mutating amino acids at the reactive site and the heparin binding site of human AT III into another amino acids with the use of the recombinant DNA technology with the use of a DNA coding for AT III as a template.
A method for mass producing the above-described mutant by incubating a host transformed by an expression vector having the cDNA of the mutant inserted therein.摘要翻译： 一种新型人类抗凝血酶III（AT III）突变体，其在不存在肝素的情况下具有高抗凝血酶活性，并且有效治疗作为抗凝血剂的血栓形成障碍，其通过在人的反应部位和肝素结合位点突变氨基酸而获得 AT III使用重组DNA技术，使用编码AT III的DNA作为模板，转化为另一种氨基酸。 通过温育由其中插入有突变体的cDNA的表达载体转化的宿主来大规模生产上述突变体的方法。
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5.发明授权Carboximide derivatives, process for their production and medicines containing same 失效碳酰亚胺衍生物，其生产方法及含有其的药物
公开(公告)号：EP0111226B1
公开(公告)日：1987-09-16
申请号：EP83111830.2
申请日：1983-11-25
申请人： Eisai Co., Ltd.
发明人： Hirose, Noriyasu , Souda, Shigeru , Miyake, Kazutoshi , Kuriyama, Shizuo , Usuki, Kazuyasu , Akiyama, Yasuhiro , Nagaoka, Naoko , Kawashima, Hidetoshi
IPC分类号： C07D209/48 , C07D209/76 , C07D401/12 , C07D403/12 , A61K31/40
CPC分类号： C07D209/48 , C07D209/76 , C07D401/12 , C07D403/12
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6.发明公开Carboximide derivatives, process for their production and medicines containing same 失效甲酰亚胺衍生物，含有它们的制备方法和药物。
公开(公告)号：EP0111226A1
公开(公告)日：1984-06-20
申请号：EP83111830.2
申请日：1983-11-25
申请人： Eisai Co., Ltd.
发明人： Hirose, Noriyasu , Souda, Shigeru , Miyake, Kazutoshi , Kuriyama, Shizuo , Usuki, Kazuyasu , Akiyama, Yasuhiro , Nagaoka, Naoko , Kawashima, Hidetoshi
IPC分类号： C07D209/48 , C07D209/76 , C07D401/12 , C07D403/12 , A61K31/40
CPC分类号： C07D209/48 , C07D209/76 , C07D401/12 , C07D403/12
摘要： A carboximide derivative represented by the general formula:
wherein X is
Z is alkyl, aralkyl, cycloalkyl, cycloalkylalkyl, alkenyl or arylalkenyl, and Y is a substituted or unsubstituted pyridyl, pyrimidyl or phenyl group, and a pharmaceutically acceptable acid addition salt thereof. The carboximide derivative and acid addition salt are useful for treating diabetes and also for depressing the central nervous system. The carboximide derivative may be produced by reacting a sodium alkoxide represented by the general formula:
wherein X and Y have the same meanings as defined above, with Z·Hal wherein Hal is a halogen and Z has the same meaning as defined above.
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