发明公开
EP0794184A1 6-METHOXY-1H-BENZOTRIAZOLE-5-CARBOXAMIDE DERIVATIVES, PROCESS FOR PRODUCING THE SAME, AND MEDICINAL COMPOSITION CONTAINING THE SAME
失效
6-甲氧基-1,5-苯并噻唑-5-羧酰胺衍生物，VERFAHREN ZUR HERSTELLUNG，DIESE ENTHALTENDE ARZNEIMITTEL
- 专利标题： 6-METHOXY-1H-BENZOTRIAZOLE-5-CARBOXAMIDE DERIVATIVES, PROCESS FOR PRODUCING THE SAME, AND MEDICINAL COMPOSITION CONTAINING THE SAME
- 专利标题（中）： 6-甲氧基-1,5-苯并噻唑-5-羧酰胺衍生物，VERFAHREN ZUR HERSTELLUNG，DIESE ENTHALTENDE ARZNEIMITTEL
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申请号： EP95936779.8申请日： 1995-11-13
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公开(公告)号： EP0794184A1公开(公告)日： 1997-09-10
- 发明人: KATO, Shiro , HIROKAWA, Yoshimi , YAMAZAKI, Hiroshi , MORIE, Toshiya , YOSHIDA, Naoyuki
- 申请人： DAINIPPON PHARMACEUTICAL CO., LTD.
- 申请人地址： 6-8, Doshomachi 2-chome Chuo-ku Osaka-shi, Osaka 541 JP
- 专利权人： DAINIPPON PHARMACEUTICAL CO., LTD.
- 当前专利权人： DAINIPPON PHARMACEUTICAL CO., LTD.
- 当前专利权人地址： 6-8, Doshomachi 2-chome Chuo-ku Osaka-shi, Osaka 541 JP
- 代理机构： Kraus, Walter, Dr.
- 优先权： JP312673/94 19941121
- 国际公布： WO9616059 19960530
- 主分类号： C07D403/12
- IPC分类号： C07D403/12 ; A61K31/55 ; A61K31/41
摘要：
6-Methoxy-1H-benzotriazole-5-carboxamide derivatives which are represented by the formula (I) below:
[in which R 1 stands for ethyl or cyclopropylmethyl group,
R 2 stands for hydrogen atom, methyl or ethyl group,
n is 1, 2 or 3, and
the wavy line ( ) signifies that configuration of the substituents on the carbon atom bound to the N-atom in the amide moiety is racemic (RS) or optically active (R or S)]
or their pharmaceutically acceptable acid addition salts; processes for their preparation; pharmaceutical compositions containing a compound of formula (I) or its pharmaceutically acceptable acid addition salt; and novel intermediates.
The compounds of the present invention possess concurrently excellent antiemetic activity and gastrointestinal motility enhancing activity. They furthermore exhibit less central nervous system (CNS) depressant activity and, therefore, are used for treatments and prophylaxis of functional disorders of gastrointestinal tract associated with various diseases and therapeutical treatments, as gastrointestinal motility enhancing agent.
[in which R 1 stands for ethyl or cyclopropylmethyl group,
R 2 stands for hydrogen atom, methyl or ethyl group,
n is 1, 2 or 3, and
the wavy line ( ) signifies that configuration of the substituents on the carbon atom bound to the N-atom in the amide moiety is racemic (RS) or optically active (R or S)]
or their pharmaceutically acceptable acid addition salts; processes for their preparation; pharmaceutical compositions containing a compound of formula (I) or its pharmaceutically acceptable acid addition salt; and novel intermediates.
The compounds of the present invention possess concurrently excellent antiemetic activity and gastrointestinal motility enhancing activity. They furthermore exhibit less central nervous system (CNS) depressant activity and, therefore, are used for treatments and prophylaxis of functional disorders of gastrointestinal tract associated with various diseases and therapeutical treatments, as gastrointestinal motility enhancing agent.
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