发明公开
- 专利标题： Sulfonamide derivatives
- 专利标题（中）： 磺酰胺衍生物
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申请号： EP91307061.1申请日： 1991-08-01
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公开(公告)号： EP0469901A1公开(公告)日： 1992-02-05
- 发明人: Sato, Masakazu , Kawashima, Yutaka , Goto, Jun , Chiba, Yoshiyuki , Satake, Mikio , Iwata, Chuzo , Imanishi, Takeshi
- 申请人： TAISHO PHARMACEUTICAL CO. LTD , NIPPON SUISAN KAISHA, LTD.
- 申请人地址： 24-1 Takata 3-chome Toshima-ku Tokyo 171 JP
- 专利权人： TAISHO PHARMACEUTICAL CO. LTD,NIPPON SUISAN KAISHA, LTD.
- 当前专利权人： TAISHO PHARMACEUTICAL CO. LTD,NIPPON SUISAN KAISHA, LTD.
- 当前专利权人地址： 24-1 Takata 3-chome Toshima-ku Tokyo 171 JP
- 代理机构： Lamb, John Baxter
- 优先权： JP204732/90 19900801
- 主分类号： C07C323/49
- IPC分类号： C07C323/49 ; C07C317/28 ; C07C317/44 ; C07C323/20 ; C07D213/71 ; A61K31/18
摘要：
Sulfonamide derivative, useful as blood platelet aggregation inhibitors, have the formula:
in which A is a naphthyl group, a pyridyl group, a phenyl group, a phenyl group substituted by 1 to 5 substituents selected from halogen atoms, alkyl groups having 1 to 4 carbon atoms, alkoxy groups having 1 to 4 carbon atoms, nitro groups and acetamido groups, or an alkyl group having 1 to 20 carbon atoms; B is an alkylene group having 1 to 3 carbon atoms, a group -OCH₂- or a group -CH=CH-; X and Y are the same or different, and each is a hydrogen or fluorine atom; R is a carboxy group, an alkyoxycarbonyl group having 2 to 5 carbon atoms, a hydroxymethyl group or a group of the formula
(in which R¹ is a hydrogen atom or an alkyl group having 1 to 3 carbon atoms; R² is a hydrogen atom, a hydroxyl group, an alkyl group having 1 to 3 carbon atoms, a carboxymethyl group or an alkoycarbonylmethyl group having 3 to 6 carbon atoms); m is 0, 1 or 2; n is 0,1,2 or 3; or salts thereof.
This invention also provided intermediates for the preparation of the sulfonamide, which intermediates are thiophenols of the formula:
(in which R, X and Y are as defined above).
in which A is a naphthyl group, a pyridyl group, a phenyl group, a phenyl group substituted by 1 to 5 substituents selected from halogen atoms, alkyl groups having 1 to 4 carbon atoms, alkoxy groups having 1 to 4 carbon atoms, nitro groups and acetamido groups, or an alkyl group having 1 to 20 carbon atoms; B is an alkylene group having 1 to 3 carbon atoms, a group -OCH₂- or a group -CH=CH-; X and Y are the same or different, and each is a hydrogen or fluorine atom; R is a carboxy group, an alkyoxycarbonyl group having 2 to 5 carbon atoms, a hydroxymethyl group or a group of the formula
(in which R¹ is a hydrogen atom or an alkyl group having 1 to 3 carbon atoms; R² is a hydrogen atom, a hydroxyl group, an alkyl group having 1 to 3 carbon atoms, a carboxymethyl group or an alkoycarbonylmethyl group having 3 to 6 carbon atoms); m is 0, 1 or 2; n is 0,1,2 or 3; or salts thereof.
This invention also provided intermediates for the preparation of the sulfonamide, which intermediates are thiophenols of the formula:
(in which R, X and Y are as defined above).
公开/授权文献
- EP0469901B1 Sulfonamide derivatives 公开/授权日：1994-10-19
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