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公开(公告)号:EP0469901A1
公开(公告)日:1992-02-05
申请号:EP91307061.1
申请日:1991-08-01
发明人: Sato, Masakazu , Kawashima, Yutaka , Goto, Jun , Chiba, Yoshiyuki , Satake, Mikio , Iwata, Chuzo , Imanishi, Takeshi
IPC分类号: C07C323/49 , C07C317/28 , C07C317/44 , C07C323/20 , C07D213/71 , A61K31/18
CPC分类号: C07C317/44 , C07C317/28 , C07C323/49 , C07C323/62 , C07D213/71
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).摘要翻译: 可用作血小板聚集抑制剂的磺酰胺衍生物具有下式:其中A是萘基,吡啶基,苯基,被1至5个选自卤素原子的取代基取代的苯基,具有1至4个碳原子的烷基 碳原子,具有1至4个碳原子的烷氧基,硝基和乙酰氨基,或具有1至20个碳原子的烷基; B是具有1-3个碳原子的亚烷基,基团-OCH 2 - 或基团-CH = CH-; X和Y相同或不同,并且各自是氢或氟原子; R为羧基,具有2至5个碳原子的烷氧基羰基,羟甲基或下式基团(其中R 1为氢原子或具有1至3个碳原子的烷基; R 2为氢原子, 羟基,碳原子数为1〜3的烷基,羧甲基或碳原子数为3〜6的烷基羰甲基)。 m是0,1或2; n是0,1,2或3; 或其盐。 本发明还提供了用于制备磺酰胺的中间体,其中间体是下式的苯硫酚:(其中R,X和Y如上所定义)。
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公开(公告)号:EP0469901B1
公开(公告)日:1994-10-19
申请号:EP91307061.1
申请日:1991-08-01
发明人: Sato, Masakazu , Kawashima, Yutaka , Goto, Jun , Chiba, Yoshiyuki , Satake, Mikio , Iwata, Chuzo , Imanishi, Takeshi
IPC分类号: C07C323/49 , C07C317/28 , C07C317/44 , C07C323/20 , C07D213/71 , A61K31/18
CPC分类号: C07C317/44 , C07C317/28 , C07C323/49 , C07C323/62 , C07D213/71
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公开(公告)号:EP0381439A1
公开(公告)日:1990-08-08
申请号:EP90300945.4
申请日:1990-01-30
发明人: Iwata, Chuzo , Imanishi, Takeshi , Chiba, Yoshiyuki , Satake, Mikio , Sato, Masakazu , Kawashima, Yutaka , Goto, Jun
IPC分类号: C07D249/14 , A61K31/41
CPC分类号: C07D249/14
摘要: Triazole derivatices useful as lipid peroxidation inhibitors have the formula:
in which R¹ is a hydrogen atom, a C₁-C₄ alkyl group, an acetyl group, a naphthylmethyl group, an anthrylmethyl group or a group of the formula
(in which X, Y and Z are the same or different and each is a hydrogen or halogen atom, a C₁-C₄ alkyl group, a C₁-C₄ alkoxy group, a hydroxyl group, a nitro group, a trifluoromethyl group, a cyano group or a benzyloxy group); R² is a hydrogen atom or an acetyl group; and R³ is a hydrogen atom, an acetyl group or a group of the formula
(in which R¹ and R² have the meanings defined above).摘要翻译: 可用作脂质过氧化抑制剂的三唑衍生物具有下式:其中R 1是氢原子,C 1 -C 4烷基,乙酰基,萘基甲基,蒽基甲基或式 CHEM>(其中X,Y和Z相同或不同,各自为氢或卤素原子,C1-C4烷基,C1-C4烷氧基,羟基,硝基,三氟甲基, 氰基或苄氧基); R 2是氢原子或乙酰基; 和R 3是氢原子,乙酰基或式CHEM的基团(其中R 1和R 2具有上述定义)。 一个
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