公开(公告)号：EP0878196A1

公开(公告)日：1998-11-18

申请号：EP96938464.3

申请日：1996-11-14

申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD.

发明人： SHISHIKURA, Jun-ichi ,  INAMI, Hiroshi ,  YASUNAGA, Tomoyuki ,  HIRANO, Masaaki ,  SAKAMOTO, Shuichi ,  OHNO, Kazushige ,  OKADA, Masamichi ,  TSUKAMOTO, Shin-ichi

IPC分类号： A61K31/54 ,  C07D513/04

CPC分类号： A61K31/5415

摘要： Neuron protective agents on the basis of the inhibition of neuronotoxicity of kainic acid and compounds useful as such agents. Pyridothiazine derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof and neuronotoxicity inhibitors containing as the active ingredient these compounds or pharmaceutically acceptable salts thereof, wherein A represents a pyridine ring; formula (II) represents formula (III) or formula (IV); and R 1 , R 2 , R 3 , R 4 and R 5 are the same or different and each represents hydrogen, optionally substituted lower alkyl, cycloalkyl, alkenyl, aryl, carboxy or lower alkoxycarbonyl or does not exist, or R 2 and R 3 together form a nitrogenous heterocycle optionally having a nitrogen atom as another heteroatom, being fused with a benzene ring, or being substituted by lower alkyl.

摘要翻译： 神经元保护剂，其基础是抑制红藻氨酸的神经毒性和用作此类药物的化合物。 通式（I）表示的吡唑并噻嗪衍生物或其药学上可接受的盐和含有这些化合物或其药学上可接受的盐的活性成分的神经毒性抑制剂，其中A表示吡啶环; 式（II）表示式（III）或式（IV）; 和R 1，R 2，R 3，R 4和R 5相同或不同，各自表示氢，任选取代的低级烷基，环烷基，烯基，芳基，羧基或低级烷氧基羰基 或不存在，或R 2和R 3一起形成任选具有氮原子作为另一杂原子的含氮杂环，与苯环稠合或被低级烷基取代。

公开(公告)号：EP0878196B1

公开(公告)日：2003-09-03

申请号：EP96938464.3

申请日：1996-11-14

申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD.

发明人： SHISHIKURA, Jun-ichi ,  INAMI, Hiroshi ,  YASUNAGA, Tomoyuki ,  HIRANO, Masaaki ,  SAKAMOTO, Shuichi ,  OHNO, Kazushige ,  OKADA, Masamichi ,  TSUKAMOTO, Shin-ichi

IPC分类号： A61K31/54 ,  C07D513/04

CPC分类号： A61K31/5415

摘要： Neuron protective agents on the basis of the inhibition of neuronotoxicity of kainic acid and compounds useful as such agents. Pyridothiazine derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof and neuronotoxicity inhibitors containing as the active ingredient these compounds or pharmaceutically acceptable salts thereof, wherein A represents a pyridine ring; formula (II) represents formula (III) or formula (IV); and R , R , R , R and R are the same or different and each represents hydrogen, optionally substituted lower alkyl, cycloalkyl, alkenyl, aryl, carboxy or lower alkoxycarbonyl or does not exist, or R and R together form a nitrogenous heterocycle optionally having a nitrogen atom as another heteroatom, being fused with a benzene ring, or being substituted by lower alkyl.