申请人:YAMANOUCHI PHARMACEUTICAL CO., LTD.
公开号:EP0878196A1
公开(公告)日:1998-11-18
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 R1, R2, R3, R4 and R5 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 R2 and R3 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.
以抑制凯宁酸神经毒性为基础的神经元保护剂以及可用作此类保护剂的化合物。通式(I)代表的吡啶噻嗪衍生物或其药学上可接受的盐,以及含有这些化合物或其药学上可接受的盐作为活性成分的神经元毒性抑制剂,其中 A 代表吡啶环;式(II)代表式(III)或式(IV);R1、R2、R3、R4 和 R5 相同或不同,各自代表氢、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 R2 和 R3 共同形成一个含氮杂环,任选具有一个氮原子作为另一个杂原子,与苯环融合,或被低级烷基取代。