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1. 发明公开

KR1020000048908A 3-알콕시이속사졸-4-일-치환 2-아미노카르복실산 화합물 无效
标题翻译： 3-烷氧基甲基-4-取代的2-氨基羧酸化合物
公开(公告)号：KR1020000048908A
公开(公告)日：2000-07-25
申请号：KR1019997002938
申请日：1997-10-03
申请人： 하. 룬트벡 아크티에 셀스카브
发明人： 방-안데르센베니 , 뵈게죄클라우스페터 , 크로크스가아르트-라르센포플 , 몰첸렌츠지빌레
IPC分类号： C07D261/12
CPC分类号： C07D275/03 , A61K31/42 , A61K31/422 , C07D261/12 , C07D261/18
摘要： PURPOSE: 3-alkoxyisoxazol-4-yl-substituted 2-amino carboxylic acid compounds are provided which are excitatory amino acid (EAA), in particular AMPA and/or NMDA receptor ligands, useful in the treatment of cerebral ischaemia, Huntington's disease, epileptic disorders, Parkinson's disease, Alzheimer's disease, schizophrenia, pain, depression and anxiety. CONSTITUTION: 3-Alkoxyisoxazol-4-yl)-substituted 2-amino carboxylic acid derivatives and sulfur analogues thereof are represented by general formula (I) or (II), wherein R1 is hydrogen, alkyl, alkenyl, alkynyl, cycloalk(en)yl, cycloalk(en)yl-alk(en/yn)yl, or optionally substituted phenyl-alk(en/yn)yl; A is a bond or a hydrocarbon spacer group; B is a group -CRa(NRbRc)-COOR5 wherein Ra-Rc are independently hydrogen or alkyl, and R5 is defined as R1 or pivaloyloxymethyl, or B is a group of formula (III), wherein R2, R3 and R4 are independently selected from hydrogen, a non-aromatic hydrocarbon group, phenyl- and thienyl-alkyl, and a hetero aliphatic group, or R3 and R4 are connected, thereby forming an alkylene, alkenylene or alkynylene group, or R4 and R2 are connected in order to form an alkylene, alkenylene or alkynylene group, optionally substituted with hydroxy or methyl, or to form CH2-O-CH2; E is COOR6, where R6 is defined as R5, or E is a tetrazolyl or triazolyl; X is O or S; and Y is O or S.
摘要翻译：目的：提供3-烷氧基异恶唑-4-基取代的2-氨基羧酸化合物，其是兴奋性氨基酸（EAA），特别是AMPA和/或NMDA受体配体，可用于治疗脑局部缺血，亨廷顿病，癫痫疾病，帕金森病，阿尔茨海默病，精神分裂症，疼痛，抑郁和焦虑。构型：3-烷氧基异恶唑-4-基） - 取代的2-氨基羧酸衍生物及其硫类似物由通式（I）或（II）表示，其中R 1是氢，烷基，烯基，炔基，环烷（烯）（烯）基（en / yn）基或任选取代的苯基 - 烯（烯/炔）基; A是键或烃间隔基; B是基团-CRa（NRbRc）-COOR5，其中Ra-Rc独立地是氢或烷基，R5定义为R1或新戊酰氧基甲基，或B是式（III）的基团，其中R2，R3和R4独立地选自从氢，非芳族烃基，苯基 - 和噻吩基 - 烷基和杂脂族基团，或R3和R4连接，从而形成亚烷基，亚烯基或亚炔基，或连接R4和R2以形成任选被羟基或甲基取代的亚烷基，亚烯基或亚炔基，或形成CH 2 -O-CH 2; E是COOR 6，其中R 6定义为R 5，或E是四唑基或三唑基; X是O或S; Y是O或S.

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