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1. 发明授权

US06200999B1 3-Alkoxyisoxazol-4-yl-substituted 2-amino carboxylic acid compounds 失效
标题翻译： 3-烷氧基异恶唑-4-基取代的2-氨基羧酸化合物
公开(公告)号：US06200999B1
公开(公告)日：2001-03-13
申请号：US09269356
申请日：1999-05-20
申请人： Benny Bang-Andersen , Klaus Peter Bøgesø , Povl Krogsgaard-Larsen , Sibylle Moltzen Lenz
发明人： Benny Bang-Andersen , Klaus Peter Bøgesø , Povl Krogsgaard-Larsen , Sibylle Moltzen Lenz
IPC分类号： A61K3142
CPC分类号： C07D275/03 , A61K31/42 , A61K31/422 , C07D261/12 , C07D261/18
摘要： (3-Alkoxyisoxazol-4-yl)-substituted 2-amino carboxylic acid derivatives and sulfur analogues thereof having 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; 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.
摘要翻译：（3-烷氧基异恶唑-4-基） - 取代的2-氨基羧酸衍生物及其具有通式（I）或（II）的硫类似物，其中R1是氢，烷基，烯基，炔基，环烷基（en）（烯）基（en / yn）基或任选取代的苯基 - 烷（烯/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被定义为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为O或S; 是兴奋性氨基酸（EAA），特别是AMPA和/或NMDA受体配体，可用于治疗脑缺血，亨廷顿病，癫痫病症，帕金森病，阿尔茨海默病，精神分裂症，疼痛，抑郁和焦虑。

2. 发明授权

US06174909B1 4-aminotetrahydrobenzisoxazole or -isothiazole compounds 失效
标题翻译： 4-氨基四氢苯并异恶唑或 - 异噻唑化合物
公开(公告)号：US06174909B1
公开(公告)日：2001-01-16
申请号：US09412721
申请日：1999-10-05
申请人： Erik Falch , Jens Kristian Perregaard , Arne Schousboe , Povl Krogsgaard-Larsen , Bente Frolund , Sibylle Moltzen Lenz
发明人： Erik Falch , Jens Kristian Perregaard , Arne Schousboe , Povl Krogsgaard-Larsen , Bente Frolund , Sibylle Moltzen Lenz
IPC分类号： A61K31428
CPC分类号： C07D275/04 , C07D261/20 , C07D417/12
摘要： The present invention relates to novel 4-aminotetrahydrobenzisoxazoles or 4-aminotetrahydrobenziothiazoles having gamma-aminobutanoic acid (GABA)-uptake inhibiting activity and thus useful in the treatment of analgesia, psychosis, convulsions, anxiety, epileptic disorders or muscular and movement disorders, such as spastic disorders or symptoms in Huntington's disease or Parkinson disease.
摘要翻译：本发明涉及具有γ-氨基丁酸（GABA） - 摄取抑制活性的新型4-氨基四氢苯并异恶唑或4-氨基四氢苯并噻唑，因此可用于治疗镇痛，精神病，惊厥，焦虑，癫痫症或肌肉和运动障碍，例如亨廷顿病或帕金森病中的痉挛性疾病或症状。

3. 发明授权

US5998613A 4-aminotetrahydrobenzisoxazole or -isothiazole compounds 失效
标题翻译： 4-氨基四氢苯并异恶唑或 - 异噻唑化合物
公开(公告)号：US5998613A
公开(公告)日：1999-12-07
申请号：US942467
申请日：1997-08-05
申请人： Erik Falch , Jens Kristian Perregaard , Arne Schousboe , Povl Krogsgaard-Larsen , Bente Frolund , Sibylle Moltzen Lenz
发明人： Erik Falch , Jens Kristian Perregaard , Arne Schousboe , Povl Krogsgaard-Larsen , Bente Frolund , Sibylle Moltzen Lenz
IPC分类号： A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61P25/00 , C07D261/20 , C07D275/04 , C07D413/12 , C07D417/12 , C07D275/03 , C07D277/02 , C07D307/02 , C07D311/78 , C07D313/20 , C07D337/00 , C07D409/14
CPC分类号： C07D275/04 , C07D261/20 , C07D417/12
摘要： The present invention relates to novel 4-aminotetrahydrobenzisoxazoles or 4-aminotetrahydrobenziothiazoles having gamma-aminobutanoic acid (GABA)-uptake inhibiting activity and thus useful in the treatment of analgesia, psychosis, convulsions, anxiety, epileptic disorders or muscular and movement disorders, such as spastic disorders or symptoms in Huntington's disease or Parkinson disease.
摘要翻译：本发明涉及具有γ-氨基丁酸（GABA） - 摄取抑制活性的新型4-氨基四氢苯并异恶唑或4-氨基四氢苯并噻唑，因此可用于治疗镇痛，精神病，惊厥，焦虑，癫痫症或肌肉和运动障碍，例如亨廷顿病或帕金森病中的痉挛性疾病或症状。

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