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1. 发明申请

WO1995012587A1 5-ARYLISOXAZOL-4-YL-SUBSTITUTED 2-AMINO CARBOXYLIC ACID COMPOUNDS 审中-公开
标题翻译： 5-ARYLISOXAZOL-4-YL-取代的2-氨基羧酸化合物
公开(公告)号：WO1995012587A1
公开(公告)日：1995-05-11
申请号：PCT/DK1994000411
申请日：1994-11-02
申请人： H. LUNDBECK A/S , MOLTZEN, Lenz, Sibylle , FALCH, Erik , BOGESO, Klaus, Peter , KROGSGAARD-LARSEN, Povl
发明人： H. LUNDBECK A/S
IPC分类号： C07D261/12
CPC分类号： C07D413/04 , C07D261/12 , C07D413/14 , C07D417/04
摘要： 2-Aminocarboxylic acid compounds substituted with 5-arylisoxazol-4-yl or 5-arylisothiazol-4-yl and having general formula (I), wherein A is a bond or a spacer group; B is a group -CH(NR'R'')-COOH wherein R' and R'' are independently hydrogen or C1-6 alkyl, or B is a group of formula (II), wherein R2, R3 and R4 are substituents; or R3 and R4 or R4 and R2 are connected in order to form a ring; E is O, S, COO, (CH2)n-COO, O-(CH2)n-COO or S-(CH2)n-COO wherein n is 1-6, 5-tetrazolyl, 5-tetrazolyl-C1-6 alkyl, 3-hydroxyisoxazolyl or 3-hydroxyisoxazolyl-C1-6 alkyl; D is O or S; and R1 is an optionally substituted aryl or heteroaryl group; are excitatory amino acid 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：用5-芳基异恶唑-4-基或5-芳基异噻唑-4-基取代的具有通式（I）的2-氨基羧酸化合物，其中A是键或间隔基; B是基团-CH（NR'R“）-COOH，其中R'和R”独立地是氢或C 1-6烷基，或B是式（II）的基团，其中R 2，R 3和R 4是取代基 ; 或R3和R4或R4和R2连接以形成环; E是O，S，COO，（CH 2）n -COO，O-（CH 2）n -COO或S-（CH 2）n -COO，其中n是1-6,5-五唑基，5-四唑基-C1-6 烷基，3-羟基异恶唑基或3-羟基异恶唑基-C 1-6烷基; D为O或S; 并且R 1是任选取代的芳基或杂芳基; 是兴奋性氨基酸受体配体，可用于治疗脑缺血，亨廷顿病，癫痫病，帕金森病，阿尔茨海默病，精神分裂症，疼痛，抑郁和焦虑。

2. 发明申请

WO1998015542A1 3-ALKOXYISOXAZOL-4-YL-SUBSTITUTED 2-AMINO CARBOXYLIC ACID COMPOUNDS 审中-公开
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：WO1998015542A1
公开(公告)日：1998-04-16
申请号：PCT/DK1997000426
申请日：1997-10-03
申请人： H. LUNDBECK A/S , BANG-ANDERSEN, Benny , BOGESO, Klaus, Peter , KROGSGAARD-LARSEN, Povl , MOLTZEN LENZ, Sibylle
发明人： H. LUNDBECK A/S
IPC分类号： C07D261/12
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，亨廷顿氏病，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。

3. 发明申请

WO1996026929A1 4-AMINOTETRAHYDROBENZISOXAZOLE OR -ISOTHIAZOLE COMPOUNDS 审中-公开
标题翻译： 4-氨基四氢唑并噻唑或异噻唑化合物
公开(公告)号：WO1996026929A1
公开(公告)日：1996-09-06
申请号：PCT/DK1996000084
申请日：1996-02-28
申请人： H. LUNDBECK A/S , FALCH, Erik , PERREGAARD, Jens, Kristian , SCHOUSBOE, Arne , KROGSGAARD-LARSEN, Povl , FROLUND, Bente , MOLTZEN, Lenz, Sibylle
发明人： H. LUNDBECK A/S
IPC分类号： C07D261/20
CPC分类号： C07D275/04 , C07D261/20 , C07D417/12
摘要： 4-aminotetrahydrobenzisoxazole or -isothiazole compounds having general formulae (Ia) and (Ib), wherein R -R , X and P are further defined in the description. The disclosed compounds have GABA (4-aminobutanoic acid) inhibiting activity and are useful in the treatment of analgesia, psychosis, convulsions, anxiety or muscular and movement disorders, especially epilepsy.
摘要翻译：在描述中进一步定义具有通式（Ia）和（Ib）的4-氨基四氢苯并异恶唑或 - 异噻唑化合物，其中R 1 -R 6，X和P。所公开的化合物具有GABA（4-氨基丁酸）抑制活性，并且可用于治疗镇痛，精神病，惊厥，焦虑或肌肉和运动障碍，特别是癫痫。

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