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1. 发明授权

US06291689B1 Method for the preparation of citalopram 失效
标题翻译：西酞普兰制备方法
公开(公告)号：US06291689B1
公开(公告)日：2001-09-18
申请号：US09565061
申请日：2000-05-03
申请人： Hans Petersen , Klaus Peter Bøgesø , Michael Bech Sommer
发明人： Hans Petersen , Klaus Peter Bøgesø , Michael Bech Sommer
IPC分类号： C07D30787
CPC分类号： C07C69/76 , C07C235/42 , C07C255/53 , C07D307/87
摘要： A method for the preparation of citalopram is described comprising reduction of the oxo group of a compound of formula (IV), wherein R1 is CN, C1-6 alkyloxycarbonyl or C1-6 alkylaminocarbonyl, ring closure of the resulting hydroxy compound thereby obtaining the corresponding 1-(4-fluorophenyl)-1,3-dihydroisobenzofuran, then if R1 is cyano using it directly in the next step and if R1 is C1-6 alkyloxycarbonyl or C1-6 alkylaminocarbonyl, conversion of the compound to the corresponding compound wherein R1 is a cyano; and alkylation of the resulting 5-cyano compound with 3-dimethyl-aminopropylhalogenide in basic conditions thereby obtaining citalopram.
摘要翻译：描述了制备西酞普兰的方法，其包括将式（Ⅳ）化合物的氧代基还原，其中R 1是CN，C 1-6烷氧基羰基或C 1-6烷基氨基羰基，所得羟基化合物闭环，从而得到相应的 1-（4-氟苯基）-1,3-二氢异苯并呋喃，然后如果R 1是氰基，则直接用于下一步骤，如果R 1是C 1-6烷氧基羰基或C 1-6烷基氨基羰基，则化合物转化成相应的化合物，其中R 1 是氰基; 并在碱性条件下用3-二甲基 - 氨基丙基卤化物烷基化所得的5-氰基化合物，从而得到西酞普兰。

2. 发明授权

US06921774B2 Compounds and their use as glycine transport inhibitors 失效
标题翻译：化合物及其作为甘氨酸转运抑制剂的用途
公开(公告)号：US06921774B2
公开(公告)日：2005-07-26
申请号：US10348490
申请日：2003-01-17
申请人： Ejner Knud Moltzen , Paul Garrick Smith , Christian Krog-Jensen , Klaus Peter Bøgesø
发明人： Ejner Knud Moltzen , Paul Garrick Smith , Christian Krog-Jensen , Klaus Peter Bøgesø
IPC分类号： A61K31/198 , A61K31/343 , A61K31/381 , A61P9/10 , A61P21/02 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/28 , C07C229/14 , C07C255/58 , C07D307/87 , C07D333/72 , C07D405/04 , A61K31/34 , A61K31/195 , C07C229/36
CPC分类号： C07D307/87 , C07C229/14 , C07C255/58 , C07C2602/08 , C07D333/72 , C07D405/04
摘要： The invention provides novel compounds of the formula I below: wherein the meaning of each substituent is defined in the application. The compounds are useful as inhibitors of the glycine transporter and useful in the treatment of diseases responsive to the inhibition of the glycine transporter. The invention provides a pharmaceutical composition comprising a compound of Formula I as defined above and the use of compounds as above for the manufacture of medicaments for treatment of diseases responsive to ligands of the glycine transporter.
摘要翻译：本发明提供新的下式I化合物：其中每个取代基的含义在本申请中定义。该化合物可用作甘氨酸转运蛋白的抑制剂，并且可用于治疗对甘氨酸转运蛋白的抑制作用的疾病。本发明提供一种药物组合物，其包含如上定义的式I化合物和上述化合物用于制备用于治疗对甘氨酸转运蛋白配体的疾病的药物。

3. 发明授权

US07351734B2 Aminoindane derivatives as serotonin and norepinephrine uptake inhibitors 失效
标题翻译：氨基茚满衍生物作为5-羟色胺和去甲肾上腺素摄取抑制剂
公开(公告)号：US07351734B2
公开(公告)日：2008-04-01
申请号：US10496730
申请日：2002-12-18
申请人： Klaus Peter Bøgesø , Ask Püschl , Jan Kehler , Peter Bregnedal
发明人： Klaus Peter Bøgesø , Ask Püschl , Jan Kehler , Peter Bregnedal
IPC分类号： A61K31/28 , C07D321/00 , C07D307/00
CPC分类号： A61K31/357 , A61K31/135 , C07C211/42 , C07C2602/08 , C07D317/58 , C07D319/18
摘要： The present invention relates to aminoindane derivatives having the formula I wherein X, Y, U, R1-2, R13-16 and R are as defined in the claims, or an acid addition salt thereof. The compounds of the invention posses the combined effect of serotonin reuptake inhibition and norepinephrine uptake inhibition.
摘要翻译：本发明涉及具有式I的氨基茚满衍生物，其中X，Y，U，R 1-2，R 13-16和R如权利要求中所定义，或其酸加成盐。本发明的化合物具有5-羟色胺再摄取抑制和去甲肾上腺素吸收抑制的综合作用。

4. 发明授权

US06492374B2 Benzofuran derivatives, their preparation and use 失效
标题翻译：苯并呋喃衍生物，其制备和用途
公开(公告)号：US06492374B2
公开(公告)日：2002-12-10
申请号：US09874392
申请日：2001-06-04
申请人： Kim Andersen , Mario Rottländer , Klaus Peter Bøgesø , Henrik Pedersen , Thomas Ruhland , Robert Dancer
发明人： Kim Andersen , Mario Rottländer , Klaus Peter Bøgesø , Henrik Pedersen , Thomas Ruhland , Robert Dancer
IPC分类号： C07D40506
CPC分类号： C07D307/87 , C07D405/12 , C07D405/14 , C07D407/12 , C07D471/04
摘要： The present invention relates to benzofuran derivatives having general Formula (I) wherein A is selected from (1), (2), (3), (4) wherein Z is O or S; s is 0 or 1; q is 0 or 1; R4 is hydrogen, C1-6-alkyl, C2-6-alkenyl, C26-alkynyl, C1-6-alkyl-aryl, or C1-6-alkyl-O-aryl; D is a spacer group selected from branched or straight chain C1-6-alkylene, C2-6-alkenylene and C2-6-alkynylene; its enantiomers, and pharmaceutically acceptable acid addition salt thereof. The compounds are potently binding to the 5-HT1A receptor.
摘要翻译：本发明涉及具有通式（I）的苯并呋喃衍生物，其中A选自（1），（2），（3），（4）其中Z是O或S; s为0或1; q为0或1; R 4是氢，C 1-6 - 烷基，C 2-6烯基，C 2-6炔基，C 1-6 - 烷基 - 芳基或C 1-6 - 烷基-O-芳基; D是选自支链或直链C 1-6 - 亚烷基，C 2-6亚烯基和C 2-6亚炔基的间隔基; 其对映体及其药学上可接受的酸加成盐。这些化合物与5-HT1A受体有很强的结合。

5. 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。

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