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1. 发明申请

WO1998019512A2 METHOD FOR THE PREPARATION OF CITALOPRAM 审中-公开
标题翻译：方法制备CITALOPRAM
公开(公告)号：WO1998019512A2
公开(公告)日：1998-05-14
申请号：PCT/DK1997000513
申请日：1997-11-11
申请人： H. LUNDBECK A/S , PETERSEN, Hans , BREGNEDAL, Peter , BOGESO, Klaus, Peter
发明人： H. LUNDBECK A/S
IPC分类号： A61K31/34 , A61K31/343 , A61P25/24 , C07C215/68 , C07C225/22 , C07C233/33 , C07C233/43 , C07D307/87 , C07D307/88
CPC分类号： C07C215/68 , C07C225/22 , C07C233/33 , C07C233/43 , C07D307/87 , C07D307/88
摘要： A method for the preparation of citalopram is described comprising reaction of a compound of Formula (IV) wherein R is H or C1-6alkylcarbonyl successively with a Grignard reagent of 4-halogen-fluorophenyl and a Grignard reagent of 3-halogen-N,N-dimethylpropylamine, effecting ring closure of the resulting compound of Formula (VI) and converting the resulting 1,3-dihydroisobenzofuran compound to the corresponding 5-cyano derivative, i.e. citalopram.
摘要翻译：描述了制备西酞普兰的方法，其包括其中R 1为H或C 1-6烷基羰基的式（IV）化合物与4-卤代 - 氟苯基的格氏试剂和3-卤素 - 氟苯基的格氏试剂反应， N，N-二甲基丙胺，使得到的式（VI）化合物闭环，并将所得的1,3-二氢异苯并呋喃化合物转化为相应的5-氰基衍生物，即西酞普兰。

2. 发明申请

WO9819512A3 METHOD FOR THE PREPARATION OF CITALOPRAM 审中-公开
标题翻译：方法制备CITALOPRAM
公开(公告)号：WO9819512A3
公开(公告)日：1998-08-13
申请号：PCT/DK9700513
申请日：1997-11-11
申请人： LUNDBECK & CO AS H , PETERSEN HANS , BREGNEDAL PETER , BOEGESOE KLAUS PETER
发明人： PETERSEN HANS , BREGNEDAL PETER , BOEGESOE KLAUS PETER
IPC分类号： A61K31/34 , A61K31/343 , A61P25/24 , C07C215/68 , C07C225/22 , C07C233/33 , C07C233/43 , C07D307/87 , C07D307/88
CPC分类号： C07C215/68 , C07C225/22 , C07C233/33 , C07C233/43 , C07D307/87 , C07D307/88
摘要： A method for the preparation of citalopram is described comprising reaction of a compound of Formula (IV) wherein R is H or C1-6alkylcarbonyl successively with a Grignard reagent of 4-halogen-fluorophenyl and a Grignard reagent of 3-halogen-N,N-dimethylpropylamine, effecting ring closure of the resulting compound of Formula (VI) and converting the resulting 1,3-dihydroisobenzofuran compound to the corresponding 5-cyano derivative, i.e. citalopram. 00000
摘要翻译：描述了制备西酞普兰的方法，其包括其中R 1为H或C 1-6烷基羰基的式（IV）化合物与4-卤代 - 氟苯基的格氏试剂和3-卤素 - 氟苯基的格氏试剂反应， N，N-二甲基丙胺，使所得到的式（VI）化合物闭环，并将所得的1,3-二氢异苯并呋喃化合物转化为相应的5-氰基衍生物，即西酞普兰。 00000

3. 发明申请

WO1992010192A1 INDAN DERIVATIVES 审中-公开
标题翻译：印度衍生物
公开(公告)号：WO1992010192A1
公开(公告)日：1992-06-25
申请号：PCT/DK1991000358
申请日：1991-11-28
申请人： H. LUNDBECK A/S , BOGESO, Klaus, P. , BREGNEDAL, Peter
发明人： H. LUNDBECK A/S
IPC分类号： A61K31/495
CPC分类号： C07D207/263 , C07D207/24 , C07D233/42 , C07D235/26 , C07D239/10 , C07D263/22 , C07D295/073 , C07D295/088
摘要： 5-Substituted trans-1-piperazinoindan derivatives having general formula (I), wherein X is halogen, trifluoromethyl, alkyl, alkylthio, alkyloxy, hydroxy, alkylsulphonyl, alkyl- or dialkylamino, trifluoromethylthio or cyano; R is hydrogen, or alkyl, alkenyl, cycloalkyl, or cycloalkyl lower alkyl, optionally substituted with hydroxy, or R is a substituent (a), wherein n is an integer from 1 to 6; U is CH or N; Y is CH2, O, S or N-R , R being hydrogen or cycloalkyl, cycloalkylmethyl, alkyl or alkenyl optionally substituted with hydroxy or an optionally substituted phenyl group; W is O or S; Z is -(CH2)4-, (b), (c), where R and R are hydrogen or lower alkyl, -CH=CH-, -CH=CH-CH2-, optionally substituted 1,2-phenylene, 1,2-C6H4CH2- (to form a quinazolidinone or -thione ring system) or 1,2-C6H4CO- (to form a quinazolidindion or thioxoquinazolidinon ring system); and Ar is an optionally substituted phenyl, thiophene or furane ring; are selective, centrally acting 5-HT2 antagonists useful in the treatment of anxiety, depression, sleeping disorders, negative symptoms of schizophrenia and migraine.
摘要翻译： 5-取代的具有通式（I）的反式-1-哌嗪基茚满二醇衍生物，其中X为卤素，三氟甲基，烷基，烷硫基，烷氧基，羟基，烷基磺酰基，烷基 - 或二烷基氨基，三氟甲硫基或氰基; R是氢或任选被羟基取代的烷基，烯基，环烷基或环烷基低级烷基，或R是取代基（a），其中n是1至6的整数; U是CH或N; Y是CH 2，O，S或N-R 1，R 1是氢或环烷基，环烷基甲基，任选被羟基或任选取代的苯基取代的烷基或链烯基; W为O或S; Z是 - （CH 2）4 - ，（b），（c），其中R 2和R 3是氢或低级烷基，-CH = CH-，-CH = CH-CH 2 - ，2-亚苯基，1,2-C 6 H 4 CH 2 - （以形成喹唑啉酮或硫酮环系）或1,2--C 6 H 4 CO-（以形成喹唑啉基或硫代喹唑啉酮环系）。并且Ar是任选取代的苯基，噻吩或呋喃环; 是选择性的中枢作用的5-HT2拮抗剂，可用于治疗焦虑，抑郁，睡眠障碍，精神分裂症和偏头痛的阴性症状。

4. 发明申请

WO2003055873A1 AMINOINDANE DERIVATIVES AS SEROTONIN AND NOREPINEPHRINE UPTAKE INHIBITORS 审中-公开
标题翻译：氨基嘌呤衍生物作为丝氨酸和诺贝宁治疗抑制剂
公开(公告)号：WO2003055873A1
公开(公告)日：2003-07-10
申请号：PCT/DK2002/000873
申请日：2002-12-18
申请人： H. LUNDBECK A/S , BØGESØ, Klaus, Peter , PÜSCHL, Ask , KEHLER, Jan , BREGNEDAL, Peter
发明人： BØGESØ, Klaus, Peter , PÜSCHL, Ask , KEHLER, Jan , BREGNEDAL, Peter
IPC分类号： C07D317/48
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, R 1-2 , R 13-16 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。

5. 发明申请

WO1993022293A1 1-PIPERAZINO-1,2-DIHYDROINDENE DERIVATIVES 审中-公开
标题翻译： 1-哌嗪-1,2-二氢化茚衍生物
公开(公告)号：WO1993022293A1
公开(公告)日：1993-11-11
申请号：PCT/DK1993000136
申请日：1993-04-23
申请人： H. LUNDBECK A/S , BOGESO, Klaus , BREGNEDAL, Peter
发明人： H. LUNDBECK A/S
IPC分类号： C07D241/04
CPC分类号： C07D241/38 , C07D295/033 , C07D295/073 , C07D333/20 , C07D471/04
摘要： Trans isomers of 1-piperazino-1,2-dihydroindene compounds having general formula (I), wherein X and Y are hydrogen, halogen, trifluoromethyl, alkyl, alkylthio, trifluoromethylthio, alkoxy, hydroxy, alkylsulfonyl, amino, alkylamino, nitro or cyano; Ar is a phenyl, thienyl or furyl group, each optionally substituted; R1 is hydrogen, or optionally hydroxy substituted alkyl, alkenyl, cycloalkyl or cycloalkylalkyl; R2 is alkyl, alkenyl, cycloalkyl, or cycloalkylalkyl; or R1 and R2 together form a 5 to 7-membered heterocyclic ring fused with the piperazine ring, which ring may be substituted with hydroxy; R3 is hydrogen, alkyl, r alkenyl, cycloalkyl or cycloalkylalkyl; or R2 and R3 together form a 3 to 7-membered carbocyclic ring which is spirofused to the piperazine ring; and R4 is hydrogen or alkyl; have potent antagonistic action on dopamine D1 receptors. The compounds are useful in the treatment of diseases in the central nervous system, in particular psychoses, schizophrenia (positive as well as negative symptoms), anxiety, depression, sleep disturbances, migraine, Parkinson's disease or cocaine abuse.
摘要翻译：具有通式（I）的1-哌嗪基-1,2-二氢茚化合物的反式异构体，其中X和Y是氢，卤素，三氟甲基，烷基，烷硫基，三氟甲硫基，烷氧基，羟基，烷基磺酰基，氨基，烷基氨基，硝基或氰基 ; Ar是苯基，噻吩基或呋喃基，各自任选被取代; R 1是氢或任选的羟基取代的烷基，烯基，环烷基或环烷基烷基; R2是烷基，烯基，环烷基或环烷基烷基; 或者R 1和R 2一起形成与哌嗪稠合的5至7元杂环，该环可以被羟基取代; R3是氢，烷基，链烯基，环烷基或环烷基烷基; 或R 2和R 3一起形成3至7元碳环，其被螺旋稠化至哌嗪环; 和R4是氢或烷基; 对多巴胺D1受体具有有力的拮抗作用。这些化合物可用于治疗中枢神经系统疾病，特别是精神病，精神分裂症（阳性和阴性症状），焦虑症，抑郁症，睡眠障碍，偏头痛，帕金森病或可卡因滥用。

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