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1. 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。

2. 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。

3. 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。

4. 发明申请

WO1998028290A1 INDANE OR DIHYDROINDOLE DERIVATIVES 审中-公开
标题翻译：吲哚或二氢吲哚衍生物
公开(公告)号：WO1998028290A1
公开(公告)日：1998-07-02
申请号：PCT/DK1997000588
申请日：1997-12-19
申请人： H. LUNDBECK A/S , PERREGAARD, Jens, Kristian , MIKKELSEN, Ivan , PEDERSEN, Henrik
发明人： H. LUNDBECK A/S
IPC分类号： C07D317/66
CPC分类号： C07D405/12 , C07D317/66
摘要： The present invention relates to substituted indane or dihydroindole compounds of Formula (I), wherein A and B are independently O or S; D is an optionally substituted methylene group; X is N or optionally substituted C; and W is a spacer group. The compounds are either selective dopamine D4 ligands or they have combined effects at dopamine D4 and serotonergic receptors and/or the serotonergic transporter. These compounds are therefore useful in the treatment of certain psychiatric and neurologic disorders, including psychosis, depression and anxiety.
摘要翻译：本发明涉及式（I）的取代的茚满或二氢吲哚化合物，其中A和B独立地是O或S; D是任选取代的亚甲基; X为N或任选取代的C; W是间隔基。这些化合物是选择性多巴胺D4配体，或它们在多巴胺D4和5-羟色胺能受体和/或血清素能转运体上具有组合效应。因此，这些化合物可用于治疗某些精神和神经障碍，包括精神病，抑郁和焦虑。

5. 发明申请

WO1996008468A1 CARBAMOYLOXY AMINE COMPOUNDS 审中-公开
标题翻译：羧甲基胺化合物
公开(公告)号：WO1996008468A1
公开(公告)日：1996-03-21
申请号：PCT/DK1995000368
申请日：1995-09-14
申请人： H. LUNDBECK A/S , FALCH, Erik , MIKKELSEN, Ivan , KROGSGAARD-LARSEN, Povl
发明人： H. LUNDBECK A/S
IPC分类号： C07C271/12
CPC分类号： C07D207/08 , C07C271/12 , C07C271/24 , C07C2601/08 , C07C2601/14 , C07D211/22 , C07D295/088
摘要： Carbamoyloxypropylamine or carbamoyloxyethylamine compounds of formula (I), wherein A represents CH2 or a bond, R1 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or phenyl; and R2 is alkyl, alkenyl, alkynyl, cycloalkyl or phenyl; or R1 and R2 together form a ring; R3 and R4 are hydrogen, alkyl, alkenyl, alkynyl, halogenated alkyl, cycloalkyl, phenyl, or phenylalkyl or R3 and R4 together form a spirojoined C4-7 carbocycle; or when R1 and R2 are not linked, R3 and R2 may form ring; R5 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, or phenylalkyl or together with R2 form a ring; or R5 together with R4 form a ring; R6 and R7 are hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or phenylalkyl; or R6 and R7 together form a ring; are ligands at the central nicotine acetylcholine receptors (nAChRs). The compounds are useful in the treatment of cognitive, neurological or mental disorders in which nAChR dysfunction is involved.
摘要翻译：式（I）的氨基甲酰氧基丙胺或氨基甲酰氧基乙胺化合物，其中A表示CH 2或键，R 1为氢，烷基，烯基，炔基，环烷基或苯基; 并且R 2是烷基，烯基，炔基，环烷基或苯基; 或R1和R2一起形成环; R 3和R 4是氢，烷基，烯基，炔基，卤代烷基，环烷基，苯基或苯基烷基，或者R3和R4一起形成螺环C4-7碳环; 或当R 1和R 2不连接时，R 3和R 2可以形成环; R5是氢，烷基，烯基，炔基，环烷基，苯基或苯基烷基，或与R2一起形成环; 或R 5与R 4一起形成环; R6和R7是氢，烷基，烯基，炔基，环烷基，苯基或苯基烷基; 或R6和R7一起形成环; 是中枢尼古丁乙酰胆碱受体（nAChRs）的配体。该化合物可用于治疗涉及nAChR功能障碍的认知，神经或精神障碍。

6. 发明申请

WO1995033729A1 SEROTONIN 5-HT1A AND DOPAMIN D2 RECEPTOR LIGANDS 审中-公开
标题翻译： SEROTONIN 5-HT1A和DOPAMIN D2受体配体
公开(公告)号：WO1995033729A1
公开(公告)日：1995-12-14
申请号：PCT/DK1995000229
申请日：1995-06-08
申请人： H. LUNDBECK A/S , PERREGAARD, Jens, Kristian , MOLTZEN, Ejner, Knud
发明人： H. LUNDBECK A/S
IPC分类号： C07D233/32
CPC分类号： C07D401/06 , C07D233/32 , C07D233/36
摘要： The present invention relates to a novel series of 4-phenylpiperazines, 4-phenyl-piperidines and 4-phenyl-1,2,3,6-tetrahydropyridines compound of general formula (I) wherein A is alkylene, alkenylene, alkynylene, and C3-7 cycloalkylene; R is a C3-10 alkyl, alkenyl, or alkynyl group, cycloalk(en)yl, cycloalk(en)yl-alk(en/yn)yl, trifluoromethylsulfonyl, or alkylsulfonyl, R - R are optional substituents; R and R are hydrogen, alkyl or together form an ethylene or propylene bridge; W is O or S; V is O, S, CR R , or NR wherein R , R , and R are hydrogen or alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, optionally substituted arylalkyl or aryl, or R and R constitute a 3-7 membered spiroring; Z is -(CH2)m-, m being 2 or 3 or Z is -CH=CH-; X is N, C or CH; show effects on central serotonin 5-HT1A and dopamine D2 receptors. Thus the novel compounds are useful in the treatment of certain psychic and neurologic disorders in particular psychosis.
摘要翻译：本发明涉及一种新的一系列4-苯基哌嗪，4-苯基 - 哌啶和4-苯基-1,2,3,6-四氢吡啶类化合物，其中A是亚烷基，亚烯基，亚炔基和C3 -7亚环烷基; R 1是C 3-10烷基，烯基或炔基，环烷（烯）基，环烷基（烯）基 - 烷（烯/炔）基，三氟甲基磺酰基或烷基磺酰基，R 2 -R 5 >是任选的取代基; R 9和R 10是氢，烷基或一起形成乙烯或丙烯桥; W为O或S; V是O，S，CR 6 R 7或NR 8，其中R 6，R 7和R 8是氢或烷基，烯基，环烷基，环烷基烷基，任选取代的芳基烷基或芳基，或R 6和R 7构成3-7元的激发; Z是 - （CH 2）m - ，m是2或3或Z是-CH = CH-; X为N，C或CH; 显示对中枢5-羟色胺5-HT1A和多巴胺D2受体的影响。因此，这些新化合物可用于治疗某些精神病和神经系统疾病，特别是精神病。

7. 发明申请

WO1993004941A1 A PILFERPROOF CONTAINER CLOSURE 审中-公开
标题翻译：防冻容器关闭
公开(公告)号：WO1993004941A1
公开(公告)日：1993-03-18
申请号：PCT/DK1992000265
申请日：1992-09-04
申请人： H. LUNDBECK A/S , CHRISTENSEN, Tom
发明人： H. LUNDBECK A/S
IPC分类号： B65D50/14
CPC分类号： B65D50/041
摘要： A container closure assembly with a child-resistant safety device and comprising a closure (1) for screwing on a container and an outer, in relation to the closure (1) rotatable and axially displaceable outer cap (2). By simultaneous pressing down and turning of the outer cap (2) ratchet ramps (213) on the outer cap engage ratchet teeth (16) on the closure (1). A coupling means consisting of a circle of tongues (17) positioned on the closure (1) passes through a central aperture (209) in the outer cap (2). By inserting a safety release means (3) with a tubular portion (301) outside on the coupling means or on the inside a permanent hold against rotation is established between the closure (1) and the outer cap (2) thereby that locking means on the tongues (17) are pressed against the outer cap (2) or thereby that ratchet teeth directly or indirectly couple the holding device with the outer cap (2).
摘要翻译：一种具有防儿童安全装置的容器封闭组件，包括用于在容器上旋紧的封闭件（1）和相对于可旋转和可轴向移位的外盖（2）的封闭件（1）的外部。通过同时按压和转动外盖（2），外盖上的棘轮斜面（213）接合封闭件（1）上的棘齿（16）。由位于封闭件（1）上的舌圈（17）组成的连接装置通过外盖（2）中的中心孔（209）。通过在封闭件（1）和外盖（2）之间建立具有管状部分（301）的安全释放装置（3），该安全释放装置（3）在外部位于联接装置上或内部上，以防止在锁定装置舌部（17）被压靠在外盖（2）上，由此棘轮齿直接或间接地将保持装置与外盖（2）相连。

8. 发明申请

WO1992015302A1 TREATMENT OF ADDICTION TO DRUGS AND SUBSTANCES OF ABUSE 审中-公开
标题翻译：治疗药物和物质滥用的治疗
公开(公告)号：WO1992015302A1
公开(公告)日：1992-09-17
申请号：PCT/DK1992000062
申请日：1992-02-28
申请人： H. LUNDBECK A/S , PERREGAARD, Jens, Kristian , COSTALL, Brenda
发明人： H. LUNDBECK A/S
IPC分类号： A61K31/445
CPC分类号： A61K31/445
摘要： 1-Aryl-3-(4-piperidyl)-indole derivatives having general formula (I), wherein R is hydrogen, halogen, alkyl, alkoxy, hydroxy, cyano, nitro, alkylthio, trifluoromethyl, trifluoromethylthio, alkylsulfonyl, amino, alkylamino or dialkylamino; R is optionally substituted phenyl or a heteroaromatic group; and R is hydrogen, cycloalkyl, alkyl or alkenyl, optionally substituted with one or two hydroxy groups, or R is a group of formula (IV), wherein n is an integer of from 2-6; W is O, S or N-R , wherein R is H, alkyl or cycloalkyl; U is N or CH, Z is -(CH2)m-, m being 2 or 3, or Z is -CH=CH-, 1,2-phenylene, or -COCH2- or -CSCH2-; V is O, S, CH2, or NR , wherein R is hydrogen, optionally hydroxy substituted alkyl, alkenyl or cycloalkylmethyl; are useful in alleviating, relieving or suppressing withdrawal or abstinence symptoms or suppressing the dependency of a drug or a substance of abuse.
摘要翻译：具有通式（I）的1-芳基-3-（4-哌啶基） - 吲哚衍生物，其中R 1是氢，卤素，烷基，烷氧基，羟基，氰基，硝基，烷硫基，三氟甲基，三氟甲硫基，烷基磺酰基，氨基，烷基氨基或二烷基氨基; R是任选取代的苯基或杂芳基; R 2是任选被一个或两个羟基取代的氢，环烷基，烷基或烯基，或者R 2是式（Ⅳ）的基团，其中n是2-6的整数; W是O，S或N-R 3，其中R 3是H，烷基或环烷基; U是N或CH，Z是 - （CH2）m-，m是2或3，或Z是-CH = CH-，1,2-亚苯基或-COCH2-或-CSCH2-; V是O，S，CH 2或NR 4，其中R 4是氢，任选羟基取代的烷基，烯基或环烷基甲基; 有助于缓解，缓解或抑制戒断或禁欲症状或抑制药物或滥用物质的依赖。

9. 发明申请

WO1992000070A1 PIPERIDYL-SUBSTITUTED INDOLES 审中-公开
标题翻译： PIPERIDYL取代的吲哚
公开(公告)号：WO1992000070A1
公开(公告)日：1992-01-09
申请号：PCT/DK1991000168
申请日：1991-06-21
申请人： H. LUNDBECK A/S , PERREGAARD, Jens, Kristian , COSTALL, Brenda
发明人： H. LUNDBECK A/S
IPC分类号： A61K31/445
CPC分类号： C07D401/04 , C07D401/14 , C07D409/14 , C07D413/14
摘要： 1-aryl-3-(4-piperidyl)-indole derivatives having general formula (I) wherein R is hydrogen, halogen, alkyl, alkoxy, hydroxy, cyano, nitro, alkylthio, trifluoromethyl, trifluoromethylthio, alkylsulfonyl, amino, alkylamino or dialkylamino; R is optionally substituted phenyl or a hetero aromatic group; and R is hydrogen, cycloalkyl, cycloalkylmethyl, alkyl or alkenyl, optionally substituted with hydroxy, or R is a group of formula (IV) wherein n is an integer from 2-6; W is oxygen, or sulphur; U is nitrogen or carbon; Z is -(CH2)m-, m being 2 or 3, or Z is -CH=CH-, 1,2-phenylene, -COCH2- or -CSCH2-; V is oxygen, sulphur, CH2, or NR , wherein R is hydrogen, or alkyl or alkenyl optionally substituted with hydroxy, or a cycloalkyl or cycloalkylmethyl group; have anxiolytic activities and are useful for therapeutical treatment of anxiety in mammals, including humans.
摘要翻译：具有通式（I）的1-芳基-3-（4-哌啶基） - 吲哚衍生物，其中R 1是氢，卤素，烷基，烷氧基，羟基，氰基，硝基，烷硫基，三氟甲基，三氟甲硫基，烷基磺酰基，氨基，烷基氨基或二烷基氨基; R是任选取代的苯基或杂芳基; R 2为任选被羟基取代的氢，环烷基，环烷基甲基，烷基或链烯基，或R 2为式（Ⅳ）的基团，其中n为2-6的整数; W是氧或硫; U是氮或碳; Z是 - （CH2）m-，m是2或3，或Z是-CH = CH-，1,2-亚苯基，-COCH2-或-CSCH2-; V是氧，硫，CH 2或NR 3，其中R 3是氢，或任选被羟基取代的烷基或链烯基或环烷基或环烷基甲基; 具有抗焦虑活性，可用于治疗哺乳动物（包括人类）的焦虑症。

10. 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。

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