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公开(公告)号:US5418237A
公开(公告)日:1995-05-23
申请号:US262256
申请日:1994-06-13
IPC分类号: A61K31/495 , A61K31/40 , A61K31/496 , A61K31/5377 , A61P9/12 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D209/14 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D405/12 , C07D413/06 , C07D498/10 , C07D403/00
CPC分类号: C07D401/06 , C07D209/14 , C07D401/12 , C07D403/04 , C07D403/06 , C07D405/12
摘要: Indole derivatives of formula I ##STR1## wherein Ind, Q and Ar are as defined herein, and their salts, are active on the central nervous system.
摘要翻译: 其中Ind,Q和Ar如本文所定义的式I的吲哚衍生物及其盐在中枢神经系统上是有活性的。
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公开(公告)号:US20060084693A1
公开(公告)日:2006-04-20
申请号:US10546029
申请日:2004-01-19
申请人: Guenter Holzemann , Kai Schiemann , Henning Bottcher , Timo Heinrich , Christoph Seyfried , Joachim Leibrock , Chrisoph Van Amsterdam , Gerd Bartoszyk
发明人: Guenter Holzemann , Kai Schiemann , Henning Bottcher , Timo Heinrich , Christoph Seyfried , Joachim Leibrock , Chrisoph Van Amsterdam , Gerd Bartoszyk
IPC分类号: A61K31/405 , C07D405/02
CPC分类号: C07D405/12
摘要: Novel benzofuranoxyethylamines of the formula (1), in which R1, R2, R3, R4, m and n have the meanings indicated in Patent Claim (1), which have a strong affinity to the 5 HT1A receptors and/or 5HT1D receptors. The compounds inhibit serotonin reuptake, exhibit serotonin-agonistic and -antagonistic properties and are suitable as antidepressants, anxiolytics, antipsychotics, neuroleptics and/or antihypertonics.
摘要翻译: 式(1)的新型苯并呋喃氧基乙胺,其中R 1,R 2,R 3,R 4, ,m和n具有与专利权利要求(1)中所示的含义,其对5HT 1A受体和/或5HT 1D受体具有强亲和力。 这些化合物抑制5-羟色胺再摄取,显示5-羟色胺 - 激动和拮抗性质,并且适合作为抗抑郁药,抗焦虑药,抗精神病药,精神安定药和/或抗高血压药。
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公开(公告)号:US06413989B1
公开(公告)日:2002-07-02
申请号:US09508059
申请日:2000-05-17
IPC分类号: A61K3145
CPC分类号: C07D413/06
摘要: The invention relates to the compound 5-[4-(4-fluorobenzyl) piperidin-1-ylmethyl]-3-(4-hydroxy-phenyl)oxazolidin-2-one of the formula I and to physiologically acceptable salts thereof. The compound acts as a neuroleptic.
摘要翻译: 本发明涉及式I的化合物5- [4-(4-氟苄基)哌啶-1-基甲基] -3-(4-羟基 - 苯基)恶唑烷-2-酮及其生理上可接受的盐。 化合物作为精神安定药物。
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公开(公告)号:US5472961A
公开(公告)日:1995-12-05
申请号:US397758
申请日:1995-03-02
申请人: Rudolf Gottschlich , Karl-August Ackermann , Christoph Seyfried , Andrew Barber , Gerd Bartoszyk , Hartmut Greiner
发明人: Rudolf Gottschlich , Karl-August Ackermann , Christoph Seyfried , Andrew Barber , Gerd Bartoszyk , Hartmut Greiner
IPC分类号: C07D413/06 , A61K31/42 , A61K31/47 , A61P9/10 , A61P25/00 , A61P25/04 , A61P43/00 , C07D235/26 , C07D263/58 , C07D265/36 , C07D265/38 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14
CPC分类号: C07D263/58 , C07D235/26 , C07D265/36 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14
摘要: Novel acetamides of the formula I ##STR1## in which Q, R, X and Y have the meanings defined herein, have analgesic and neuroprotective properties and bind with high affinity to kappa receptors.
摘要翻译: 其中Q,R,X和Y具有本文定义的含义的式I“I”的新型乙酰胺具有止痛和神经保护性质,并以高亲和力结合κ受体。
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公开(公告)号:US07618988B2
公开(公告)日:2009-11-17
申请号:US10489960
申请日:2002-08-12
申请人: Henning Böttcher , Ralf Devant , Maria Devant, legal representative , Gerd Bartoszyk , Hermann Russ , Frank Weber , Christoph Seyfried
发明人: Henning Böttcher , Ralf Devant , Gerd Bartoszyk , Hermann Russ , Frank Weber , Christoph Seyfried
IPC分类号: A61K31/135 , A61K31/33 , A61K31/395 , A61K31/535 , A61K31/54 , A61K31/58
CPC分类号: C07D405/12
摘要: Compounds of formula I in which R has a meaning as indicated in claim 1, or one of their optical isomers or pharmaceutically acceptable salts, used for the treatment of extrapyramidal movement disorders and/or adverse effects in extrapyramidal movement disorders and/or for the treatment of extrapyramidal symptoms (EPS) induced by neuroleptics.
摘要翻译: 其中R具有权利要求1所述含义的式I化合物或其用于治疗锥体束外运动障碍和/或锥体外系运动障碍和/或治疗中的副作用的其旋光异构体或药学上可接受的盐之一 的精神分裂症引起的锥体外系症状(EPS)。
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公开(公告)号:US07482465B2
公开(公告)日:2009-01-27
申请号:US10538639
申请日:2003-11-17
申请人: Günter Hölzemann , Helene Crassier , Henning Böttcher , Timo Heinrich , Kai Schiemann , Joachim Leibrock , Chrisoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
发明人: Günter Hölzemann , Helene Crassier , Henning Böttcher , Timo Heinrich , Kai Schiemann , Joachim Leibrock , Chrisoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
IPC分类号: C07D271/12 , C07D285/10
CPC分类号: C07D413/12 , C07D417/12
摘要: The invention relates to indol derivatives of Formula (I) in which R1, R2, R3, X, A, n, m and p have the meanings indicated above.
摘要翻译: 本发明涉及式(I)的吲哚衍生物,其中R 1,R 2,R 3,X,A,n,m和p具有上述含义。
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公开(公告)号:US20060229339A1
公开(公告)日:2006-10-12
申请号:US10489960
申请日:2002-08-12
申请人: Henning Böttcher , Ralf Devant , Maria Devant , Gerd Bartoszyk , Hermann Russ , Frank Weber , Christoph Seyfried
发明人: Henning Böttcher , Ralf Devant , Maria Devant , Gerd Bartoszyk , Hermann Russ , Frank Weber , Christoph Seyfried
IPC分类号: A61K31/4433
CPC分类号: C07D405/12
摘要: Compounds of formula I in which R has a meaning as indicated in claim 1, or one of their optical isomers or pharmaceutically acceptable salts, used for the treatment of extrapyramidal movement disorders and/or adverse effects in extrapyramidal movement disorders and/or for the treatment of extrapyramidal symptoms (EPS) induced by neuroleptics.
摘要翻译: 其中R具有权利要求1所述含义的式I化合物或其用于治疗锥体束外运动障碍和/或锥体外系运动障碍和/或治疗中的副作用的其旋光异构体或药学上可接受的盐之一 的精神分裂症引起的锥体外系症状(EPS)。
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公开(公告)号:US06462056B1
公开(公告)日:2002-10-08
申请号:US09380202
申请日:1999-08-25
IPC分类号: A61K31454
CPC分类号: C07D413/14
摘要: The invention relates to novel oxazolidine derivatives of the formula in which R1, R2 and R3 have the meanings stated in claim 1, their salts and processes for preparing the compounds according to the invention. The compounds of the formula I act as 5-HT2A antagonists with a 5-HT reuptake-inhibiting, antidepressant or anxiolytic effect and can be used to produce pharmaceuticals.
摘要翻译: 本发明涉及式(1)的新的恶唑烷衍生物,其中R1,R2和R3具有权利要求1所述的含义,其盐和制备本发明化合物的方法。式I化合物作为5-HT2A拮抗剂, 5-HT再摄取抑制,抗抑郁或抗焦虑作用,可用于生产药物。
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公开(公告)号:US5776972A
公开(公告)日:1998-07-07
申请号:US671502
申请日:1996-06-27
IPC分类号: C07D207/08 , A61K31/135 , A61K31/165 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61P1/00 , A61P1/04 , A61P29/00 , A61P43/00 , C07D207/12
CPC分类号: A61K31/4025
摘要: Pharmaceutical preparations which are suitable for the treatment of inflammatory bowel disorders and contain at least one compound of the formula I ##STR1## in which R.sup.1 is Ar, cycloalkyl having 3-7 C atoms or cycloalkylalkyl having 4-8 C atoms, R.sup.2 is Ar, or R.sup.1 and R.sup.2 together are ##STR2## R.sup.3 is H, OH, OA or A, R.sup.4 is A or phenyl which can optionally be mono- or disubstituted by Hal, OH, OA, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NHCOA, NHSO.sub.2 A and/or NA.sub.2, R.sup.5 is OH, CH.sub.2 OH, R.sup.6 and R.sup.7 in each case independently of one another are H, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA, NHCONH.sub.2, NO.sub.2 or methylenedioxy, with the oxy groups bonded to adjacent carbons on the ring, A is alkyl having 1-7 C atoms, Ar is a mono- or bicyclic aromatic radical which can optionally contain an N, O or S atom in the ring and can be mono-, di- or trisubstituted by A, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA and/or NHCONH.sub.2,D is CH.sub.2, O, S, NH, NA, --CH.sub.2 --CH.sub.2 --,--CH.dbd.CH--,--CH.sub.2 --NH--,--CH.sub.2 --NA-- or a bond and Hal is F, Cl, Br or I; and/or physiologically acceptable salts and/or one of its glycosylated derivatives , and at least one physiologically acceptable excipient or auxiliary.
摘要翻译: 适用于治疗炎症性肠病并含有至少一种式I g 3-7 C原子的化合物或具有4-8个C原子的环烷基烷基的药物制剂,R 2为Ar或R 1和R 2一起为“ R3是H,OH,OA或A,R4是A或可以被Hal,OH,OA,CF3,NO2,NH2,NHA,NHCOA,NHSO2A和/或NA2单取代或二取代的苯基,R5是OH, CH 2 OH,R 6和R 7各自独立地为H,Hal,OH,OA,CF 3,NH 2,NHA,NA 2,NHCOA,NHCONH 2,NO 2或亚甲二氧基,氧基与环上的相邻碳键合,A 是具有1-7个C原子的烷基,Ar是单环或双环芳族基团,其可以任选地在环中含有N,O或S原子,并且可以被A,Hal,OH,OA单取代,二取代或三取代 ,CF 3,NH 2,NHA,NA 2,NHCOA和/或NHCONH 2,D是CH 2,O,S,NH,NA,-CH 2 -CH 2 - , - CH = CH - , - CH 2 -NH-, - CH 2 - 或键,Hal为F,Cl,Br或I; 和/或生理上可接受的盐和/或其糖基化衍生物之一,和至少一种生理上可接受的赋形剂或辅助剂。
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公开(公告)号:US5693655A
公开(公告)日:1997-12-02
申请号:US426405
申请日:1995-04-21
IPC分类号: A61K31/4427 , A61K31/445 , A61K31/454 , A61P9/10 , A61P9/12 , A61P25/04 , A61P25/20 , A61P25/24 , A61P43/00 , C07D209/14 , C07D211/14 , C07D401/14 , C07D491/04 , C07D491/056
CPC分类号: C07D401/14 , C07D491/04
摘要: 3-Indolylpiperidines of the formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are in each case independently of one another H, A, OH, OA, F, Cl, Br, Z, CN, CF.sub.3, COOH, CONH.sub.2, CONHA, CONA.sub.2, or COOA, or R.sup.1 and R.sup.2 and also R.sup.3 and R.sup.4 in each case together are also methylenedioxy, R.sup.5 is H or OH, R.sup.6 is H or R.sup.5 and R.sup.6 together are also a bond, A is alkyl having 1 to 6 C atoms and n is 2, 3, 4, 5 or 6, and to their physiologically acceptable salts, exhibit action on the central nervous system, in particular dopamine-agonistic or dopamine-antagonistic action.
摘要翻译: 式I的3-吲哚基哌啶其中R 1,R 2,R 3和R 4各自独立地为H,A,OH,OA,F,Cl,Br,Z,CN,CF 3,COOH,CONH 2 ,CONHA,CONA2或COOA,或者R 1和R 2以及R 3和R 4在一起也是亚甲二氧基,R 5是H或OH,R 6是H或R 5,R 6一起也是键,A是具有1至 6个C原子,n为2,3,4,5或6及其生理上可接受的盐,对中枢神经系统,特别是多巴胺激动剂或多巴胺拮抗作用表现出作用。
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