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公开(公告)号：US4937347A
公开(公告)日：1990-06-26
申请号：US348323
申请日：1989-05-05
IPC分类号： C07D209/94 , C07D223/32 , C07D401/06 , C07D403/06
CPC分类号： C07D401/06 , C07D209/94 , C07D223/32 , C07D403/06
摘要： These are disclosed compounds of the formula ##STR1## wherein R represents ##STR2## where X is lower alkylene, vinylene or O;Y is lower alkylene or vinylene;the dotted line represents an optional double bond;m is 1-3;n is 2-4;A is phenyl, benzoyl, pyridinyl, quinolinyl or quinoxalinyl, or any of the foregoing substituted with lower alkyl, lower alkoxy, halo, cyano, nitro or trifluoromethyl; or when m is >1, A represents the grouping ##STR3## where B is phenyl, pyrimidinyl, pyridinyl or pyrazinyl, or any of the foregoing substituted with lower alkyl, lower alkoxy, halo, cyano, nitro or trifluoromethyl, with the proviso that where R is ##STR4## A is other than unsubstituted or substituted benzoyl or pyridinyl; and the pharmacologically acceptable salts thereof and their use as antipsychotic/anxiolytic and antidepressant agents and in the treatment of sexual dysfunction and having a low liability for extrapyramidal side effects.
摘要翻译： 这些被公开的式“IMAGE”的化合物，其中R代表下式，其中X是低级亚烷基，亚乙烯基或O; Y是低级亚烷基或亚乙烯基; 虚线表示可选的双键; m为1-3; n为2-4; A是苯基，苯甲酰基，吡啶基，喹啉基或喹喔啉基，或任何前述基团被低级烷基，低级烷氧基，卤素，氰基，硝基或三氟甲基取代; 或当m> 1时，A表示分组“IMAGE”，其中B是苯基，嘧啶基，吡啶基或吡嗪基，或任何前述基团被低级烷基，低级烷氧基，卤素，氰基，硝基或三氟甲基取代，条件是 其中R是未取代或取代的苯甲酰基或吡啶基; 及其药理学上可接受的盐及其作为抗精神病药/抗焦虑药和抗抑郁药的用途，用于治疗性功能障碍，对锥体束外副作用的责任低。
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公开(公告)号：US4672117A
公开(公告)日：1987-06-09
申请号：US776349
申请日：1985-09-16
IPC分类号： A61K31/435 , A61P25/18 , C07D471/04 , C07D401/06 , C07D241/36
CPC分类号： C07D471/04
摘要： The compounds: ##STR1## in which R.sup.1 is hydrogen, halogen, hydroxy, or alkyl;R.sup.2 is substituted or unsubstituted pyridinyl, pyrazinyl, quinolinyl or quinoxalinyl and said substituents are alkyl, alkoxy, alkoxycarbonyl, halogen, cyano or nitro;R.sup.5 and R.sup.6 are, independently, hydrogen, alkyl, phenyl, halophenyl, methylphenyl, trifluoromethylphenyl, cyanophenyl or nitrophenyl; with the proviso that one of R.sup.5 and R.sup.6 is other than hydrogen;and n is an integer from 1 to 7;or a pharmaceutically acceptable salt thereof, are antipsychotic and anxiolytic agents.
摘要翻译： 化合物：其中R 1是氢，卤素，羟基或烷基的
R 2是取代或未取代的吡啶基，吡嗪基，喹啉基或喹喔啉基，所述取代基是烷基，烷氧基，烷氧基羰基，卤素，氰基或硝基; R5和R6独立地是氢，烷基，苯基，卤代苯基，甲基苯基，三氟甲基苯基，氰基苯基或硝基苯基; 条件是R5和R6中的一个不是氢; n为1〜7的整数。 或其药学上可接受的盐是抗精神病药和抗焦虑剂。 -
公开(公告)号：US4942234A
公开(公告)日：1990-07-17
申请号：US316888
申请日：1989-02-28
IPC分类号： C07D417/06 , C07D513/18
CPC分类号： C07D417/06
摘要： There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, lower alkyl, aryl or halo, or R.sup.1 and R.sup.2 taken together represent ##STR2## where the dotted lines represent optional double bonds; R.sup.3, R.sup.4 and R.sup.5 are each, independently, hydrogen, lower alkyl, aryl or halo;R.sup.6 is 2-pyridinyl, 2-pyrazinyl, 2-quinolyl, 2-quinoxalinyl or any of the foregoing R.sup.6 moieties substituted by lower alkyl, lower alkoxy, trifluoromethyl, cyano, nitro or halo; or ##STR3## wherein R.sup.7 is phenyl, 2-pyridinyl, 2-pyrimidinyl, 3-pyridazinyl or 2-pyrazinyl or any of the foregoing R.sup.7 moieties substituted by lower alkyl, lower alkoxy, halo, cyano, trifluoromethyl or nitro;Z is ##STR4## X is lower alkylene, vinylene, O or NH; m is 1-5;n is 0-4;p is 1-4;q is 1-2;and the pharmaceutically acceptable salts thereof, and their use as antipsychotic/anxiolytic agents having a low liability for extrapyramidal side effects.
摘要翻译： 公开了式（IMAGE）的化合物，其中R 1和R 2各自独立地为氢，低级烷基，芳基或卤素，或者R 1和R 2一起表示
+ TR 其中 虚线表示可选的双键; R 3，R 4和R 5各自独立地为氢，低级烷基，芳基或卤素; R6是2-吡啶基，2-吡嗪基，2-喹啉基，2-喹喔啉基或由低级烷基，低级烷氧基，三氟甲基，氰基，硝基或卤素取代的任何前述R 6部分; 或其中R 7为苯基，2-吡啶基，2-嘧啶基，3-哒嗪基或2-吡嗪基或由低级烷基，低级烷氧基，卤素，氰基，三氟甲基或硝基取代的前述R7部分中的任一个。 Z是低级亚烷基，亚乙烯基，O或NH; m为1-5; n为0-4; p为1-4; q是1-2; 及其药学上可接受的盐，以及它们作为锥体束外副作用负担低的抗精神病药/抗焦虑剂的用途。 -
公开(公告)号：US4833249A
公开(公告)日：1989-05-23
申请号：US022197
申请日：1987-03-05
IPC分类号： C07D417/06 , C07D513/18
CPC分类号： C07D417/06
摘要： There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, lower alkyl, aryl or halo, or R.sup.1 and R.sup.2 taken together represent ##STR2## where the dotted lines represent optional double bonds; R.sup.3, R.sup.4 and R.sup.5 are each, independently, hydrogen, lower alkyl, aryl or halo;R.sup.6 is 2-pyridinyl, 2-pyrazinyl, 2-quinolyl, 2-quinoxalinyl or any of the foregoing R.sup.6 moieties substituted by lower alkyl, lower alkoxy, trifluoromethyl, cyano, nitro or halo; orR.sup.6 is ##STR3## wherein R.sup.7 is phenyl, 2-pyridinyl, 2-pyrimidinyl, 3-pyridazinyl or 2-pyrazinyl or any of the foregoing R.sup.7 moieties substituted by lower alkyl, lower alkoxy, halo, cyano, trifluoromethyl or nitro;Z is --(CH.sub.2).sub.n --, --O--, or ##STR4## X is lower alkylene, vinylene, O or NH; m is 1-5;n is 0-4;p is 1-4;q is 1-2;and the pharmaceutically acceptable salts thereof, and their use as antipsychotic/anxiolytic agents having a low liability for extrapyramidal side effects.
摘要翻译： 公开了式（IMAGE）的化合物，其中R 1和R 2各自独立地为氢，低级烷基，芳基或卤素，或者R 1和R 2一起表示
+ TR 其中 虚线表示可选的双键; R 3，R 4和R 5各自独立地为氢，低级烷基，芳基或卤素; R6是2-吡啶基，2-吡嗪基，2-喹啉基，2-喹喔啉基或由低级烷基，低级烷氧基，三氟甲基，氰基，硝基或卤素取代的任何前述R 6部分; 或R6是其中R7是苯基，2-吡啶基，2-嘧啶基，3-哒嗪基或2-吡嗪基或由低级烷基，低级烷氧基，卤素，氰基，三氟甲基或硝基取代的前述R7部分中的任何一个; Z是 - （CH 2）n - ， - O-或X是低级亚烷基，亚乙烯基，O或NH; m为1-5; n为0-4; p为1-4; q是1-2; 及其药学上可接受的盐，以及它们作为锥体束外副作用负担低的抗精神病药/抗焦虑剂的用途。 -
公开(公告)号：US4927934A
公开(公告)日：1990-05-22
申请号：US348332
申请日：1989-05-05
IPC分类号： C07D209/94 , C07D223/32 , C07D401/06 , C07D403/06
CPC分类号： C07D401/06 , C07D209/94 , C07D223/32 , C07D403/06
摘要： There are disclosed compounds of the formula ##STR1## wherein R represents ##STR2## where X is lower alkylene, vinylene or O;Y is lower alkylene or vinylene;the dotted line represents an optional double bond;m is 1-3;n is 2-4;A is phenyl, benzoyl, pyridinyl, quinolinyl or quinoxalinyl, or any of the foregoing substituted with lower alkyl, lower alkoxy, halo, cyano, nitro or trifluoromethyl; or when m is>1, A represents the grouping ##STR3## where B is phenyl, pyrimidinyl, pyridinyl or pyrazinyl, or any of the foregoing substituted with lower alkyl, lower alkoxy, halo, cyano, nitro or trifluoromethyl, with the proviso that were R is ##STR4## A is other than unsubstituted or substituted benzoyl or pyridinyl; and the pharmacologically acceptable salts thereof and their use as antipsychotic/anxiolytic and antidepressant agents and in the treatment of sexual dysfunction and having a low liability for extrapyramidal side effects.
摘要翻译： 公开了下式的化合物：其中R表示低级亚烷基，亚乙烯基或O; Y是低级亚烷基或亚乙烯基; 虚线表示可选的双键; m为1-3; n为2-4; A是苯基，苯甲酰基，吡啶基，喹啉基或喹喔啉基，或任何前述基团被低级烷基，低级烷氧基，卤素，氰基，硝基或三氟甲基取代; 或当m> 1时，A表示分组“IMAGE”，其中B是苯基，嘧啶基，吡啶基或吡嗪基，或任何前述基团被低级烷基，低级烷氧基，卤素，氰基，硝基或三氟甲基取代，条件是 R是不是未取代或取代的苯甲酰基或吡啶基; 及其药理学上可接受的盐及其作为抗精神病药/抗焦虑药和抗抑郁药的用途，用于治疗性功能障碍，对锥体束外副作用的责任低。
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公开(公告)号：US4855430A
公开(公告)日：1989-08-08
申请号：US119530
申请日：1987-11-12
IPC分类号： C07D209/56 , A61K31/395 , A61K31/40 , A61K31/403 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/495 , A61K31/555 , A61P25/00 , A61P25/20 , A61P25/24 , A61P25/26 , C07D209/72 , C07D209/94 , C07D213/38 , C07D223/32 , C07D239/42 , C07D239/47 , C07D241/20 , C07D241/26 , C07D241/44 , C07D295/04 , C07D401/06 , C07D403/06
CPC分类号： C07D401/06 , C07D209/94 , C07D223/32 , C07D403/06
摘要： There are disclosed compounds of the formula ##STR1## wherein R represents ##STR2## where X is lower alkylene, vinylene or O;Y is lower alkylene or vinylene;the dotted line represents an optional double bond;m is 1-3;n is 2-4;A is phenyl, benzoyl, pyridinyl, quinolinyl or quinoxalinyl, or any of the foregoing substituted with lower alkyl, lower alkoxy, halo, cyano, nitro or trifluoromethyl; or when m is>1, A represents the grouping ##STR3## where B is phenyl, pyrimidinyl, pyridinyl or pyrazinyl, or any of the foregoing substituted with lower alkyl, lower alkoxy, halo, cyano, nitro or trifluoromethyl, with the proviso that where R is ##STR4## A is other than unsubstituted or substituted benzoyl or pyridinyl; and the pharmacologically acceptable salts thereof and their use as antipsychotic/anxiolytic and antidepressant agents and in the treatment of sexual dysfunction and having a low liability for extrapyramidal side effects.
摘要翻译： 公开了式“IMAGE”的化合物，其中R代表其中X是低级亚烷基，亚乙烯基或O; Y是低级亚烷基或亚乙烯基; 虚线表示可选的双键; m为1-3; n为2-4; A是苯基，苯甲酰基，吡啶基，喹啉基或喹喔啉基，或任何前述基团被低级烷基，低级烷氧基，卤素，氰基，硝基或三氟甲基取代; 或当m> 1时，A表示分组“IMAGE”，其中B是苯基，嘧啶基，吡啶基或吡嗪基，或任何前述基团被低级烷基，低级烷氧基，卤素，氰基，硝基或三氟甲基取代，条件是 其中R是未取代或取代的苯甲酰基或吡啶基; 及其药理学上可接受的盐及其作为抗精神病药/抗焦虑药和抗抑郁药的用途，用于治疗性功能障碍，对锥体束外副作用的责任低。
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公开(公告)号：US4766215A
公开(公告)日：1988-08-23
申请号：US19730
申请日：1987-02-27
IPC分类号： C07D239/42 , C07D241/18 , C07D241/20 , C07D401/12 , C07D403/04 , A61K31/495
CPC分类号： C07D239/42 , C07D241/18 , C07D241/20 , C07D401/12
摘要： The compounds of the following formula are histamine H.sub.1 -receptor antagonists: ##STR1## where R.sup.3 and R.sup.4 are, independently, hydrogen, halo, alkoxy of 1 to 3 carbon atoms or alkyl of 1 to 3 carbon atoms; R.sup.2 is hydrogen or halo;n is one of the integers 0, 1 or 2;p is one of the integers 0 or 1;Y is --N.dbd. or --CH.dbd., with the proviso that when Y is --N.dbd., p is zero, and when Y is --CH.dbd., p is one; andone of X.sub.1 and X.sub.2 is nitrogen and the other is --CH.dbd.; or a pharmaceutically acceptable salt thereof.
摘要翻译： 下式的化合物是组胺H1受体拮抗剂：其中其中R 3和R 4独立地是氢，卤素，1至3个碳原子的烷氧基或1至3个碳原子的烷基的
R2是氢或卤素; n是整数0,1或2之一; p是0或1的整数之一; Y为-N =或-CH =，条件是当Y为-N =时，p为0，当Y为-CH =时，p为1。 X1和X2之一是氮，另一个是-CH =; 或其药学上可接受的盐。 -
公开(公告)号：US20120065240A1
公开(公告)日：2012-03-15
申请号：US13049238
申请日：2011-03-16
IPC分类号： A61K31/403 , A61P25/00
CPC分类号： A61K31/495 , A61K31/403 , A61K31/4184 , A61K31/445 , A61K31/4458
摘要： The present invention is directed to selective dopamine reuptake inhibitors, including (−)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane, (−)-1-(4-methylphenyl)-3-azabicyclo[3.1.0]hexane, and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine, and methods of their use for treating certain nervous system disorders and conditions, including, inter alia, vasomotor symptoms (VMS), chronic pain, and Shy Drager syndrome.
摘要翻译： 本发明涉及选择性多巴胺再摄取抑制剂，包括（ - ） - 1-（3,4-二氯苯基）-3-氮杂双环[3.1.0]己烷，（ - ） - 1-（4-甲基苯基）-3- 氮杂双环[3.1.0]己烷和1- [2- [双（4-氟苯基）甲氧基]乙基] -4-（3-苯基丙基）哌嗪的方法及其用于治疗某些神经系统疾病和病症的方法，包括 尤其是血管舒缩症状（VMS），慢性疼痛和Shy Drager综合征。
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9.发明授权Branched adamantyl and noradamantyl aryl-and aralkylpiperazines with serotonin 5-HT1A activity 失效分支金刚烷基和去甲月桂酰基芳基 - 和芳烷基哌嗪与5-羟色胺5-HT1A活性公开(公告)号：US06828324B2
公开(公告)日：2004-12-07
申请号：US10783109
申请日：2004-02-20
IPC分类号： A61K31495
CPC分类号： C07D239/42 , A61K31/496 , C07D295/13
摘要： This invention provides compounds and methods using them to provide neuroprotection and prevent or limit processes of neurodegeneration in mammals, including Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, AIDS dementia, retinal disease, diabetic peripheral neuropathy, multiple sclerosis, stroke, acute thromboembolic stroke, focal ischemia, global ischemia, transient ischemic attack, ischemia resulting from surgery, head trauma, spinal trauma, hypoxia, fetal hypoxia, and neuroprotection. The compounds having the structure: wherein X is —CH2— or a bond; Y is —(CH2)m— or —(CH2)—O—(CH2)—; m 0 or 1; n is 0 or 1; R1 and R2 are independently selected from optionally substituted aryl or heteroaryl; the optical isomers and the pharmaceutically acceptable salts thereof.
摘要翻译： 本发明提供了使用它们提供神经保护并预防或限制哺乳动物（包括阿尔茨海默氏病，亨廷顿病，帕金森病，艾滋病痴呆，视网膜疾病，糖尿病性周围神经病，多发性硬化，中风，急性血栓栓塞性中风等）的神经退行性进程的化合物和方法。 局灶缺血，全身缺血，短暂性脑缺血发作，手术导致的局部缺血，头部外伤，脊柱创伤，缺氧，胎儿缺氧和神经保护。 具有以下结构的化合物：其中X为-CH 2 - 或键; Y是 - （CH 2）m - 或 - （CH 2）-O-（CH 2） - ; m 0或1; n为0或1; R 1和R 2独立地选自任选取代的芳基或杂芳基; 光学异构体及其药学上可接受的盐。
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公开(公告)号：US5519031A
公开(公告)日：1996-05-21
申请号：US391398
申请日：1995-02-27
IPC分类号： A61K31/395 , A61K31/44 , A61K31/675 , C07D491/06 , C07D498/04 , C07D498/16
CPC分类号： A61K31/70
摘要： A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, hydrogen, ##STR2## R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CN, --NO.sub.2, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --OR.sup.5, --SR.sup.5, or Ar;R.sup.4 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, or Ar; ##STR3## are each, independently, a 5-7 member saturated, unsaturated, or partially unsaturated heterocyclic radical, that is optionally fused to a phenyl ring or a cycloalkane or cycloalkene ring, wherein the heterocyclic ring may optionally contain O, S, or NR.sup.8 in the heterocyclic ring, and may be optionally substituted by R.sup.7 ;R.sup.7 is alkyl of 1-6 carbon atoms, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;R.sup.8 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3,--NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;Ar is phenyl, naphthyl, or hetaryl, wherein the foregoing may be optionally substituted; with the proviso that R and R.sup.1 are both not hydrogen, or a pharmaceutically acceptable salt thereof. which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译： 结构式II的化合物，其中R和R 1各自独立地为氢，R 2和R 3各自独立地为氢，烷基，烯基，炔基，-CO 2 R 5， COR 5，-CN，-NO 2，-SO 2 R 5，-SO 3 R 5，-OR 5，-SR 5或Ar; R 4是氢，烷基，烯基，炔基，-CF 3，-NR 5 R 6，-CO 2 R 5，-COR 5，CONR 5 R 6，-NO 2，卤素，-OR 5，-SR 5，-CN，-SO 2 R 5，-SO 3 R 5，-SO 2 NR 5 R 6或Ar; R 5和R 6各自独立地为氢，烷基，烯基，炔基或Ar; ＆lt; IMAGE＆gt;和＆lt; IMAGE＆gt;各自独立地是5-7元饱和，不饱和或部分不饱和的杂环基团，其任选地与苯环或环烷烃或环烯烃稠合，其中杂环可以 任选地在杂环中含有O，S或NR8，并且可以任选被R 7取代; R7是1-6个碳原子的烷基，烯基，炔基，-CF3，-NR5R6，-CO2R5，-COR5，CONR5R6，-NO2，卤素，-OR5，-SR5，-CN，-SO2R5，-SO3R5，-SO2NR5R6 ，或Ar; R 8是氢，烷基，烯基，炔基，-CF 3，-NR 5 R 6，-CO 2 R 5，-COR 5，CONR 5 R 6，-OR 5，-SR 5，-CN，-SO 2 R 5，-SO 3 R 5，-SO 2 NR 5 R 6或Ar; Ar是苯基，萘基或杂芳基，其中前述可以任选被取代; 条件是R和R 1都不是氢，或其药学上可接受的盐。 其可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。
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