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公开(公告)号：US4540806A
公开(公告)日：1985-09-10
申请号：US564588
申请日：1983-12-22
IPC分类号： A61K31/215 , C07C87/02 , A61K31/22 , C07C101/72 , C07C103/127
CPC分类号： A61K31/215 , Y10S514/816
摘要： Benzocycloalkane amine derivatives and their non-toxic acid addition salts as novel analgesic agents.
摘要翻译： 苯环链烷胺衍生物及其无毒酸加成盐作为新型止痛剂。
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2.发明授权2,3,4,9-tetrahydro-2-heteroarylalkyl-1H-pyrido(3,4-B)indoles having antihypertensive properties 失效具有抗高血压性质的2,3,4,9-四氢-2-杂芳基烷基-1H-吡啶并（3,4-B）吲哚
公开(公告)号：US4719211A
公开(公告)日：1988-01-12
申请号：US837612
申请日：1986-03-07
IPC分类号： C07D471/04 , A61K31/495 , C07D471/06
CPC分类号： C07D471/04
摘要： This invention concerns tetrahydropyridoindoles of the formula: ##STR1## wherein Q represents ##STR2## in which R.sub.3 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, or --COO(C.sub.1-2) alkyl, and n is an integer from 1 to 7; R.sub.1 is hydrogen, halogen, hydroxy, or C.sub.1-3 alkyl; and R.sub.2 is hydrogen, C.sub.1-4 alkyl or --(CH.sub.2).sub.m --A where A is --N(CH.sub.3).sub.2,--N(C.sub.2 H.sub.5).sub.2, ##STR3## in which Ar is 2-pyrimidinyl, 2-pyrazinyl, phenyl, or phenyl substituted by a methyl, ethyl, methoxy, ethoxy, or trifluoromethyl group; and m is an integer from 1-4, or physiologically acceptable salts thereof, providing however that when n is 1, Q may not be quinolinyl. These compounds exhibit antihypertensive properties. Four of the disclosed compounds also exhibit antipsychotic properties.Also disclosed are compounds of Formula XX in which Q of Formula I is replaced by Q.sub.1, wherein Q.sub.1 is 2- or 3-pyridinyl, and R.sub.2 of Formula I is restricted to hydrogen. The compounds of Formula XX exhibit antipsychotic properties.
摘要翻译： 本发明涉及下式的四氢吡啶并吲哚：其中Q代表其中R3是氢，C1-4烷基，C1-4烷氧基或-COO（C1-2）烷基，其中n是 1至7; R 1是氢，卤素，羟基或C 1-3烷基; 其中A为-N（CH 3）2，-N（C 2 H 5）2，其中Ar为2-嘧啶基，2-吡嗪基，苯基或 被甲基，乙基，甲氧基，乙氧基或三氟甲基取代的苯基; 并且m是1-4的整数或其生理上可接受的盐，但是当n为1时，Q可能不是喹啉基。 这些化合物显示抗高血压性质。 所公开的化合物中的四种也显示出抗精神病性质。 还公开了式XX的化合物，其中式I的Q被Q1代替，其中Q1是2-或3-吡啶基，式I的R2限于氢。 式XX的化合物显示出抗精神病性质。
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公开(公告)号：US4546193A
公开(公告)日：1985-10-08
申请号：US684211
申请日：1984-12-20
IPC分类号： C07D209/94 , C07D209/70
CPC分类号： C07D209/94
摘要： This invention provides a group of antiarrhythmic agents of the formula: ##STR1## in which R.sub.1 is --CO.sub.2 H, --CO.sub.2 (CH.sub.2).sub.n --NR.sub.4 R.sub.5, --CONR.sub.6 R.sub.7, --NHCO.sub.2 R.sub.8 or --NHCO.sub.2 (CH.sub.2).sub.o --NR.sub.9 R.sub.10 where R.sub.4 and R.sub.5 are H or alkyl of 1 to 6 carbon atoms and n is 1 to 6; R.sub.6 and R.sub.7 are H or alkyl of 1 to 6 carbon atoms; R.sub.8 is alkyl of 1 to 6 carbon atoms; and R.sub.9 and R.sub.10 are alkyl of 2 to 6 carbon atoms and o is 1 to 6;R.sub.2 and R.sub.3 are, independently, hydrogen or alkyl of 1 to 6 carbon atoms; andm is one of the integers 1, 2, 3 or 4;or a pharmaceutically acceptable salt thereof, and a method for their use.
摘要翻译： 本发明提供一组下式的抗心律不齐药物：其中R 1是-CO 2 H，-CO 2（CH 2）n -NR 4 R 5，-CONR 6 R 7，-NHCO 2 R 8或-NHCO 2（CH 2）o -NR 9 R 10，其中R 4和R 5是 H或1〜6个碳原子的烷基，n为1〜6; R6和R7是H或1至6个碳原子的烷基; R8是1-6个碳原子的烷基; 并且R 9和R 10为2至6个碳原子的烷基，o为1至6; R2和R3独立地是氢或1至6个碳原子的烷基; 并且m是整数1,2,3或4之一; 或其药学上可接受的盐及其使用方法。
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公开(公告)号：US4562255A
公开(公告)日：1985-12-31
申请号：US595138
申请日：1984-03-30
IPC分类号： C07D403/12 , C07D498/16 , C07D403/14 , C07D405/14 , C07D409/14
CPC分类号： C07D403/12
摘要： There are disclosed compounds having the formula ##STR1## wherein X is a group selected from ##STR2## Y represents a single or double bond; R.sup.1 is hydrogen or lower alkyl;n is an integer 2-4;n' is an integer 1-2; andR is 2-pyrimidinyl, 2-pyridinyl, 2-pyrazinyl, halo-substituted 2-pyrazinyl, 5-tetrazolyl, phenyl or phenyl substituted by halo, lower alkyl or lower alkoxy;and the pharmacologically acceptable salts thereof, which exhibit anti-hypertensive activity.
摘要翻译： 公开了具有式“IMAGE”的化合物，其中X是选自下式的基团：Y表示单键或双键; R1是氢或低级烷基; n是整数2-4; n'是整数1-2; 并且R是2-嘧啶基，2-吡啶基，2-吡嗪基，卤素取代的2-吡嗪基，5-四唑基，苯基或被卤素，低级烷基或低级烷氧基取代的苯基; 和其药理学上可接受的盐，其具有抗高血压活性。
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公开(公告)号：US4638008A
公开(公告)日：1987-01-20
申请号：US740651
申请日：1985-06-03
IPC分类号： C07D209/94 , A61K31/40
CPC分类号： C07D209/94 , Y10S514/821
摘要： This invention provides a group of antiarrythmic agents of the formula: ##STR1## in which R.sub.1 is --CO.sub.2 H, --CO.sub.2 (CH.sub.2).sub.n --NR.sub.4 R.sub.5, --CONR.sub.6 R.sub.7, --NHCO.sub.2 R.sub.8 or --NHCO.sub.2 (CH.sub.2).sub.o --NR.sub.9 R.sub.10 where R.sub.4 and R.sub.5 are H or alkyl of 1 to 6 carbon atoms and n is 1 to 6; R.sub.6 and R.sub.7 are H or alkyl of 1 to 6 carbon atoms; R.sub.8 is alkyl of 1 to 6 carbon atoms; and R.sub.9 and R.sub.10 are alkyl of 2 to 6 carbon atoms and o is 1 to 6;R.sub.2 and R.sub.3 are, independently, hydrogen or alkyl of 1 to 6 carbon atoms; andm is one of the integers 1, 2, 3 or 4;or a pharmaceutically acceptable salt thereof, and a method for their use.
摘要翻译： 本发明提供一组下式的抗焦虑剂：其中R 1是-CO 2 H，-CO 2（CH 2）n -NR 4 R 5，-CONR 6 R 7，-NHCO 2 R 8或-NHCO 2（CH 2）o -NR 9 R 10，其中R 4和R 5是 H或1〜6个碳原子的烷基，n为1〜6; R6和R7是H或1至6个碳原子的烷基; R8是1-6个碳原子的烷基; 并且R 9和R 10为2至6个碳原子的烷基，o为1至6; R2和R3独立地是氢或1至6个碳原子的烷基; 并且m是整数1,2,3或4之一; 或其药学上可接受的盐及其使用方法。
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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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7.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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公开(公告)号：US5508399A
公开(公告)日：1996-04-16
申请号：US450835
申请日：1995-05-25
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.sup.1 and R.sup.2 are each, independently, hydrogen, --CONH--[(CR.sup.3 R.sup.4).sub.m (--A--(CR.sup.5 R.sup.6).sub.n).sub.p ].sub.q --B; ##STR2## R.sup.3, R.sup.4, R.sup.5, R.sup.6, and B are each, independently, hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl, cycloalkyl, --OR.sup.7, --SR.sup.7, halogen, --CN, --NO.sub.2, --CF.sub.3, --COR.sup.7, --CO.sub.2 R.sup.7, --CONHR.sup.7, --SO.sub.2 R.sup.7, --OSO.sub.3 R.sup.7, --NR.sup.7 R.sup.8, --NHCOR.sup.7, --NHSO.sub.2 R.sup.7, or Ar;R.sup.7 and R.sup.8 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloallcyl;R.sup.9 and R.sup.10 are each, independently, alkyl , alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl,, --CF.sub.3, --COR.sup.7, --CO.sub.2 R.sup.7, --CONHR.sup.7, --SO.sub.2 R.sup.7, or Ar;A is --CH.sub.2 --, --NR.sup.7 --, --O--, --S--, --SO--, --SO.sub.2 --, --PR.sup.7 --, --CO--, --NHCO--, --NHSO--, or --P(O)(R.sup.7)--;Ar is phenyl, naphthyl, pyridyl, quinolyl, isoquinolyl, quinoxalyl, thienyl, thionaphthyl, furyl, benzofuryl, benzodioxyl, benzoxazolyl, benzoisoxazolyl, indolyl, thiazolyl, isoxazolyl, pyrimidinyl, pyrazinyl, imidazolyl, benzopyranyl, benz[b]thiophenolyl, benzimidazolyl, benzthiazolyl, benzodioxolyl, piperidinyl, morpholinyl, piperazinyl, tetrahydrofuranyl, or pyrrolidinyl; wherein the Ar group may be optionally mono-, di-, or tri-substituted; ##STR3## is a nitrogen containing heterocycle that may be saturated, unsaturated, or partially unsaturated, and may be optionally mono-, di-, or tri- substituted; with the proviso that R.sup.1 and R.sup.2 are not both hydrogen;m=0-6;n=0-6;p=0-1;q=0-1;or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
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公开(公告)号：US5486523A
公开(公告)日：1996-01-23
申请号：US449444
申请日：1995-05-24
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.sup.1 and R.sup.2 are each, independently, hydrogen, --CONR.sup.3 (CR.sup.4 R.sup.5).sub.m (CR.sup.6 R.sup.7).sub.n (CR.sup.8 R.sup.9).sub.p NR.sup.10 R.sup.11, or ##STR2## or --CONR.sup.3 R.sup.13 ; R.sup.3 is hydrogen, alkyl, or arylalkyl;R.sup.4, R.sup.5, R.sup.8, and R.sup.9 are each, independently, hydrogen, alkyl, --OH, --CF.sub.3, or --F;R.sup.6 is hydrogen or --OR.sup.13 ;R.sup.7 is hydrogen or alkyl;R.sup.10 is hydrogen, alkyl, or arylalkyl;R.sup.11, R.sup.12, and R.sup.13 are each, independently, --(CR.sup.15 R.sup.16).sub.r R.sup.17 ;R.sup.14 is hydrogen, alkyl of 1-6 carbon atoms, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, or tetrahydropyranyl;R.sup.15 and R.sup.16 are each, independently, hydrogen or alkyl;R.sup.17 is ##STR3## or --C.ident.C--R.sup.21 ; R.sup.18, R.sup.19, R.sup.20, and R.sup.21 are each, independently, hydrogen, alkyl, halogen, or phenyl, wherein the phenyl group may be optionally mono-, dio, or tri-substituted; ##STR4## is a 5-7 membered saturated or partially unsaturated heterocyclic radical containing at least 2 ring nitrogens, wherein the heterocyclic ring may optionally contain NR.sup.22 in the heterocyclic ring, and the ring carbons may optionally be substituted by alkyl, arylalkyl, halogen, --CF.sub.3, --OR.sup.14, or --CO.sub.2 R.sup.10 ;R.sup.22 is hydrogen, alkyl, or arylalkyl;m=0-6;n=1-6;p=0-6; andr=1-6with the proviso that R.sup.1 and R.sup.2 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 1和R 2各自独立地为氢，-CONR 3（CR 4 R 5）m（CR 6 R 7）n（CR 8 R 9）pNR 10 R 11或者或者-CONR 3 R 13; R3是氢，烷基或芳基烷基; R 4，R 5，R 8和R 9各自独立地为氢，烷基，-OH，-CF 3或-F; R6是氢或-OR13; R7是氢或烷基; R 10是氢，烷基或芳基烷基; R 11，R 12和R 13各自独立地为 - （CR 15 R 16）r R 17; R 14为氢，1-6个碳原子的烷基，三（烷基）甲硅烷基，三（烷基）甲硅烷基乙基，三苯基甲基，苄基，烷氧基甲基，三（烷基）甲基乙氧基甲基或四氢吡喃基; R 15和R 16各自独立地为氢或烷基; R17是
或-C = C-R21; R 18，R 19，R 20和R 21各自独立地为氢，烷基，卤素或苯基，其中苯基可以是任选的单，二取代或三取代的; 含有至少2个环氮的5-7元饱和或部分不饱和杂环基，其中该杂环可以在杂环中任意含有NR 22，并且环碳可任选地被烷基，芳基烷基，卤素， -CF 3，-OR 14或-CO 2 R 10; R 22是氢，烷基或芳基烷基; m = 0-6; n = 1-6; p = 0-6; 并且r = 1-6，条件是R 1和R 2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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