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公开(公告)号：US4748240A
公开(公告)日：1988-05-31
申请号：US34525
申请日：1987-04-03
IPC分类号： C07D313/00 , A61K31/495 , A61K31/535 , A61P25/18 , A61P25/26 , C07D221/22 , C07D221/24 , C07D401/00 , C07D401/06 , C07D401/12 , C07D491/08 , C07D495/08 , C07D498/00 , C07D498/08 , C07D513/08 , C07D401/14 , C07D405/14 , C07D409/14
CPC分类号： C07D221/22 , C07D221/24 , C07D513/08
摘要： Substituted imides of the following formula are antipsychotic, anxiolytic agents with very little extrapyramidal side effects: ##STR1## in which X is --O--, --S--, --SO--, --SO.sub.2 --, --CR.sub.3 R.sub.4 --where R.sub.3 and R.sub.4, independently, are hydrogen, alkyl of 1 to 4 carbon atoms or, taken together with the carbon atom to which they are attached, R.sub.3 and R.sub.4 form a cycloalkyl group of 3 to 5 carbon atoms; Y is alkylene of 1 to 3 carbon atoms or alkenylene of 2 to 3 carbon atoms; n is one of the integers 0 to 1; m is one of the integers 2, 3, 4 or 5; R is phenyl, halophenyl, trifluoromethylphenyl, alkoxyphenyl in which the alkoxy substituent contains 1 to 3 carbon atoms, 2-pyrimidinyl, halopyrimidin-2-yl, 2-pyrazinyl, halopyrazin-2-yl, 2-pyridinyl, cyanopyridin-2-yl, halopyridin-2-yl, quinolyl, or haloquinolyl; or a pharmaceutically acceptable salt thereof.
摘要翻译： 下列配方的取代酰亚胺是抗精神病药，抗焦虑剂，具有极少的锥体束外副作用：其中X是-O - ， - S - ， - SO - ， - SO 2 - ， - CR 3 R 4 - 的化合物，其中R3和R4独立地 是氢，1至4个碳原子的烷基，或与它们所连接的碳原子一起，R3和R4形成3至5个碳原子的环烷基; Y为1〜3个碳原子的亚烷基或2〜3个碳原子的亚烯基; n是整数0到1之一; m是整数2,3,4或5之一; R是苯基，卤代苯基，三氟甲基苯基，烷氧基取代基含有1至3个碳原子的烷氧基苯基，2-嘧啶基，卤代嘧啶-2-基，2-吡嗪基，卤代吡嗪-2-基，2-吡啶基，氰基吡啶-2-基 ，卤代吡啶-2-基，喹啉基或卤代喹啉基; 或其药学上可接受的盐。
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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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13.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。 -
17.发明授权Aryl- and heteroaryl piperazinyl carboxamides having central nervous system activity 失效具有中枢神经系统活性的芳基和杂芳基哌嗪基甲酰胺
公开(公告)号：US5380725A
公开(公告)日：1995-01-10
申请号：US91495
申请日：1993-07-14
IPC分类号： C07D209/42 , C07D239/42 , C07D295/13 , A61K31/495 , C07D295/145 , C07D403/12
CPC分类号： C07D239/42 , C07D209/42 , C07D295/13
摘要： There are disclosed compounds of the formula (I) ##STR1## wherein R.sup.1 is 1-adamantyl, 3-methyl-1-adamantyl, 3-noradamantyl, unsubstituted or substituted-2-indolyl, 3-indolyl, 2-benzofuranyl and 3-benzofuranyl wherein the substituents are selected from lower alkyl, lower alkoxy and halo; R.sup.2 is unsubstituted or substituted phenyl, benzyl, pyridinyl, pyrimidinyl or pyrazinyl, wherein the substituents are selected from lower alkyl, lower alkoxy, trifluoromethyl and halo; R.sup.3 is H or lower alkyl of 1 to 3 carbon atoms; n is the integer 0 or 1; m is the integer from 2 to 5; and the pharmaceutically acceptable salts thereof.
摘要翻译： 公开了式（I）的化合物其中R1是1-金刚烷基，3-甲基-1-金刚烷基，3-降金刚烷基，未取代的或取代的-2-吲哚基，3-吲哚基，2-苯并呋喃基 和3-苯并呋喃基，其中取代基选自低级烷基，低级烷氧基和卤素; R2是未取代或取代的苯基，苄基，吡啶基，嘧啶基或吡嗪基，其中取代基选自低级烷基，低级烷氧基，三氟甲基和卤素; R3是H或1〜3个碳原子的低级烷基; n是整数0或1; m是2至5的整数; 及其药学上可接受的盐。
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18.发明授权Aryl-and heteroaryl piperazinyl carboxamides having central nervous system activity 失效具有中枢神经系统活性的芳基和杂芳基哌嗪基甲酰胺
公开(公告)号：US5254552A
公开(公告)日：1993-10-19
申请号：US852119
申请日：1992-03-16
IPC分类号： C07D209/42 , C07D239/42 , C07D295/13 , A61K31/495 , C07D295/145 , C07D401/04 , C07D401/14
CPC分类号： C07D239/42 , C07D209/42 , C07D295/13
摘要： There are disclosed compounds of the formula (I) ##STR1## wherein R.sup.1 is 1-adamantyl, 3-methyl-1-adamantyl, 3-noradamantyl, unsubstituted or substituted-2-indolyl, 3-indolyl, 2-benzofuranyl and 3-benzofuranyl wherein the substituents are selected from lower alkyl, lower alkoxy and halo; R.sup.2 is unsubstituted or substituted phenyl, benzyl, pyridinyl, pyrimidinyl or pyrazinyl, wherein the substituents are selected from lower alkyl, lower alkoxy, trifluoromethyl and halo; R.sup.3 is H or lower alkyl of 1 to 3 carbon atoms; n is the integer 0 or 1; m is the integer from 2 to 5; and the pharmaceutically acceptable salts thereof.The compounds of this invention which demonstrate selectivity at the 5-HT.sub.1A and 5-HT.sub.2 versus D.sub.2 receptor binding sites are useful as potential anxiolytic-antidepressant agents.Compounds of this invention with equal high affinity for the 5-HT.sub.1A and D.sub.2 -receptor binding sites are useful as mixed antipsychotic-anxiolytic agents.Compounds of this invention which demonstrate central cholinergic activity are useful in the treatment of senile dementia of the Alzheimer type (SDAT) and Huntingdon's chorea.
摘要翻译： 公开了式（I）的化合物其中R1是1-金刚烷基，3-甲基-1-金刚烷基，3-降金刚烷基，未取代的或取代的-2-吲哚基，3-吲哚基，2-苯并呋喃基 和3-苯并呋喃基，其中取代基选自低级烷基，低级烷氧基和卤素; R2是未取代或取代的苯基，苄基，吡啶基，嘧啶基或吡嗪基，其中取代基选自低级烷基，低级烷氧基，三氟甲基和卤素; R3是H或1〜3个碳原子的低级烷基; n是整数0或1; m是2至5的整数; 及其药学上可接受的盐。 在5-HT1A和5-HT2与D2受体结合位点上证明选择性的本发明化合物可用作潜在的抗焦虑药物 - 抗抑郁剂。 对于5-HT1A和D2-受体结合位点具有相等高亲和力的本发明化合物可用作混合抗精神病药 - 抗焦虑剂。 显示中枢胆碱能活性的本发明化合物可用于治疗老年痴呆型（SDAT）和亨廷顿氏舞蹈病的老年性痴呆。
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公开(公告)号：US4985560A
公开(公告)日：1991-01-15
申请号：US464468
申请日：1990-01-12
IPC分类号： C07D471/14 , C07D519/00
CPC分类号： C07D471/14
摘要： The compound of the formula: ##STR1## in which R.sup.1 is hydrogen, alkoxy, cyano, halo, nitro, amino, or mono- or dialkylamino; R.sup.2 is hydrogen, alkyl, phenyl, benzyl, 2-thienyl, 3-thienyl or 2-,3- or 4-pyridinyl; R.sup.3 is hydrogen, alkyl or phenyl; R.sup.4 is N-methyl-pyrrolidin-2yl, 2-, 3- or 4-pyridinyl, 3-quinuclidinyl or ##STR2## where n is 1 to 5; m is 0 to 3; and R.sup.8 is hydrogen or alkyl of 1 to 6 carbon atoms; or R.sup.4 is ##STR3## wherein: (a) n is 2, R.sup.5 taken with R.sup.3 is ethylene and R.sup.6 is --CHO, alkyl, unsubstituted or substituted phenyl, pyrimidinyl, pyridinyl, or pyrazinyl, where the substituents are alkyl, alkoxyl, halo, cyano, nitro or trifluoromethyl; (b) n is 1 to 5, and R.sup.5 and R.sup.6 taken together are polymethylene which may be alkyl substituted or R.sup.5 nd R.sup.6 are morpholino, 3-azabicyclo[3.2.2]nonan-3-yl, pyrrol-1-yl, pyrrolidin-2-on-1-ytl, pyrrolidin-2-thion-1-yl, imidazol-1-yl, alkyl-piperidin-1-yl or a piperazin-1-yl moiety in the 4-position of which is hydrogen, --CHO, alkyl or unsubstituted or substituted phenyl, pyrimidinyl, pyridinyl, or pyrazinyl, alkoxy, halo, cyano, nitro or trifluoromethyl; or (c) n is 1 to 5, and R.sup.5 and R.sup.6 are, independently, hydrogen, alkyl, phenyl, 3-quinuclidinyl, 2-adamantyl, bicyclo[3.2.1]octan-1-yl, bicyclo[3.3.1]nonan-9-yl or 2-,3- or 4- pyridinyl; or a pharmaceutically acceptable salt thereof are M.sub.1 receptor agonists useful in treatment of dementias involving the cholinergic system. dd
摘要翻译： 下式的化合物：其中R 1是氢，烷氧基，氰基，卤素，硝基，氨基或单或二烷基氨基; R2是氢，烷基，苯基，苄基，2-噻吩基，3-噻吩基或2-，3-或4-吡啶基; R3是氢，烷基或苯基; R4是N-甲基 - 吡咯烷-2-基，2-，3-或4-吡啶基，3-奎宁环基或其中n为1至5; m为0〜3; 和R8是氢或1至6个碳原子的烷基; 其中：（a）n为2，R5取R5为乙烯，R6为-CHO，烷基，未取代或取代的苯基，嘧啶基，吡啶基或吡嗪基，其中取代基为烷基，烷氧基，卤素 ，氰基，硝基或三氟甲基; （b）n为1至5，R 5和R 6一起为可被烷基取代的多亚甲基或R 5和R 6为吗啉代，3-氮杂双环[3.2.2]壬烷-3-基，吡咯-1-基，吡咯烷 -2-对-1-基，吡咯烷-2-硫基-1-基，咪唑-1-基，烷基 - 哌啶-1-基或哌嗪-1-基部分，其4-位是氢， -CHO，烷基或未取代或取代的苯基，嘧啶基，吡啶基或吡嗪基，烷氧基，卤素，氰基，硝基或三氟甲基; 或（c）n为1至5，并且R 5和R 6独立地为氢，烷基，苯基，3-奎宁环基，2-金刚烷基，双环[3.2.1]辛-1-基，双环[3.3.1] 壬-9-基或2-，3-或4-吡啶基; 或其药学上可接受的盐是可用于治疗涉及胆碱能系统的痴呆症的M1受体激动剂。
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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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