CAS: 118156-93-7; Tert-Butyl 3-Formylpiperidine-1-Carboxylate

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1008562-87-5 194726-46-0 116574-71-1

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CAS号116574-71-1 1-B°C-3-羟甲基哌啶 | CAS号189442-78-2 1-B°C-N-甲氧基-N-甲... | CAS号4606-65-9 3-哌啶甲醇 | CAS号114615-82-6 四丙基高钌酸铵 | CAS号24424-99-5 二碳酸二叔丁酯 | CAS号7529-22-8 N-甲基吗啉氧化物 | CAS号79-37-8 草酰氯 | CAS号71381-75-4 1-B°C-哌啶-3-羧酸 | CAS号498-95-3 3-哌啶甲酸 | CAS号514842-98-9 3-(吡咯烷-1-甲基)哌啶双盐酸盐 | CAS号78190-11-1 (|R|)-N-Cbz-3-哌啶甲酸 | CAS号664362-16-7 3-乙炔基哌啶-1-甲酸叔丁酯 | CAS号146667-87-0 1-B°C-3-乙烯基-哌啶 | CAS号405239-75-0 3-吡啶羧酸,2-氨基-6-[...

3-哌啶甲酸置于lithium Aluminium Tetrahydride,O-(Benzotriazol-1-yl)-N,N,N',N'-Tetramethyluronium Tetrafluoroborate,三乙胺,Sodium Hydroxide体系中,用 四氢呋喃,1,4-二氧六环,二氯甲烷 用作溶剂,化学反应 2.0H,反应生成1-Boc-哌啶-3-甲醛
参考文献:1-Propargyl-4-Styrylpiperidine类类似物的立体选择性活性可以区分单胺氧化酶同工型a和b.
标题:1-Propargyl-4-Styrylpiperidine类类似物的立体选择性活性可以区分单胺氧化酶同工型a和b.
摘要:最近,这种酶活性与心血管疾病,神经疾病和肿瘤疾病之间的相关性加剧了人们对单胺氧化酶(maos)兴趣的兴起.这促进了对选择性mao-A和mao-B抑制剂的更多研究.在这里,我们阐明了如何通过顺式和反式1-炔丙基-4-苯乙烯基哌啶的几何异构体实现对mao-A和mao-B的选择性抑制.尽管顺式异构体是有效的人mao-A抑制剂,但反式类似物仅选择性靶向mao-B同工型.通过动力学分析,Uv-可见光谱测量和x射线晶体学研究了抑制作用.在小鼠脑匀浆中离体证实了对mao-A和mao-B同工型的选择性抑制,小鼠中的其他体内研究表明1-炔丙基-4-苯乙烯基哌啶对中枢神经系统疾病的治疗潜力.这项研究代表了顺式/反式异构体立体选择性活性的独特案例,可以区分结构上相关的酶同工型.
Doi:10.1021/acs.Jmedchem.9B01886

专利信息

专利号:US-7816375-B2
优先权日:2000-09-11
标 题 :Ligands for monoamine receptors and transporters, and methods of use thereof
发明人：AQUILA BRIAN M; BANNISTER THOMAS D; CUNY GREGORY D; HAUSKE JAMES R; HOLLAND JOANNE M; PERSONS PAUL E; RADEKE HEIKE; WANG FENGJIANG; SHAO LIMING
权利人:SEPRACOR INC
摘要:One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.

专利号:US-6872716-B2
优先权日:2000-09-11
标题:Antipsychotic sulfonamide-heterocycles, and methods of use thereof
发明人：WU XINHE; AQUILA BRIAN M; SHAO LIMING; RADEKE HEIKE; CUNY GREGORY D; HAUSKE JAMES R; XIE ROGER L
权利人:SEPRACOR INC
摘要:One aspect of the present invention relates to heterocyclic compounds comprising a sulfonamide moiety. A second aspect of the present invention relates to the use of the heterocyclic compounds comprising a sulfonamide moiety to treat diseases, afflictions or maladies caused at least in part by abnormal activity of one or more GPCRs or ligand-gated ion channels. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds comprising a sulfonamide moiety, and the screening of those libraries for biological activity, e.g., in animal models of psychosis.

专利号:CN-103588699-B
优先权日:2012-08-15
标题:Asymmetric Synthesis of (R)-3-Aminopiperidine (I) and Related Intermediates

专利号:US-2008194629-A1
优先权日:2005-05-03
标题 :3-Mono-and 3,5-Disubstituted Piperidine Derivatives as Renin Inhibitors
发明人：BAESCHLIN DANIEL KASPAR; BREITENSTEIN WERNER; EHRHARDT CLAUS; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; ZIMMERMANN JUERG; RUDISSER SIMON; VANGREVELINGHE ERIC; IRIE OSAMU; UMEMURA ICHIRO; SUZUKI MASAKI; MOGI MUNETO; KANAZAWA TAKANORI; YOKOKAWA FUMIAKI; NIHONYANAGI ATSUKO
权利人:BAESCHLIN DANIEL KASPAR; BREITENSTEIN WERNER; EHRHARDT CLAUS; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; ZIMMERMANN JUERG; RUDISSER SIMON; VANGREVELINGHE ERIC; IRIE OSAMU; UMEMURA ICHIRO; SUZUKI MASAKI; MOGI MUNETO; KANAZAWA TAKANORI; YOKOKAWA FUMIAKI; NIHONYANAGI ATSUKO
摘要:The invention relates to 3,5-piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-piperidine compound, and/or a method of treatment comprising administering a 3,5-piperidine compound, a method for the manufacture of a 3,5-piperidine compound, and novel intermediates and partial steps for their synthesis. Especially, the 3,5-piperidine compounds have the formula I, wherein the symbols have the meanings described in the specification.

专利号:WO-2025026392-A1
优先权日:2023-08-02
标题 :Kinesin kif18a inhibitor and use thereof
发明人：XIAO YISONG; LAI KUNMIN; GU XIAOHUI; WANG MINGHUA; DENG JIACHEN; HU MIN
权利人:SHANGHAI APEIRON THERAPEUTICS COMPANY LTD
摘要:A KIF18 inhibitor having a structure as shown in formula (I) and a synthesis method therefor. The compound can be used to adjust the KIF18A protein, thereby affecting a cell cycle and cell proliferation process for the treatment of cancer and cancer-related diseases. Further disclosed are a pharmaceutical composition containing the compound, and a method for the treatment of conditions associated with KIF18A activity.