CAS: 36507-30-9; Carbamazepine 10,11-Epoxide

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CAS号298-46-4 卡马西平 | CAS号28721-07-5 奥卡西平 | CAS号104746-04-5 艾司利卡西平 | CAS号29331-92-8 10-羟基-10,11-二氢-... | CAS号68011-71-2 9-hydroxymethyl... | CAS号885-23-4 吖啶-9-甲醛 | CAS号106680-74-4 9-formyl-10-car...

卡马西平置于过氧乙酸,Aluminum Oxide,Potassium Permanganate,Sodium Carbonate体系中,用 二氯甲烷 作为反应溶剂,化学反应 2.0H,以66%的收率获得产物卡马西平 10,11-环氧化物
参考文献:卡马西平衍生物具有p2X4受体阻断活性
标题:卡马西平衍生物具有p2X4受体阻断活性
摘要:P2受体亚型p2X4(一种atp激活的阳离子通道受体)的拮抗剂作为治疗神经性疼痛和其他炎症性疾病的新型药物具有潜力.在本研究中,设计,合成了一系列47种卡马西平衍生物,包括32种新化合物,并将其评估为p2X4受体拮抗剂.确定了它们在稳定转染了人类p2X4受体的1321N1星形细胞瘤细胞中抑制atp诱导的钙内流的能力.此外,还针对选定的衍生物研究了物种选择性(人,大鼠,小鼠)和受体亚型选择性(p2X4与p2X1,2,3,7).表现出p2X4抑制变构机制的本系列中最有效的化合物是n,N-二异丙基-5 H-Dibenz [B,F] Azepine-5-Carboxamide(34,Ic 50为3.44μm).到目前为止,本研究扩展了关于p2X4受体拮抗剂的结构-活性关系的非常有限的知识.
DOI:10.1016/j.Bmc.2013.12.035

专利信息

专利号:US-9751877-B2
优先权日:2012-09-21
标题 :Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders
发明人：PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; PATEL NANDINI CHATURBHAI; STIFF CORY MICHAEL; TRAN TUAN PHONG; KAUFFMAN GREGORY WAYNE; STEPAN ANTONIA FRIEDERIKE; VERHOEST PATRICK ROBERT
权利人:PFIZER
摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:US-9550795-B2
优先权日:2011-08-31
标 题:Hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
发明人：BRODNEY MICHAEL AARON; BUTLER CHRISTOPHER RYAN; HELAL CHRISTOPHER JOHN; O'NEILL BRIAN THOMAS
权利人:BRODNEY MICHAEL AARON; BUTLER CHRISTOPHER RYAN; HELAL CHRISTOPHER JOHN; O'NEILL BRIAN THOMAS; PFIZER
摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:WO-2012172449-A1
优先权日:2011-06-13
标题:Lactams as beta secretase inhibitors
发明人：BRODNEY MICHAEL AARON
权利人:PFIZER; BRODNEY MICHAEL AARON
摘要:Compound and pharmaceutically acceptable salts of the compound are disclosed, wherein the compound has the structure (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed. The compound of formula I is useful as beta secretase inhibitor for use in the treatment of Alzheimer's and other neurodegenerative and/or neurological disorders.

专利号:US-2016229847-A1
优先权日:2013-10-04
标 题:Novel bicyclic pyridinones as gamma-secretase modulators
发明人：PETTERSSON MARTIN YOUNGJIN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; JOHNSON DOUGLAS SCOTT; KAUFFMAN GREGORY WAYNE; O'DONNELL CHRISTOPHER WILLIAM; PATEL NANDINI CHATURBHAI; STEPAN ANTONIA FRIEDERIKE; STIFF CORY MICHAEL; SUBRAMANYAM CHAKRAPANI; TRAN TUAN PHONG; VERHOEST PATRICK ROBERT
权利人:PFIZER
摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula II as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:US-9067934-B2
优先权日:2011-03-31
标题 :Bicyclic pyridinones
发明人：PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; FISH BENJAMIN ADAM; GREEN MICHAEL ERIC; MULLINS PATRICK BRADLEY; STIFF CORY MICHAEL; TRAN TUAN PHONG; NAVARATNAM THAYALAN
权利人:PFIZER
摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n nas defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:US-2003069698-A1
优先权日:2000-06-14
标 题 :Method and system for predicting pharmacokinetic properties
发明人：UCHIYAMA MAMORU; HATTORI KAZUNARI; SHIMADA KAORU
摘要:This invention provides a method for predicting pharmacokinetic properties of molecules comprising the steps of: n (a) preparing 2D-structures of molecules used as a training set; n (b) constructing a 2D-fingerprint by counting the number of structural descriptors that potentially relate to a pharmacokinetic property, either manually or automatically using internally developed macro; wherein said structural descriptors consist of predefined 20 to 80 atoms/fragments or substructures; n (c) analyzing the obtained 2D-fingerprint by a statistical analysis method to correlate with the pharmacokinetic property of the molecule to yield a quantitative structure-property relationship (QSPR) model; and n (d) calculating the pharmacokinetic property of a trial molecule using the above obtained QSPR model. n A system for this invention is also provided. According to this method and system, it is possible to predict pharmacokinetic properties of molecules prior to synthesis, without labor-intensive and time-consuming experimentation.