CAS: 209984-56-5; (S)-2-(2-(3,5-Difluorophenyl)Acetamido)-N-((S)-5-Methyl-6-Oxo-6,7-Dihydro-5H-Dibenzo[b,D]Azepin-7-yl)Propanamide

该化合物是一个复杂的有机化合物,具有独特的结构特征,含有一种二苯甲苯丙胺核心,有助于其潜在的生物活动,特别是在药理学方面.二氟苯基集团的存在表明其脂性增强,并可能影响该化合物与生物目标的互动.此外,L-alamamide 协会表示,该物质可能表现出与氨酸相关的特性,有可能影响其溶性与再活性.该化合物可能会对药物化学产生兴趣,因为其结构复杂,并且存在能够参与各种化学互动的功能组.其具体特性,例如溶性,稳定性和生物活动,需要实证性调查其在不同环境中的行为.

结构式图片

物理性质

MSDS等安全信息

欧盟法规

C&L通报

上下游产品

7-amino-5-methyl-5H-dibenzo[b,d]azepin-6(7H)-one hydr°Chloride N-(3,5-Difluorophenylacetyl)-L-alanine

合成工艺路线路线简述

    📜7-Amino-5-Methyl-5H-Dibenzo[b,D]Azepin-6(7H)-One Hydrochloride,N-[2-(3,5-二氟苯基)乙酰基]-L-丙氨酸置于1-羟基苯并三唑,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺体系中,化学反应 17.0H,反应生成环维黄杨星d
    参考文献:Cycloalkyl,Lactam,Lactone And Related Compounds,Pharmaceutical Compositions Comprising Same,And Methods For Inhibiting Beta-Amyloid Peptide Release And/or Its Synthesis By Use Of Such Compounds
    标题:Cycloalkyl,Lactam,Lactone And Related Compounds,Pharmaceutical Compositions Comprising Same,And Methods For Inhibiting Beta-Amyloid Peptide Release And/or Its Synthesis By Use Of Such Compounds

    海关参考信息

    专利信息


    专利号:EP-0951466-B1
    优先权日:1996-12-23
    标题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
    发明人：WU JING; TUNG JAY S; THORSETT EUGENE D; PLEISS MICHAEL A; NISSEN JEFFREY S; NEITZ JEFFREY; LATIMER LEE H; JOHN VARGHESE; FREEDMAN STEPHEN; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; DROSTE JAMES J; HENRY STEVEN S; MCDANIEL STACEY L; SCOTT WILLIAM L; STUCKY RUSSELL D
    权利人:ELAN PHARM INC; LILLY CO ELI
    摘要:Disclosed are compounds for Formula (I) wherein the substituents are as defined in the claims which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

    专利号:US-7390801-B2
    优先权日:1996-12-23
    标题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
    发明人：THORSETT EUGENE D; PLEISS MICHAEL A; LATIMER LEE H; JOHN VARGHESE; FREEDMAN STEPHEN; BRITTON THOMAS C; AUDIA JAMES A; REEL JON K; DRESSMAN BRUCE A; DROSTE JAMES J; HENRY STEVEN S; STUCKY RUSSELL D; PORTER WARREN J
    权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI
    摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

    专利号:US-2002045747-A1
    优先权日:1996-12-23
    标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds

    专利号:US-2002052359-A1
    优先权日:1996-12-23
    标题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting B-amyloid peptide release and/or its synthesis by use of such compounds

    专利号:US-2002173504-A1
    优先权日:1996-12-23
    标题 :Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting B-amyloid peptide release and/or its synthesis by use of such compounds

    专利号:US-2004043977-A1
    优先权日:1996-12-23
    标题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds

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    主要参考文献


    1: Sanabría CM, Palma A, Cobo J, Glidewell C. Three closely related dibenzazepine carboxylic acids: hydrogen-bonded aggregation in one, two and three dimensions. Acta Crystallogr C Struct Chem. 2014 Mar;70(Pt 3):332-7. doi: 10.1107/S2053229614003568. Epub 2014 Feb 22. doi: 10.1371/journal.pone.0083310. eCollection 2013.
    3: Tsoung J, Panteleev J, Tesch M, Lautens M. Multicomponent-multicatalyst reactions (MC)(2)R: efficient dibenzazepine synthesis. Org Lett. 2014 Jan 3;16(1):110-3. doi: 10.1021/ol4030925. Epub 2013 Dec 13. doi: 10.1021/jm9008482. doi: 10.1016/j.bmcl.2008.11.001. Epub 2008 Nov 6. Epub 2004 Dec 24. Epub 2004 May 11. Russian. Russian. Russian. Russian. German.

    合成参考文献


    参考文献:10.1007/s10495-014-1029-5
    摘要:Yoon SO, Zapata MC, Singh A, Jo WS, Spencer N, Choi YS. Gamma secretase inhibitors enhance vincristine-induced apoptosis in T-ALL in a NOTCH-independent manner. Apoptosis. 2014 Nov;19(11):1616–26.
    参考文献:10.1124/mol.119.115964
    摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.
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