CAS: 1383982-64-6; Lanabecestat

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    📜,[5-(丙炔-1-基)吡啶-3-基]硼酸置于[5-(丙炔-1-基)吡啶-3-基]硼酸体系中,化学反应生成(1α,1'R,4β)-4-甲氧基-5''-甲基-6'-[5-(1-丙炔基-1)-3-吡啶基]双螺[环己烷-1,2'-[2H]Indene
    参考文献:Compounds And Their Use As Bace Inhibitors
    标题:Compounds And Their Use As Bace Inhibitors
    摘要:本发明涉及式(i)化合物及其制药组合物.此外,本发明还涉及用于治疗和/或预防与aβ相关的病理学,例如唐氏综合症,β淀粉样蛋白病变(如但不限于脑淀粉样血管病变或遗传性脑出血),与认知障碍相关的疾病(如但不限于轻度认知障碍),阿尔茨海默病,记忆丧失,与阿尔茨海默病相关的注意力缺陷症状,与疾病相关的神经退行性疾病(如阿尔茨海默病或痴呆症,包括混合血管性和退行性起源的痴呆,早老性痴呆,老年性痴呆和与帕金森病,进行性核上性麻痹或皮质基底节变性相关的痴呆).

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    主要参考文献


    1: Eketjäll S, Janson J, Kaspersson K, Bogstedt A, Jeppsson F, Fälting J, Haeberlein SB, Kugler AR, Alexander RC, Cebers G. AZD3293: A Novel, Orally Active BACE1 Inhibitor with High Potency and Permeability and Markedly Slow Off-Rate Kinetics. J Alzheimers Dis. 2016;50(4):1109-23. doi: 10.3233/JAD-150834.
    2: Cebers G, Alexander RC, Haeberlein SB, Han D, Goldwater R, Ereshefsky L, Olsson T, Ye N, Rosen L, Russell M, Maltby J, Eketjäll S, Kugler AR. AZD3293: Pharmacokinetic and Pharmacodynamic Effects in Healthy Subjects and Patients with Alzheimer's Disease. J Alzheimers Dis. 2017;55(3):1039-1053. doi: 10.1002/cmdc.201500216.

    合成参考文献


    参考文献:10.1021/ml300324q
    摘要:Blass B. Compounds and Their Use as BACE Inhibitors: Patent Highlight. ACS Med Chem Lett. 2012 Nov 08;3(11):875–6.
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