CAS: 1388651-30-6; N-(3-((4As,5R,7As)-2-Amino-5-Methyl-4A,5-Dihydro-4H-Furo[3,4-D][1,3]Thiazin-7A(7H)-yl)-4-Fluorophenyl)-5-(Difluoromethyl)Pyrazine-2-Carboxamide

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      专利号:US-8962858-B2
      优先权日:2011-01-21
      标题 :Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives
      发明人:MITASEV BRANKO; KIM DAE-SHIK; ZHANG HUIMING; FARTHING CHRISTOPHER N
      权利人:EISAI R&D MAN CO LTD
      摘要:Provided are compounds and methods useful for the preparation of compounds useful as inhibitors of beta-site amyloid precursor protein (APP)-cleaving enzyme.

      专利号:US-8802871-B2
      优先权日:2011-01-21
      标 题:Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives

      专利号:US-2013197244-A1
      优先权日:2011-01-21
      标题 :Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives

      专利号:US-8426584-B2
      优先权日:2011-01-21
      标题:Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives

      专利号:EP-2665716-B1
      优先权日:2011-01-21
      标 题:Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives

      专利号:US-2014309429-A1
      优先权日:2011-01-21
      标题:Methods and compounds useful in the synthesis of fusednaminodihydrothiazine derivatives

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      1: Roberts C, Kaplow J, Giroux M, Krause S, Kanekiyo M. Amyloid and APOE Status of Screened Subjects in the Elenbecestat MissionAD Phase 3 Program. J Prev Alzheimers Dis. 2021;8(2):218-223. doi: 10.14283/jpad.2021.4. 81(1):1-17. doi: 10.3233/JAD-201027. 28(11):967-975. doi: 10.1080/13543784.2019.1683160. Epub 2019 Oct 29. 20(6):1174-1193. doi: 10.2174/1570159X19666211201094031.
      5: Pratsch K, Unemura C, Ito M, Lichtenthaler SF, Horiguchi N, Herms J. New Highly Selective BACE1 Inhibitors and Their Effects on Dendritic Spine Density In Vivo. Int J Mol Sci. 2023 Jul 31;24(15):12283. doi: 10.3390/ijms241512283.
      6: Madrasi K, Das R, Mohmmadabdul H, Lin L, Hyman BT, Lauffenburger DA, Albers MW, Rissman RA, Burke JM, Apgar JF, Wille L, Gruenbaum L, Hua F. Systematic in silico analysis of clinically tested drugs for reducing amyloid-beta plaque accumulation in Alzheimer's disease. Alzheimers Dement. 2021 Sep;17(9):1487-1498. doi: 10.1002/alz.12312. Epub 2021 May 2.

      合成参考文献


      参考文献:10.1007/s00115-019-0751-1
      摘要:Haass C, Levin J. [Did Alzheimer research fail entirely : Failure of amyloid-based clinical studies]. Nervenarzt. 2019 Sep;90(9):884–90. doi: 10.1007/s00115-019-0751-1.
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