(2R,3S)-3-amino-4-phenyl-1-(prop-2-ynylamino)butan-2-ol | 388074-74-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (2R,3S)-3-amino-4-phenyl-1-(prop-2-ynylamino)butan-2-ol
• CAS: 388074-74-6
• 化学式: C₁₃H₁₈N₂O
• 分子量: 218.299
• InChiKey: WTUCSYXAZXMWHN-QWHCGFSZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  16
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  58.3
• 氢给体数：
  3
• 氢受体数：
  3

文献信息

• [EN] NOVEL GAMMA-LACTAMS AS BETA-SECRETASE INHIBITORS<br/>[FR] NOUVEAUX GAMMA-LACTAMES EN TANT QU'INHIBITEURS DE LA BETA-SECRETASE
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2004013098A1

  公开（公告）日：2004-02-12

  There is provided a series of novel substituted gamma-lactams of Formula (I) wherein R1, R2, R3, R4 and R5 are defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of aβ-peptide. The present invention is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.

  提供了一系列新颖的取代γ-内酰胺化合物，其化学式为（I），其中R1、R2、R3、R4和R5在此有定义，以及它们的药物组合物和使用方法。这些新颖化合物抑制β-分泌酶对淀粉样前体蛋白（APP）的加工，更具体地，抑制aβ-肽的产生。本发明涉及用于治疗与β-淀粉样蛋白产生相关的神经系统疾病的化合物，如阿尔茨海默病和其他受抗淀粉样活性影响的疾病。
• [EN] ASPARTYL PROTEASE INHIBITORS<br/>[FR] INHIBITEURS D'ASPARTYL PROTÉASE
  申请人：MEDIVIR AB

  公开号：WO2010107384A1

  公开（公告）日：2010-09-23

  A compound of formula (I) N-oxides, addition salts, quaternary amines metal complexes stereochemically isomeric forms and metabolites thereof, wherein A is CR1 Or N; formula (A) or formula (B) D is H, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, G is NR10 or O Q is C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C6Cycloalkyl, aryl or heterocyclyl; W is H, C1-C6alkyl, C3-C6Cycloalkyl, CH2F, CHF2 or CF3; one of X' and X" is H or CH3, the other is C1-C3alkyl, F, OH, NRaRb, CF3 or N3; or X' and X" are both F; Y is NRd or O; Z is O, NRa, CHRd, CF2 or S(=0)r or a bond; the other variables are as defined in the specification. The compounds of the invention are inhibitors of BACE and are among other things useful for the treatment and/or prevention of conditions associated with BACE activity such as Alzheimer's disease.

  公式（I）的化合物N-氧化物，加成盐，季铵盐金属配合物立体化异构体及其代谢物，其中A为CR1或N；公式（A）或公式（B）D为H，C1-C6烷基，C2-C6烯基，C2-C6炔基，G为NR10或O，Q为C1-C6烷基，C2-C6烯基，C2-C6炔基，C3-C6环烷基，芳基或杂环烷基；W为H，C1-C6烷基，C3-C6环烷基，CH2F，CHF2或CF3；X'和X"中的一个为H或CH3，另一个为C1-C3烷基，F，OH，NRaRb， 或N3；或者X'和X"都是F；Y为NRd或O；Z为O，NRa，CHRd，CF2或S（=0）r或键；其他变量如规范中定义。本发明的化合物是BACE的抑制剂，除其他用途外，还可用于治疗和/或预防与BACE活性相关的疾病，如阿尔茨海默病。
• Substituted hydroxyethylamines
  申请人：John Varghese

  公开号：US20060106256A1

  公开（公告）日：2006-05-18

  This invention relates to prodrugs of a class of amine compounds which are useful in the treatment of Alzheimer's disease and similar diseases.

  本发明涉及一类氨基化合物的前药，该类化合物在治疗阿尔茨海默病和类似疾病方面具有用途。
• Compounds to treat alzheimer's disease
  申请人：——

  公开号：US20020128255A1

  公开（公告）日：2002-09-12

  The present invention is substituted amines of formula (X) 1 and of the formula (X′) 2 useful in treating Alzheimer's disease and other similar diseases.

  本发明提供的公式（X）1和公式（X'）2的取代胺在治疗阿尔茨海默病和其他类似疾病中有用。
• Tricyclic indole derivatives and their use in the treatment of alzheimer's disease
  申请人：Demont Hubert Emmanuel

  公开号：US20060229302A1

  公开（公告）日：2006-10-12

  The present invention to novel hydroxyethylamine compounds having Asp2 (β-secretase, BACE1 or Memapsin) inhibitory activit, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated β-amyloid levels or β-amyloid deposits, Particularly Alzheimer's disease.

  本发明涉及一种新型的羟乙基胺化合物，具有Asp2（β-分泌酶，BACE1或Memapsin）抑制活性，其制备方法，含有它们的组合物以及它们在治疗由升高的β-淀粉样蛋白水平或β-淀粉样蛋白沉积物所特征的疾病，特别是阿尔茨海默病中的应用。