6-neopentyl-3,4-dihydro-2H-chromen-4-ylamine | 676134-04-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 英文名称: 6-neopentyl-3,4-dihydro-2H-chromen-4-ylamine
• 英文别名: 6-(2,2-dimethylpropyl)-3,4-dihydro-2H-chromen-4-amine
• CAS: 676134-04-6
• 化学式: C₁₄H₂₁NO
• 分子量: 219.327
• InChiKey: ZEYQVHGNQZUPQV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  35.2
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• [EN] SUBSTITUTED HYDROXYETHYL AMINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE<br/>[FR] COMPOSÉS D'HYDROXYÉTHYLAMINE SUBSTITUÉE EN TANT QUE MODULATEURS DE BÊTA-SÉCRÉTASE ET LEURS PROCÉDÉS D'UTILISATION
  申请人：AMGEN INC

  公开号：WO2009064418A1

  公开（公告）日：2009-05-22

  The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I) I wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, X and Z are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formula II, intermediates and processes useful for the preparation of compounds of Formulas I and II.

  本发明涵盖了一类新化合物，用于调节Beta-分泌酶酶活性，治疗由Beta-分泌酶介导的疾病，包括阿尔茨海默病（AD）及相关疾病。在一种实施方案中，这些化合物具有一般的化学式（I），其中R1、R2、R3、R4、R5、A1、A2、A3、A4、X和Z在此定义。该发明还包括将这些化合物用于制备药物组合物，用于治疗与beta-分泌酶蛋白活性相关的疾病和症状，如阿尔茨海默病（AD）、认知缺陷和损伤、精神分裂症和其他类似的中枢神经系统疾病。该发明还包括进一步的化学式II实施方案，以及用于制备化合物I和II的中间体和工艺。
• Methods of treatment of amyloidosis using bi-cyclic aspartyl protease inhibitors
  申请人：John Varghese

  公开号：US20050239832A1

  公开（公告）日：2005-10-27

  The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.

  本发明涉及新型化合物和治疗与淀粉样变性相关的疾病、紊乱和状况的方法。淀粉样变性是指与A-beta蛋白异常沉积相关的一系列疾病、紊乱和状况的集合。
• 2-Amino- and 2-thio- substituted 1,3-diaminopropanes
  申请人：Hom Roy

  公开号：US20050267199A1

  公开（公告）日：2005-12-01

  Disclosed are compounds of the formula: where variables Q, Z, X, R 15 , R 2 , R 3 , and R c are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal.

  本发明揭示了以下式子的化合物：其中变量Q、Z、X、R15、R2、R3和R4在此定义。本发明揭示的化合物是β-分泌酶酶的抑制剂，因此在治疗老年痴呆症和其他以哺乳动物体内A beta 肽沉积为特征的疾病中有用。
• Acetyl 2-hydroxy-1, 3-diaminoalkanes
  申请人：——

  公开号：US20040180939A1

  公开（公告）日：2004-09-16

  Disclosed are compounds of the formula: 1 where variables Z, X, R 15 , R 2 , R 3 , and R c are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal.

  本发明揭示了公式1的化合物：其中变量Z、X、R15、R2、R3和Rc的定义如下。本发明所揭示的化合物是β-分泌酶酶的抑制剂，因此在治疗老年痴呆症和其他以A beta肽在哺乳动物中沉积为特征的疾病方面有用。
• ACETYL 2-HYDROXY-1,3-DIAMINOALKANES
  申请人：John Varghese

  公开号：US20100145056A1

  公开（公告）日：2010-06-10

  Disclosed are compounds of the formula: where variables Z, X, R 15 , R 2 , R 3 , and R c are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal.

  公开了以下式子的化合物：其中变量Z，X，R15，R2，R3和R4在此处定义。本文所披露的化合物是β-分泌酶酶的抑制剂，因此在治疗阿尔茨海默病和其他以A beta肽在哺乳动物中沉积为特征的疾病中有用。