1-(4-Methylpentanoylamino)cyclopentane-1-carboxylic acid | 946860-57-7

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 1-(4-Methylpentanoylamino)cyclopentane-1-carboxylic acid
• CAS: 946860-57-7
• 化学式: C₁₂H₂₁NO₃
• 分子量: 227.304
• InChiKey: FCRXXFGCOBPILN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  16
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  66.4
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (3S)-3-amino-1-methyl-5-[4-(trifluoromethyl)phenyl]-3H-1,4-benzodiazepin-2-one;hydron;bromide 、 1-(4-Methylpentanoylamino)cyclopentane-1-carboxylic acid 在 N,N-二异丙基乙胺 、 N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成
  参考文献：
  名称：

  Design and synthesis of benzoazepinone-derived cyclic malonamides and aminoamides as potent γ-secretase inhibitors

  摘要：

  We report the synthesis of benzoazepine-derived cyclic malonamides (2) and aminoamides (3) as gamma-secretase inhibitors for the potential treatment of Alzheimer's disease. The in vitro structure-activity relationships of 2 and 3 along with dog pharmacokinetic results are described. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.04.102
• 作为产物：
  描述：

  4-甲基戊酸 在 lithium hydroxide 、 N,N-二异丙基乙胺 、 N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate 作用下， 以 四氢呋喃 、 N,N-二甲基甲酰胺 为溶剂， 生成 1-(4-Methylpentanoylamino)cyclopentane-1-carboxylic acid
  参考文献：
  名称：

  Design and synthesis of benzoazepinone-derived cyclic malonamides and aminoamides as potent γ-secretase inhibitors

  摘要：

  We report the synthesis of benzoazepine-derived cyclic malonamides (2) and aminoamides (3) as gamma-secretase inhibitors for the potential treatment of Alzheimer's disease. The in vitro structure-activity relationships of 2 and 3 along with dog pharmacokinetic results are described. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.04.102

文献信息

• CYCLIC MALONAMIDES AS INHIBITORS OF ABETA PROTEIN PRODUCTION
  申请人：Olson Richard E.

  公开号：US20100009965A1

  公开（公告）日：2010-01-14

  This invention relates to novel cyclic malonamides having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.

  本发明涉及具有公式（I）的新型环状马隆酰胺，其药物组成物和使用方法。这些新化合物抑制淀粉样前体蛋白的加工，更具体地抑制Aβ-肽的产生，从而防止神经沉积物的淀粉样蛋白形成。更具体地，本发明涉及治疗与β-淀粉样蛋白产生相关的神经疾病，如阿尔茨海默病和唐氏综合症。
• CYCLIC MALONAMIDES AS INHIBITORS OF Abeta PROTEIN PRODUCTION
  申请人：Olson Richard E.

  公开号：US20090264419A1

  公开（公告）日：2009-10-22

  This invention relates to novel cyclic malonamides having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.

  本发明涉及具有以下公式（I）的新型环状马隆酰胺、其制药组合物以及使用方法。这些新化合物抑制淀粉样前体蛋白的加工，更具体地抑制Aβ-肽的产生，从而防止神经沉积物的淀粉样蛋白形成。更具体地，本发明涉及与β-淀粉样蛋白产生有关的神经系统疾病的治疗，例如阿尔茨海默病和唐氏综合症。
• CYCLIC MALONAMIDES AS INHIBITORS OF ASS PROTEIN PRODUCTION
  申请人：Olson Richard E.

  公开号：US20080275024A1

  公开（公告）日：2008-11-06

  This invention relates to novel cyclic malonamides having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.

  本发明涉及具有以下式子（I）的新型环状马隆酰胺，其药物组成和使用方法。这些新化合物抑制淀粉样前体蛋白的处理，更具体地抑制Aβ肽的产生，从而防止神经沉积物的淀粉样蛋白的形成。更具体地，本发明涉及与β-淀粉样蛋白产生相关的神经系统疾病的治疗，例如阿尔茨海默病和唐氏综合症。
• CYCLIC MALONAMIDES AS INHIBITORS OF A BETA PROTEIN PRODUCTION
  申请人：Olson Richard E.

  公开号：US20100041639A1

  公开（公告）日：2010-02-18

  This invention relates to novel cyclic malonamides having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.

  本发明涉及具有公式（I）的新型环状马隆酰胺，其药物组成和使用方法。这些新的化合物抑制淀粉样前体蛋白的处理，更具体地抑制Aβ肽的产生，从而防止神经沉积物的淀粉样蛋白的形成。更具体地，本发明涉及与β-淀粉样蛋白产生相关的神经系统疾病的治疗，如阿尔茨海默病和唐氏综合症。
• US7276496B2
  申请人：——

  公开号：US7276496B2

  公开（公告）日：2007-10-02