benzyl N-[1-(benzotriazol-1-yl)-2-oxo-2-[2-(pyridine-4-carbonyl)anilino]ethyl]carbamate | 280568-15-2

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: benzyl N-[1-(benzotriazol-1-yl)-2-oxo-2-[2-(pyridine-4-carbonyl)anilino]ethyl]carbamate
• CAS: 280568-15-2
• 化学式: C₂₈H₂₂N₆O₄
• 分子量: 506.52
• InChiKey: GQTKCOKLBOPXGU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  38
• 可旋转键数：
  9
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  128
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  benzyl N-[1-(benzotriazol-1-yl)-2-oxo-2-[2-(pyridine-4-carbonyl)anilino]ethyl]carbamate 在 氨 作用下， 以 甲醇 为溶剂， 生成 1,3-Dihydro-5-(pyridin-4-yl)-3(R,S)-[(benzyloxycarbonyl)-amino]-2H-1,4-benzodiazepin-2-one
  参考文献：
  名称：

  Synthesis and biological activity of 5-heteroaryl benzodiazepines: analogues of YM022

  摘要：

  A novel series of analogues of the potent gastrin/CCK-B receptor antagonist YM022 have been prepared which incorporate 5- and 6-membered heteroaromatic rings in the benzodiazepine 5-position. The 5-(2-pyridyl) derivatives in particular retained good in vitro and in vivo potency and one such compound 9i was shown to inhibit acid secretion after oral dosing in dogs. improved bioavailability for 9i over the 5-phenyl analogue, 9h was demonstrated in rats.

  DOI：

  10.1016/0960-894x(95)00557-a
• 作为产物：
  描述：

  邻-4-吡啶酰基苯胺 、 2-(1H-苯并[d][1,2,3]噻唑-1-基)-2-(((苄氧基)羰基)氨基)乙酸 在 1-(3-二甲基氨基丙基)-3-乙基碳二亚胺 作用下， 生成 benzyl N-[1-(benzotriazol-1-yl)-2-oxo-2-[2-(pyridine-4-carbonyl)anilino]ethyl]carbamate
  参考文献：
  名称：

  Synthesis and biological activity of 5-heteroaryl benzodiazepines: analogues of YM022

  摘要：

  A novel series of analogues of the potent gastrin/CCK-B receptor antagonist YM022 have been prepared which incorporate 5- and 6-membered heteroaromatic rings in the benzodiazepine 5-position. The 5-(2-pyridyl) derivatives in particular retained good in vitro and in vivo potency and one such compound 9i was shown to inhibit acid secretion after oral dosing in dogs. improved bioavailability for 9i over the 5-phenyl analogue, 9h was demonstrated in rats.

  DOI：

  10.1016/0960-894x(95)00557-a

文献信息

• Succinoylamino benzodiazepines as inhibitors of Abeta protein production
  申请人：Olson E. Richard

  公开号：US20060122169A1

  公开（公告）日：2006-06-08

  This invention relates to novel lactams 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）的新型内酰胺，其制药组合物以及使用方法。这些新型化合物抑制淀粉样前体蛋白的加工，更具体地说，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。
• SUCCINOYLAMINO BENZODIAZEPINES AS INHIBITORS OF ABETA PROTEIN PRODUCTION
  申请人：Olson Richard E.

  公开号：US20080207602A1

  公开（公告）日：2008-08-28

  This invention relates to novel lactams 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）的新型内酰胺，它们的制药组合物及其使用方法。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，从而防止神经蛋白淀积的形成。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。
• SUCCINOYLAMINO BENZODIAZEPINES AS INHIBITORS OF AB PROTEIN PRODUCTION
  申请人：Olson Richard E.

  公开号：US20090069293A1

  公开（公告）日：2009-03-12

  This invention relates to novel lactams 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化学式（I）的新型内酰胺，它们的药物组合物以及它们的使用方法。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，从而防止淀粉样蛋白的神经沉积物的形成。更具体地，本发明涉及与β-淀粉样蛋白产生相关的神经疾病的治疗，如阿尔茨海默病和唐氏综合症。
• SUCCINOYLAMINO BENZODIAZEPINES AS INHIBITORS OF Abeta PROTEIN PRODUCTION
  申请人：Olson Richard E.

  公开号：US20080171735A1

  公开（公告）日：2008-07-17

  This invention relates to novel lactams 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）的新型内酰胺，以及它们的制药组合物和使用方法。这些新型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。
• US7304049B2
  申请人：——

  公开号：US7304049B2

  公开（公告）日：2007-12-04