Boc-Nle-NH2 | 119038-19-6

• 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: Boc-Nle-NH2
• 英文别名: BOC-Norleucine Amide；tert-butyl N-[(2S)-1-amino-1-oxohexan-2-yl]carbamate
• CAS: 119038-19-6
• 化学式: C₁₁H₂₂N₂O₃
• 分子量: 230.307
• InChiKey: UJWXUMMFSUYXGB-QMMMGPOBSA-N

物化性质

• 沸点：
  381.2±25.0 °C(Predicted)
• 密度：
  1.029±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  16
• 可旋转键数：
  7
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.82
• 拓扑面积：
  81.4
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  Boc-O-苄基-L-酪氨酸 、 Boc-Nle-NH2 在 N-甲基吗啉 、 N,N-二异丙基乙胺 、 三氟乙酸 、 氯甲酸异丁酯 作用下， 生成 Boc-Tyr(Bzl)-Nle-NH2
  参考文献：
  名称：

  Peptide and pseudopeptide analogues of cholecystokinin, chemical modifications of the met28-gly29 region

  摘要：

  DOI：

  10.1016/s0040-4020(01)86144-5
• 作为产物：
  描述：

  N-Boc-L-正亮氨酸 在 N-甲基吗啉 、 ammonium hydroxide 、 氯甲酸异丁酯 作用下， 生成 Boc-Nle-NH2
  参考文献：
  名称：

  Peptide and pseudopeptide analogues of cholecystokinin, chemical modifications of the met28-gly29 region

  摘要：

  DOI：

  10.1016/s0040-4020(01)86144-5

文献信息

• Compounds for inhibiting &bgr;-amyloid peptide release and/or its synthesis
  申请人：Elan Pharmaceuticals, Inc.

  公开号：US06211235B1

  公开（公告）日：2001-04-03

  Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis.

  揭示了一种抑制β-淀粉样肽释放和/或其合成的化合物，因此在治疗阿尔茨海默病方面具有用途。还揭示了包含抑制β-淀粉样肽释放和/或其合成的化合物的药物组合物。
• Methods and compounds for inhibiting &bgr;-amyloid peptide release and/or its synthesis
  申请人：Elan Pharmaceuticals, Inc.

  公开号：US06191166B1

  公开（公告）日：2001-02-20

  Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

  揭示了一种抑制β-淀粉样肽释放和/或合成的化合物，因此在治疗阿尔茨海默病方面具有用途。还揭示了包括抑制β-淀粉样肽释放和/或合成的化合物的药物组合物，以及使用这种药物组合物预防性和治疗性地治疗阿尔茨海默病的方法。
• N-(ARYL/HETEROARYL) AMINO ACID DERIVATIVES, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, AND METHODS FOR INHIBITING BETA-AMYLOID PEPTIDE RELEASE AND/OR ITS SYNTHESIS BY USE OF SUCH COMPOUNDS
  申请人：——

  公开号：US20010020097A1

  公开（公告）日：2001-09-06

  Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

  本发明涉及一种抑制β-淀粉样肽释放和/或其合成的化合物，因此在治疗阿尔茨海默病方面具有用途。还公开了包括抑制β-淀粉样肽释放和/或其合成的化合物的药物组合物，以及使用这种药物组合物预防和治疗阿尔茨海默病的方法。
• Methods and compounds for inhibiting beta-amyloid peptide release and/or its synthesis
  申请人：——

  公开号：US20030229024A1

  公开（公告）日：2003-12-11

  Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

  本发明涉及一种抑制&bgr;-淀粉样肽释放和/或合成的化合物，因此具有治疗阿尔茨海默病的用途。还公开了药物组合物，包括抑制&bgr;-淀粉样肽释放和/或合成的化合物，以及使用这样的药物组合物进行预防和治疗阿尔茨海默病的方法。
• Peptide and peptide analog protease inhibitors
  申请人：SIBIA Neurosciences, Inc.

  公开号：US05714471A1

  公开（公告）日：1998-02-03

  Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds are those of formulae I and II: ##STR1## in which R.sub.1 is preferably 2-methyl propene, 2-butene, cyclohexyl or cyclohexylmethyl; R.sub.2, R.sub.4, and R.sub.8 are each independently methyl or ethyl; R.sub.3 is preferably iso-butyl or phenyl; R.sub.5 is preferably iso-butyl; R.sub.6 is H or methyl; R.sub.7 --(Q).sub.n is preferably benzyloxycarbonyl or acetyl; Q is preferably --C(O)--; R.sub.8 is preferbly iso-butyl; R.sub.A =--(T).sub.m --(D).sub.m --R.sub.1, is which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C.sub.3-4 alkenyl being more preferred; and X is preferably an .alpha.-ketoester or .alpha.-ketoamide.

  提供了用于治疗以淀粉样物质沉积为特征的疾病的化合物的使用方法和化合物。其中化合物包括式I和式II：##STR1## 其中R.sub.1优选为2-甲基丙烯，2-丁烯，环己基或环己基甲基；R.sub.2，R.sub.4和R.sub.8各自独立地为甲基或乙基；R.sub.3优选为异丁基或苯基；R.sub.5优选为异丁基；R.sub.6为H或甲基；R.sub.7--(Q).sub.n优选为苄氧羰基或乙酰基；Q优选为--C(O)--；R.sub.8优选为异丁基；R.sub.A=--(T).sub.m--(D).sub.m--R.sub.1，其中T优选为氧或碳，D优选为一种单不饱和的C.sub.3-4烯烃，更优选；X优选为α-酮酸酯或α-酮酰胺。