(12aR)-N-[2-(4-benzylpiperidin-1-yl)ethyl]-5-[(3-fluorophenyl)methyl]-6-oxo-7,9,10,11,12,12a-hexahydropyrido[1,2-d][1,4]benzodiazepine-3-carboxamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: (12aR)-N-[2-(4-benzylpiperidin-1-yl)ethyl]-5-[(3-fluorophenyl)methyl]-6-oxo-7,9,10,11,12,12a-hexahydropyrido[1,2-d][1,4]benzodiazepine-3-carboxamide
• 化学式: C₃₅H₄₁FN₄O₂
• 分子量: 568.7
• InChiKey: XPPBCXSMFHFWEJ-JGCGQSQUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.4
• 重原子数：
  42
• 可旋转键数：
  8
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  55.9
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• COMPOSITIONS OF PROTEIN RECEPTOR TYROSINE KINASE INHIBITORS
  申请人：Wu Jay Jie-Qiang

  公开号：US20110301133A1

  公开（公告）日：2011-12-08

  The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.

  本发明涉及新型合成取代杂环化合物及包含其的制药组合物，这些化合物能够抑制或拮抗一类受体酪氨酸激酶，即肌动蛋白相关激酶（Trk），特别是神经生长因子（NGF）受体TrkA。本发明进一步涉及在治疗和/或预防疼痛、癌症、再狭窄、动脉粥样硬化、银屑病、血栓形成或与失髓鞘化或脱髓鞘化有关的疾病、紊乱或损伤以及与NGF受体TrkA异常活动相关的疾病或紊乱中使用这些化合物的方法。
• Compositions of protein receptor tyrosine kinase inhibitors
  申请人：Purdue Pharma L.P.

  公开号：US10421763B2

  公开（公告）日：2019-09-24

  The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.

  本发明涉及新型合成取代杂环化合物和含有这些化合物的药物组合物，它们能够抑制或拮抗受体酪氨酸激酶家族--托品溶酶相关激酶（Trk），特别是神经生长因子（NGF）受体TrkA。本发明进一步涉及此类化合物在治疗和/或预防疼痛、癌症、再狭窄、动脉粥样硬化、银屑病、血栓形成或与髓鞘脱落或脱髓鞘有关的疾病、紊乱或损伤或与 NGF 受体 TrkA 异常活动有关的疾病或紊乱中的用途。
• US8809530B1
  申请人：——

  公开号：US8809530B1

  公开（公告）日：2014-08-19
• US9040508B2
  申请人：——

  公开号：US9040508B2

  公开（公告）日：2015-05-26
• US9738659B2
  申请人：——

  公开号：US9738659B2

  公开（公告）日：2017-08-22