18-O-(3,4,5-Trimethoxybenzoyl)-reserpinsaeure | 5868-09-7

• 分子结构分类: 有机化合物 - 生物碱及其衍生物
• 英文名称: 18-O-(3,4,5-Trimethoxybenzoyl)-reserpinsaeure
• 英文别名: 11,17-dimethoxy-18-(3,4,5-trimethoxy-benzoyloxy)-yohimbane-16-carboxylic acid；6,18-Dimethoxy-17-(3,4,5-trimethoxybenzoyl)oxy-1,3,11,12,14,15,16,17,18,19,20,21-dodecahydroyohimban-19-carboxylic acid
• CAS: 5868-09-7
• 化学式: C₃₂H₃₈N₂O₉
• 分子量: 594.662
• InChiKey: KMRXYOHGCCGFKN-UHFFFAOYSA-N

物化性质

• 熔点：
  211-215 °C
• 沸点：
  736.1±60.0 °C(Predicted)
• 密度：
  1.37±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  43
• 可旋转键数：
  9
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  129
• 氢给体数：
  2
• 氢受体数：
  10

文献信息

• VMAT INHIBITORY COMPOUNDS
  申请人：Oregon Health & Science University

  公开号：US20160031852A1

  公开（公告）日：2016-02-04

  Disclosed herein are compounds that bind to the vesicular monoamine transporter 2 (VMAT2), pharmaceutical compositions comprising those compounds, and methods of treatment using said compounds and pharmaceutical compositions.

  本文揭示了与囊泡式单胺转运体2（VMAT2）结合的化合物，包括这些化合物的制药组合物，以及使用这些化合物和制药组合物的治疗方法。
• Use of selective serotonin 5-HT1A receptor agonists for treating side-effects of VMAT inhibitors
  申请人：Neurolixis

  公开号：US11191758B2

  公开（公告）日：2021-12-07

  The present invention relates to the reduction of the side-effects induced by tetrabenazine or other inhibitors of vesicular monoamine transporter (VMAT), in the treatment of central nervous system disorders such as Huntington's disease, L-DOPA-induced dyskinesias in Parkinson's disease, Tourette's syndrome or tardive dyskinesia. The invention comprises administering to a patient in need thereof an effective amount of activates selective serotonin 5-HT1A receptors agonist, whereby the side-effects of depression or Parkinsonism induced by tetrabenazine or other VMAT inhibitors are minimized.

  本发明涉及在治疗亨廷顿氏病、帕金森氏病中L-DOPA诱导的运动障碍、抽动秽语综合征或迟发性运动障碍等中枢神经系统疾病时，减少四苯嗪或其他囊泡单胺转运体（VMAT）抑制剂诱发的副作用。本发明包括向有需要的患者施用有效量的活化选择性5-羟色胺5-HT1A受体激动剂，从而最大限度地减少由四苯嗪或其他VMAT抑制剂诱发的抑郁症或帕金森病的副作用。
• Therapeutic and research application of PDCL3
  申请人：TRUSTEES OF BOSTON UNIVERSITY

  公开号：US11406709B2

  公开（公告）日：2022-08-09

  Described herein are novel compositions comprising, for example, PDCL3 polypeptides having VEGFR-2 inhibitory activity, inhibitory PDCL3 antibodies and PDCL3-binding fragments thereof, or PDCL3 inhibitory nucleic acid molecules, and methods of their use in anti-angiogenesis and anti-tumor proliferation and invasiveness therapies, such as the treatment of cancer, as well as the treatment of those vascular diseases where pathological angiogenesis plays a role, such as in carotid artery disease, macular degeneration, and plaque neovascularization. Also described herein are novel compositions comprising engineered PDCL3 polypeptides having enhanced chaperone activity, recombinant cells comprising such engineered PDCL3 polypeptides having enhanced chaperone activity, and methods thereof for therapeutic protein production and in vitro protein synthesis.

  本文描述了新型组合物，例如包括具有 VEGFR-2 抑制活性的 PDCL3 多肽、抑制性 PDCL3 抗体及其 PDCL3 结合片段或 PDCL3 抑制性核酸分子、以及它们在抗血管生成、抗肿瘤增殖和侵袭性疗法中的使用方法，如治疗癌症，以及治疗病理性血管生成起作用的血管疾病，如颈动脉疾病、黄斑变性和斑块新生血管。本文还描述了包含具有增强伴侣活性的工程化 PDCL3 多肽的新型组合物、包含这种具有增强伴侣活性的工程化 PDCL3 多肽的重组细胞及其用于治疗性蛋白质生产和体外蛋白质合成的方法。
• Cobalamin compounds useful as cardiovascular agents and as imaging agents
  申请人：——

  公开号：US20020049155A1

  公开（公告）日：2002-04-25

  The invention provides cobalamin derivatives linked to a cardiovascular agent, as well as pharmaceutical compositions comprising the compounds and methods for using the compounds in treatment or diagnosis of a cardiovascular disease.

  本发明提供了与心血管药物相连的钴胺衍生物，以及包含这些化合物的药物组合物和使用这些化合物治疗或诊断心血管疾病的方法。
• USE OF SELECTIVE SEROTONIN 5-HT1A RECEPTOR AGONISTS FOR TREATING SIDE-EFFECTS OF VMAT INHIBITORS
  申请人：Neurolixis

  公开号：EP3664787B1

  公开（公告）日：2022-07-20