L-703 606 Oxalate salt

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: L-703 606 Oxalate salt
• 英文别名: 2-benzhydryl-N-[(2-iodophenyl)methyl]-1-azabicyclo[2.2.2]octan-3-amine
• 化学式: C₂₇H₂₉IN₂
• 分子量: 508.4
• InChiKey: WSLTYZVXORBNLB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6
• 重原子数：
  30
• 可旋转键数：
  6
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  15.3
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• Neurofibromatoses therapeutic agents and screening for same
  申请人：Fernandez-Valle Cristina

  公开号：US10105351B2

  公开（公告）日：2018-10-23

  Disclosed herein are methods of treating a patient at risk of developing or having a neurofibromatosis or a sporadic schwannoma. In exemplary embodiments, the method involves administering to a subject in need an effective amount of a modulator of a target related to neurofibromatosis. Also disclosed are screening assays involving the implementation of Merlin-null Schwann cells, and to compounds identified using same.

  本文公开了治疗有患神经纤维瘤病或散发性分裂瘤风险的患者的方法。在示例性实施方案中，该方法涉及向有需要的受试者施用有效量的神经纤维瘤病相关靶点的调节剂。还公开了涉及实施Merlin-null许旺细胞的筛选试验，以及利用这些试验鉴定的化合物。
• Emulsion formulations of an NK-1 receptor antagonist and uses thereof
  申请人：Heron Therapeutics, Inc.

  公开号：US10624850B2

  公开（公告）日：2020-04-21

  Disclosed herein are novel pharmaceutical formulations of a neurokinin-1 (NK-1) receptor antagonist suitable for parenteral administration including intravenous administration. Also included are formulations including both the NK-1 receptor antagonist and dexamethasone sodium phosphate. The pharmaceutical formulations are stable oil-in-water emulsions for non-oral treatment of emesis and are particularly useful for treatment of subjects undergoing highly emetogenic cancer chemotherapy.

  本文公开了一种神经激肽-1（NK-1）受体拮抗剂的新型药物制剂，适合肠外给药，包括静脉给药。还包括同时含有 NK-1 受体拮抗剂和地塞米松磷酸钠的制剂。这些药物制剂是稳定的水包油乳剂，用于非口服治疗呕吐，尤其适用于治疗正在接受高致呕吐癌症化疗的患者。
• Process for the synthesis of 2-benzhydryl-3 quinuclidinone
  申请人：Procos S.P.A.

  公开号：US11286254B2

  公开（公告）日：2022-03-29

  The present invention discloses a process for the preparation of 2-benzhydryl-3-quinuclidinone (1). (I). The process of the invention allows to obtain the intermediate 2-benzhydryl-3-quinuclidinone (1) by reaction of 2-benzylidene-3-quinuclidinone (2) with the Grignard reagent phenyl-magnesium halide, in particular chloride or bromide, in the presence of catalytic amounts of copper (I) salts. Taking advantage of the high efficiency of the catalytic system of the copper (I) salts, 2-benzhydryl-3-quinuclidinone (1) is obtained in higher yields than those of the known processes. Advantageously, since the amounts of copper (I) salts are catalytic, the latter can easily be removed from the reaction mixture, and the process is carried out in the presence of solvents less toxic and expensive than those used in the state of the art.

  本发明公开了一种制备2-双苯甲基-3-喹诺里西啶酮(1)的方法。(I)。本发明的方法允许通过将2-苯甲酰基-3-喹诺里西啶酮(2)与格氏试剂苯基镁卤化物反应，特别是在铜(I)盐催化量的存在下，获得中间体2-双苯甲基-3-喹诺里西啶酮(1)。利用铜(I)盐催化系统的高效性，可获得比已知方法更高的产率的2-双苯甲基-3-喹诺里西啶酮(1)。而且，由于铜(I)盐的使用量是催化量，它们可以很容易地从反应混合物中去除，并且该过程在毒性较低、成本较低的溶剂存在下进行，与现有技术中使用的溶剂相比。
• NEUROFIBROMATOSES THERAPEUTIC AGENTS AND SCREENING FOR SAME
  申请人：University of Central Florida Research Foundation, Inc.

  公开号：EP2825209B1

  公开（公告）日：2018-08-29
• PHARMACEUTICAL COMPOSITION COMPRISING ANTIEMETIC COMPOUNDS AND POLYORTHOESTER
  申请人：Heron Therapeutics, Inc.

  公开号：EP2931253A1

  公开（公告）日：2015-10-21