Ladostigil Tartrate | 209394-46-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 茚满类
• 英文名称: Ladostigil Tartrate
• 英文别名: (2R,3R)-2,3-dihydroxybutanedioic acid;[(3R)-3-(prop-2-ynylamino)-2,3-dihydro-1H-inden-5-yl] N-ethyl-N-methylcarbamate
• CAS: 209394-46-7
• 化学式: C36H46N4O10
• 分子量: 694.8
• InChiKey: PRLVBVAJMQZMJN-OGOSNNLPSA-N

物化性质

• 溶解度：
  DMSO：50 mg/mL（71.97 mM；需要超声波）

计算性质

• 辛醇/水分配系数(LogP)：
  2.57
• 重原子数：
  50
• 可旋转键数：
  13
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  198
• 氢给体数：
  6
• 氢受体数：
  12

文献信息

• Propargylated aminoindans, processes for preparation, and uses thereof
  申请人：Piryatinsky Victor

  公开号：US20070203232A1

  公开（公告）日：2007-08-30

  This invention provides compounds having the structure: wherein R 1 is methyl and R 2 is H, or R 1 is ethyl and R 2 is hydroxymethyl; R 3 is H or propargyl; and R 4 is either H or t-butyloxycarbonyl; or an enantiomer or a pharmaceutically acceptable salt thereof. This invention further provides the use of a therapeutically effective amount of such compounds to treat a subject afflicted with a psychiatric disorder, Parkinson's disease, Alzheimer's disease, dementia, or a neurological disorder.

  这项发明提供了具有以下结构的化合物： 其中R1为甲基且R2为H，或者R1为乙基且R2为羟甲基； R3为H或丙炔基；以及 R4为H或叔丁氧羰基； 或其对映体或药用可接受的盐。此发明进一步提供了使用这些化合物的治疗有效量来治疗患有精神障碍、帕金森病、阿尔茨海默病、痴呆症或神经障碍的受试者。
• Methods for isolating propargylated aminoindans
  申请人：Frenkel Anton

  公开号：US20070112217A1

  公开（公告）日：2007-05-17

  Disclosed is a process for isolating from a reaction mixture a salt of a mono-propargylated aminoindan having the structure wherein R 1 is H, hydroxyl, alkoxy or wherein Y is O or S; R 2 and R 3 is each, independently, C 1-8 alkyl, C 6-12 aryl, C 6-12 aralkyl, each optionally halo substituted, or hydrogen; where the reaction mixture further comprises a solvent, a primary aminoindan having the structure wherein R 1 is defined as above, and a tertiary aminoindan having the structure the process comprising d) adding an acid to the reaction mixture; e) crystallizing the mono-propargylated aminoindan under conditions suitable for the formation of a crystalline salt of the mono-propargylated aminoindan; and f) recovering the crystalline salt of the mono-propargylated aminoindan, wherein the process is performed without addition of an organic solvent. Also disclosed are the crystalline diastereomeric salts produced by the process and pharmaceutical compositions containing the salts.

  公开了一种从反应混合物中分离出一种单丙炔基氨基间醚盐的方法，其具有以下结构：其中R1为H、羟基、烷氧基或；其中Y为O或S；R2和R3分别独立地为C1-8烷基、C6-12芳基、C6-12芳基烷基，每种均可选择地取代卤素，或氢；其中反应混合物进一步包括溶剂、具有以下结构的初级氨基间醚和具有以下结构的三级氨基间醚；所述方法包括d)向反应混合物中加入酸；e)在适合形成单丙炔基氨基间醚的结晶盐的条件下结晶化单丙炔基氨基间醚；和f)回收单丙炔基氨基间醚的结晶盐，其中该方法在不添加有机溶剂的情况下执行。还公开了该方法产生的晶体对映异构盐以及含有这些盐的药物组合物。
• Process for the synthesis of enantiomeric indanylamine derivatives
  申请人：Boulton Terence Lee

  公开号：US20060199974A1

  公开（公告）日：2006-09-07

  A process for manufacturing (R)-propynylaminoindans, and alternatively, a process for manufacturing (S)-propynylaminoindans. The chiral propynylaminoindans include alkoxy or alkylcarbamates derivatives. The process comprises transfer or pressure hydrogenation in the presence of an optically active catalyst to reduce 1-indanones. The chiral product, either (S)- or (R)-indanols undergo nucleophilic substitution to produce the named product. In an additional aspect, the invention relates to novel intermediates and compounds, namely, substituted indanones, substituted (S)-indanols and substituted (R)-indanols.

  一种制造(R)-丙炔基氨基茚和(S)-丙炔基氨基茚的工艺。这些手性丙炔基氨基茚包括烷氧基或烷基氨基甲酸酯衍生物。该工艺包括在光学活性催化剂存在下进行转移或压力加氢以还原1-茚酮。手性产物，无论是(S)-还是(R)-茚醇，经历亲核取代以产生所述的产品。此外，该发明涉及新型中间体和化合物，即取代茚酮，取代(S)-茚醇和取代(R)-茚醇。
• Formulations of ladostigil tartrate
  申请人：Licht Daniella

  公开号：US20060189685A1

  公开（公告）日：2006-08-24

  Disclosed are formulations of ladostigil tartrate, including pharmaceutical compositions, process for the manufacture, and use thereof.

  本发明涉及拉多司吉酒石酸盐的配方，包括制药组合物、制造过程和使用方法。
• Crystals of ladostigil tartrate, methods of production and pharmaceutical compositions thereof
  申请人：Bahar Eliezer

  公开号：US20060189819A1

  公开（公告）日：2006-08-24

  Disclosed is crystalline ladostigil tartrate of a specified density, compositions, including pharmaceutical compositions comprising such ladostigil tartrate, and a process for the manufacture thereof.

  公开了指定密度的结晶拉多司吉酸酒石酸盐，包括含有该拉多司吉酸酒石酸盐的组合物，包括制造该拉多司吉酸酒石酸盐的过程。