二甲他林酒石酸氢盐 | 3759-07-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 中文名称: 二甲他林酒石酸氢盐
• 英文名称: Dimetacrine bitartrate
• 英文别名: (2R,3R)-2,3-dihydroxybutanedioic acid;3-(9,9-dimethylacridin-10-yl)-N,N-dimethylpropan-1-amine
• CAS: 3759-07-7
• 化学式: C24H32N2O6
• 分子量: 444.5
• InChiKey: IIYKUJVECNNTEY-LREBCSMRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.29
• 重原子数：
  32
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  122
• 氢给体数：
  4
• 氢受体数：
  8

文献信息

• [EN] PHARMACEUTICAL COMPOSITION COMPRISING 5-METHOXY-N,N-DIMETHYLTRYPTAMINE<br/>[FR] COMPOSITION PHARMACEUTIQUE COMPRENANT DE LA 5-MÉTHOXY-N, N-DIMÉTHYLTRYPTAMINE
  申请人：BECKLEY PSYTECH LTD

  公开号：WO2021250435A1

  公开（公告）日：2021-12-16

  An intranasal composition comprising a dosage amount of 50-150mg/ml 5-methoxy-N,N-dimethyltryptamine (5MeODMT) in a liquid medium, wherein the 5MeODMT is formulated as the chloride salt of 5MeODMT (5MeODMT hydrochloride) and wherein the 5MeODMT hydrochloride is crystalline and characterised by one or more of: peaks in an XRPD diffractogram; an endothermic event in a DSC thermograph; an onset of decomposition in a TGA thermograph; and a DVS isotherm profile.

  一种鼻内制剂，包括50-150mg/ml 5-甲氧基-N，N-二甲基色胺（5MeODMT）的剂量量和液体介质，其中5MeODMT以5MeODMT的氯化物盐（5MeODMT盐酸盐）的形式配制，5MeODMT盐酸盐是结晶的，并具有以下特征之一或多个：XRPD衍射图中的峰值；DSC热图中的吸热事件；TGA热图中的分解起始点；以及DVS等温线剖面。
• [EN] PHARMACEUTICAL COMPOSITION COMPRISING PSILOCYBIN OR ITS POLYMORPHS<br/>[FR] COMPOSITION PHARMACEUTIQUE COMPRENANT DE LA PSILOCYBINE OU SES POLYMORPHES
  申请人：BECKLEY PSYTECH LTD

  公开号：WO2022123232A1

  公开（公告）日：2022-06-16

  A composition for use in a method of treatment of short-lasting unilateral neuralgiform headache with conjunctival injection and tearing (SUNCT) or short-lasting neuralgiform headaches with cranial autonomic symptoms (SUNA), wherein the composition comprises a pharmaceutically effective amount of psilocybin, psilocin or a prodrug thereof, wherein the psilocybin, psilocin or a prodrug thereof, has been synthesised, or has been isolated from a naturally occurring substance or product.

  这是一种用于治疗短暂单侧神经痛性头痛伴结膜充血和流泪（SUNCT）或短暂神经痛性头痛伴颅内自主神经症状（SUNA）的方法的组合物，其中该组合物包括药效学上有效的量的蘑菇素、蘑菇素或其前体药物，其中蘑菇素、蘑菇素或其前体药物已经被合成或从天然产物或制品中分离出来。
• Parenteral formulations of lipophilic pharmaceutical agents and methods for preparing and using the same
  申请人：Platform Brightworks Two, Ltd.

  公开号：US10028949B2

  公开（公告）日：2018-07-24

  There may be provided compositions of lipophilic pharmaceutical agents with improved solubility and stability. For example, there may be provided a non-aqueous composition that comprises a lipophilic pharmaceutical agent, and an amphiphilic polymeric solvent such as PEG400 but essentially free of organic solvents and non-solubilized particles. The composition may be further diluted with a desired aqueous diluent such as an infusion fluid for parenteral administration to a subject such as a human. The compositions may be useful for the treatment for diseases or conditions that are sensitive to lipophilic agents, such as infectious diseases, malignant or autoimmune diseases.

  可提供具有更好溶解性和稳定性的亲脂性药剂组合物。例如，可以提供一种非水性组合物，其中包括亲脂性药剂和两亲性聚合物溶剂（如 PEG400），但基本上不含有机溶剂和非增溶颗粒。该组合物可进一步用所需的水性稀释剂稀释，如输液，用于人等受试者的非肠道给药。该组合物可用于治疗对亲脂性制剂敏感的疾病或病症，如传染性疾病、恶性或自身免疫性疾病。
• GPR156 variants and uses thereof
  申请人：Regeneron Pharmaceuticals, Inc.

  公开号：US10266582B2

  公开（公告）日：2019-04-23

  The disclosure provides nucleic acids, including cDNA, comprising alterations that encode aspartic acid at a position corresponding to position 533 of the human G protein-coupled receptor 156 protein (GPR156). The disclosure also provides isolated and recombinant human GPR156 protein variants that comprise an aspartic acid at a position corresponding to position 533. The change to aspartic acid, and the gene encoding this change, associate with unipolar depression. The disclosure also provides methods for determining whether a subject has or has a risk of developing unipolar depression, based on the identification of such alterations in the gene (DNA or RNA) encoding GPR156.

  本公开提供了核酸（包括 cDNA），其包含编码人 G 蛋白偶联受体 156 蛋白（GPR156）533 位相应位置上的天冬氨酸的改变。本公开还提供了分离的和重组的人 GPR156 蛋白变体，这些变体在与位置 533 相对应的位置上包含一个天冬氨酸。天冬氨酸的变化以及编码这种变化的基因与单极抑郁症有关。本公开内容还提供了根据识别编码 GPR156 的基因（DNA 或 RNA）中的这种变化来确定受试者是否患有单极抑郁症或是否有患单极抑郁症的风险的方法。
• Pharmaceutical capsule compositions comprising lumateperone mono-tosylate
  申请人：INTRA-CELLULAR THERAPIES, INC.

  公开号：US10695345B2

  公开（公告）日：2020-06-30

  The present disclosure relates to pharmaceutical capsules comprising lumateperone, in free, or pharmaceutically acceptable salt form, optionally in combination with one or more additional therapeutic agents, processes for manufacture thereof and methods of use in the treatment or prophylaxis of disease.

  本公开涉及包含游离或药学上可接受的盐形式的鲁米培酮的药用胶囊（可选择与一种或多种额外的治疗剂结合使用）、其制造工艺以及用于治疗或预防疾病的方法。