特立卡兰 | 121277-96-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 中文名称: 特立卡兰
• 英文名称: Terikalant
• 英文别名: 1-[2-[(4S)-3,4-dihydro-2H-chromen-4-yl]ethyl]-4-(3,4-dimethoxyphenyl)piperidine
• CAS: 121277-96-1
• 化学式: C₂₄H₃₁NO₃
• 分子量: 381.5
• InChiKey: UIZPEXQHMIZQPQ-IBGZPJMESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  28
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  30.9
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  (E)-2-(chroman-4-ylidene)acetaldehyde 在 三乙酰氧基硼氢化钠 、 (1S,6S)-5,5-diphenyl-2,4-dioxa-7-azabicyclo[4.2.1]nonane 、 苯甲酸 作用下， 以 氯仿 、 1,2-二氯乙烷 为溶剂， 反应 48.25h， 生成 特立卡兰
  参考文献：
  名称：

  非甲硅烷基双环仲胺催化剂用于 α,β-不饱和醛的不对称转移氢化

  摘要：

  公开了非甲硅烷基双环仲胺有机催化剂的首次手性合成及其在α,β-不饱和醛不对称转移氢化中的应用。较低的催化负载量 (5 mol%) 可还原多种 α,β-不饱和醛（产率高达 97%， ee高达 99%）。展示了这种可扩展方法在苯恶醇、香茅醇、雷美替胺和特立卡兰等生物活性分子的不对称合成中的应用。

  DOI：

  10.1021/acs.joc.4c00523

文献信息

• Pharmaceutical preparation comprising an active dispersed on a matrix
  申请人：——

  公开号：US20040058896A1

  公开（公告）日：2004-03-25

  The present invention relates to the field of pharmaceutical technology and describes a novel advantageous preparation for an active ingredient. The novel preparation is suitable for producing a large number of pharmaceutical dosage forms. In the new preparation an active ingredient is present essentially uniformly dispersed in an excipient matrix composed of one or more excipients selected from the group of fatty alcohol, triglyceride, partial glyceride and fatty acid ester.

  本发明涉及制药技术领域，描述了一种新的有利的活性成分制备方法。这种新的制备方法适用于生产大量的药物剂型。在这种新的制备方法中，活性成分基本上均匀地分散在由脂肪醇、甘油三酯、部分甘油酯和脂肪酸酯等多种赋形剂中选择的一种或多种赋形剂组成的赋形剂基质中。
• Benzopyran derivatives and pharmaceutical compositions containing them
  申请人：Rhone-Poulenc Sante

  公开号：US04977166A1

  公开（公告）日：1990-12-11

  New benzopyran derivatives of formula: ##STR1## in which R.sub.1 is hydrogen, halogen, hydroxy, alkoxy, nitro, amino, alkylsulphonamido, bis(alkylsulphonyl) amino or acylamino, X is nitrogen or a >CH-radical R is a radical of formula: ##STR2## in which A denotes a single bond or methylene or, when X is nitrogen, A may denote carbonyl, and R.sub.2 and R.sub.3, which are identical or different, are hydrogen, halogen, hydroxy, alkyl, alkoxy, nitro, amino, alkylsulphonamido, bis(alkylsulphonyl)amino, acylamino, sulphamoyl or cyano, or, when they are adjacent, together form a methylenedioxy or ethylenedioxy radical, or else R is pyridyl or 2(2H)-benzimidazolonyl if X denotes >CH--, and R' and R" are identical and are hydrogen or alkyl, their isomeric forms and mixtures thereof, and their acid addition salts, can be used as antiarrhythmic and antifibrillation agents.

  化学式为：##STR1##的新苯并吡喃衍生物，其中R.sub.1是氢、卤素、羟基、烷氧基、硝基、氨基、烷基磺酰胺基、双(烷基磺酰基)氨基或酰胺基，X是氮或一个 >CH-基团，R是一个公式的基团：##STR2##其中A表示单键或亚甲基或当X为氮时，A可以表示羰基，R.sub.2和R.sub.3相同或不同，是氢、卤素、羟基、烷基、烷氧基、硝基、氨基、烷基磺酰胺基、双(烷基磺酰基)氨基、酰胺基、磺酰胺基或氰基，或者当它们相邻时，共同形成亚甲二氧基或乙二氧基基团，否则当X表示 >CH-时，R是吡啶基或2(2H)-苯并咪唑基，R'和R"相同且为氢或烷基，它们的同分异构体和混合物，以及它们的酸加合物，可用作抗心律失常和抗心房颤动剂。
• Benzofuranes and their use in the treatment of atrial fibrillation
  申请人：Brandts Bodo

  公开号：US20050065208A1

  公开（公告）日：2005-03-24

  This intention relates to new compounds and their pharmaceutical use, and to the pharmaceutical use of known compounds, which compounds inhibit certain transmembrane potassium currents in the atrium of the heart of a mammal without significantly affecting other ion channels, for the treatment of heart disease particularly atrial fibrillation. The invention also relates to pharmaceutical compositions comprising such compounds.

  本意图涉及新化合物及其药物用途，以及已知化合物的药物用途，这些化合物可抑制哺乳动物心房中某些跨膜钾电流，而不显著影响其他离子通道，用于治疗心脏疾病，特别是心房颤动。本发明还涉及包含这些化合物的药物组合物。
• COMPOSITION FOR IMMUNITY INDUCTION PROMOTION AND VACCINE PHARMACEUTICAL COMPOSITION
  申请人：Nitto Denko Corporation

  公开号：EP3412308A1

  公开（公告）日：2018-12-12

  The present invention aims to provide a composition for immunity induction promotion and a vaccine pharmaceutical composition each universally usable for induction of cellular immunity and/or humoral immunity against various antigens and exerting a high effect of inducing cellular immunity and/or humoral immunity. Provided is a composition for immunity induction promotion, containing a first immunity induction promoter, the first immunity induction promoter being an ion channel drug that affects an ion channel or an ion pump.

  本发明旨在提供一种免疫诱导促进组合物和一种疫苗药物组合物，这两种组合物均可普遍用于诱导针对各种抗原的细胞免疫和/或体液免疫，并能发挥较高的诱导细胞免疫和/或体液免疫的效果。本发明提供了一种用于免疫诱导促进的组合物，该组合物含有第一免疫诱导促进剂，第一免疫诱导促进剂是一种影响离子通道或离子泵的离子通道药物。
• Controlled absorption water-soluble pharmaceutically active organic compound formulation for once-daily administration
  申请人：Counts David F.

  公开号：US10463611B2

  公开（公告）日：2019-11-05

  The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a water-soluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound. In some embodiments, the formulation of the invention are designed to extend release of the pharmaceutically active organic compound for about 3 hours to about 8 hours, thereby enabling preparation of an extended release formulation for any pharmaceutically active compound with a half-life of from about 16 hours to about 21 hours.

  本公开提供了一种用于口服的每日一次水溶性药用活性制剂。在某些实施方案中，该组合物包括掺入小颗粒中的水溶性药用活性有机化合物，每个颗粒都有一个水溶性药用活性有机化合物或其可接受盐的核心，该核心与药学上可接受的药物结合聚合物可逆结合。组合物的核心由不溶性透水膜包围，该膜能够延迟其中的药用活性化合物的溶解，并延长药用活性化合物的释放时间。在某些实施方案中，本发明的制剂可将药用活性有机化合物的释放时间延长约 3 小时至约 8 小时，从而能够制备半衰期为约 16 小时至约 21 小时的任何药用活性化合物的缓释制剂。