1-<<5'-(3"-methoxy-4-"-ethoxycarbonyloxyphenyl)-2',4'-pentadienoyl>aminoethyl>-4-diphenylmethoxypiperidine | 110501-66-1

• 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: 1-<<5'-(3"-methoxy-4-"-ethoxycarbonyloxyphenyl)-2',4'-pentadienoyl>aminoethyl>-4-diphenylmethoxypiperidine
• 英文别名: TMK-688；TMK688；1-[{5'-(3"-Methoxy-4"-ethoxycarbonyloxyphenyl)-2',4'-pentadienoyl}aminoethyl]-4-diphenylmethoxypiperidine；linetastine；linazolast；[4-[(1E,3E)-5-[2-(4-benzhydryloxypiperidin-1-yl)ethylamino]-5-oxopenta-1,3-dienyl]-2-methoxyphenyl] ethyl carbonate
• CAS: 110501-66-1
• 化学式: C₃₅H₄₀N₂O₆
• 分子量: 584.712
• InChiKey: LUOUCHOLMUUZBO-SVSXJNCISA-N

物化性质

• 沸点：
  760.9±60.0 °C(Predicted)
• 密度：
  1.20±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  6.4
• 重原子数：
  43
• 可旋转键数：
  15
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  86.3
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  2-(4-benzhydryloxy-piperidin-1-yl)-ethylamine 、 (2E,4E)-5-(4-hydroxy-3-methoxyphenyl)penta-2,4-dienoic acid 在 (2E,4E)-5-(4-hydroxy-3-methoxyphenyl)penta-2,4-dienoic acid 作用下， 生成 1-<<5'-(3"-methoxy-4-"-ethoxycarbonyloxyphenyl)-2',4'-pentadienoyl>aminoethyl>-4-diphenylmethoxypiperidine
  参考文献：
  名称：

  Amide derivatives and antiallergic agents containing the same

  摘要：

  本发明涉及新的酰胺衍生物。所述酰胺衍生物的例子包括1-[2-[5-(3-甲氧基-4-乙氧羰基氧基苯基)-2,4-戊二烯酰基]-氨基乙基]-4-苯甲醇哌啶，1-[2-[3-(3-甲氧基-4-乙氧羰基氧基苯基)-2-丙烯酰基]氨基乙基]-4-苯甲醇哌啶，1-[3-[5-(3-甲氧基-4-乙氧羰基氧基苯基)-2,4-戊二烯酰基]氨基丙基]-4-苯甲醇哌嗪等。这些酰胺衍生物可用作抗过敏剂。

  公开号：

  US04795752A1

文献信息

• Treatment of inflammatory disorders with 2,3- benzodiazepines
  申请人：Vela Pharmaceuticals, Inc.

  公开号：US20040138209A1

  公开（公告）日：2004-07-15

  Compounds according to formula I: 1 wherein R 1 , R 2 , R 3 , R 4 , R 5 and n are as defined herein, are administered for the treatment of inflammatory disorders, particularly inflammatory disorders mediated by LTB 4 ,

  根据公式I:1，其中R1、R2、R3、R4、R5和n的定义如本文所述，用于治疗炎症性疾病，特别是由LTB4介导的炎症性疾病。
• 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。
• Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases
  申请人：Scaramuzzino, Giovanni

  公开号：EP1336602A1

  公开（公告）日：2003-08-20

  New pharmaceutical compounds of general formula (I): F-(X)q where q is an integer from 1 to 5, preferably 1; -F is chosen among drugs described in the text, -X is chosen among 4 groups -M, -T, -V and -Y as described in the text. The compounds of general formula (I) are nitrate prodrugs which can release nitric oxide in vivo in a controlled and selective way and without hypotensive side effects and for this reason they are useful for the preparation of medicines for prevention and treatment of inflammatory, ischemic, degenerative and proliferative diseases of musculoskeletal, tegumental, respiratory, gastrointestinal, genito-urinary and central nervous systems.

  通式（I）的新药物化合物：F-（X）q，其中q是1到5的整数，最好是1；-F是在文本中描述的药物中选择的，-X是在文本中描述的4个组-M，-T，-V和-Y中选择的。通式（I）的化合物是硝酸盐前药，可以在体内以受控和选择性的方式释放一氧化氮，而不会产生降压副作用，因此它们非常适用于制备用于预防和治疗肌肉骨骼，皮肤，呼吸，消化，泌尿和中枢神经系统的炎症，缺血，退行性和增生性疾病的药物。
• Liquid composition containing amide derivative
  申请人：TERUMO KABUSHIKI KAISHA

  公开号：EP0639376A1

  公开（公告）日：1995-02-22

  The present invention is an aqueous liquid composition comprising an anti-allergic amide derivative of which the solubility has been increased by the presence of a nonionic surfactant and a pH adjusting agent so that the composition has a pH of from 4 to 5. Solubility of the amide is further increased if the amount of surfactant is at least 10 times that of the amide and its stability is improved if the amount of surfactant is 0.1 W/V % or more. The composition finds use as eye or nose drops in the treatment of allergic conditions.

  本发明是一种含抗过敏酰胺衍生物的水性液体组合物，通过非离子表面活性剂和 pH 值调节剂的存在提高了该衍生物的溶解度，使该组合物的 pH 值为 4 至 5。如果表面活性剂的用量至少是酰胺用量的 10 倍，则酰胺的溶解度会进一步提高；如果表面活性剂的用量为 0.1 W/V % 或更多，则酰胺的稳定性会得到改善。该组合物可用作治疗过敏症的滴眼液或滴鼻液。
• 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。