1-[(3-甲氧基苯基)亚甲基氨基]氧基-3-[4-(2-甲氧基苯基)哌嗪-1-基]丙-2-醇 | 67254-81-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 中文名称: 1-[(3-甲氧基苯基)亚甲基氨基]氧基-3-[4-(2-甲氧基苯基)哌嗪-1-基]丙-2-醇
• 中文别名: 哌拉肟；哌那多兴
• 英文名称: O-(3-<4-(2-Methoxyphenyl)-1-piperazinyl>-2-hydroxypropyl)-3-methoxybenzaldoxim
• 英文别名: 3-methoxy-benzaldehyde O-{2-hydroxy-3-[4-(2-methoxy-phenyl)-piperazin-1-yl]-propyl}-oxime；Peradoxime；1-[(3-methoxyphenyl)methylideneamino]oxy-3-[4-(2-methoxyphenyl)piperazin-1-yl]propan-2-ol
• CAS: 67254-81-3
• 化学式: C₂₂H₂₉N₃O₄
• 分子量: 399.49
• InChiKey: QSOFMSXQETVQGE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  29
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.409
• 拓扑面积：
  66.8
• 氢给体数：
  1
• 氢受体数：
  7

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。
• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• (Phenylmethylene)-2-(alkyl)-1- omega-(amino)-alkoxyimino -cycloalkane derivatives, a process for preparing them as well as medicaments containing them and the use of them
  申请人：EGIS GYOGYSZERGYAR RT.

  公开号：EP0619298A2

  公开（公告）日：1994-10-12

  A subject-matter of the invention are (phenylmethylene)-2-(alkyl)-1-[ω-(amino)-alkoxyimino]-cycloalkane derivatives of general formula wherein Rrepresents hydrogen, C₁₋₄ alkyl or hydroxyl, R₁stands for C₁₋₁₂ alkyl, R₂ and R₃independently each represents hydrogen, a C₁₋₁₂ alkyl group, optionally substituted by hydroxy, or a C₂₋₁₂ alkenyl group, or R₂ and R₃together with the nitrogen atom to which they are attached form a 4- to 7-membered heterocyclic ring, optionally comprising an oxygen, sulfur or a further nitrogen atom, which latter optionally may carry a phenyl, benzyl or C₁₋₄ alkyl substituent, R₄ and R₅independently each stands for hydrogen, halogen or a C₁₋₄ alkoxy group, or together represent a 3,4-methylenedioxy group, nis an integer from 2 to 5 and Arepresents a valency bond or a -CH₂-group, as well as stereo and optically active isomers and their mixtures, acid-addition salts and quaternary ammonium derivatives thereof. Furthermore the invention is concerned with a process for preparing these compounds as well as medicaments containing them and the use of them for preparing medicaments, particularly having ulcus and gastric-acid-secretion inhibiting effects.

  本发明的一个主题是通式为(苯基亚甲基)-2-(烷基)-1-[ω-(氨基)-烷氧基亚氨基]-环烷烃衍生物 其中 R 代表氢、C₁₋₄ 烷基或羟基、 R₁ 代表 C₁₋₁₂ 烷基、 R₂ 和 R₃ 各自独立地代表氢、任选被羟基取代的 C₁₋₁₂ 烷基或 C₂₋₁₂ 烯基、 或 R₂ 和 R₃ 与它们所连接的氮原子一起形成一个 4-7 元杂环，该杂环可选择包含氧、硫或另一个氮原子，后者可选择带有苯基、苄基或 C₁₋₄烷基取代基、 R₄ 和 R₅ 各自代表氢、卤素或 C₁₋₄ 烷氧基，或共同代表 3,4-亚甲二氧基、 n 是 2 到 5 的整数 和 代表价键或 -CH₂ 基团、 以及立体异构体和光学活性异构体及其混合物、酸加成盐和季铵衍生物。 此外，本发明还涉及到制备这些化合物的工艺以及含有这些化合物的药物，以及使用这些化合物制备药物，特别是具有抑制溃疡和胃酸分泌作用的药物。
• 1-(Phenyl)-3-[omega-(amino)-alkoxyimino]-alk-1-ene derivatives, a process for preparing them as well as medicaments containing them and the use of them
  申请人：EGIS GYOGYSZERGYAR RT.

  公开号：EP0619299A2

  公开（公告）日：1994-10-12

  A subject-matter of the invention are 1-(Phenyl)-3-[ω-(amino)-alkoxyimino]-alk-1-ene derivatives of general formula wherein R₁ and R₂independently each stands for hydrogen, halogen or a C₁₋₄ alkoxy group or together represent a 3,4-methylenedioxy group, Rstands for C₁₋₈ alkyl, R₃represents hydrogen, C₁₋₄ alkyl or hydroxy, R₄ and R₅independently each represents hydrogen, a C₁₋₁₂ alkyl group, optionally substituted by hydroxy, or a C₂₋₁₂ alkenyl or C₃₋₆ cycloalkyl group, óóóor R₄ and R₅together with the nitrogen atom to which they are attached form a 4- to 7-membered heterocyclic ring, optionally comprising an oxygen, sulfur or a further nitrogen atom, which latter optionally may carry a phenyl, benzyl or C₁₋₄ alkyl substituent óóóand Arepresents a valency bond or a -CH₂-group, as well as stereo and optically active isomers and their mixtures, acid-addition salts and quaternary ammonium derivatives thereof. Furthermore the invention is concerned with a process for preparing these compounds as well as medicaments containing them and the use of them for preparing medicaments, particularly having ulcus and gastric-acid-secretion inhibiting and anxiolytic effects.

  本发明的一个主题是通式为 1-(苯基)-3-[ω-(氨基)-烷氧基亚氨基]-烷-1-烯衍生物 其中 R₁ 和 R₂ 各自代表氢、卤素或 C₁₋₄ 烷氧基，或共同代表 3,4-亚甲二氧基、 R 代表 C₁₋₈ 烷基、 R₃ 代表氢、C₁₋₄ 烷基或羟基、 R₄ 和 R₅ 各自独立地代表氢、任选被羟基取代的 C₁₋₁₂ 烷基或 C₂₋₁₂ 烯基或 C₃₋₆ 环烷基、 或 R₄ 和 R₅ 与它们所连接的氮原子一起形成一个 4 至 7 元杂环，可选地包括一个氧原子、硫原子或另一个氮原子，后者可选地带有一个苯基、苄基或 C₁₋₄ 烷基取代基。 和 代表价键或 -CH₂ 基团、 以及立体异构体和光学活性异构体及其混合物、酸加成盐和季铵衍生物。 此外，本发明还涉及到制备这些化合物的工艺以及含有这些化合物的药物，以及使用这些化合物制备药物，特别是具有抑制溃疡和胃酸分泌以及抗焦虑作用的药物。
• 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。