阿里可拉唑 | 63824-12-4

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 中文名称: 阿里可拉唑
• 中文别名: 阿利康唑
• 英文名称: aliconazole
• 英文别名: 1-[2-(4-chloro-phenyl)-3-(2,4-dichloro-phenyl)-allyl]-1H-imidazole；1-[(Z)-2-(4-chlorophenyl)-3-(2,4-dichlorophenyl)prop-2-enyl]imidazole
• CAS: 63824-12-4
• 化学式: C₁₈H₁₃Cl₃N₂
• 分子量: 363.674
• InChiKey: WNGFKUOERJDDIY-OQLLNIDSSA-N

物化性质

• 沸点：
  545.0±50.0 °C(Predicted)
• 密度：
  1.29±0.1 g/cm3(Predicted)
• 溶解度：
  溶于二甲基亚砜

计算性质

• 辛醇/水分配系数(LogP)：
  6
• 重原子数：
  23
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  17.8
• 氢给体数：
  0
• 氢受体数：
  1

安全信息

• 海关编码：
  2933290090

制备方法与用途

生物活性

Aliconazole 是一种抗真菌（antifungal）的咪唑衍生物。

靶点

Fungal

体内研究

Aliconazole 曾经在 III 期临床试验中用于确定其在外用治疗皮肤真菌感染方面的疗效。该药物提议用于治疗浅表性真菌感染，包括皮癣、花斑癣以及皮肤和阴道念珠菌病。

文献信息

• Enhanced propertied pharmaceuticals
  申请人：——

  公开号：US20040254182A1

  公开（公告）日：2004-12-16

  This invention relates to compounds which are useful as enhanced propertied pharmaceutical compounds for both human and veterinary application. The pharmaceutical compounds which are suitable for use in this invention are those compounds which can be substituted with a moiety, said moiety comprising a substituent which enhances or changes the properties of the pharmaceutical compound. The chemical modification of drugs into labile derivatives with enhanced physicochemical properties that enable better transport through biological barriers is a useful approach for improving-drug delivery.

  这项发明涉及一种化合物，该化合物可用作增强性质的药用化合物，适用于人类和兽医应用。适用于本发明的药用化合物是那些可以被取代为一种基团的化合物，该基团包括一种增强或改变药用化合物性质的取代基。将药物化学修饰为具有增强的物理化学性质的不稳定衍生物，从而能够更好地穿过生物屏障，这是改善药物输送的一种有用方法。
• 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。
• Pharmaceutical composition comprising a quinone derivative or a hydroquinone thereof for treating dermatitis
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP0719552A2

  公开（公告）日：1996-07-03

  To provide a pharmaceutical composition for anti-atopic dermatitis exhibiting excellent therapeutic effect against dermatitis, especially atopic dermatitis A pharmaceutical composition for dermatitis comprising as an active ingredient a quinone derivative of the formula: wherein    R1 and R2 are independently are a hydrogen atom, methyl or methoxy group, or R1 and R2 are linked together to form -CH=CH-CH=CH-;    R3 is an aliphatic, aromatic or heterocyclic group which may be substituted;    R4 is a hydrogen atom, methyl group, an optionally substituted hydroxyl group or a carboxyl group which may be esterified or amidated;    R5 is a hydrogen atom or methyl group;    Z is a group selected from the group consisting of -C≡C-, -CH=CH-,    n is an integer of 0 to 15;    m is an integer of 0 to 3; and    k is an integer of 0 to 5, provided that in the case of m being 2 or 3, Z and k can vary arbitrarily within the bracketed repeating unit, or a hydroquinone derivative thereof, or a salt thereof.

  提供一种抗特应性皮炎的药物组合物，对皮炎，尤其是特应性皮炎具有优异的治疗效果 一种治疗皮炎的药物组合物，其活性成分包括式中的醌衍生物： 其中 R1 和 R2 独立地为氢原子、甲基或甲氧基，或 R1 和 R2 连接在一起形成 -CH=CH-CH=CH- ； R3 是脂肪族、芳香族或杂环族基团，可被取代； R4 是氢原子、甲基、任选取代的羟基或可被酯化或酰胺化的羧基； R5 是氢原子或甲基； Z 是选自-C≡C-、-CH=CH-的基团、 n 是 0 至 15 的整数； m 是 0 至 3 的整数；以及 k 是 0 至 5 的整数、 但在 m 为 2 或 3 的情况下，Z 和 k 可在括号内的重复单元内任意变化，或其对苯二酚衍生物或其盐。
• 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。
• ENHANCED PROPERTIED PHARMACEUTICALS
  申请人：ROHM AND HAAS COMPANY

  公开号：EP1272463A1

  公开（公告）日：2003-01-08