匹克洛尼定 | 72467-44-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 匹克洛尼定
• 中文别名: 吡可乐定
• 英文名称: 2--2-imidazoline
• 英文别名: 2-[N-2,6-dichlorophenyl-N-(2-tetrahydropyranyl)amino]-imidazoline；Piclonidine；N-(2,6-dichlorophenyl)-N-(oxan-2-yl)-4,5-dihydro-1H-imidazol-2-amine
• CAS: 72467-44-8
• 化学式: C₁₄H₁₇Cl₂N₃O
• 分子量: 314.214
• InChiKey: NYQGJEQCYOJBPV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  36.9
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• 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。
• Treatment of length dependent neuropathy
  申请人：Arcion Therapeutics, Inc.

  公开号：EP2343068A2

  公开（公告）日：2011-07-13

  Compositions, and methods of use thereof, are provided for the treatment of painful neuropathy by local or topical delivery of compounds that interact with α-adrenergic receptors, especially an alpha2 adrenergic agonist such as clonidine, to the entire painful area such that the need for systemic dosing is minimized. The compounds are delivered to or adjacent to painful areas in patients with painful length dependent neuropathy, and other neuropathies that affect the pain signaling fibers in the skin. A preferred compound for the treatment of patients with length dependent neuropathy is clonidine applied in a transdermal patch, gel, ointment, lotion, liposomal formulation, cream, or emulsion, wherein the concentration is sufficient to provide an effective dose in the painful area or immediately adjacent areas.

  本发明提供了用于治疗疼痛性神经病变的组合物及其使用方法，方法是将与α-肾上腺素能受体相互作用的化合物，特别是α2肾上腺素能激动剂（如氯尼丁）局部或局部递送至整个疼痛区域，从而最大限度地减少全身给药的需要。对于患有疼痛性长度依赖性神经病变和其他影响皮肤疼痛信号纤维的神经病变的患者，可将化合物输送到疼痛部位或疼痛部位附近。用于治疗长度依赖性神经病患者的一种优选化合物是以透皮贴剂、凝胶、软膏、乳液、脂质体制剂、霜剂或乳剂形式使用的氯尼丁，其中的浓度足以在疼痛部位或邻近部位提供有效剂量。
• 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。
• Compositions and methods for on-demand high-efficiency triggerable anesthesia
  申请人：The Children's Medical Center Corporation

  公开号：US11344498B2

  公开（公告）日：2022-05-31

  Compositions and methods for administration of local anesthetics that are delivered by a single injection and enable repeated on-demand or high influx analgesia over extended periods have been developed. Pharmaceutical compositions including an effective amount of one or more sodium channel blockers including site 1 sodium channel blockers, optionally one or more alpha-2-adrenergic agonists, which are optionally encapsulated in liposomes, particles or microbubbles, and one or more triggerable elements are provided. The triggerable elements allow delivery of the encapsulated anesthetic drugs when an appropriate triggering stimuli are applied. Exemplary triggering agents or stimuli include near-infrared irradiation, UV- and visible light, ultrasound and magnetic field. In one embodiment, ultrasound is used to trigger a burst of microbubbles to enhance penetration of local anesthetic.

  目前已开发出通过单次注射提供局部麻醉剂的组合物和方法，可在较长时间内重复按需或高流量镇痛。提供的药物组合物包括有效量的一种或多种钠通道阻滞剂（包括位点 1 钠通道阻滞剂）、可选的一种或多种α-2-肾上腺素能激动剂（可选地封装在脂质体、颗粒或微气泡中）以及一种或多种可触发元件。当施加适当的触发刺激时，可触发元件可输送封装的麻醉药物。示例性触发剂或刺激物包括近红外照射、紫外线和可见光、超声波和磁场。在一个实施方案中，超声波用于触发微气泡的爆发，以增强局部麻醉剂的渗透。
• EP0573581A4
  申请人：——

  公开号：EP0573581A4

  公开（公告）日：1994-06-29