喹乙唑胺 | 77197-48-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 中文名称: 喹乙唑胺
• 中文别名: 喹唑米得
• 英文名称: 1-acetamino-5-methylpyrazolo[1,5-c]quinazoline
• 英文别名: Quinezamide；N-(5-methylpyrazolo[1,5-c]quinazolin-1-yl)acetamide
• CAS: 77197-48-9
• 化学式: C₁₃H₁₂N₄O
• 分子量: 240.264
• InChiKey: JTIDKHDQCMBOEG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  59.3
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  1-amino-5-methylpyrazolo[1,5-c]quinazoline 在 乙酸酐 作用下， 以89%的产率得到喹乙唑胺
  参考文献：
  名称：

  Pyrazolo[1,5-c]quinazoline derivatives and analgesic compositions

  摘要：

  该发明涉及一种新型的吡唑并[1,5-c]喹唑啉衍生物，其通式为I，其中R代表氢原子，C.sub.1-4烷基或酰基，R.sub.1代表氢原子，C.sub.1-12烷基，C.sub.3-8环烷基，C.sub.2-4烯基，芳基烷基，其中烷基含有1至4个碳原子，苯基烯基，其中烯基含有2至4个碳原子，此外还是一个羧基或者一个苯基，该苯基可以选择一个或多个卤素、羟基、C.sub.1-4烷氧基、硝基或二(C.sub.1-4烷基)氨基等取代基，或者R和R.sub.1可能共同形成一个价键，R.sub.2代表氢原子，C.sub.1-4烷基或苯基，或者R.sub.1和R.sub.2可能共同形成一个C.sub.2-7烷基烯基，R.sub.3代表硝基，氨基，烷基氨基，二烷基氨基，其中烷基含有1至4个碳原子，烷基亚胺基，其中烷基亚胺基含有1至4个碳原子，苯甲亚胺基或酰氨基，以及其药学上可接受的酸盐。通式I的新化合物主要可用作镇痛剂。

  公开号：

  US04303660A1

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。
• 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。
• LYOPHILIZATION PROCESS AND PRODUCTS OBTAINED THEREBY
  申请人：Scidose, Llc

  公开号：EP1954244A1

  公开（公告）日：2008-08-13
• CONTROLLED ABSORPTION WATER-SOLUBLE PHARMACEUTICALLY ACTIVE ORGANIC COMPOUND FORMULATION FOR ONCE-DAILY ADMINISTRATION
  申请人：STI Pharma, LLC

  公开号：EP2717860A1

  公开（公告）日：2014-04-16
• Methods and devices for the treatment of ocular conditions
  申请人：deJuan Eugene

  公开号：US20060110428A1

  公开（公告）日：2006-05-25

  Featured is a method for instilling one or more bioactive agents into ocular tissue within an eye of a patient for the treatment of an ocular condition, the method comprising concurrently using at least two of the following bioactive agent delivery methods (A)-(C): (A) implanting a sustained release delivery device comprising one or more bioactive agents in a posterior region of the eye so that it delivers the one or more bioactive agents into the vitreous humor of the eye; (B) instilling (e.g., injecting or implanting) one or more bioactive agents subretinally; and (C) instilling (e.g., injecting or delivering by ocular iontophoresis) one or more bioactive agents into the vitreous humor of the eye.