奥达匹泮 | 131796-63-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 中文名称: 奥达匹泮
• 英文名称: Odapipam
• 英文别名: (5S)-8-chloro-5-(2,3-dihydro-1-benzofuran-7-yl)-3-methyl-1,2,4,5-tetrahydro-3-benzazepin-7-ol
• CAS: 131796-63-9
• 化学式: C₁₉H₂₀ClNO₂
• 分子量: 329.8
• InChiKey: SKMVRXPBCSTNKE-MRXNPFEDSA-N

物化性质

• 沸点：
  460.4±45.0 °C(Predicted)
• 密度：
  1.269
• 溶解度：
  溶于二甲基亚砜

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  23
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  32.7
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 海关编码：
  2934999090

反应信息

• 作为反应物：
  描述：

  奥达匹泮 以76的产率得到
  参考文献：
  名称：

  Novel benzazepine derivatives

  摘要：

  这段文字是关于化合物的描述，化合物的名称为2,3,4,5-四氢-1H-3-苯并氮平，其化学式为 ##STR1## 其中R.sup.3代表氢，C.sub.1-3-烷基或C.sub.3-7-环烷基；R.sup.4代表氢或R.sup.4与R.sup.10一起代表桥，连接R.sup.4和R.sup.10连接的位置，该桥为--CH.sub.2--CH.sub.2--, --CH.dbd.CH--, --O--CH.sub.2--或--S--CH.sub.2--; R.sup.7代表羟基，较低的烷氧基；R.sup.10，R.sup.11，R.sup.12独立地代表氢，卤素，烷基，烷氧基或三氟甲基，或R.sup.10与R.sup.4一起代表如上所述的桥；或R.sup.10与R.sup.11一起代表桥，或R.sup.11与R.sup.12一起代表桥，在这两种情况下，桥被选择在--O--CH.sub.2--CH.sub.2--, --O--CH.sub.2--CH.sub.2--CH.sub.2--, --O-CH.dbd.CH--, --CH.sub.2-CH.sub.2-CH.sub.2--, --CH.sub.2-CH.dbd.CH--或--CH.sub.2--CH.sub.2--CH.sub.2--CH.sub.2--之间；R.sup.13代表氢，卤素或较低的烷基。这些化合物在治疗中枢神经系统疾病的制剂中有用。

  公开号：

  US05010074A1
• 作为产物：
  描述：

  生成 奥达匹泮
  参考文献：
  名称：

  2,3,4,5-tetrahydro-1H-3-benzazepines and CNS affecting use thereof

  摘要：

  这段话的中文翻译如下：具有噻吩基、呋喃基、吡啶基或由苯基与苯、环己烷、环己烯、环戊烷或环戊烯环组成、其中一个碳原子可被氧、硫或氮取代的五位苯并环2,3,4,5-四氢-1H-3-苯并嗪类化合物，具有有趣的中枢神经系统和心血管效应。

  公开号：

  US04751222A1

文献信息

• Microparticles With Modified Release of At Least One Active Principle and Oral Pharmaceutical Form Comprising Same
  申请人：Dargelas Frederic

  公开号：US20090220611A1

  公开（公告）日：2009-09-03

  The invention concerns microparticulate systems with modified release of oral active principle(s). The invention aims at providing a novel pharmaceutical with time-dependent and pH-dependent release mechanism, enabling: a) the latent period preceding the release of the active principle in the stomach; b) the pH triggering the release of the active principle in the intestine; c) the release speed of the active principle. This is achieved through the use of coated microparticles made from particles of active principle each coated with two coating films A and B. A comprises: film-forming (co)polymer (A1) insoluble in fluids of the gastrointestinal tract; ethylcellulose (co)polymer (A2) soluble in fluids of the gastrointestinal tract; plasticizing polyvinylpyrrolidone (A3); castor oil/optionally a surfactant and/or magnesium stearate lubricant (A4). B comprises a hydrophilic polymer (B1) bearing ionized groups with neutral pH (EUDRAGIT® L100-55) and a hydrophobic compound (B2) (LUBRITAB®). The invention also concerns medicines based on said microparticles.

  该发明涉及具有口服活性原理改性释放的微粒系统。该发明旨在提供一种具有时间依赖性和pH依赖性释放机制的新型药物，实现：a）在胃中释放活性原理之前的潜伏期；b）在肠道中触发释放活性原理的pH值；c）活性原理的释放速度。这是通过使用由活性原理颗粒制成的被包覆的微粒来实现的，每个微粒都涂有两层涂膜A和B。A包括：在胃肠道液体中不溶解的成膜（共）聚合物（A1）；在胃肠道液体中可溶解的乙基纤维素（共）聚合物（A2）；增塑剂聚乙烯吡咯烷酮（A3）；蓖麻油/可选的表面活性剂和/或硬脂酸镁润滑剂（A4）。B包括具有中性pH的离子化基团的亲水性聚合物（B1）（EUDRAGIT® L100-55）和疏水化合物（B2）（LUBRITAB®）。该发明还涉及基于这些微粒的药物。
• Gastric retention controlled drug delivery system
  申请人：Sun Pharma Advanced Research Company Ltd

  公开号：EP2238975A1

  公开（公告）日：2010-10-13

  The present invention provides a gastric retention controlled drug delivery system comprising: (a) a controlled release core comprising a drug, a highly swellable polymer and a gas generating agent, said core being capable of swelling and achieving floatation rapidly while maintaining its physical integrity in gastrointestinal fluids for prolonged periods, and (b) a rapidly releasing coat composition comprising the same drug as in the core and pharmaceutically acceptable excipients, wherein the coating composition surrounds the core such that the system provides a biphasic release of the drug in gastrointestinal fluids.

  本发明提供了一种胃滞留控释给药系统，包括：(a) 由药物、高溶胀性聚合物和气体发生剂组成的控释核心，所述核心能够快速溶胀并实现漂浮，同时在胃肠液中长时间保持其物理完整性；(b) 由与核心中相同的药物和药学上可接受的赋形剂组成的快速释放包衣组合物，其中包衣组合物包围核心，从而使该系统在胃肠液中实现药物的双相释放。
• Compostions and methods for treating chemosensory dysfunction
  申请人：CYRANO THERAPEUTICS, INC.

  公开号：US10206927B2

  公开（公告）日：2019-02-19

  The invention is directed to a method of detecting a biological substance in the nasal secretion and diagnosing a disease following the detection of the biological substance wherein the biological substance is not related to a respiratory disease. The invention also provides treatment of the diseases following the detection of the biological substance and/or diagnosis of the disease. In some embodiments, the diseases are cancer, hepatitis, smell loss, taste loss, diabetes, and leprosy. The invention also provides a kit for diagnosing a disease. The present invention includes methods of analyzing samples from the nose for the detection of biological substances. In particular, nasal secretion or nasal mucus is collected and analyzed for biological substances. The results of this analysis are then suitable for use in diagnosis, prognosis, and determination of suitability of therapeutic interventions.

  本发明涉及一种检测鼻腔分泌物中生物物质的方法，以及在检测到生物物质后诊断疾病的方法，其中生物物质与呼吸道疾病无关。本发明还提供了在检测到生物物质和/或诊断出疾病后的疾病治疗方法。在某些实施例中，疾病是癌症、肝炎、嗅觉减退、味觉减退、糖尿病和麻风病。本发明还提供了一种用于诊断疾病的试剂盒。本发明包括分析鼻腔样本以检测生物物质的方法。特别是，收集鼻分泌物或鼻涕并分析其中的生物物质。分析结果适用于诊断、预后和确定治疗干预的适宜性。
• 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 treating chemosensory dysfunction
  申请人：Cyrano Therapeutics, Inc.

  公开号：US11389453B2

  公开（公告）日：2022-07-19

  The invention is directed to a method of detecting a biological substance in the nasal secretion and diagnosing a disease following the detection of the biological substance wherein the biological substance is not related to a respiratory disease. The invention also provides treatment of the diseases following the detection of the biological substance and/or diagnosis of the disease. In some embodiments, the diseases are cancer, hepatitis, smell loss, taste loss, diabetes, and leprosy. The invention also provides a kit for diagnosing a disease. The present invention includes methods of analyzing samples from the nose for the detection of biological substances. In particular, nasal secretion or nasal mucus is collected and analyzed for biological substances. The results of this analysis are then suitable for use in diagnosis, prognosis, and determination of suitability of therapeutic interventions.

  本发明涉及一种检测鼻腔分泌物中生物物质的方法，以及在检测到生物物质后诊断疾病的方法，其中生物物质与呼吸道疾病无关。本发明还提供了在检测到生物物质和/或诊断出疾病后的疾病治疗方法。在某些实施例中，疾病是癌症、肝炎、嗅觉减退、味觉减退、糖尿病和麻风病。本发明还提供了一种用于诊断疾病的试剂盒。 本发明包括分析鼻腔样本以检测生物物质的方法。特别是，收集鼻分泌物或鼻涕并分析其中的生物物质。分析结果适用于诊断、预后和确定治疗干预的适宜性。