环丙三氟拉嗪 | 17692-26-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻嗪类
• 中文名称: 环丙三氟拉嗪
• 中文别名: 环丙奋乃静
• 英文名称: 10-<3-(4-Cyclopropylpiperazino)-propyl>-2-trifluormethylphenthiazin
• 英文别名: 10-[3-(4-cyclopropyl-piperazin-1-yl)-propyl]-2-trifluoromethyl-10H-phenothiazine；Cyclophenazine；10-[3-(4-cyclopropylpiperazin-1-yl)propyl]-2-(trifluoromethyl)phenothiazine
• CAS: 17692-26-1
• 化学式: C₂₃H₂₆F₃N₃S
• 分子量: 433.541
• InChiKey: NPYDSZQCCSLZPP-UHFFFAOYSA-N

物化性质

• 沸点：
  536.6±50.0 °C(Predicted)
• 密度：
  1.291±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  5.6
• 重原子数：
  30
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  35
• 氢给体数：
  0
• 氢受体数：
  7

安全信息

• 海关编码：
  2934300000

文献信息

• METHODS OF TREATING FRAGILE X SYNDROME, DOWN'S SYNDROME, AUTISM AND RELATED DISORDERS
  申请人：Wustrow David J.

  公开号：US20120016021A1

  公开（公告）日：2012-01-19

  Disclosed herein are methods of treating fragile X syndrome, fragile X-associated tremor/ataxia syndrome, Down's syndrome and other forms of mental retardation, and/or autism comprising administering a GABA B agonist prodrug to a subject suffering therefrom. The GABA B agonist prodrugs can be compounds of Formula (I), (II) or (III) as disclosed herein.

  本文披露了治疗脆性X综合症、脆性X相关性震颤/共济失调综合症、唐氏综合症和其他形式智力障碍和/或自闭症的方法，包括向患者施用GABAB受体激动剂前药。GABAB受体激动剂前药可以是公式(I)、(II)或(III)中所披露的化合物。
• 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。
• 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。
• SUBSTITUTED PYRAZINONE DERIVATIVES FOR USE AS A MEDICINE
  申请人：Andrés-Gil José Ignacio

  公开号：US20100105694A1

  公开（公告）日：2010-04-29

  The present invention concerns substituted pyrazinone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in claim 1 , having selective 2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.

  本发明涉及通式（I）的取代吡唑酮衍生物，其为药学上可接受的酸性或碱性盐、立体化学异构体形式、N-氧化物形式或季铵盐，其中变量在权利要求1中定义，具有选择性2C-肾上腺素受体拮抗剂活性。本发明还涉及它们的制备、包含它们的组合物及其用作药物。根据本发明的化合物对于预防和/或治疗中枢神经系统疾病、情绪障碍、焦虑症、与抑郁和/或焦虑有关的应激相关障碍、认知障碍、人格障碍、情感性精神病、帕金森病、阿尔茨海默病型痴呆、慢性疼痛症状、神经退行性疾病、成瘾障碍、情感障碍和性功能障碍方面具有用处。
• 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。