8,9,10,11,11a,12-六氢-8,10-二甲基-7ah-萘并[1',2':5,6]吡喃并[3,2-c]吡啶-7alpha-醇 | 22292-91-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 萘并吡喃类
• 中文名称: 8,9,10,11,11a,12-六氢-8,10-二甲基-7ah-萘并[1',2':5,6]吡喃并[3,2-c]吡啶-7alpha-醇
• 中文别名: 萘拉诺
• 英文名称: naranol
• 英文别名: 13,15-dimethyl-11-oxa-15-azatetracyclo[8.8.0.02,7.012,17]octadeca-1(10),2,4,6,8-pentaen-12-ol
• CAS: 22292-91-7
• 化学式: C₁₈H₂₁NO₂
• 分子量: 283.37
• InChiKey: RQYOELZDSAMKIU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  21
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  32.7
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• [EN] SUBSTITUTED PYRAZINONE DERIVATIVES FOR USE AS A MEDICINE<br/>[FR] DÉRIVÉS DE PYRAZINONE SUBSTITUÉS À UTILISER COMME MÉDICAMENT
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2007135131A1

  公开（公告）日：2007-11-29

  (EN) 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 &agr;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 usefull 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.(FR) La présente invention concerne des dérivés de pyrazinone substitués selon la formule générale (I), un sel d'addition acide ou basique pharmaceutiquement acceptable de ceux-ci, une forme stéréochimiquement isomère de ceux-ci, une forme N-oxyde de ceux-ci ou un sel d'ammonium quaternaire de ceux-ci, les variables étant définies dans la revendication 1, ayant une activité d'antagoniste de récepteur adrénergique α2C sélective. L'invention concerne en outre leur préparation, les compositions les contenant et leur utilisation comme médicament. Les composés selon l'invention sont utiles pour la prévention et/ou le traitement des troubles du système nerveux central, les troubles de l'humeur, les troubles de l'anxiété, les troubles liés au stress associés à la dépression et/ou à l'anxiété, les troubles cognitifs, les troubles de la personnalité, les troubles schizo-affectifs, la maladie de Parkinson, les démences du type Alzheimer, les conditions de douleur chronique, les maladies neurodégénératives, les troubles de l'addiction, les troubles de l'humeur et les dysfonctionnements sexuels.

  本发明涉及根据一般公式（I）的取代吡嗪酮衍生物，其具有药学上可接受的酸或碱盐、立体化异构体、N-氧化物形式或季铵盐形式，其中变量在权利要求1中定义，具有选择性α2C-肾上腺素受体拮抗活性。它还涉及它们的制备、包含它们的组合物以及它们作为药物的用途。根据本发明的化合物对于预防和/或治疗中枢神经系统障碍、情绪障碍、焦虑障碍、与抑郁和/或焦虑相关的应激障碍、认知障碍、人格障碍、分裂情感障碍、帕金森病、阿尔茨海默型痴呆、慢性疼痛症状、神经退行性疾病、成瘾障碍、情绪障碍和性功能障碍方面是有用的。
• 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。
• 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。