(R)-(5-ethenyl-1-azabicyclo[2.2.2]octan-2-yl)-(6-methoxyquinolin-4-yl)methanol;hydrochloride

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 金鸡纳生物碱
• 英文名称: (R)-(5-ethenyl-1-azabicyclo[2.2.2]octan-2-yl)-(6-methoxyquinolin-4-yl)methanol;hydrochloride
• 化学式: C20H25ClN2O2
• 分子量: 360.9
• InChiKey: LBSFSRMTJJPTCW-CYAVNPPASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  25
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  45.6
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• METHODS AND COMPOSITIONS FOR TREATING INFECTION
  申请人：UNIVERSITY OF ROCHESTER

  公开号：US20150238473A1

  公开（公告）日：2015-08-27

  Provided herein are compositions and methods for treating or preventing infection.

  本文提供了用于治疗或预防感染的组合物和方法。
• Pharmaceutical composition
  申请人：LEJUS MEDICAL AKTIEBOLAG

  公开号：EP0148811A1

  公开（公告）日：1985-07-17

  The present invention relates to a new oral pharmaceutical composition having an improved release of therapeutically active compound present, in the lower part of the gastro-intestinal duct having a pH exceeding 4.5, whereby the composition comprises a core comprising a therapeutically active compound in the form of a weak base, or a weak acid, on which core there is applied a first, inner layer of a diffusion membrane in the form of ethyl cellulose, and/or a copolymer of polyethyl methacrylate-methyl methacrylate-trimethylammonium ethyl methacrylate chloride, and thereabove a second layer is applied of at least one anionic polymer and/or fatty acid having a pka of 4.5 to 7. The invention further relates to a process for the preparation of said composition, a pharmaceutical composition containing said composition, and a method for the treatment using such a composition.

  本发明涉及一种新的口服药物组合物，该组合物在胃肠道下部pH值超过4.5，其中该组合物包括一个由弱碱或弱酸形式的治疗活性化合物组成的核心，在该核心上涂敷有第一层内层扩散膜，其形式为乙基纤维素和/或聚甲基丙烯酸甲酯-甲基丙烯酸甲酯-甲基丙烯酸乙基氯酯三甲基铵的共聚物，在其上涂敷有第二层至少一种阴离子聚合物和/或pka为4.5至7的脂肪酸。 本发明还涉及一种制备上述组合物的工艺、一种含有上述组合物的药物组合物以及一种使用这种组合物进行治疗的方法。
• Method for the manufacture of drug permeable materials
  申请人：Dow Corning Kabushiki Kaisha

  公开号：EP0326278A1

  公开（公告）日：1989-08-02

  In the present invention, a mixture of a curable silicone rubber and a hydrous polyvinyl alcohol (hereafter "hydrous PVA"), is subjected to a treatment which cures the silicone rubber and causes low temperature (ie, below -5°C) gelation of the hydrous PVA. The resultant permeable materials are used to manufacture drug delivery systems, which systems may be of the transdermal drug delivery type or of a type which is implanted either subcutaneously or in a body cavity.

  在本发明中，将可固化硅橡胶和含水聚乙烯醇（以下简称 "含水 PVA"）的混合物进行处理，使硅橡胶固化，并使含水 PVA 低温（即低于 -5°C）凝胶化。由此产生的可渗透材料可用于制造给药系统，这种系统可以是透皮给药型的，也可以是皮下或体腔植入型的。
• Skin penetration system for salts of amine-functional drugs
  申请人：THE PROCTER & GAMBLE COMPANY

  公开号：EP0351897A2

  公开（公告）日：1990-01-24

  The invention involves pharmaceutical compositions for topical application comprising: (a) a pharmaceutically-acceptable salt of addition of an amine-functional drug (other than opioid analgesic drugs); (b) a C₇ to C₂₂ straight-chain or branched-chain, saturated or unsaturated, fatty acid having a melting point of less than about 50°C; and (c) a C₃-C₄ alkane diol.

  本发明涉及用于局部应用的药物组合物，包括 (a) 一种胺功能药物（阿片类镇痛药除外）的药学上可接受的加成盐； (b) C₇ 至 C₂₂ 直链或支链、饱和或不饱和脂肪酸，熔点低于约 50°C；以及 (c) C₃-C₄ 烷二醇。
• AMORPHOUS COMPOSITION
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP1829549A1

  公开（公告）日：2007-09-05

  To provide an amorphous composition for nasal administration or for administration by adhering to oral mucosa in which absorption property and chemical and physical stabilities of (2R)-N-(1-benzylpiperidin-4-yl)-3-cyclohexylmethylthio-2-[(4R)-3-tert-butoxycarbonylthiazolidin-4-ylcarbonylamino]propanamide which is useful as an N type calcium channel inhibitor are improved. A preparation comprising the amorphous composition of the present invention has been found to be excellent in physical stability and chemical stability and to be useful as a nasal preparation or a preparation for adhering to the oral mucosa. As a result, the resulting preparation has a high BA value and is useful for prevention and/or the treatment of a disease mediated by the N type calcium channel including pain (such as neuropathic pain, cancerous pain, intractable pain, postoperative pain, acute pain, chronic pain, neuralgia and infectious pain).

  提供一种用于鼻腔给药或粘附在口腔粘膜上给药的无定形组合物，该组合物改善了作为 N 型钙通道抑制剂的 (2R)-N-(1-苄基哌啶-4-基)-3-环己基甲基硫-2-[(4R)-3-叔丁氧羰基噻唑烷-4-基羰基氨基]丙酰胺的吸收性能和化学及物理稳定性。 研究发现，包含本发明无定形组合物的制剂具有优异的物理稳定性和化学稳定性，可用作鼻腔制剂或粘附在口腔粘膜上的制剂。因此，本发明制剂具有很高的 BA 值，可用于预防和/或治疗由 N 型钙通道介导的疾病，包括疼痛（如神经性疼痛、癌痛、难治性疼痛、术后疼痛、急性疼痛、慢性疼痛、神经痛和感染性疼痛）。