羟吡溴铵 | 561-43-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 羟吡溴铵
• 中文别名: 2-异丙基-6-甲基异氰酸苯酯；2-异丙基-6-甲基苯基异氰酸酯
• 英文名称: Oxypyrronium bromide
• 英文别名: (1,1-dimethylpyrrolidin-1-ium-2-yl)methyl 2-cyclohexyl-2-hydroxy-2-phenylacetate;bromide
• CAS: 561-43-3
• 化学式: C21H32BrNO3
• 分子量: 426.4
• InChiKey: SXGOKQARVJHRML-UHFFFAOYSA-M

计算性质

• 辛醇/水分配系数(LogP)：
  0.24
• 重原子数：
  26
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  46.5
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] ANTICHOLINERGIC NEUROPROTECTIVE COMPOSITION AND METHODS<br/>[FR] COMPOSITION ET PROCÉDÉS NEUROPROTECTEURS ANTICHOLINERGIQUES
  申请人：CHASE PHARMACEUTICALS CORP

  公开号：WO2014039627A1

  公开（公告）日：2014-03-13

  The present invention relates to a pharmaceutical composition comprising propiverine, trospium or glycopyrrolate; and a non-anticholinergic antiemetic agent. It is also related to a pharmaceutical composition comprising a high dose of solifenacin or a pharmaceutically acceptable salts thereof; and a non-anticholinergic antiemetic agent. Pharmaceutical compositions containing high dose of nsPAChA for use for increasing the AChEI blood concentrations and for combating neurodegeneration are also described. The invention also relates to a method for inducing neuroprotection and combating neurodegeneration in a patient suffering from Alzheimer type dementia as well as to a method for increasing the blood levels of an acetyl choline esterase inhibitor (AChEI) in a human subject treated with an AChEI dose.

  本发明涉及一种包含丙烯胺、托斯匹铵或格隆溴铵的药物组合物；以及一种非抗胆碱能的抗恶心药物。它还涉及一种包含高剂量索利那非或其药用盐的药物组合物；以及一种非抗胆碱能的抗恶心药物。还描述了含有高剂量nsPAChA的药物组合物，用于增加AChEI血浓度并对抗神经退行性疾病。该发明还涉及一种诱导神经保护和对抗神经退行性疾病的方法，适用于患有阿尔茨海默型痴呆症的患者，以及一种用于增加接受AChEI剂量治疗的人体受试者的乙酰胆碱酯酶抑制剂（AChEI）血液水平的方法。
• 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。
• Synthesis of optically active cyclohexylphenylglycolate esters
  申请人：Sepracor, Inc.

  公开号：EP1424321A1

  公开（公告）日：2004-06-02

  A process for the preparation of optically active cyclohexylglycolate esters is described. The process utilizes carboxylic acid activation to couple (R)- or (S)-cyclohexylphenylglycolic acid (CHPGA) with 4-N,N-diethylamino butynol or other propargyl alcohol derivatives. The preparation of the hydrochloride salt is also described.

  本发明描述了一种制备光学活性环己基乙醇酸酯的工艺。该工艺利用羧酸活化作用将(R)-或(S)-环己基苯基乙醇酸（CHPGA）与 4-N,N-二乙氨基丁炔醇或其他丙炔醇衍生物偶联。此外，还介绍了盐酸盐的制备方法。
• Optically active cyclohexylphenylglycolate esters
  申请人：SEPRACOR Inc

  公开号：EP1642883A2

  公开（公告）日：2006-04-05

  The invention concerns intermediates of formula or wherein R5 is alkyl or alkenyl of one to ten carbons. Preferably, R5 is isobutyl.

  本发明涉及式 或 其中 R5 是一至十个碳原子的烷基或烯基。R5 最好是异丁基。
• COMBINATION OF A NSPACHA (PERIPHERAL ANTICHOLINERGIC AGENT) LIKE SOLIFENACIN AND AN ACHEI (ACETYL CHOLINE ESTERASE INHIBITOR) LIKE DONEPEZIL FOR TREATING DEMENTIA
  申请人：Chase Pharmaceuticals Corporation

  公开号：EP3178477A1

  公开（公告）日：2017-06-14

  There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-selective, peripheral anticholinergic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent. The use of a non-selective, peripheral anticholinergic agent (nsPAChA) for the preparation of a pharmaceutical composition for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia and pharmaceutical compositions comprising a non-selective peripheral anticholinergic agent of formula II as illustrated in the description and an acetylcholine esterase inhibitor are also described.

  本文描述了一种方法，通过将乙酰胆碱酯酶抑制剂（AChEI）与一种非选择性外周抗胆碱能药物联合使用，降低伴随的不良反应，从而提高乙酰胆碱酯酶抑制剂（AChEI）在阿尔茨海默型痴呆患者中的最大耐受剂量，进而提高其疗效、外周抗胆碱能药物，从而增强对患者中枢神经系统中乙酰胆碱酯酶的抑制作用，并在更大程度上缓解患者的阿尔茨海默型痴呆症状。此外，还描述了使用非选择性外周抗胆碱能剂（nsPAChA）制备药物组合物，以提高最大耐受剂量，从而提高乙酰胆碱酯酶抑制剂（AChEI）在阿尔茨海默型痴呆症患者中的疗效，以及包含描述中所示式 II 的非选择性外周抗胆碱能剂和乙酰胆碱酯酶抑制剂的药物组合物。