羟甲基-7-氨基头孢烷酸 | 6109-70-2

• 物质功能分类: 原料药 - 抗生素类药物 - 头孢菌素类药
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 奎宁环
• 中文名称: 羟甲基-7-氨基头孢烷酸
• 中文别名: 盐酸醋克利定
• 英文名称: 1-Azabicyclo[2.2.2]octan-3-yl acetate;hydron;chloride
• CAS: 6109-70-2
• 化学式: C9H16ClNO2
• mdl: MFCD00136230
• 分子量: 205.68
• InChiKey: LWWSARSTZGNKGV-UHFFFAOYSA-N

物化性质

• 熔点：
  166°C
• 溶解度：
  H2O：在 60°C 时≥15mg/mL

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.888
• 拓扑面积：
  29.5
• 氢给体数：
  1
• 氢受体数：
  3

制备方法与用途

乙酰胆碱是一种天然拟胆碱生物碱，类似于槟榔碱的合成物。作为一种胆碱能受体的激动剂，乙酰胆碱在青光眼中具有降低眼压的治疗作用，并且它还是一种抗胆碱酯酶活性较弱的副交感神经病理模拟药物。

文献信息

• Theranostics platform and methods of use
  申请人：Sanford Burnham Prebys Medical Discovery Institute

  公开号：US10161929B2

  公开（公告）日：2018-12-25

  Theranostics platforms for identifying drugs and nutraceuticals for treatment of rare disease are described. The platforms comprise (a) a cell-phenotype image-enhancing instrument; (b) a drug/nutraceutical library; and (c) a computer-implemented system for analyzing a response of an optically-visible rare-disease cell phenotype to a drug or nutraceutical from the drug/nutraceutical library.

  本文描述了用于识别治疗罕见病的药物和营养保健品的血清学平台。这些平台包括：(a) 细胞表型图像增强仪器；(b) 药物/营养保健品库；(c) 计算机实施系统，用于分析光学可视罕见疾病细胞表型对药物/营养保健品库中药物或营养保健品的反应。
• Directed differentiation of oligodendrocyte precursor cells to a myelinating cell fate
  申请人：The Scripps Research Institute

  公开号：US10660899B2

  公开（公告）日：2020-05-26

  The present invention provides methods of inducing differentiation of oligodendrocyte progenitor cells to a mature myelinating cell fate with a neurotransmitter receptor modulating agent. The present invention also provides methods of stimulating increased myelination in a subject in need thereof by administering said neurotransmitter receptor modulating agent. Methods of treating a subject having a demyelinating disease using a neurotransmitter receptor modulating agent are also provided.

  本发明提供了用神经递质受体调节剂诱导少突胶质祖细胞向成熟髓鞘细胞命运分化的方法。本发明还提供了通过施用所述神经递质受体调节剂刺激有需要的受试者增加髓鞘化的方法。本发明还提供了使用神经递质受体调节剂治疗脱髓鞘疾病的方法。
• Compositions and methods for the treatment of presbyopia
  申请人：Presbyopia Therapies, LLC

  公开号：US10959990B2

  公开（公告）日：2021-03-30

  The invention provides compositions and methods for the treatment of presbyopia. The compositions comprise aceclidine hydrochloride, polysorbate 80, mannitol, anhydrous hypromellose, disodium edetate dihydrate, benzalkonium chloride, sorbic acid and anhydrous sodium citrate and optionally tropicamide.

  本发明提供了治疗老花眼的组合物和方法。这些组合物包括盐酸阿西环定、聚山梨醇酯 80、甘露醇、无水低聚果糖、二水依地酸二钠、苯扎氯铵、山梨酸和无水柠檬酸钠以及可选的托吡卡胺。
• Methods and compositions for treatment of presbyopia, mydriasis, and other ocular disorders
  申请人：Ocuphire Pharma, Inc.

  公开号：US10993932B2

  公开（公告）日：2021-05-04

  The invention provides methods, compositions, and kits containing an alpha-adrenergic antagonist, such as phentolamine, for use in monotherapy or as part of a combination therapy to treat patients suffering from presbyopia, mydriasis, and/or other ocular disorders.

  本发明提供了含有α-肾上腺素能拮抗剂（如酚妥拉明）的方法、组合物和试剂盒，用于单药治疗或作为联合疗法的一部分，治疗患有老花眼、近视和/或其他眼部疾病的患者。
• Prodrugs of quinuclidine ring-containing muscarinic agonists and compositions and methods thereof
  申请人：Lenz Therapeutics, Inc.

  公开号：US11214569B2

  公开（公告）日：2022-01-04

  The present invention is directed to compounds of the formula and salts or esters thereof. The present invention is further directed to ophthalmological compositions comprising a therapeutically effective amount of a compound of the present invention and one or more pharmaceutically acceptable excipients. The present invention is further directed to a methods of treating presbyopia or glaucoma or reducing hyperemia comprising administering to a patient in need thereof a therapeutically effective amount of a compound of the present invention.

  本发明涉及式如下的化合物 及其盐或酯。本发明进一步涉及眼科组合物，其包含治疗有效量的本发明化合物和一种或多种药学上可接受的赋形剂。本发明进一步涉及一种治疗老花眼或青光眼或减少高眼压症的方法，包括向有需要的患者施用治疗有效量的本发明化合物。