(S)-quinuclidin-3-yl 1-(4-bromophenyl)cyclopropylcarbamate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 奎宁环
• 英文名称: (S)-quinuclidin-3-yl 1-(4-bromophenyl)cyclopropylcarbamate
• 英文别名: [(3S)-1-azabicyclo[2.2.2]octan-3-yl] N-[1-(4-bromophenyl)cyclopropyl]carbamate
• 化学式: C₁₇H₂₁BrN₂O₂
• 分子量: 365.3
• InChiKey: VQGHWWJDOZXTNL-OAHLLOKOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  22
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.59
• 拓扑面积：
  41.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (S)-quinuclidin-3-yl 1-(4-bromophenyl)cyclopropylcarbamate 、 2,4-二氟苯硼酸 在 醋酸钯 作用下， 以gave the title compound as a tan solid (0.111 g, 23%)的产率得到(S)-1-azabicyclo[2.2.2]oct-3-yl [1-(2',4'-difluorobiphenyl-4-yl)cyclopropyl]carbamate
  参考文献：
  名称：

  GLUCOSYLCERAMIDE SYNTHASE INHIBITORS

  摘要：

  该发明涉及对葡萄糖酰胺合成酶（GCS）的抑制剂，可用于治疗代谢性疾病，如溶酶体贮存病，单独使用或与酶替代疗法联合使用，以及用于治疗癌症。

  公开号：

  US20160207933A1

文献信息

• [EN] METHODS FOR TREATING PROTEINOPATHIES<br/>[FR] PROCÉDÉS DE TRAITEMENT DE PROTÉINOPATHIES
  申请人：GENZYME CORP

  公开号：WO2016145046A1

  公开（公告）日：2016-09-15

  This disclosure relates to a method of treating a proteinopathy in a subject, the method comprising administering to the subject an effective amount of a quinuclidine compound. The disclosure also relates to a method of reducing, reversing or preventing the accumulation of protein aggregates in tissue of a subject diagnosed as having a proteinopathy, or being at risk of developing a proteinopathy, the method comprising administering to the subject an effective amount of a quinuclidine compound. Also disclosed is a pharmaceutical composition comprising a quinuclidine compound for use in said methods. The proteinopathy may be a synucleinopathy or a tauopathy, such as Parkinson's disease, Alzheimer's disease or dementia with Lewy bodies.

  这份披露涉及一种治疗受试者蛋白病的方法，该方法包括向受试者施用有效量的环丙胺化合物。该披露还涉及一种减少、逆转或预防被诊断为患有蛋白病或有患蛋白病风险的受试者组织中蛋白聚集物积累的方法，该方法包括向受试者施用有效量的环丙胺化合物。还披露了一种包含环丙胺化合物的药物组合物，用于上述方法。蛋白病可能是突触核蛋白病或tau蛋白病，如帕金森病、阿尔茨海默病或带有Lewy小体的痴呆症。
• Glucosylceramide synthase inhibitors
  申请人：GENZYME CORPORATION

  公开号：US09139580B2

  公开（公告）日：2015-09-22

  The invention relates to inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer.

  该发明涉及抑制葡糖鞘氨醇合成酶（GCS）的抑制剂，可用于治疗代谢性疾病，如溶酶体贮积症，单独或与酶替代治疗结合使用，并用于治疗癌症。
• US20140255381A1
  申请人：——

  公开号：——

  公开（公告）日：——
• METHODS FOR TREATING PROTEINOPATHIES
  申请人：Genzyme Corporation

  公开号：EP3267983A1

  公开（公告）日：2018-01-17
• METHODS FOR TREATING NEUROLOGICAL SYMPTOMS ASSOCIATED WITH LYSOSOMAL STORAGE DISEASES
  申请人：Genzyme Corporation

  公开号：US20210251982A1

  公开（公告）日：2021-08-19

  Methods are provided for treating or preventing neurological symptoms and disorders which are associated with, e.g., lysosomal storage diseases. The methods include enhancing neuronal connectivity within the brain of a subject, increasing brain tissue volume, or preventing or delaying loss of brain tissue volume in a subject. Also provided are methods for monitoring the progression or regression of a neurological disorder, or assessing the onset of a neurological disorder, associated with a lysosomal storage disease, in which brain tissue volume of the subject is measured.