Cilobamine | 69429-84-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: Cilobamine
• 英文别名: (2R,3R)-2-(3,4-dichlorophenyl)-3-(propan-2-ylamino)bicyclo[2.2.2]octan-2-ol
• CAS: 69429-84-1
• 化学式: C₁₇H₂₃Cl₂NO
• 分子量: 328.3
• InChiKey: MQILJMOEUMZBHK-FIMMUYGNSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.65
• 拓扑面积：
  32.3
• 氢给体数：
  2
• 氢受体数：
  2

文献信息

• 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。
• Prodrugs of antidepressants and their use for treating depressions
  申请人：——

  公开号：US20040242594A1

  公开（公告）日：2004-12-02

  This invention relates to prodrugs of antidepressants and the use of these prodrugs in a method for therapy and to pharmaceutical compositions comprising the prodrugs of the invention.

  本发明涉及抗抑郁药的前药及其在治疗方法中的使用，以及包含本发明的前药的制药组合物。
• 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。
• Compositions and methods for selective delivery of oligonucleotide molecules to specific neuron types
  申请人：Nlife Therapeutics S.L.

  公开号：EP2380595A1

  公开（公告）日：2011-10-26

  The invention provides a conjugate comprising (i) a nucleic acid which is complementary to a target nucleic acid sequence and which expression prevents or reduces expression of the target nucleic acid and (ii) a selectivity agent which is capable of binding with high affinity to a neurotransmitter transporter. The conjugates of the present invention are useful for the delivery of the nucleuc acid toi cell of interests and thus, for the treatment of diseases which require a down-regulation of the protein encoded by the target nucleic acid as well as for the delivery of contrast agents to the cells for diagnostic purposes.

  本发明提供了一种共轭物，该共轭物包含(i)与靶核酸序列互补的核酸，该核酸的表达可防止或减少靶核酸的表达；(ii)能够与神经递质转运体高亲和力结合的选择剂。本发明的共轭物可用于将核酸递送至相关细胞，从而治疗需要下调靶核酸编码蛋白的疾病，也可用于将造影剂递送至细胞以进行诊断。
• Compositions and methods for the treatment of parkinson disease by the selective delivery of oligonucleotide molecules to specific neuron types
  申请人：nLife Therapeutics, S.L.

  公开号：US10125363B2

  公开（公告）日：2018-11-13

  The invention provides a conjugate comprising (i) a selectivity agent which binds specifically to one or more neurotransmitter transporters selected from the group consisting of a dopamine transporter (DAT), serotonin transporter (SERT) or a norepinephrine transporter (NET) and (ii) a nucleic acid capable of specifically binding to a target molecule which is expressed in the same cell as the neurotransmitter transporter wherein said target molecule is α-synuclein or the mRNA encoding α-synuclein. The conjugates of the present invention are useful for the delivery of the nucleic acid to a cell of interest and thus, for the treatment of diseases which require a down-regulation of the protein encoded by the target nucleic acid as well as for the delivery of imaging agents to the cells for diagnostic purposes.

  本发明提供了一种共轭物，该共轭物包含：(i) 一种选择性制剂，它能与一种或多种神经递质转运体特异性结合，这些神经递质转运体选自由多巴胺转运体（DAT）、5-羟色胺转运体（SERT）或去甲肾上腺素转运体（NET）组成的组、多巴胺转运体 (DAT)、5-羟色胺转运体 (SERT) 或去甲肾上腺素转运体 (NET)；(ii) 能够与靶分子特异性结合的核酸，该靶分子与神经递质转运体在同一细胞中表达，其中所述靶分子为 α-突触核蛋白或编码 α-突触核蛋白的 mRNA。本发明的共轭物可用于将核酸递送至相关细胞，从而治疗需要下调靶核酸编码蛋白的疾病，也可用于将成像剂递送至细胞以进行诊断。