(2S,3S,4R,5R)-2-[[(Z)-1-amino-8-(3-aminopropylamino)oct-2-en-3-yl]sulfanylmethyl]-5-(6-aminopurin-9-yl)oxolane-3,4-diol

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物 - 5'-脱氧核糖核苷
• 英文名称: (2S,3S,4R,5R)-2-[[(Z)-1-amino-8-(3-aminopropylamino)oct-2-en-3-yl]sulfanylmethyl]-5-(6-aminopurin-9-yl)oxolane-3,4-diol
• 化学式: C₂₁H₃₆N₈O₃S
• 分子量: 480.6
• InChiKey: UMZRPWOFFHRUNX-QWZVAEQCSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.7
• 重原子数：
  33
• 可旋转键数：
  14
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  209
• 氢给体数：
  6
• 氢受体数：
  11

文献信息

• Polyamine-metal chelator conjugates
  申请人：Bergeron J. Raymond

  公开号：US20060211773A1

  公开（公告）日：2006-09-21

  Many metal collators have polar or charged functional groups, which render them difficult to transport across a cell membrane. Polyimide-metal collator conjugates of the invention are compounds comprising a first moiety which is a metal collator and a second moiety which is a polyimide, where the polyimide moiety includes three or more nitrogen atoms which are capable of being positively charged at physiological pH. A sperms-L1 conjugate has been shown to accumulate in L1210 cells several hundred fold more than the unconjugated L1 chelator.

  许多金属配体具有极性或带电的功能基团，这使它们难以穿过细胞膜。本发明的聚酰亚胺-金属配体共轭物是由第一部分为金属配体，第二部分为聚酰亚胺的化合物组成，其中聚酰亚胺部分包含三个或更多的氮原子，在生理pH下能够呈正电荷。已经证明，精子-L1共轭物在L1210细胞中的积累量比未共轭的L1螯合剂高出数百倍。
• Polyamine-Metal Chelator Conjugates
  申请人：Bergeron Raymond

  公开号：US20080096974A2

  公开（公告）日：2008-04-24

  Many metal chelators have polar or charged functional groups, which render them difficult to transport across a cell membrane. Polyamine-metal chelator conjugates of the invention are compounds comprising a first moiety which is a metal chelator and a second moiety which is a polyamine, where the polyamine moiety includes three or more nitrogen atoms which are capable of being positively charged at physiological pH. A spermine-L1 conjugate has been shown to accumulate in L1210 cells several hundred fold more than the unconjugated L1 chelator.

  许多金属螯合剂具有极性或带电的功能基团，这使得它们难以跨越细胞膜。本发明的多胺-金属螯合剂共轭物是化合物，包括第一部分是金属螯合剂，第二部分是多胺，其中多胺部分包括三个或更多的氮原子，在生理pH下能够呈正电荷。已经证明精胺-L1共轭物在L1210细胞中的积累比未共轭的L1螯合剂高出数百倍。
• Hair growth compositions and methods
  申请人：Pilosciences

  公开号：EP2735303A1

  公开（公告）日：2014-05-28

  The present invention relates to hair modifying compositions and methods, as well as to compositions and methods for modifying hair growth. The invention more specifically relates to targeted approaches using antibodies or agonists thereof for altering or stimulating hair growth, structure or number. The invention also relates to compositions, such as cosmetic compositions, comprising antibodies and/or further active agents, and their use to modify hair growth and/or to remove unwanted hair. The invention may be used in any mammalian subject, optionally in combination with any other depilation or hair stimulating method or any other hair treatment.

  本发明涉及毛发修饰组合物和方法，以及用于修饰毛发生长的组合物和方法。本发明更具体地涉及使用抗体或其激动剂改变或刺激毛发生长、结构或数量的靶向方法。本发明还涉及包含抗体和/或其他活性剂的组合物，如化妆品组合物，以及它们用于改变毛发生长和/或去除多余毛发的用途。本发明可用于任何哺乳动物，也可与任何其他脱毛或毛发刺激方法或任何其他毛发治疗方法结合使用。
• COMPOSITION FOR ORAL DELIVERY COMPRISING MGBG FOR USE IN TREATING MULTIPLE SCLEROSIS
  申请人：Pathologica LLC

  公开号：EP3473247A1

  公开（公告）日：2019-04-24

  The present invention relates to an oral pharmaceutical composition, comprising methylglyoxal bis(guanylhydrazone) (MGBG) together with at least one oral pharmaceutically acceptable excipient, for use in the treatment or delaying the onset or development of multiple sclerosis when orally administered to a subject.

  本发明涉及一种口服药物组合物，包括甲基乙二醛双（鸟苷腙）（MGBG）和至少一种口服药物可接受赋形剂，用于口服给受试者治疗或延缓多发性硬化症的发作或发展。
• MITOGUAZONE FOR PREVENTING THE RELAPSE OR THE PROGRESSION OF MULTIPLE SCLEROSIS
  申请人：Pathologica LLC

  公开号：EP3831372A1

  公开（公告）日：2021-06-09

  Disclosed herein are new oral pharmaceutical compositions of SAMDC inhibitors, polyamine analogs, and polyamine biosynthesis inhibitors, and their application for the treatment of conditions including demyelinating diseases, autoimmune disorders affecting the nervous system, and other neurodegenerative conditions.

  本文公开了SAMDC抑制剂、多胺类似物和多胺生物合成抑制剂的新型口服药物组合物，以及它们在治疗脱髓鞘疾病、影响神经系统的自身免疫性疾病和其他神经退行性疾病等疾病中的应用。