L-Altro-oct-3-enitol, 5,8-anhydro-6-((3Z)-6-carboxy-3-hexenyl)-1-O-(3-chlorophenyl)-3,4,6-trideoxy-, (3E)- | 748816-43-5

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 英文名称: L-Altro-oct-3-enitol, 5,8-anhydro-6-((3Z)-6-carboxy-3-hexenyl)-1-O-(3-chlorophenyl)-3,4,6-trideoxy-, (3E)-
• 英文别名: (Z)-7-[(2R,3S,4R)-2-[(E,3R)-4-(3-chlorophenoxy)-3-hydroxybut-1-enyl]-4-hydroxyoxolan-3-yl]hept-4-enoic acid
• CAS: 748816-43-5
• 化学式: C₂₁H₂₇ClO₆
• 分子量: 410.9
• InChiKey: GLYAVTUPQOQHAD-MOBTWWNESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  28
• 可旋转键数：
  11
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  96.2
• 氢给体数：
  3
• 氢受体数：
  6

文献信息

• METHODS AND COMPOSTIONS FOR REDUCING BODY FAT
  申请人：Topokine Therapeutics, Inc.

  公开号：EP2982373A1

  公开（公告）日：2016-02-10

  Provided are methods, compositions, systems, and kits for treating metabolic syndrome or a disorder associated with metabolic syndrome, e.g., obesity, dyslipidemia, and/or a diabetic condition, comprising administering systemically to a subject one or more compounds of the Formula (I) and/or (II): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, or prodrug thereof, wherein - - - - - - , L, R1, R2, Z, X, A and B are defined herein.

  本发明提供了用于治疗代谢综合征或与代谢综合征相关的疾病（如肥胖、血脂异常和/或糖尿病）的方法、组合物、系统和试剂盒，包括向受试者全身施用一种或多种式（I）和/或（II）化合物： 或其药学上可接受的盐、水合物、溶液、立体异构体、多晶型、同分异构体、同位素富集衍生物或原药，其中 - - - - - - 、L、R1、R2、Z、X、A 和 B 在本文中定义。
• Topical dosage regimen
  申请人：Topokine Therapeutics, Inc.

  公开号：US10188661B2

  公开（公告）日：2019-01-29

  Described herein is a novel dosage regimen, and related uses and methods, for a prostaglandin FP receptor agonist (PFPRA) compound topically administered to the skin. The dosage regimen is useful for reduction of subcutaneous fat, for example, in patients who suffer from local excesses of subcutaneous fat. A particular advantage of the dosage regimen is the ability to reduce composition exposure and thereby promote convenience and comfort, while maintaining the desired exposure and therapeutic effect in subcutaneous fat. Further provided are kits according to the novel dosage regimen, comprising a PFPRA composition and instructions for use.

  本文描述了一种用于皮肤局部给药的前列腺素FP受体激动剂（PFPRA）化合物的新型剂量方案及相关用途和方法。该剂量方案可用于减少皮下脂肪，例如减少局部皮下脂肪过多患者的皮下脂肪。该剂量方案的一个特别优点是能够减少组合物的暴露量，从而提高方便性和舒适性，同时保持所需的皮下脂肪暴露量和治疗效果。此外，还提供了根据新型剂量方案制成的试剂盒，其中包括 PFPRA 组合物和使用说明。
• Methods and compositions for treating metabolic syndrome
  申请人：Topokine Therapeutics, Inc.

  公开号：US10335418B2

  公开（公告）日：2019-07-02

  Provided are methods, compositions, systems, and kits for treating metabolic syndrome or a disorder associated with metabolic syndrome, e.g., obesity, dyslipidemia, and/or a diabetic condition, comprising administering systemically to a subject one or more compounds of the Formula (I) and/or (II): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, or prodrug thereof, wherein , L, R1, R2, Z, X, A and B are defined herein.

  本发明提供了用于治疗代谢综合征或与代谢综合征相关的疾病（如肥胖、血脂异常和/或糖尿病）的方法、组合物、系统和试剂盒，包括向受试者全身施用一种或多种式（I）和/或（II）化合物： 或其药学上可接受的盐、水合物、溶液、立体异构体、多晶型、同系物、同位素富集衍生物或原药，其中 ，L、R1、R2、Z、X、A 和 B 在本文中定义。
• Compositions and methods for topical delivery of prostaglandins to subcutaneous fat
  申请人：Topokine Therapeutics, Inc.

  公开号：US10556012B2

  公开（公告）日：2020-02-11

  Described herein are compositions comprising a prostaglandin FP receptor agonist (PFPRA) compound and a fatty acid ester (e.g., isopropyl myristate), optionally comprising an ointment base such as a hydrocarbon base (e.g., petroleum jelly) and/or an organic alcohol (e.g., propylene glycol), that, when topically applied to the skin, locally delivers a therapeutically effective amount of the PFPRA compound to subcutaneous fat under the skin, and methods of preparation. The therapeutic effect is, for example, reduction of the subcutaneous fat under the skin. Further provided are methods of reducing body fat in a subject comprising topically administering the composition to the subject.

  本文描述了包含前列腺素FP受体激动剂（PFPRA）化合物和脂肪酸酯（如肉豆蔻酸异丙酯）的组合物，该组合物可选地包含软膏基质，如烃类基质（如凡士林）和/或有机醇（如丙二醇），当局部应用于皮肤时，可将治疗有效量的PFPRA化合物局部递送至皮下脂肪，以及制备方法。例如，治疗效果是减少皮下脂肪。进一步提供了减少受试者体内脂肪的方法，包括对受试者局部施用组合物。
• Methods and compositions for topical delivery of prostaglandins to subcutaneous fat
  申请人：Topokine Therapeutics, Inc.

  公开号：US10869874B2

  公开（公告）日：2020-12-22

  Described herein are compositions comprising a prostaglandin FP receptor agonist (PFPRA) compound and a fatty acid, e.g., oleic acid, that, when topically applied to the skin, locally delivers a therapeutically effective amount of the PFPRA compound or active metabolite thereof to subcutaneous fat under the skin. The therapeutic effect is, for example, reduction of the subcutaneous fat under the skin. Further provided are methods of reducing body fat in a subject comprising topically administering the composition to the subject. The present invention also provides kits comprising the composition and instructions for use.

  本文描述的组合物包含前列腺素 FP 受体激动剂（PFPRA）化合物和脂肪酸（如油酸），当局部施用到皮肤上时，可将治疗有效量的 PFPRA 化合物或其活性代谢物局部输送到皮下脂肪。治疗效果是减少皮下脂肪等。进一步提供了减少受试者体内脂肪的方法，包括对受试者局部施用组合物。本发明还提供了包含该组合物和使用说明的试剂盒。