CSA-90 | 946047-41-2

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 英文名称: CSA-90
• 英文别名: (4R)-N,N-dipentyl-4-[(3R,5S,7R,8R,9S,10S,12S,13R,14S,17R)-3,7,12-tris(3-aminopropoxy)-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentan-1-amine
• CAS: 946047-41-2
• 化学式: C₄₃H₈₄N₄O₃
• 分子量: 705.165
• InChiKey: WJTLOVQDZWPCSK-KFQGXTKGSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.9
• 重原子数：
  50
• 可旋转键数：
  25
• 环数：
  4.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  109
• 氢给体数：
  3
• 氢受体数：
  7

文献信息

• METHODS FOR THE SYNTHESIS OF CERAGENINS
  申请人：Savage Paul B.

  公开号：US20160311851A1

  公开（公告）日：2016-10-27

  Disclosed herein are methods of making ceragnenin compounds for treating, preventing, or diagnosing diseases, disorders, or conditions associated with bacterial or viral infections, cancer, inflammation, and osteogenesis. Ceragenin compounds display broad-spectrum antibacterial activity utilizing a mode of action similar to antimicrobial peptides, but without the high synthesis costs and susceptibility to proteolytic degradation. Ceragenin compounds reproduce the amphiphilic morphology found in many antimicrobial peptides and display potent and diverse biological activities, including anti-bacterial, anti-cancer, anti-inflammatory, bone growth promotion, and wound healing promotion.

  本公开涉及一种用于治疗、预防或诊断与细菌或病毒感染、癌症、炎症和骨生成相关的疾病、疾病或状况的方法。Ceragenin化合物展示了广谱抗菌活性，利用类似于抗菌肽的作用方式，但不具有高合成成本和易受蛋白酶降解的特性。Ceragenin化合物复制了许多抗菌肽中发现的两性形态，并展示出强大而多样的生物活性，包括抗菌、抗癌、抗炎、促进骨生长和促进伤口愈合。
• CATIONIC STEROIDAL ANTIMICROBIAL SALTS
  申请人：Savage Paul B.

  公开号：US20160311850A1

  公开（公告）日：2016-10-27

  Disclosed herein are acid addition salts of cationic steroidal antimicrobials (“CSAs” or “ceragenins”) and methods of making the same. Particularly advantageous salt forms are identified, such as 1,5-naphthalenedisulfonic acid addition salts and sulfate addition salts. The acid addition salts may be formulated for treating subjects with ailments responsive to CSAs, including but not limited to treating bacterial infections. Accordingly, some embodiments include formulations and methods of administering acid addition salts of CSAs.

  本发明涉及阳离子类固醇抗微生物剂（“CSAs”或“ceragenins”）的酸盐和制备方法。特别有利的盐形式被确定，例如1,5-萘二磺酸盐和硫酸盐。这些酸盐可以用于治疗对CSAs有反应的患者，包括但不限于治疗细菌感染。因此，一些实施例包括CSAs的酸盐配方和给药方法。
• CATIONIC STEROIDAL ANTIMICROBIAL PRODRUG COMPOSITIONS AND USES THEREOF
  申请人：Savage Paul B.

  公开号：US20160096864A1

  公开（公告）日：2016-04-07

  Prodrugs or pharmaceutically acceptable salts, stereoisomers, solvates, or polymorphs thereof include a pharmaceutically and/or diagnostically active cationic steroidal antimicrobial (hereinafter “CSA”) compound or pharmaceutically acceptable salt, stereoisomer, solvate, or polymorph thereof, and one or more cleavable groups (C.G.). Some embodiments include a CSA compound prepared in an inactive or less active form and that is capable of conversion to a fully active form upon administration to a subject, upon preparation of a pharmaceutical formulation containing the CSA composition, and/or upon exposure to physiological conditions. Pharmaceutical compositions include the prodrug or pharmaceutically acceptable salt, stereoisomer, solvate, or polymorph thereof and one or more pharmaceutically acceptable excipients. Methods of treatment of bacterial infections in a patient in need utilize prodrugs or pharmaceutically acceptable salts, stereoisomers, solvates, polymorphs thereof and/or the pharmaceutical compositions described herein.

  前药或药学上可接受的盐、立体异构体、溶剂化物或其多晶体包括一种药学上和/或诊断上活性的阳离子类固醇抗微生物化合物（以下简称“CSA”）化合物或药学上可接受的盐、立体异构体、溶剂化物或其多晶体，以及一个或多个可裂解基团（C.G.）。一些实施例包括以不活性或较不活性形式制备的CSA化合物，该化合物能够在给予受试者、制备含有CSA组分的制药配方和/或暴露于生理条件下时转化为完全活性形式。制药组合物包括前药或药学上可接受的盐、立体异构体、溶剂化物或其多晶体以及一个或多个药学上可接受的辅料。需要治疗细菌感染的患者的治疗方法利用前药或药学上可接受的盐、立体异构体、溶剂化物、多晶体和/或本文所述的制药组合物。
• CERAGENIN PARTICULATE MATERIALS AND METHODS FOR MAKING SAME
  申请人：Brigham Young University

  公开号：EP3225113A1

  公开（公告）日：2017-10-04

  Particulate ceragenin materials may be manufactured by (i) providing a ceragenin feed material comprised of ceragenin molecules, each having a sterol backbone and a plurality cationic groups attached thereto; (ii) fracturing the ceragenin feed material in a milling apparatus to produce a ceragenin particulate material having a particle size distribution with a median particle size in a range from 5 nm to 20 µm; and (iii) during fracturing, maintaining the ceragenin feed with a moisture content of less than or equal to 10% by weight.

  可通过以下方法制造微粒陶醉素材料：(i) 提供由陶醉素分子组成的陶醉素进料，每个陶醉素分子都有一个甾醇骨架和连接在其上的多个阳离子基团；(ii) 在研磨设备中对陶醉素进料进行破碎，生产出陶醉素微粒材料，其粒度分布的中值粒度范围为 5 纳米到 20 微米；(iii) 在破碎过程中，保持陶醉素进料的水分含量小于或等于 10%（按重量计）。
• Ceragenin particulate materials and methods for making same
  申请人：BRIGHAM YOUNG UNIVERSITY

  公开号：US10039285B2

  公开（公告）日：2018-08-07

  Particulate ceragenin materials may be manufactured by (i) providing a ceragenin feed material comprised of ceragenin molecules, each having a sterol backbone and a plurality cationic groups attached thereto; (ii) fracturing the ceragenin feed material in a milling apparatus to produce a ceragenin particulate material having a particle size distribution with a median particle size in a range from 5 nm to 20 μm; and (iii) during fracturing, maintaining the ceragenin feed with a moisture content of less than or equal to 10% by weight.

  可通过以下方法制造微粒陶醉素材料：(i) 提供由陶醉素分子组成的陶醉素进料，每个陶醉素分子都有一个甾醇骨架和连接在其上的多个阳离子基团；(ii) 在研磨设备中对陶醉素进料进行破碎，以产生陶醉素微粒材料，该材料的粒度分布为中值粒度在 5 纳米到 20 微米之间；(iii) 在破碎过程中，保持陶醉素进料的水分含量小于或等于 10%（按重量计）。