(R)-3-acetyl-2,2-dimethylthiazolidine-4-carboxylic acid | 942518-79-8

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: (R)-3-acetyl-2,2-dimethylthiazolidine-4-carboxylic acid
• 英文别名: (4R)-3-acetyl-2,2-dimethyl-1,3-thiazolidine-4-carboxylic acid
• CAS: 942518-79-8
• 化学式: C₈H₁₃NO₃S
• 分子量: 203.262
• InChiKey: WGUDNYLDZNNYDB-LURJTMIESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  82.9
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (R)-3-acetyl-2,2-dimethylthiazolidine-4-carboxylic acid 在 三乙胺 、 N,N-二异丙基乙胺 、 Methanaminium,N-[(dimethylamino)(3H-1,2,3-triazolo[4,5-b]pyridin-3-yloxy)methylene]-N-methyl-, hexafluorophosphate(1-) 、 三氟乙酸 作用下， 以 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 24.0h， 生成 cyanomethyl (6S,8S,9R,10S,11S,13S,14S,16R,17R)-17-((acetyl-L-cysteinyl)oxy)-6,9-difluoro-11-hydroxy-10,13,16-trimethyl-3-oxo- 6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carboxylate
  参考文献：
  名称：

  WO2023/67387

  摘要：

  公开号：
• 作为产物：
  描述：

  (4R)-2,2-二甲基-4-噻唑烷甲酸 在 乙酸酐 、 1,8-二氮杂双环[5.4.0]十一碳-7-烯 作用下， 以56 %的产率得到(R)-3-acetyl-2,2-dimethylthiazolidine-4-carboxylic acid
  参考文献：
  名称：

  Compounds and methods for the treatment of ocular disorders

  摘要：

  本文描述了用于治疗或预防眼表面疾病的组合物和方法，包括睑板腺功能障碍、眼睑炎、干眼症和其他前表面炎症和/或感染性眼疾。所述组合物和方法包括角质溶解偶联物，其表现出角质溶解活性和抗炎或其他理想活性。将所述组合物局部给药于眼睑边缘或周围区域，可为患有眼表面疾病的患者提供治疗益处。

  公开号：

  US11459351B1

文献信息

• PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE OF HIGHLY LIPOPHILIC SULFHYDRYL COMPOUNDS
  申请人：Gately Stephen

  公开号：US20090306015A1

  公开（公告）日：2009-12-10

  Novel compositions of silicon-containing sulfhydryl compounds, their preparation and use in methods for treating disease are described. Silicon confers lipophilicity that can enhance the penetration of the silicon derivative sulfhydryl compounds across the gut wall, cell membranes and blood brain barrier, thus improving therapeutic properties including bioavailability, metabolism, and/or pharmacokinetics. The organosilyl group provides compounds having improved pharmacokinetics. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for treatment of diseases and other maladies or conditions and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

  本文描述了含硅硫醇化合物的新型组合物、其制备方法以及在治疗疾病方面的应用。硅赋予化合物亲脂性，可以增强硅衍生硫醇化合物穿过肠壁、细胞膜和血脑屏障的渗透性，从而提高治疗性能，包括生物利用度、代谢和/或药物动力学。有机硅基团提供了具有改进药物动力学的化合物。本发明包括新型化合物、类似物、前药和其药学上可接受的盐、制药组合物以及治疗疾病和其他疾患或病况等的方法。本发明还涉及制备这些化合物的过程以及在这些过程中有用的中间体。
• [EN] COMBINATIONS OF LANOSTEROL OR 25-HYDROXYCHOLESTEROL INCLUDING DERIVATIVES THEREOF USEFUL IN THE TREATMENT OF LENS DISORDERS<br/>[FR] COMBINAISONS DE LANOSTÉROL OU DE 25-HYDROXYCHOLESTÉROL COMPRENANT DES DÉRIVÉS DE CEUX-CI UTILES DANS LE TRAITEMENT DE TROUBLES DU CRISTALLIN
  申请人：PIRAEE MAHMOOD

  公开号：WO2019097434A1

  公开（公告）日：2019-05-23

  The aspects of the present disclosure relates to novel lanosterol derivatives and novel 25-hydroxycholesterol derivatives including their pharmaceutically acceptable salts as well as methods of treatment and pharmaceutical compositions and formulations of lanosterol and derivatives thereof and 25-hydroxycholesterol and derivatives thereof useful in treating ophthalmic disorders including cataracts and presbyopia.

  本公开涉及的方面涉及新型鲎甾醇衍生物和新型25-羟基胆固醇衍生物，包括它们的药学上可接受的盐，以及用于治疗眼科疾病，包括白内障和老视症的鲎甾醇及其衍生物和25-羟基胆固醇及其衍生物的治疗方法和制药组合物和制剂。
• Synthesis of lipophilic sila derivatives of<i>N</i>-acetylcysteineamide, a cell permeating thiol
  作者：Uzma I. Zakai、Galina Bikzhanova、Daryl Staveness、Stephen Gately、Robert West

  DOI：10.1002/aoc.1572

  日期：2010.3

  N‐acetyl‐cysteine‐amide, the amide form of L‐NAC, has recently been reported to be more lipophilic and permeable through cell membranes than NAC, and to be able to traverse the blood–brain barrier. In this communication we report the synthesis and characterization of highly lipophilic sila‐amide derivatives of L‐NAC that may show enhanced cell penetration and bioavailability. Copyright © 2009 John Wiley & Sons, Ltd

  N-乙酰基-L-半胱氨酸（L- NAC）是一种有效的抗氧化剂，可降低活性氧的含量。据报道，L- NAC的酰胺形式N-乙酰-半胱氨酸-酰胺比NAC具有更高的亲脂性和细胞膜渗透性，并且能够穿过血脑屏障。在本交流中，我们报道了L -NAC的高度亲脂性硅酰胺衍生物的合成和表征，这些衍生物可能显示出更高的细胞渗透性和生物利用度。版权所有©2009 John Wiley＆Sons，Ltd.
• Combinations Of Lanosterol Or 25-Hydroxycholesterol Including Derivatives Thereof Useful In The Treatment Of Lens Disorders
  申请人：Piraee Mahmood

  公开号：US20200281944A1

  公开（公告）日：2020-09-10

  Novel lanosterol derivatives and novel 25-hydroxycholesterol derivatives including their pharmaceutically acceptable salts as well as methods of treatment and pharmaceutical compositions and formulations of lanosterol and derivatives thereof and 25-hydroxycholesterol and derivatives thereof useful in treating ophthalmic disorders including cataracts and presbyopia.
• COMPOUNDS AND METHODS FOR THE TREATMENT OF OCULAR DISORDERS
  申请人：Azura Ophthalmics Ltd.

  公开号：US20220332749A1

  公开（公告）日：2022-10-20

  Described herein are compositions and methods for the treatment or prevention of ocular surface disorders including meibomian gland dysfunction, blepharitis, dry eye disease and other inflammatory and/or infectious diseases of the anterior surface of the eye(s). Said compositions and methods comprise keratolytic conjugates which demonstrate keratolytic activity, and anti-inflammatory or other desirable activities. Topical administration of said compositions to the eyelid margin or surrounding areas provides therapeutic benefit to patients suffering from ocular surface disorders.