皮质醇21-丙酸酯 | 6677-98-1

• 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
• 中文名称: 皮质醇21-丙酸酯
• 英文名称: hydrocortisone 21-propionate
• 英文别名: hydrocortisone propionate；[2-[(8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-10,13-dimethyl-3-oxo-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-17-yl]-2-oxoethyl] propanoate
• CAS: 6677-98-1
• 化学式: C₂₄H₃₄O₆
• 分子量: 418.53
• InChiKey: MRECAIZOMKKXOZ-RPPPWEFESA-N

物化性质

• 熔点：
  206.0-208.5 °C
• 沸点：
  496.27°C (rough estimate)
• 密度：
  1.0933 (rough estimate)
• 溶解度：
  乙醇（微溶）、甲醇（微溶）

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  30
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.79
• 拓扑面积：
  101
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  皮质醇21-丙酸酯 生成 11β-hydroxy-17α-methylthiomethoxy-21-propionyloxy-4-pregnene-3,20-dione
  参考文献：
  名称：

  Novel corticoid 17-thioacetals, their preparation and use

  摘要：

  新型皮质类固醇17-硫代缩醛的化学式为：##STR1## 其中X是氢、氟或甲基，R.sub.1是氢或C.sub.1-C.sub.6烷基，R.sub.2是氢或C.sub.1-16烃基羧酸的酰基，在药物上具有重要的价值，例如作为抗炎药。

  公开号：

  US04330541A1

文献信息

• TERPENE COUPLING CONJUGATE
  申请人：LABORATOIRES ERIGER

  公开号：US20210361771A1

  公开（公告）日：2021-11-25

  The subject matter of the present invention relates to the use of an optionally branched linear terpene having at most one C═C unsaturation for the production of conjugates provided with self-assembly properties, as well as a self-assembly agent of formula (I): X(-Spacer-Y-Terpene) p (I) in which: “Terpene” is linear, optionally branched, having at most one C═C unsaturation; “Y” is a bond or a molecular fragment with a biodegradable bond; “Spacer” is a bond or a fragment comprising at least one carbon atom; “X” is a molecular fragment comprising at least one biodegradable bond; “p” ranges between 0.1 and 4; and the “-Spacer-Y-” group optionally can be a bond, as well as the conjugate resulting from the combination of the self-assembly agent of formula (I) with an active molecule MA.

  本发明的主题涉及使用最多具有一个C═C不饱和度的线性可选择分支的萜烯，用于具有自组装特性的共轭物的生产，以及具有以下式(I)的自组装剂： X(-Spacer-Y-Terpene) p (I) 其中： “萜烯”是线性的，可选择分支的，最多具有一个C═C不饱和度； “Y”是一个具有可生物降解键的键或分子片段； “Spacer”是一个包含至少一个碳原子的键或片段； “X”是一个包含至少一个可生物降解键的分子片段； “p”范围在0.1至4之间；以及 “-Spacer-Y-”基团可以选择是一个键， 以及由式(I)的自组装剂与活性分子MA的组合产生的共轭物。
• [EN] POLYMERIC NANOPARTICLES FOR ULTRASOUND IMAGING AND THERAPY<br/>[FR] NANOPARTICULES POLYMÈRES UTILISÉES POUR L'IMAGERIE ET LE TRAITEMENT PAR ULTRASONS
  申请人：UNIV MICHIGAN

  公开号：WO2013055791A1

  公开（公告）日：2013-04-18

  Provided herein are nanobubbles designed for use in ultrasound-mediated ablation of cancer cells. The nanobubbles undergo ultrasound-mediated cavitation at an ablation threshold which is significantly decreased, relative to standard ultrasound- mediated treatment of cancer cells. In exemplary embodiments, the nanobubbles comprise an amphiphilic ABC triblock copolymer, wherein block A comprises a hydrophilic polymer, block B comprises a crosslinking polymer, and block C comprises a hydrophobic copolymer comprising (i) methyl methacrylate (MMA) and (ii) a fluorinated monomer, wherein the fluorinated monomer is present in the hydrophobic copolymer of block C at 25 mole percent or less. Related treatment and diagnostic methods, as well as materials relating to the nanobubbles are provided herein. Methods of making a random copolymer are furthermore provided herein.

  本文提供了设计用于超声介导癌细胞消融的纳米气泡。这些纳米气泡在消融阈值下经历超声介导的空化作用，相对于标准的超声介导癌细胞治疗，其消融阈值显著降低。在示范性实施例中，这些纳米气泡包括一种两性ABC三嵌段共聚物，其中嵌段A包括一个亲水性聚合物，嵌段B包括一个交联聚合物，而嵌段C包括一个亲脂性共聚物，包括(i) 甲基丙烯酸甲酯（MMA）和(ii) 一种氟化单体，其中氟化单体以25摩尔%或更低的比例存在于嵌段C的亲脂性共聚物中。此外，本文还提供了与纳米气泡相关的治疗和诊断方法，以及相关材料。此外，本文还提供了制备随机共聚物的方法。
• [EN] TAZAROTENE DERIVATIVES<br/>[FR] DÉRIVÉS DE TAZAROTÈNE
  申请人：STIEFEL LABORATORIES

  公开号：WO2011009023A1

  公开（公告）日：2011-01-20

  The presently described subject matter relates to new derivatives of tazarotene that also exhibit retinoid activity, pharmaceutical compositions comprising the derivatives, method of treating skin disorders with the pharmaceutical compositions, and process of making the derivatives.

  目前所描述的主题涉及到新的他扎罗汀衍生物，它们也表现出类视黄醇活性，包括这些衍生物的制药组合物，使用这些制药组合物治疗皮肤疾病的方法，以及制造这些衍生物的过程。
• Formulation of an erodible, gastric retentive oral dosage form using in vitro disintegration test data
  申请人：——

  公开号：US20030133985A1

  公开（公告）日：2003-07-17

  Erodible, gastric-retentive dosage forms are provided that are formulated using the in vitro drug release profile obtained with USP Disintegration test equipment rather the USP Dissolution Apparatus. The invention is premised on the discovery that the USP Disintegration Test and modified versions thereof are far more predictive of the in vivo release profile for a controlled release dosage form than is the standard USP Dissolution Test, particularly controlled release dosage forms of the swellable, erodible type. The dosage forms generally comprise particles of a biocompatible, hydrophilic polymer having the active agent incorporated therein, wherein the particles are optionally but preferably compacted into a tablet or loaded into a capsule. The dosage forms can be used to deliver water-insoluble or sparingly soluble drugs as well as water-soluble drugs, providing that the latter are coated with a protective coating or contained in a protective vesicle.

  提供可侵蚀的、胃滞留的剂型，其配方使用USP分散测试设备获得的体外药物释放剖面，而不是USP溶解器。该发明是基于发现，USP分散测试及其修改版本比标准的USP溶解测试更能预测可控释放剂型的体内释放剖面，特别是膨胀、侵蚀型的可控释放剂型。该剂型通常包括生物相容性、亲水性聚合物的颗粒，其中活性成分被纳入其中，颗粒可以选择但最好是压缩成片剂或装入胶囊。该剂型可用于输送水不溶性或难溶性药物，以及水溶性药物，前提是后者被涂上保护涂层或包含在保护小囊中。
• Formulation of an erodible, gastric retentive oral diuretic
  申请人：——

  公开号：US20030152622A1

  公开（公告）日：2003-08-14

  An erodible, gastric-retentive oral diuretic is provided that is formulated using the in vitro drug release profile obtained with USP Disintegration test equipment rather the USP Dissolution Apparatus. The invention is premised on the discovery that the USP Disintegration Test and modified versions thereof are far more predictive of the in vivo release profile for a controlled release dosage form than is the standard USP Dissolution Test, particularly controlled release dosage forms of the swellable, erodible type. The dosage forms generally comprise particles of a biocompatible, hydrophilic polymer having the active agent incorporated therein, wherein the particles are optionally but preferably compacted into a tablet or loaded into a capsule. The dosage forms can be used to deliver water-insoluble or sparingly soluble drugs as well as water-soluble drugs, providing that the latter are coated with a protective coating or contained in a protective vesicle. Using the controlled release dosage form, adverse side effects associated with peak diuresis are diminished or eliminated, while the overall diuretic effect of the drug is maintained.

  提供了一种可侵蚀、胃内停留的口服利尿剂，其配方使用了通过美国药典溶解试验设备获得的体外药物释放特性，而不是使用美国药典溶出仪。该发明基于发现，美国药典溶解试验及其修改版本远比标准的美国药典溶出试验更具预测性，特别是对于可膨胀、可侵蚀类型的控释剂型的体内释放特性。这些剂型通常包括含有活性成分的生物相容性、亲水性聚合物颗粒，其中这些颗粒可以选择性地但最好是被压制成片剂或装入胶囊中。这些剂型可用于输送水不溶性或难溶性药物以及水溶性药物，只要后者被覆盖有保护层或包含在保护泡囊中。使用控释剂型，可以减轻或消除与高峰利尿相关的不良副作用，同时保持药物的整体利尿效果。