(11beta,16alpha)-9-Fluoro-3,11,17,21-tetrahydroxy-16-methylpregna-1,4-dien-20-one | 922713-68-6

• 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: (11beta,16alpha)-9-Fluoro-3,11,17,21-tetrahydroxy-16-methylpregna-1,4-dien-20-one
• 英文别名: 1-[(8S,9R,10S,11S,13S,14S,16R,17R)-9-fluoro-3,11,17-trihydroxy-10,13,16-trimethyl-6,7,8,11,12,14,15,16-octahydro-3H-cyclopenta[a]phenanthren-17-yl]-2-hydroxyethanone
• CAS: 922713-68-6
• 化学式: C₂₂H₃₁FO₅
• 分子量: 394.5
• InChiKey: AHCZVAORYHARLA-PYZGQABGSA-N

物化性质

• 沸点：
  569.3±50.0 °C(Predicted)
• 密度：
  1.32±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  28
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.77
• 拓扑面积：
  98
• 氢给体数：
  4
• 氢受体数：
  6

文献信息

• Phosphate based linkers for intracellular delivery of drug conjugates
  申请人：Merck Sharp & Dohme Corp.

  公开号：US10550190B2

  公开（公告）日：2020-02-04

  Phosphate-based linkers with tunable stability for intracellular delivery of drug conjugates are described. The phosphate-based linkers comprise a monophosphate, diphosphate, triphosphate, or tetraphosphate group (phosphate group) and a linker arm comprising a tuning element and optionally a spacer. A payload is covalently linked to the phosphate group at the distal end of the linker arm and the functional group at the proximal end of the linker arm is covalently linked to a cell-specific targeting ligand such as an antibody. These phosphate-based linkers have a differentiated and tunable stability in blood vs. an intracellular environment (e.g. lysosomal compartment).

  本文描述了用于细胞内输送药物共轭物的稳定性可调的磷酸盐基连接体。磷酸盐基连接体包括一个单磷酸、二磷酸、三磷酸或四磷酸基团（磷酸盐基团）和一个连接臂，连接臂包括一个调谐元件和可选的间隔物。有效载荷与连接臂远端磷酸基团共价连接，连接臂近端官能团与细胞特异性靶向配体（如抗体）共价连接。这些基于磷酸盐的连接体在血液与细胞内环境（如溶酶体区）中具有不同的可调稳定性。
• Intravitreal drug delivery systems for the treatment of ocular conditions
  申请人：Aerie Pharmaceuticals, Inc.

  公开号：US11116776B2

  公开（公告）日：2021-09-14

  The disclosure teaches precisely engineered biodegradable drug delivery systems and methods of making and utilizing such systems. In aspects, the biodegradable drug delivery systems taught herein comprise intravitreal ocular implants suitable for delivery of corticosteroids to the posterior segment of a human eye. The intravitreal ocular implants described herein have a desired extended drug release profile suitable for treating inflammation of the human eye.

  本公开教导精确设计的生物可降解给药系统以及制造和利用这种系统的方法。在某些方面，本文教导的生物可降解药物递送系统包括适合向人眼后段递送皮质类固醇的玻璃体内眼植入物。本文所述的玻璃体内眼植入物具有理想的延长药物释放曲线，适用于治疗人眼炎症。
• NOVEL METHOD FOR THE PRODUCTION OF DIFFERENTIATED RESPIRATORY EPITHELIAL CELLS
  申请人：Medizinische Hochschule Hannover

  公开号：EP2670841B1

  公开（公告）日：2017-11-22
• METHODS TO INDUCE TARGETED PROTEIN DEGRADATION THROUGH BIFUNCTIONAL MOLECULES
  申请人：Dana-Farber Cancer Institute, Inc.

  公开号：US20180085465A1

  公开（公告）日：2018-03-29

  The present application provides bifunctional compounds which act as protein degradation inducing moieties. The present application also relates to methods for the targeted degradation of endogenous proteins through the use of the bifunctional compounds that link a cereblon-binding moiety to a ligand that is capable of binding to the targeted protein which can be utilized in the treatment of proliferative disorders. The present application also provides methods for making compounds of the application and intermediates thereof.
• CYCLODEXTRIN-BASED POLYMERS FOR THERAPEUTIC DELIVERY
  申请人：Novartis AG

  公开号：US20200046845A1

  公开（公告）日：2020-02-13

  Provided are methods relating to the use of CDP-therapeutic agent conjugates for the treatment of a disease or disorder, e.g., autoimmune disease, inflammatory disease, central nervous system disorder, cardiovascular disease, or metabolic disorder. Also provided are CDP-therapeutic agent conjugates, particles comprising CDP-therapeutic agent conjugates, and compositions comprising CDP-therapeutic agent conjugates.