3-(2-Methylpropyl)-1-propan-2-ylpyrrolidine-2,5-dione

• 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: 3-(2-Methylpropyl)-1-propan-2-ylpyrrolidine-2,5-dione
• 英文别名: 3-(2-methylpropyl)-1-propan-2-ylpyrrolidine-2,5-dione
• 化学式: C₁₁H₁₉NO₂
• 分子量: 197.27
• InChiKey: XCFUWHOBSCDEMC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.82
• 拓扑面积：
  37.4
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• HYDROPHOBICALLY TAGGED SMALL MOLECULES AS INDUCERS OF PROTEIN DEGRADATION
  申请人：DANA-FARBER CANCER INSTITUTE, INC.

  公开号：US20150274738A1

  公开（公告）日：2015-10-01

  Provided are bifunctional small molecules of Formula (I): or pharmaceutically acceptable salts thereof, wherein M represents a small organic molecule which binds, covalently or non-covalently, a kinase, such as Her3 protein kinase; L 1 represents a linker; and R H represents a hydrophobic group. An example of a compound of Formula (I) is a compound of Formula (II): Also provided are pharmaceutical compositions comprising a compound of Formula (I) or (II) and methods of using such compounds for treating proliferative diseases.

  提供的是公式（I）的双功能小分子或其药学上可接受的盐，其中M代表结合激酶的小有机分子，可以是共价或非共价结合，例如Her3蛋白激酶；L1代表连接物；RH代表疏水基团。公式（I）的一个化合物示例是公式（II）的化合物： 还提供了包含公式（I）或（II）化合物的药物组合物，以及使用这些化合物治疗增殖性疾病的方法。
• Gas-filled stabilized particles and methods of use
  申请人：Children's Medical Center Corporation

  公开号：US10577554B2

  公开（公告）日：2020-03-03

  Provided herein are various gas-filled particles having a stabilized membrane that encapsulates the gas. Pharmaceutical compositions, methods of use and treatment, and methods of preparation are also described.

  本文提供了各种充满气体的颗粒，这些颗粒具有封装气体的稳定膜。此外，还介绍了药物组合物、使用和处理方法以及制备方法。
• Trioxacarcins, trioxacarcin#antibody conjugates, and uses thereof
  申请人：President and Fellows of Harvard College

  公开号：US10639381B2

  公开（公告）日：2020-05-05

  Provided herein are trioxacarcin-antibody drug conjugates of Formula (A): and pharmaceutically acceptable salts thereof, comprising at least one instance of the group -L1-(A-L2)a-B attached thereto, wherein a is an integer between 1 and 10, inclusive, L1 is absent or is a linking group, A is a moiety formed from the reaction of two complimentary groups (X and Y), L2 is absent or is another linking group, and B is an antibody or antibody fragment. Also provided are methods of preparing these antibody-drug conjugates, pharmaceutically acceptable compositions thereof, and methods of their use and treatment. Further provided are precursors to the trioxacarcin-antibody drug conjugates, novel trioxacarcins without an antibody conjugated thereto, pharmaceutical compositions thereof, and methods of their use and treatment.

  本文提供的是式 (A) 的三氧羰基霉素-抗体药物共轭物： 及其药学上可接受的盐，包含至少一个连接在其上的基团-L1-(A-L2)a-B 的实例，其中 a 是 1 至 10（包括 10）之间的整数，L1 不存在或为连接基团，A 是由两个互补基团（X 和 Y）反应形成的分子，L2 不存在或为另一个连接基团，B 是抗体或抗体片段。此外，还提供了制备这些抗体-药物共轭物的方法、其药学上可接受的组合物及其使用和治疗方法。此外，还提供了三氧嘧啶-抗体药物共轭物的前体、不含抗体的新型三氧嘧啶、其药用组合物及其使用和治疗方法。
• Macrolides and methods of their preparation and use
  申请人：President and Fellows of Harvard College

  公开号：US10913764B2

  公开（公告）日：2021-02-09

  Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.

  本文提供了通过东半部和西半部偶联，然后大环化来制备大环内酯的方法，以提供大环内酯，包括已知大环内酯和新型大环内酯。还提供了合成大环内酯（包括东半部和西半部）的中间体。还提供了使用本发明大环内酯类药物治疗传染性疾病和炎症的药物组合物和方法。还提供了用于合成西半部分的一般非对映选择性醛醇方法。
• USING SORTASES TO INSTALL CLICK CHEMISTRY HANDLES FOR PROTEIN LIGATION
  申请人：Ploegh Hidde L

  公开号：US20140249296A1

  公开（公告）日：2014-09-04

  Methods and reagents for the installation of click chemistry handles on target proteins are provided, as well as modified proteins comprising click chemistry handles. Further, chimeric proteins, for example, bi-specific antibodies, that comprise two proteins conjugated via click chemistry, as well as methods for their generation and use are disclosed herein.