2-(Propan-2-yl)-3a,4,7,7a-tetrahydro-1h-4,7-methanoisoindole-1,3(2h)-dione | 5443-38-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 英文名称: 2-(Propan-2-yl)-3a,4,7,7a-tetrahydro-1h-4,7-methanoisoindole-1,3(2h)-dione
• 英文别名: 4-propan-2-yl-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione
• CAS: 5443-38-9
• 化学式: C₁₂H₁₅NO₂
• 分子量: 205.25
• InChiKey: CCGKCUKWRHWJSR-UHFFFAOYSA-N

物化性质

• 沸点：
  340.0±42.0 °C(Predicted)
• 密度：
  1?+-.0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  37.4
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• [EN] BORONIC ESTER PRODRUGS AND USES THEREOF<br/>[FR] PROMÉDICAMENTS D'ESTER BORONIQUE ET LEURS UTILISATIONS
  申请人：MASSACHUSETTS INST TECHNOLOGY

  公开号：WO2020236253A1

  公开（公告）日：2020-11-26

  Disclosed herein are compounds of Formula (I) or (II). The compounds include an agent (e.g., pharmaceutical agent, cosmetic agent, or nutraceutical agent) through a linker that includes a boronic ester moiety in the backbone of the linker. The compounds may be monomers. Also provided are polymers prepared by polymerizing the monomers. The polymers may be useful for delivering the agent to a subject, tissue, biological sample, or a cell. Also provided are methods of preparing the polymers, compositions and kits comprising the polymers, and methods of use (e.g., use in delivering the agent, treating a disease, preventing a disease, diagnosing a disease) involving the polymers or compositions. The structure of the boronic ester moiety may be fine tuned so that the properties related to delivery to a subject, biological sample, tissue, or cell may be fine tuned.

  本文披露了化合物的化学式(I)或(II)。这些化合物包括通过含有硼酸酯基团的连接剂（例如，药物剂、化妆品剂或营养剂）连接的活性物质。这些化合物可以是单体。还提供了通过聚合单体制备的聚合物。这些聚合物可能用于将活性物质传递给受试者、组织、生物样本或细胞。还提供了制备这些聚合物的方法、包含这些聚合物的组合物和试剂盒，以及涉及这些聚合物或组合物的使用方法（例如，用于传递活性物质、治疗疾病、预防疾病、诊断疾病）。硼酸酯基团的结构可以进行微调，以便微调与传递给受试者、生物样本、组织或细胞相关的性质。
• ABHD6 AND DUAL ABHD6/MGL INHIBITORS AND THEIR USES
  申请人：Malamas Michael

  公开号：US20190152917A1

  公开（公告）日：2019-05-23

  Provided herein are compounds and pharmaceutical compositions for selectively inhibiting serine hydrolase a/b-hydrolase domain 6 (ABHD6) and dually inhibiting ABHD6 and monoacylglycerol lipase (MGL). The compounds and pharmaceutical compositions disclosed herein are useful for treating a number of therapeutic conditions related to cannabinergic receptor function such as pain, inflammation, neuropathy, neurodegenerative diseases, anxiety disorders, motor function disorder, metabolic disorder, glaucoma and chemotherapy-induced nausea and vomiting and cancer.

  本文提供了一些化合物和药物组合物，用于选择性抑制丝氨酸水解酶a/b-水解酶结构域6（ABHD6），以及双重抑制ABHD6和单酰基甘油脂酶（MGL）。本文披露的化合物和药物组合物对治疗与大麻受体功能相关的多种治疗条件具有用处，如疼痛、炎症、神经病变、神经退行性疾病、焦虑症、运动功能障碍、代谢紊乱、青光眼、化疗引起的恶心和呕吐以及癌症。
• DEGRADABLE POLYMERS OF A CYCLIC SILYL ETHER AND USES THEREOF
  申请人：Massachusetts Institute of Technology

  公开号：US20200055879A1

  公开（公告）日：2020-02-20

  The present disclosure provides cyclic silyl ethers of the formula: and salts thereof. The cyclic silyl ethers may be useful as monomers for preparing polymers. Also described herein are polymers prepared by polymerizing a cyclic silyl ether and optionally one or more additional monomers. The polymers may be degradable (e.g., biodegradable). One or more O—Si bonds of the polymers may be the degradation sites. Also described herein are compositions and kits including the cyclic silyl ethers or polymers; methods of preparing the polymers; and methods of using the polymers, compositions, and kits.

  本公开提供了下述结构的环状硅醚及其盐。这些环状硅醚可能用作制备聚合物的单体。本文还描述了通过聚合环状硅醚以及可选地使用一个或多个额外单体制备的聚合物。这些聚合物可能是可降解的（例如，生物降解的）。聚合物的一个或多个O—Si键可能是降解位点。本文还描述了包括环状硅醚或聚合物的组合物和套装；制备聚合物的方法；以及使用聚合物、组合物和套装的方法。
• RADIOFLUORINATION METHODS
  申请人：Srinivasan Ananth

  公开号：US20090317326A1

  公开（公告）日：2009-12-24

  The present invention relates to radiolabelled substitute benzene compounds for diagnostic imaging. The present invention provides methods for preparation of such compounds, in particular, preparation of novel compounds which serve as precursors for 18 F-labeling, and the use of thus 18 F-labeled compounds for diagnostic imaging.

  本发明涉及用于诊断成像的放射性标记替代苯化合物。本发明提供了制备这种化合物的方法，特别是制备作为18F标记的前体的新化合物的方法，以及使用这样18F标记的化合物进行诊断成像的方法。
• Targeted Drug-Formaldehyde Conjugates and Methods of Making and Using the Same
  申请人：Koch H. Tad

  公开号：US20070275911A1

  公开（公告）日：2007-11-29

  The invention provides a prodrug platform technology for improving the therapeutic value of a variety of parent drug compounds by altering and improving drug characteristics such as aqueous solubility, hydrolytic stability, therapeutic index, toxicity profile, pharmacolcinetics and selectivity while allowing the potential for synthetic elaboration. The prodrug platform is particularly well suited for targeting therapeutic drugs, including anti-tumor drugs and antibiotics, to specific receptors on target cells (e.g., cancer cells and bacteria). The platform is a technology for providing an improved, preactivated form of a therapeutic drug, and for optionally targeting such drug to target cells or biological molecules. The invention is broadly applicable to many different therapeutic drugs, as well as to a variety of diseases and conditions, including a variety of forms of cancer and bacterial infections.

  本发明提供了一种前药平台技术，通过改变和改进药物特性，如水溶性、水解稳定性、治疗指数、毒性谱、药代动力学和选择性，从而提高各种原始药物化合物的治疗价值，同时允许潜在的合成扩展。该前药平台特别适用于将治疗药物，包括抗肿瘤药物和抗生素，定向靶向到目标细胞（例如癌细胞和细菌）上的特定受体。该平台是一种提供改进的、预激活形式的治疗药物的技术，并可选择性地将该药物定向到目标细胞或生物分子。本发明广泛适用于许多不同的治疗药物，以及多种癌症和细菌感染等不同疾病和病况。