1-ethyl-3-methyl-pyrrolidine-2,5-dione | 65168-02-7

• 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: 1-ethyl-3-methyl-pyrrolidine-2,5-dione
• 英文别名: 1-Aethyl-3-methyl-pyrrolidin-2,5-dion；3-Methyl-N-ethylsuccinimid；1-Ethyl-3-methylpyrrolidine-2,5-dione
• CAS: 65168-02-7
• 化学式: C₇H₁₁NO₂
• 分子量: 141.17
• InChiKey: AIUFESORTUMJGT-UHFFFAOYSA-N

物化性质

• 沸点：
  115-117 °C(Press: 20.5 Torr)
• 密度：
  1.083±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.71
• 拓扑面积：
  37.4
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-ethyl-3-methyl-pyrrolidine-2,5-dione 以14%的产率得到
  参考文献：
  名称：

  KANAOKA Y.; OKAJIMA H.; HATANAKA Y., HETEROCYCLES, 1977, 8, SPEC. ISSUE, 339-344

  摘要：

  DOI：
• 作为产物：
  描述：

  alkaline earth salt of/the/ methylsulfuric acid 生成 1-ethyl-3-methyl-pyrrolidine-2,5-dione
  参考文献：
  名称：

  Kling, Chemische Berichte, 1897, vol. 30, p. 3041

  摘要：

  DOI：

文献信息

• [EN] ANTIBODY CONJUGATES COMPRISING TOLL-LIKE RECEPTOR AGONIST<br/>[FR] CONJUGUÉS D'ANTICORPS COMPRENANT UN AGONISTE DU RÉCEPTEUR DE TYPE TOLL
  申请人：NOVARTIS AG

  公开号：WO2017072662A1

  公开（公告）日：2017-05-04

  Provided herein are antibody conjugates comprising toll-like receptor agonists and the use of such conjugates for the treatment of cancer. In some embodiments, the conjugates comprise anti-HER2 antibodies.

  本文提供了包含Toll样受体激动剂的抗体偶联物，以及利用这些偶联物治疗癌症的用途。在某些实施例中，这些偶联物包括抗HER2抗体。
• [EN] TARGETED PLASMA PROTEIN DEGRADATION<br/>[FR] DÉGRADATION CIBLÉE DE PROTÉINES DE PLASMA
  申请人：NOVARTIS AG

  公开号：WO2021156792A1

  公开（公告）日：2021-08-12

  The present invention is directed to the bifunctional compounds and the use of such bifunctional compounds to lower plasma levels of extracellular target molecules by lysosomal degradation. Such bifunctional compounds have a cell surface receptor ligand covalently linked to a ligand that is capable of binding to an extracellular target molecule (such as a ligand for a growth factor, a cytokine, a chemokine, a hormone, a neurotransmitter, a capsid, a soluble receptor, an extracellular secreted protein, an antibody, a lipoprotein, an exosome, a virus, a cell, or a plasma membrane protein), where the cell surface receptor is associated with receptor mediated endocytosis, including asialoglycoprotein receptor (ASGPR) mediated lysosomal degradation and mannose-6-phosphate (M6PR) mediated lysosomal degradation. Pharmaceutical compositions comprising such bifunctional compounds and methods of treating a disease or disorder mediated by an extracellular molecule using such bifunctional compounds are also provided herein.

  本发明涉及双功能化合物及利用这种双功能化合物通过溶酶体降解降低细胞外靶分子血浆水平的用途。这种双功能化合物具有与细胞表面受体配体共价连接的配体，该配体能够结合到细胞外靶分子（例如生长因子、细胞因子、趋化因子、激素、神经递质、外壳蛋白、可溶性受体、细胞外分泌蛋白、抗体、脂蛋白、外泌体、病毒、细胞或血浆膜蛋白的配体），其中细胞表面受体与受体介导的内吞作用相关联，包括以阿斯利康蛋白受体（ASGPR）介导的溶酶体降解和甘露糖-6-磷酸（M6PR）介导的溶酶体降解。本文还提供了包括这种双功能化合物的药物组合物以及利用这种双功能化合物治疗通过细胞外分子介导的疾病或紊乱的方法。
• [EN] ANTIBACTERIAL AGENT<br/>[FR] AGENT ANTIBACTÉRIEN
  申请人：UNIV OXFORD INNOVATION LTD

  公开号：WO2016185200A1

  公开（公告）日：2016-11-24

  The invention provides a compound which is a peptide derivative of formula (1) as defined in the claims or a salt thereof: RG is H, -CH2-RGA or C1-12 hydrocarbyl optionally substituted with 1 to 4 substituents selected from -OR', -NO2, -CN, halogen and 5-6 membered heterocyclyl; or RG and RN1 together form a 5-6 membered heterocyclic ring which is optionally substituted with 1 to 3 substituents selected from Ra, -OR' and halogen; RGA is C1-11 hydrocarbyl optionally substituted with 1 to 4 substituents selected from -NR'R", -OR', -NO2, -CN, halogen and 5-6 membered heterocyclyl; RSis C1-16 hydrocarbyl, a 5-10 membered heterocyclyl or heteroaryl group, -(C1-4 alkylene)-RSA or -(C1-4 alkylene)-L-RSA; RSA is C1-16 hydrocarbyl, or a 5-10 membered heterocyclyl or heteroaryl group; L is -SO2-; and wherein RS and RSA are optionally substituted with a group Rb and/or from 1 to 5 substituents selected from Ra, -NR'R", -OR', -NO2, -CN, -C(O)R', -C(O)OR', -C(O)NR'R", -0-C(0)R', -N(R')-C(0)R", -SR', -S(O)R', -S(O)2R', -S(O)2OR', -P(O)(OR')(OR"), =O, -SiR'R"R" and halogen; or Rs and an RC1 together form a 5-6 membered heterocyclyl ring which is optionally substituted with 1 to 3 substituents selected from Ra, -OR' and halogen; Rb is phenyl, benzyl, C3-6 cycloalkyl or 5-6 membered heterocyclyl; Q is -C(O)-N(RN2)-, -C(O)-C(R'R")-, -C(O)-O- -N(RN2)-C(O)-, -C(R'R")- C(O)-, -O-C(O)-, -C(R'R")-C(R"'R"")-, -C(R'R")-O- -O-C(R'R")-, -C(R'R")-N(RN2)-, -N(RN2)-C(R'R")- or -C(R')=C(R")-; Z is a group selected from -C(O)-O-RO and -CN4R' (tetrazolyl); RO is H or C1-12 hydrocarbyl optionally substituted with 1 to 4 substituents selected from -NR'R", -OR', -NO2, -CN, -C(O)R', -C(O)OR', -C(O)NR'R", -O-C(O)R', -N(R')- C(O)R", -SR', -S(O)R', -S(O)2R', -S(O)2OR', -P(O)(OR')(OR"), =O, halogen and 5-6 membered heterocyclyl; or RO and an RC2 together form a 5-6 membered heterocyclyl ring which is optionally substituted with 1 to 3 substituents selected from Ra, -OR' and halogen; each RN1 and RN2 is independently H or C1-4 alkyl; each RC1, RC2, R', R", R" and R"" is independently H or C1-4 alkyl and is optionally substituted with 1 to 3 substituents selected from halogen, -OH and -O-C1-4 alkyl; and each Ra is independently C1-4 alkyl which is optionally substituted with 1 to 3 halogen atoms.

  该发明提供了一种化合物，其为以下公式（1）中所定义的肽衍生物或其盐：RG为H，-CH2-RGA或C1-12烃基，可选地取代为1至4个从-OR'，-NO2，-CN，卤素和5-6成员杂环基中选择的取代基；或RG和RN1一起形成一个5-6成员杂环环，可选地取代为1至3个从Ra，-OR'和卤素中选择的取代基；RGA为C1-11烃基，可选地取代为1至4个从-NR'R"，-OR'，- ，-CN，卤素和5-6成员杂环基中选择的取代基；RS为C1-16烃基，一个5-10成员杂环基或杂芳基，-(C1-4烷基)-RSA或-(C1-4烷基)-L-RSA；RSA为C1-16烃基，或一个5-10成员杂环基或杂芳基；L为-SO2-；其中RS和RSA可选地取代为一个基团Rb和/或从Ra，-NR'R"，-OR'，- ，-CN，-C(O)R'，-C(O)OR'，-C(O)NR'R"，-O-C(0)R'，-N(R')-C(0)R"，-SR'，-S(O)R'，-S(O)2R'，-S(O)2OR'，-P(O)(OR')(OR")，=O，-SiR'R"R"和卤素中选择的1至5个取代基；或Rs和RC1一起形成一个5-6成员杂环环，可选地取代为1至3个从Ra，-OR'和卤素中选择的取代基；Rb为苯基，苄基，C3-6环烷基或5-6成员杂环基；Q为-C(O)-N(RN2)-，-C(O)-C(R'R")-，-C(O)-O- -N(RN2)-C(O)-，-C(R'R")- C(O)-，-O-C(O)-，-C(R'R")-C(R"'R"")-，-C(R'R")-O- -O-C(R'R")-，-C(R'R")-N(RN2)-，-N(RN2)-C(R'R")-或-C(R')=C(R")-；Z为从-C(O)-O-RO和-CN4R'（四唑基）中选择的基团；RO为H或C1-12烃基，可选地取代为1至4个从-NR'R"，-OR'，- ，-CN，-C(O)R'，-C(O)OR'，-C(O)NR'R"，-O-C(O)R'，-N(R')-C(O)R"，-SR'，-S(O)R'，-S(O)2R'，-S(O)2OR'，-P(O)(OR')(OR")，=O，卤素和5-6成员杂环基中选择的取代基；或RO和RC2一起形成一个5-6成员杂环环，可选地取代为1至3个从Ra，-OR'和卤素中选择的取代基；每个RN1和RN2独立地为H或C1-4烷基；每个RC1，RC2，R'，R"，R"和R""独立地为H或C1-4烷基，并可选地取代为1至3个从卤素，-OH和-O-C1-4烷基中选择的取代基；每个Ra独立地为可选地取代为1至3个卤素原子的C1-4烷基。
• ANTIBODY DRUG CONJUGATES (ADCS) AND ANTIBODY PRODRUG CONJUGATES (APDCS) WITH ENZYMATICALLY CLEAVABLE GROUPS
  申请人：Bayer Pharma Aktiengesellschaft

  公开号：US20180169256A1

  公开（公告）日：2018-06-21

  The present invention relates to novel binder-prodrug conjugates (APDCs) where binders are conjugated with inactive precursor compounds of kinesin spindle protein inhibitors, and to antibody-drug conjugates ADCs and to processes for producing these APDCs and ADCs.

  这项发明涉及新型结合物-前药偶联物（APDCs），其中结合物与动力蛋白纺锤体抑制剂的非活性前体化合物偶联，以及抗体药物偶联物ADCs以及制备这些APDCs和ADCs的方法。
• Conjugates of Cell Binding Molecules with Cytotoxic Agents
  申请人：Zhao R. Yongxin

  公开号：US20170296663A1

  公开（公告）日：2017-10-19

  A conjugate of a potent cytotoxic agent with a cell-surface receptor binding molecule having a Formula (I), wherein T, L, m, n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , and R 13 are defined herein, can be used for targeted treatment of cancer, autoimmune disease, and infectious disease.

  一种有效的细胞毒性药物的共轭物，带有具有化学式（I）的细胞表面受体结合分子，其中T、L、m、n、R1、R2、R3、R4、R5、R6、R7、R8、R9、R10、R11、R12和R13在此有定义，可用于靶向治疗癌症、自身免疫疾病和传染性疾病。