(2-Methylpropan-2-yl)oxycarbonyl piperidine-2-carboxylate | 1033132-65-8

• 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: (2-Methylpropan-2-yl)oxycarbonyl piperidine-2-carboxylate
• CAS: 1033132-65-8
• 化学式: C₁₁H₁₉NO₄
• 分子量: 229.276
• InChiKey: ZTRIIKQVNPJAHK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  16
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.82
• 拓扑面积：
  64.6
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  (2-Methylpropan-2-yl)oxycarbonyl piperidine-2-carboxylate 、 对硝基苯磺酰氯 在 吡啶 作用下， 以 二氯甲烷 为溶剂， 生成
  参考文献：
  名称：

  Potent Non-Nucleoside Inhibitors of the Measles Virus RNA-Dependent RNA Polymerase Complex

  摘要：

  Measles virus (MV) is one of the most infectious pathogens known. In spite of the existence of a vaccine, approximately 350000 deaths/year result from MV or associated complications. Antimeasles compounds Could conceivably diminish these statistics and provide a therapy that complements vaccine treatment. We recently described a high-throughput screening hit compound 1 (16677) against MV-infected cells with the capacity to eliminate viral reproduction at 250 nM by inhibiting the action of the virus's RNA-dependent RNA polymerase complex (RdRp). The compound, 1-methyl-3-(trifluoroi-nethyl)-N-[4-sulfonylphenyl]-1H-pyrazole-5-carboxamide, 1 carries a critical CF3 moiety on the 1,2-pyrazole ring. Elaborating on the preliminary structure-activity (SAR) study, the present work presents the synthesis and SAR of a much broader range of low nanomolar nonpeptidic MV inhibitors and speculates on the role of the CF3 functionality.

  DOI：

  10.1021/jm701239a

文献信息

• [EN] MODULATORS OF THE INTEGRATED STRESS RESPONSE PATHWAY<br/>[FR] MODULATEURS DE LA VOIE DE RÉPONSE AU STRESS INTÉGRÉE
  申请人：EVOTEC INT GMBH

  公开号：WO2020216766A1

  公开（公告）日：2020-10-29

  The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts, solvates, hydrates, tautomers or stereoisomers thereof, wherein R1, R2, R2a, R3, Ra2, Ra4, Ra5, Ra6, Ra7, X1, X1a, A1 and A2 have the meaning as indicated in the description and claims. The invention further relates to pharmaceutical compositions comprising said compounds, their use as medicament and in a method for treating and preventing of one or more diseases or disorders associated with integrated stress response.

  本发明涉及具有式（I）的化合物或其药学上可接受的盐、溶剂化合物、水合物、互变异构体或立体异构体，其中R1、R2、R2a、R3、Ra2、Ra4、Ra5、Ra6、Ra7、X1、X1a、A1和A2的含义如描述和权利要求中所示。该发明还涉及包含所述化合物的药物组合物，其用作药物以及用于治疗和预防与整合应激反应相关的一种或多种疾病或紊乱的方法。
• [EN] PARAMYXOVIRUS FAMILY INHIBITORS AND METHODS OF USE THEREOF<br/>[FR] INHIBITEURS DE LA FAMILLE DES PARAMYXOVIRUS ET PROCÉDÉS D'UTILISATION DE CEUX-CI
  申请人：UNIV EMORY

  公开号：WO2008098239A2

  公开（公告）日：2008-08-14

  [EN] Embodiments of the present disclosure include methods for identifying a compound or compounds useful as therapeutic agents in the treatment of paramyxovirus infections, compounds for the treatment of measles, and high throughput screening methods for identifying compounds capable of inhibiting the proliferation of a paramyxovirus.
  [FR] L'invention concerne des procédés d'identification d'un composé ou de composés utiles en tant qu'agents thérapeutiques dans le traitement d'infections à paramyxovirus, de composés pour le traitement de la rougeole et des procédés de criblage à haut débit pour l'identification de composés capables d'inhiber la prolifération d'un paramyxovirus.
• Potent Non-Nucleoside Inhibitors of the Measles Virus RNA-Dependent RNA Polymerase Complex
  作者：Aiming Sun、Jeong-Joong Yoon、Yan Yin、Andrew Prussia、Yutao Yang、Jaeki Min、Richard K. Plemper、James P. Snyder

  DOI：10.1021/jm701239a

  日期：2008.7

  Measles virus (MV) is one of the most infectious pathogens known. In spite of the existence of a vaccine, approximately 350000 deaths/year result from MV or associated complications. Antimeasles compounds Could conceivably diminish these statistics and provide a therapy that complements vaccine treatment. We recently described a high-throughput screening hit compound 1 (16677) against MV-infected cells with the capacity to eliminate viral reproduction at 250 nM by inhibiting the action of the virus's RNA-dependent RNA polymerase complex (RdRp). The compound, 1-methyl-3-(trifluoroi-nethyl)-N-[4-sulfonylphenyl]-1H-pyrazole-5-carboxamide, 1 carries a critical CF3 moiety on the 1,2-pyrazole ring. Elaborating on the preliminary structure-activity (SAR) study, the present work presents the synthesis and SAR of a much broader range of low nanomolar nonpeptidic MV inhibitors and speculates on the role of the CF3 functionality.