3-(3-(2,5-dioxopyrrolidin-1-ylmethyl)phenyl)-5-isobutylthiophene-2-(N-butoxycarbonyl)sulfonamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩类
• 英文名称: 3-(3-(2,5-dioxopyrrolidin-1-ylmethyl)phenyl)-5-isobutylthiophene-2-(N-butoxycarbonyl)sulfonamide
• 英文别名: N-butyloxycarbonyl-3-(3-pyrrolidine-2,5-dione-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide；butyl N-[3-[3-[(2,5-dioxopyrrolidin-1-yl)methyl]phenyl]-5-(2-methylpropyl)thiophen-2-yl]sulfonylcarbamate
• 化学式: C₂₄H₃₀N₂O₆S₂
• 分子量: 506.644
• InChiKey: FEXQGBIWZJBQEB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  34
• 可旋转键数：
  11
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  147
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  3-溴苯甲醇 在 吡啶 、 四(三苯基膦)钯 、 四溴化碳 、 potassium tert-butylate 、 三氯化硼 、 4-吡咯烷基吡啶 、 三苯基膦 、 sodium hydroxide 作用下， 以 1,4-二氧六环 、 乙醇 、 正己烷 、 二氯甲烷 、 水 、 N,N-二甲基甲酰胺 、 甲苯 为溶剂， 反应 6.5h， 生成 3-(3-(2,5-dioxopyrrolidin-1-ylmethyl)phenyl)-5-isobutylthiophene-2-(N-butoxycarbonyl)sulfonamide
  参考文献：
  名称：

  From the First Selective Non-Peptide AT₂ Receptor Agonist to Structurally Related Antagonists

  摘要：

  A para substitution pattern of the phenyl ring is a characteristic feature of the first reported selective AT(2) receptor agonist M024/C21 (1) and all the nonpeptidic AT(2) receptor agonists described so far. Two series of compounds structurally related to 1 but with a meta substitution pattern have now been synthesized and biologically evaluated for their affinity to the AT(1) and AT(2) receptors. A high AT(2)/AT(1) receptor selectivity was obtained with all 41 compounds synthesized, and the majority exhibited K-i ranging from 2 to 100 nM. Five compounds were evaluated for their functional activity at the AT(2) receptor, applying a neurite outgrowth assay in NG108-15 cells.. Notably, four of the five compounds, with representatives from both series, acted as potent AT(2) receptor antagonists. These compounds were found to be considerably more effective than PD 123,319, the standard AT(2) receptor antagonist used in most laboratories. No AT(2) receptor antagonists were previously reported among the derivatives with a para substitution pattern. Hence, by a minor modification of the agonist 1 it could be transformed into the antagonist, compound 38. These compounds should serve as valuable tools in the assessment of the role of the AT(2) receptor in more complex physiological models.

  DOI：

  10.1021/jm2015099

文献信息

• CORONAVIRUS VACCINE
  申请人：BioNTech RNA Pharmaceuticals GmbH

  公开号：EP3901261A1

  公开（公告）日：2021-10-27

  This disclosure relates to the field of RNA to prevent or treat coronavirus infection. In particular, the present disclosure relates to methods and agents for vaccination against coronavirus infection and inducing effective coronavirus antigen-specific immune responses such as antibody and/or T cell responses. Specifically, in one embodiment, the present disclosure relates to methods comprising administering to a subject RNA encoding a peptide or protein comprising an epitope of SARS-CoV-2 spike protein (S protein) for inducing an immune response against coronavirus S protein, in particular S protein of SARS-CoV-2, in the subject, i.e., vaccine RNA encoding vaccine antigen.

  该披露涉及RNA领域，用于预防或治疗冠状病毒感染。具体来说，本披露涉及用于预防冠状病毒感染和诱导有效的冠状病毒抗原特异性免疫应答（如抗体和/或T细胞应答）的方法和药剂。具体而言，在一种实施方式中，本披露涉及通过向受试者给予编码SARS-CoV-2尖刺蛋白（S蛋白）表位的肽或蛋白的RNA来诱导免疫应答，特别是在受试者中诱导对冠状病毒S蛋白的免疫应答，即编码疫苗抗原的疫苗RNA。
• [EN] ALKYLATED NUCLEOSIDES, AND COMPOSITIONS AND METHODS THEREOF FOR NUCLEIC ACID DELIVERY<br/>[FR] NUCLÉOSIDES ALKYLÉS, COMPOSITIONS ET PROCÉDÉS ASSOCIÉS POUR L'ADMINISTRATION D'ACIDES NUCLÉIQUES
  申请人：MICROVASCULAR THERAPEUTICS LLC

  公开号：WO2021142059A1

  公开（公告）日：2021-07-15

  The invention provides novel compounds, compositions and formulations of liposomes, microbubbles and/or nanodroplets, and emulsions thereof, that are useful in delivery of various nucleic acids and genes (e.g., single stranded RNA, DNA, si-RNA and CRISPR constructs), as well as methods of preparation and use thereof including methods of imaging and gene delivery using ultrasound activation.

  本发明提供了新型化合物、组合物和脂质体、微气泡和/或纳米液滴以及它们的乳化物，这些化合物和组合物在传递各种核酸和基因（例如单链RNA、DNA、siRNA和CRISPR构建）方面是有用的，以及它们的制备和使用方法，包括使用超声激活的成像和基因传递方法。
• Tricyclic Angiotensin II Agonists
  申请人：Alterman Mathias

  公开号：US20090215847A1

  公开（公告）日：2009-08-27

  There is provided compounds of formula I, wherein the dotted line, X 1 , X 2 , X 3 , A, Y 1 , Y 2 , Y 3 , Y 4 , Z 1 , Z 2 , R 2 and R 3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.

  提供了一些公式为I的化合物，其中虚线，X1，X2，X3，A，Y1，Y2，Y3，Y4，Z1，Z2，R2和R3的含义在说明中给出，并且其药学上可接受的盐，这些化合物可用作AT2受体的选择性激动剂，因此特别适用于治疗胃肠疾病，如消化不良，肠易激综合征和多器官功能障碍等，以及心血管疾病。
• Tricyclic angiotensin II agonists
  申请人：Vicore Pharma AB

  公开号：US08067418B2

  公开（公告）日：2011-11-29

  There is provided compounds of formula I, wherein the dotted line, X1, X2, X3, A, Y1, Y2, Y3, Y4, Z1, Z2, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.

  提供了公式I的化合物，其中虚线、X1、X2、X3、A、Y1、Y2、Y3、Y4、Z1、Z2、R2和R3的含义在描述中给出，并且其药学上可接受的盐，这些化合物可用作AT2受体的选择性激动剂，因此，特别适用于治疗胃肠疾病，如消化不良、肠易激综合征和多器官功能障碍等，以及心血管疾病。
• IMMUNITY ENHANCING COMPOSITION INCLUDING IMMUNE RESPONSE REGULATOR AND CATIONIC LIPOSOME, AND USE OF SAME
  申请人：Eyegene Inc.

  公开号：EP3533464A1

  公开（公告）日：2019-09-04

  The present invention relates to an immunity enhancing composition including an immune response regulator having a novel structure and, more specifically, to an immunity enhancing composition and a use of the same, wherein the immunity enhancing composition includes a lipopolysaccharide (LPS) analogue with reduced toxicity, and a cationic liposome. The present invention overcomes the physicochemical instability of a liposome, is advantageous in terms of production, transportation, and storage, and improves stability, thus being beneficial as an immune delivery system. In addition, the present invention includes an antigen, an immune response regulator, and a cationic liposome, and thus exhibits an enhanced immunity-improving effect compared to the case in which an immune response regulator is used alone.

  本发明涉及一种免疫增强组合物，其中包括一种具有新型结构的免疫反应调节剂，更具体地说，涉及一种免疫增强组合物及其用途，其中免疫增强组合物包括一种毒性降低的脂多糖（LPS）类似物和一种阳离子脂质体。本发明克服了脂质体的理化不稳定性，在生产、运输和储存方面具有优势，并提高了稳定性，因此有利于作为免疫传递系统。此外，本发明包括抗原、免疫反应调节剂和阳离子脂质体，因此与单独使用免疫反应调节剂的情况相比，本发明具有更强的免疫增强效果。