4-Benzyl-10-oxa-4-azatricyclo[5.2.1.0^{2,6}]dec-8-ene-3,5-dione

• 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: 4-Benzyl-10-oxa-4-azatricyclo[5.2.1.0^{2,6}]dec-8-ene-3,5-dione
• 英文别名: 2-benzyl-3a,4,7,7a-tetrahydro-4,7-epoxyisoindole-1,3-dione
• 化学式: C₁₅H₁₃NO₃
• mdl: MFCD00553450
• 分子量: 255.273
• InChiKey: HPAYEMRCHCWDMA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  19
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.333
• 拓扑面积：
  46.6
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-Benzyl-10-oxa-4-azatricyclo[5.2.1.0^{2,6}]dec-8-ene-3,5-dione 以 甲苯 为溶剂， 以67 %的产率得到N-苄基马来酰亚胺
  参考文献：
  名称：

  金属有机框架中的可逆合成后修饰

  摘要：

  在这项工作中，使用热可逆呋喃-马来酰亚胺 Diels-Alder 化学在多元金属有机框架 (MTV-MOF) 中演示了可逆共价合成后修饰 (PSM)。 MOF 用侧挂呋喃官能团进行修饰，然后能够进行 PSM 的重复循环并用不同官能化的马来酰亚胺进行去修饰。可逆 PSM 的实现完全保留了 MOF 的结构完整性、结晶度和孔隙率。

  DOI：

  10.1002/anie.202317062
• 作为产物：
  描述：

  sodium;3a,4,7,7a-tetrahydro-4,7-epoxyisoindol-2-ide-1,3-dione 以83%的产率得到
  参考文献：
  名称：

  KUROSAKI, T.;MATSUMOTO, T.;SAWADA, K.;KURISHIMA, S.;NUMAKURA, T., J. PHOTOGR. SCI., 36,(1988) N 3, C. 122-124

  摘要：

  DOI：

文献信息

• PEPTIDE DEFORMYLASE INHIBITORS
  申请人：Qin Donghui

  公开号：US20090306066A1

  公开（公告）日：2009-12-10

  The present invention is directed to certain 2-(alkyl)-3-[2-(5-fluoro-4-pyrimidinyl)hydrazino]-3-oxopropyl}hydroxyformamide derivatives, compositions containing them, the use of such compounds in the inhibition of bacterial peptide deformylase (PDF) activity, and in the treatment of bacterial infections. Specifically, the invention is directed to compounds of formula (I): wherein R1, R2 and R3 are defined herein and to pharmaceutically acceptable salts thereof. The compounds of this invention are bacterial peptide deformylase inhibitors and can be useful in the treatment of bacterial infections.

  本发明涉及某些2-(烷基)-3-[2-(5-氟-4-嘧啶基)肼基]-3-氧代丙基}羟基甲酰胺衍生物，包含它们的组合物，这些化合物在抑制细菌肽变形酶（PDF）活性和治疗细菌感染方面的使用。具体而言，本发明涉及式（I）的化合物：其中R1，R2和R3在此定义，并且其药学上可接受的盐。本发明的化合物是细菌肽变形酶抑制剂，可用于治疗细菌感染。
• Modulated guanidine-containing polymers or nanoparticles
  申请人：Moon Joong Ho

  公开号：US10688189B1

  公开（公告）日：2020-06-23

  A modulated guanidine substituted polymer or nanoparticle has a guanidine moiety or on a plurality of repeating units of a polymer or on the surface of a nanoparticle where the guanidine moiety is modulated as a substituted amidinourea or amidinocarbamate or salt thereof. The modulated guanidine substituted polymer or nanoparticle can be prepared by direct amination of a N-Boc protected guanidine substituted conjugated polymer or N-Boc protected guanidine substituted nanoparticle, where an amine or alcohol is combined in solution or suspension with the protected conjugated polymer or nanoparticle and the resulting mixture is heated. The modulated guanidine substituted polymer or nanoparticle can be used in a cancer treatment formulation.

  调制胍取代聚合物或纳米粒子具有胍基，或位于聚合物的多个重复单元上，或位于纳米粒子的表面，其中胍基被调制为取代的脒基脲或脒基氨基甲酸酯或其盐。调制胍基取代的聚合物或纳米粒子可通过直接胺化 N-Boc 保护的胍基取代的共轭聚合物或 N-Boc 保护的胍基取代的纳米粒子来制备，胺或醇在溶液或悬浮液中与保护的共轭聚合物或纳米粒子结合，并加热所得混合物。调制后的胍基取代聚合物或纳米粒子可用于癌症治疗配方。
• Modified guanidine-containing polymers for biologic delivery
  申请人：Moon Joong Ho

  公开号：US11529315B1

  公开（公告）日：2022-12-20

  The subject invention provides materials and methods for intracellular deliver of molecules and/or therapeutic agents. The subject invention also provides methods for synthesizing polymeric systems and nanomaterials that enhance or assist the passage of molecules and/or therapeutic agents across biological membranes. The compound, polymer or nanoparticle of the subject invention comprises a modified guanidine moiety in a plurality of repeating units of a polymer or on the surface of a nanoparticle where the guanidine moiety comprises, for example, a carbamoyl or thiourea modification. The polymer or nanoparticle can be used in a cancer treatment formulation.

  本发明提供了用于细胞内输送分子和/或治疗剂的材料和方法。本发明还提供了合成聚合物系统和纳米材料的方法，这些聚合物系统和纳米材料可增强或辅助分子和/或治疗剂穿过生物膜。本发明的化合物、聚合物或纳米粒子包括聚合物多个重复单元中或纳米粒子表面上的改性胍基，其中胍基包括例如氨基甲酰基或硫脲基改性。聚合物或纳米粒子可用于癌症治疗配方。
• Carbamoylated Guanidine‐Containing Polymers for Non‐Covalent Functional Protein Delivery in Serum‐Containing Media
  作者：Alfonso Barrios、Marilen Estrada、Joong Ho Moon

  DOI：10.1002/anie.202116722

  日期：2022.3.14

  AbstractDespite the high potential of controlling cellular processes and treating various diseases by intracellularly delivered proteins, current delivery systems exhibit poor efficiency due to poor serum stability, cellular entry, and cytosolic availability of proteins. Here, we report a novel functional group, phenyl carbamoylated guanidine (Ph‐CG), that greatly enhances the delivery efficiency to various types of cells. Owing to the substantially lowered pKa, the hydrophobic Ph‐CG offers optimized inter‐macromolecular interactions via enhanced hydrogen‐bonding and hydrophobic interactions. The coplanarity of Ph‐CG also leads to the better intracellular entry of protein complexes. Intracellularly delivered apoptosis‐inducing enzymes and antibodies significantly induce cell viability inhibitions in a serum‐containing medium. The newly developed Ph‐CG can be introduced to various existing carriers, leading to the realization of future therapeutic protein delivery.
• OPTICAL FILM AND DISPLAY DEVICE INCLUDING SAME
  申请人：Samsung Electronics Co., Ltd.

  公开号：US20130172503A1

  公开（公告）日：2013-07-04

  An optical film including a polymer including a repeating unit A including a repeating unit represented by the following Chemical Formulas 1 to 3, or a combination thereof; and a repeating unit B derived from a monomer having an unsaturated bond copolymerizable with the repeating unit A, wherein the optical film has a short wavelength dispersion of an in-plane phase-difference value (R e ) (450 nm/550 nm) ranging from about 0.81 to about 1.20, and a long wavelength dispersion of an in-plane phase-difference value (R e ) (650 nm/550 nm) ranging from about 0.90 to about 1.18: wherein, in Chemical Formulas 1 to 3, the variables R 1 to R 21 are defined herein.