N-[2-(2,5-dioxopyrrol-1-yl)ethyl]-2-(4-methylphenyl)acetamide

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-[2-(2,5-dioxopyrrol-1-yl)ethyl]-2-(4-methylphenyl)acetamide
• 化学式: C₁₅H₁₆N₂O₃
• 分子量: 272.3
• InChiKey: HWOCDAOVZHVSAE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  20
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  66.5
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• CONJUGATES AND SMALL MOLECULES WHICH INTERACT WITH THE CD16A RECEPTOR
  申请人："Biointegrator" Limited Liability Company (OOO "Biointegrator")

  公开号：EP2947074A1

  公开（公告）日：2015-11-25

  The invention is related to medicine, in particular, to oncology and immunology. The novel compounds of the general formula 1 or 2, exhibiting affinity for CD16a receptor have been proposed. There were also proposed novel modified proteins active towards CD16a receptor, selected from antibody or autogen conjugated by a modifying compound selected from compound of the general formula 1 or 2, which stimulate and direct antibody-dependent cellular cytotoxicity. The novel modified proteins (conjugates) could be used for destruction of definite targeted group of cells in organism, for example, cancerous cells or autoimmune lymphocytes. There were also proposed methods for conjugate preparation, pharmaceutical composition, and medicament, comprising modified proteins for treating oncology and autoimmune diseases.

  本发明涉及医学，特别是肿瘤学和免疫学。已经提出了对 CD16a 受体具有亲和力的通式 1 或 2 的新型化合物。此外，还提出了对 CD16a 受体具有活性的新型修饰蛋白，这些蛋白选自抗体或自体原，与选自通式 1 或 2 化合物的修饰化合物共轭，可刺激和引导抗体依赖性细胞毒性。新型修饰蛋白（共轭物）可用于消灭生物体内的特定目标细胞群，例如癌细胞或自身免疫淋巴细胞。此外，还提出了包含修饰蛋白质的共轭物制备方法、药物组合物和药品，用于治疗肿瘤和自身免疫性疾病。
• COMPOUNDS FOR POSITRON EMISSION TOMOGRAPHY
  申请人：Endocyte, Inc.

  公开号：EP3533473A2

  公开（公告）日：2019-09-04

  Described herein are compounds, compositions, and methods for diagnosing and/or monitoring pathogenic disease using positron emission tomography. Also described are conjugates of the formula B-L-P, wherein B is a radical of a targeting agent selected from vitamin receptor binding ligands (such as folate), PSMA binding ligands, or PSMA inhibitors; L is a divalent linker comprising aspartic acid, lysine, or arginine, and P is a radical of an imaging agent or radiotherapy agent, such as a radionuclide or radionuclide containing group, or a radical of a compound capable of binding a radionuclide, such as a metal chelating group.

  本文描述了利用正电子发射断层扫描诊断和/或监测致病性疾病的化合物、组合物和方法。还描述了式 B-L-P 的共轭物，其中 B 是选自维生素受体结合配体（如叶酸）、PSMA 结合配体或 PSMA 抑制剂的靶向药的基团；L 是由天冬氨酸、赖氨酸或精氨酸组成的二价连接体，P 是成像剂或放疗剂的基团，如放射性核素或含放射性核素的基团，或能结合放射性核素的化合物的基团，如金属螯合基团。
• Compounds for Positron Emission Tomography
  申请人：ENDOCYTE, INC.

  公开号：US20160287731A1

  公开（公告）日：2016-10-06

  Described herein are compounds, compositions, and methods for diagnosing and/or monitoring pathogenic disease using positron emission tomography. Also described are conjugates of the formula B-L-P, wherein B is a radical of a targeting agent selected from vitamin receptor binding ligands (such as folate), PSMA binding ligands, or PSMA inhibitors; L is a divalent linker comprising aspartic acid, lysine, or arginine, and P is a radical of an imaging agent or radiotherapy agent, such as a radionuclide or radionuclide containing group, or a radical of a compound capable of binding a radionuclide, such as a metal chelating group.
• [EN] CONJUGATES AND SMALL MOLECULES WHICH INTERACT WITH THE CD16A RECEPTOR<br/>[FR] CONJUGUÉS ET MOLÉCULES DE FAIBLES DIMENSIONS RÉAGISSANT AVEC LE RÉCEPTEUR CD16A
  申请人：BIOINTEGRATOR LTD LIABILITY COMPANY OOO BIOINTEGRATOR

  公开号：WO2014112898A1

  公开（公告）日：2014-07-24

  Изобретение относится к области медицины, в частности к онкологии и иммунологии. Предложены новые соединения общей формулы (1) или (2). обладающие сродством к CD16a. Предложены новые модифицированные белки, активные в отношении CD16a рецептора, выбранные из антитела или аутогена, конъюгированные модифицирующим соединением, выбранным из соединения общей формулы (1) или (2). усиливающие и направляющие антитело-зависимую клеточную цитотоксичность. Новые модифицированные белки (конъюгаты) могут быть использованы для уничтожения в организме определенной целевой группы клеток, например, раковых клеток или аутоиммунных лимфоцитов. Предложены также способы получения конъюгатов, фармацевтическая композиция и лекарственное средство, содержащие модифицированные белки для лечения онкологических и аутоиммунных заболеваний.
• [EN] COMPOUNDS FOR POSITRON EMISSION TOMOGRAPHY<br/>[FR] COMPOSÉS POUR LA TOMOGRAPHIE PAR ÉMISSION DE POSITRONS
  申请人：ENDOCYTE INC

  公开号：WO2015073678A1

  公开（公告）日：2015-05-21

  Described herein are compounds, compositions, and methods for diagnosing and/or monitoring pathogenic disease using positron emission tomography. Also described are conjugates of the formula B-L-P, wherein B is a radical of a targeting agent selected from vitamin receptor binding ligands (such as folate), PSMA binding ligands, or PSMA inhibitors; L is a divalent linker comprising aspartic acid, lysine, or arginine, and P is a radical of an imaging agent or radiotherapy agent, such as a radionuclide or radionuclide containing group, or a radical of a compound capable of binding a radionuclide, such as a metal chelating group.