2-(4-Methoxyphenyl)-3-(2-phenylethyl)-1,3-thiazolidin-4-one

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: 2-(4-Methoxyphenyl)-3-(2-phenylethyl)-1,3-thiazolidin-4-one
• 化学式: C₁₈H₁₉NO₂S
• 分子量: 313.4
• InChiKey: XSZFNGBSMIARBY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  22
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  54.8
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• Targeted polymeric inflammation-resolving nanoparticles
  申请人：The Brigham and Women's Hospital, Inc.

  公开号：US10314917B2

  公开（公告）日：2019-06-11

  Sub-100 micron multimodal nanoparticles have four main components: 1) a target element (peptides, lipids, antibodies, small molecules, etc.) that can selectively bind to cells, tissues, or organs of the body; 2) a diagnostic agent such as a fluorophore or NMR contrast agent that allows visualization of nanoparticles at the site of delivery and/or a therapeutic or prophylactic agent; 3) an outside “stealth” layer that allows the particles to evade recognition by immune system components and increase particle circulation half-life; and 4) a biodegradable polymeric material, forming an inner core which can carry therapeutics and release the payloads at a sustained rate after systemic, intraperitoneal, or mucosal administration. These particles possess excellent stability, high loading efficiency, multiple agent encapsulation, targeting and imaging. They are targeted to sites of, or associated with, inflammation caused by a disease, disorder; trauma, chemotherapy or radiation.

  100 微米以下的多模式纳米粒子有四个主要成分：1) 目标元素（肽、脂质、抗体、小分子等），可选择性地与细胞、组织或人体器官结合；2) 诊断剂，如荧光团或核磁共振成像剂。2) 一种诊断剂，如荧光团或核磁共振造影剂，可使纳米粒子在输送部位可视化，和/或一种治疗或预防剂；3) 外层 "隐形 "层，可使微粒避开免疫系统成分的识别，并延长微粒的循环半衰期；以及 4) 生物可降解聚合物材料，形成内核，可携带治疗剂，并在全身、腹腔或粘膜给药后持续释放有效载荷。这些微粒具有出色的稳定性、高负载效率、多药剂封装、靶向性和成像性。它们可以靶向治疗由疾病、失调、创伤、化疗或放疗引起的炎症或与之相关的炎症部位。
• Mucus penetrating particles with high molecular weight and dense coatings
  申请人：The Johns Hopkins University

  公开号：US10668025B2

  公开（公告）日：2020-06-02

  Mucus penetrating particles (MPPs) include one or more core polymers, one or more therapeutic, prophylactic and/or diagnostic agents; and one or more surface modifying agents. The surface modifying agents coat the surface of the particle in a sufficient density to enhance the diffusion of the modified nanoparticles throughout the mucosa, relative to equivalent nanoparticles that are not surface modified. Nanoparticles can be sufficiently densely coated with poly(ethylene glycol) (PEG) with a molecular weight of from 10 kD to 40 kD or greater coated with a surface density from about 0.1 to about 100 molecules/100 nm2, preferably from about 0.5 to about 50 molecules/100 nm2, more preferably from about 0.9 to about 45 molecules/100 nm2.

  粘液渗透粒子（MPPs）包括一种或多种核心聚合物，一种或多种治疗、预防和/或诊断药剂，以及一种或多种表面修饰剂。相对于未进行表面修饰的等效纳米颗粒，表面修饰剂以足够的密度包覆颗粒表面，以增强修饰纳米颗粒在整个粘膜中的扩散。纳米颗粒可以充分致密地包覆分子量为 10 kD 至 40 kD 或更大的聚乙二醇 (PEG)，包覆的表面密度约为 0.1 至约 100 个分子/100 nm2，优选约 0.5 至约 50 个分子/100 nm2，更优选约 0.9 至约 45 个分子/100 nm2。
• Drug delivery composition and method of fabrication
  申请人：DIGNITY HEALTH

  公开号：US10952967B2

  公开（公告）日：2021-03-23

  The methods of manufacture of a drug delivery composition. In some aspects, the methods include providing an organic phase, a biologically active ingredient, and an aqueous phase with a desirable pH (e.g., a pH at which the active ingredient has increased solubility in the aqueous phase compared to at neutral pH). After mixing of one or more of the aforementioned components, the resultant mixture is processed to provide the desired drug delivery composition.

  给药组合物的制造方法。在某些方面，这些方法包括提供有机相、生物活性成分和具有理想 pH 值的水相（例如，与中性 pH 值相比，活性成分在水相中的溶解度增加的 pH 值）。将上述一种或多种成分混合后，对所得混合物进行加工，以提供所需的给药组合物。
• Decreased adhesivity receptor-targeted nanoparticles for Fn14-positive tumors
  申请人：UNIVERSITY OF MARYLAND, BALTIMORE

  公开号：US11045428B2

  公开（公告）日：2021-06-29

  Metastatic triple negative breast cancer (TNBC) still carries a dismal prognosis with the current treatment paradigms. The effectiveness of drug treatment for many solid tumors such as TNBC is limited by tumor heterogeneity, lack of tumor specificity, off-target toxicities, and transient therapeutic action(s). Strategies that provide tumor-specific, sustained concentrations of drugs to the tumors and tumor receptor-specific binding, while reducing off-target effects are needed to ensure sufficient tumor cell uptake within the primary and metastatic tumor microenvironment. The decreased non-specific adhesivity, receptor-targeted nanoparticle formulations (“DART” nanoparticles) of the invention were assessed for clinical potential in directing biological agents to the cell surface receptor Fn14, which is expressed in many solid cancer types, including TNBC primary tumors and metastatic lesions. They are contemplated for use against solid tumors, particularly brain tumors such as glioblastoma and breast cancer, including metastatic breast cancer.

  在目前的治疗模式下，转移性三阴性乳腺癌（TNBC）的预后仍然不容乐观。由于肿瘤异质性、缺乏肿瘤特异性、脱靶毒性和短暂的治疗作用，许多实体瘤（如 TNBC）的药物治疗效果受到限制。为了确保原发性和转移性肿瘤微环境中有足够的肿瘤细胞摄取，我们需要能向肿瘤提供肿瘤特异性、持续的药物浓度和肿瘤受体特异性结合的策略，同时减少脱靶效应。本发明的非特异性粘附性降低、受体靶向纳米粒子制剂（"DART "纳米粒子）在将生物制剂导向细胞表面受体 Fn14 方面的临床潜力得到了评估，Fn14 在许多实体瘤类型中都有表达，包括 TNBC 原发肿瘤和转移病灶。考虑将它们用于治疗实体瘤，特别是脑瘤，如胶质母细胞瘤和乳腺癌，包括转移性乳腺癌。
• Immunogenic peptides specific to BCMA and TACI antigens
  申请人：Dana-Farber Cancer Institute, Inc.

  公开号：US11517591B2

  公开（公告）日：2022-12-06

  This disclosure relates to immunogenic peptides that are specific to B-cell maturation antigen (BCMA) and Transmembrane activator and CAML interactor (TACI), and methods of use thereof.

  本公开涉及对 B 细胞成熟抗原（BCMA）和跨膜激活剂与 CAML 间体（TACI）特异的免疫原肽及其使用方法。