(2R)-2-(naphthalen-1-ylmethyl)pyrrolidin-1-ium-2-carboxylate

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: (2R)-2-(naphthalen-1-ylmethyl)pyrrolidin-1-ium-2-carboxylate
• 化学式: C16H17NO2
• 分子量: 255.31
• InChiKey: XUIISGXVNJTYLV-MRXNPFEDSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  49.3
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• [EN] CONJUGATES FOR SELECTIVE RESPONSIVENESS TO VICINAL DIOLS<br/>[FR] CONJUGUÉS POUR UNE RÉACTIVITÉ SÉLECTIVE À DES DIOLS VICINAUX
  申请人：PROTOMER TECH INC

  公开号：WO2021202802A1

  公开（公告）日：2021-10-07

  Embodiments of the present disclosure relate to sensors that can selectively bind to specific vicinal diols in the presence of other diols. These boronated vicinal diol-responsive sensor compounds can sense levels of specific vicinal diols and respond to these molecules in the body. In certain embodiments, the vicinal diol is a cis diol, for example, a hexose such as glucose. In certain embodiments the sensors are conjugated to a drug substance, and the sensors may change the biophysical characteristics, pharmacokinetics, and/or activity of the drug substance in response to the vicinal diol. The drug substance may be or include a polypeptide, such as an insulin, a human endocrine or incretin peptide, or an analogue thereof, and may contain one or more modified amino acids containing a vicinal diol-responsive sensor.

  本公开的实施例涉及传感器，该传感器可以在其他二醇存在的情况下选择性地结合特定的邻二醇。这些硼化邻二醇响应传感器化合物可以感知特定邻二醇的水平，并对这些分子在体内做出反应。在某些实施例中，邻二醇是顺式二醇，例如六糖，如葡萄糖。在某些实施例中，传感器与药物物质结合，传感器可以改变药物物质的生物物理特性，药代动力学和/或活性，以响应邻二醇。药物物质可以是或包括多肽，例如胰岛素，人类内分泌或肠促素肽或其类似物，并且可能包含一个或多个含有邻二醇响应传感器的修饰氨基酸。
• Fap-activated therapeutic agents, and uses related thereto
  申请人：BACH BIOSCIENCES, LLC

  公开号：US11033525B2

  公开（公告）日：2021-06-15

  Disclosed are prodrugs of cytotoxic anthracyclines (such as doxorubicin) and other therapeutic agents that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of cytotoxic and other agents to FAP-expressing tissues, including cancer (e.g., solid tumors). Also provided are pharmaceutical compounds comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation, e.g., cancer, fibrosis, and inflammation.

  所公开的是细胞毒性蒽环类（如多柔比星）和其他治疗剂的原药，它们可被成纤维细胞活化蛋白（FAP）选择性地裂解和激活。这些原药可用于向表达 FAP 的组织（包括癌症（如实体瘤））靶向输送细胞毒性药物和其他药物。此外，还提供了包含这些原药的药物化合物，以及使用这些原药治疗以 FAP 上调为特征的疾病（如癌症、纤维化和炎症）的方法。
• [EN] PEPTIDES AND USE THEREOF<br/>[FR] PEPTIDES ET LEUR UTILISATION
  申请人：ANEXIGEN INC

  公开号：WO2021081110A2

  公开（公告）日：2021-04-29

  Described herein are peptides comprising anti-microbial activity. Such peptides in some embodiments are used as pharmaceutical compositions to treat infectious diseases, such as bacterial infections. In some embodiments, the bacterial infections are caused by multi-drug resistant bacteria.
• [EN] AROMATIC BORON-CONTAINING COMPOUNDS AND INSULIN ANALOGS<br/>[FR] COMPOSÉS AROMATIQUES CONTENANT DU BORE ET ANALOGUES D'INSULINE
  申请人：[en]PROTOMER TECHNOLOGIES INC.

  公开号：WO2022109078A1

  公开（公告）日：2022-05-27

  The present disclosure relates to novel compounds that include one or more aromatic boron-containing groups. The present disclosure further relates to pharmaceutical compositions containing such compounds, and their use in prevention and treatment of disorders, such as hyperglycemia, type 2 diabetes, impaired glucose tolerance, type 1 diabetes, obesity, metabolic syndrome X, or dyslipidemia, diabetes during pregnancy, pre-diabetes, Alzheimer's disease, MODY 1, MODY 2 or MODY 3 diabetes, mood disorders, and psychiatric disorders.