O-[(5-氨基-2-苯基-7-苯并恶唑基)甲基]-3,5-二氯-L-酪氨酸 | 1037592-40-7

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: O-[(5-氨基-2-苯基-7-苯并恶唑基)甲基]-3,5-二氯-L-酪氨酸
• 中文别名: LAT1抑制剂(JPH203)
• 英文名称: L-Tyrosine, O-((5-amino-2-phenyl-7-benzoxazolyl)methyl)-3,5-dichloro-
• 英文别名: (2S)-2-amino-3-[4-[(5-amino-2-phenyl-1,3-benzoxazol-7-yl)methoxy]-3,5-dichlorophenyl]propanoic acid
• CAS: 1037592-40-7
• 化学式: C₂₃H₁₉Cl₂N₃O₄
• 分子量: 472.3
• InChiKey: XNRZJPQTMQZBCE-SFHVURJKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  32
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.13
• 拓扑面积：
  125
• 氢给体数：
  3
• 氢受体数：
  7

文献信息

• NANNOCYSTIN PROCESS AND PRODUCTS
  申请人：THE RESEARCH FOUNDATION FOR THE STATE UNIVERSITY OF NEW YORK

  公开号：US20170320893A1

  公开（公告）日：2017-11-09

  Described herein is a process for the total synthesis of macrolactones and macrolactams of formula I including E- and Z-configuration thereof, in particular, nannocystins.

  本文描述了一种用于合成式I的大环内酯和大环内酰胺的全合成过程，包括其E-和Z-构型，特别是纳诺西斯汀。
• METHOD FOR PREDICTING EFFICACY OF ANTI-PD-1 ANTIBODY OR ANTI-PD-L1 ANTIBODY THERAPY, METHOD FOR EVALUATING CANCER GRADE, AND METHOD FOR ENHANCING EFFICACY OF ANTI-PD-1 ANTIBODY OR ANTI-PD-L1 ANTIBODY THERAPY
  申请人：J-Pharma Co., Ltd.

  公开号：EP3709021A1

  公开（公告）日：2020-09-16

  The present invention aims at providing a method for predicting a response to an anti-PD-1 antibody or anti-PD-Ll antibody therapy based on a new biomarker and a method for evaluating a malignancy of cancer. The method for predicting a response of a subject to an anti-PD-1 antibody or anti-PD-Ll antibody therapy according to the present invention comprises steps of: measuring an expression level of LAT1 in a sample collected from a cancer tissue of the subject; and predicting a response of the subject to the anti-PD-1 antibody or anti-PD-Ll antibody therapy based on the expression level of LAT1. The method for evaluating a malignancy of cancer in a subject, comprising steps of: staining a sample collected from a cancer tissue of the subject with an anti-LAT1 antibody and an anti-PD-Ll antibody; and evaluating a malignancy of the cancer in the subject based on a presence or absence of a LAT1-positive and PD-L1-positive site.

  本发明旨在提供一种基于新生物标志物的预测抗PD-1抗体或抗PD-Ll抗体治疗反应的方法，以及一种评估癌症恶性程度的方法。根据本发明的预测受试者对抗PD-1抗体或抗PD-Ll抗体疗法的反应的方法包括以下步骤：测量从受试者的癌症组织中采集的样本中LAT1的表达水平；根据LAT1的表达水平预测受试者对抗PD-1抗体或抗PD-Ll抗体疗法的反应。评估受试者癌症恶性程度的方法，包括以下步骤：用抗LAT1抗体和抗PD-Ll抗体对从受试者癌症组织中采集的样本进行染色；根据是否存在LAT1阳性和PD-L1阳性部位评估受试者癌症的恶性程度。
• CANCER THERAPEUTIC
  申请人：J-Pharma Co., Ltd.

  公开号：EP3733175A1

  公开（公告）日：2020-11-04

  O-(5-amino-2-phenylbenzoxazol-7-yl)methyl-3,5-dichloro-L-tyr osine or a pharmacologically acceptable salt thereof exhibits high therapeutic effects on bile duct cancer, colorectal cancer, esophageal cancer, breast cancer, and pancreatic cancer.

  O-(5-氨基-2-苯基苯并恶唑-7-基)甲基-3,5-二氯-L-酪氨酸或其药理上可接受的盐对胆管癌、结肠直肠癌、食道癌、乳腺癌和胰腺癌有很好的治疗效果。
• COMBINED INHIBITION OF AMINO ACID TRANSPORTERS FOR INHIBITING HUMAN PLASMACYTOID DENDRITIC CELL ACTIVITY DURING AUTOIMMUNITY
  申请人：Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.

  公开号：EP4008330A1

  公开（公告）日：2022-06-08

  The present invention relates to the treatment of autoimmune diseases through inhibition of human plasmacytoid dendritic cell activity. The treatment is based on a combination of one inhibitor of antiporter system xc-, and at least one inhibitor selected from the group consisting of a JAK2 inhibitor, a SLC7A5:SLC3A2 inhibitor, an inhibitor targeting IL-3 receptor alpha, IL-3 receptor beta, an inhibitor targeting GM-CSF, an inhibitor targeting GM-CSF receptor alpha, and an inhibitor targeting STAT5. The present invention also provided pharmaceutical compositions comprising said combination.

  本发明涉及通过抑制人类浆细胞树突状细胞活性来治疗自身免疫性疾病。该治疗方法基于一种抗转运体系统xc-的抑制剂和至少一种选自JAK2抑制剂、SLC7A5:SLC3A2抑制剂、靶向IL-3受体α的抑制剂、IL-3受体β的抑制剂、靶向GM-CSF的抑制剂、靶向GM-CSF受体α的抑制剂和靶向STAT5的抑制剂组成的组的抑制剂的组合。本发明还提供了包含所述组合物的药物组合物。
• PHARMACEUTICAL COMPOSITION USED IN PATIENTS HAVING SPECIFIC GENE MARKER
  申请人：J-Pharma Co., Ltd.

  公开号：EP4023296A1

  公开（公告）日：2022-07-06

  Provided is a pharmaceutical composition including O-(5-amino-2-phenylbenzoxazole-7-yl)methyl-3,5-dichloro-L-tyrosine, or a pharmaceutically acceptable salt thereof, for use in treatment of a disease such as an allergic disease, an autoimmune disease, or an inflammatory disease in a subject, the pharmaceutical composition being administered to the subject having a Non-Rapid (Slow and/or Intermediate) type NAT2 gene.

  本发明提供了一种药物组合物，该药物组合物包括 O-(5-氨基-2-苯基苯并恶唑-7-基)甲基-3,5-二氯-L-酪氨酸或其药学上可接受的盐，用于治疗受试者的过敏性疾病、自身免疫性疾病或炎症性疾病等疾病，该药物组合物施用给具有非快速（慢速和/或中间）型 NAT2 基因的受试者。