{2-[(2-Methylphenyl)amino]-1,3-thiazol-4-yl}[4-(pyrimidin-2-yl)piperazin-1-yl]methanone

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: {2-[(2-Methylphenyl)amino]-1,3-thiazol-4-yl}[4-(pyrimidin-2-yl)piperazin-1-yl]methanone
• 英文别名: [2-(2-methylanilino)-1,3-thiazol-4-yl]-(4-pyrimidin-2-ylpiperazin-1-yl)methanone
• 化学式: C₁₉H₂₀N₆OS
• 分子量: 380.5
• InChiKey: OUNMWDLGJJSBDE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  103
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• Tissue protective erythropoietin receptor (nepor) and methods of use
  申请人：Life Biosystems GmbH

  公开号：EP2492355A1

  公开（公告）日：2012-08-29

  There is disclosed a molecular composition(s) of a novel tissue protective erythropoietin (EPO) binding receptor protein complex, termed NEPOR. Presence of NEPOR components on a tumour allows EPO to impinge on the survival of associated cells thereby enhancing tumour progression and negatively effecting patient survival. There is disclosed that presence of NEPOR represents a prognostic biomarker for poorer patient outcome. Thus, the method disclosed is for stratifying patients having a tumour as suitable (i.e. NEPOR not present) or non-suitable (i.e., NEPOR present) for EPO treatment, comprising: (a) isolating a tissue sample from an individual who is receiving or is a candidate for receiving erythropoietin, (b) determining the level of expression of the NEPOR gene(s) (mRNA) and/or the presence of the NEPOR gene product (protein) from the isolated tissue, and (c) correlating the presence of an NEPOR gene expression product or the presence of NEPOR protein to a physiological response to the treatment with erythropoietin. Furthermore, by disclosing the molecular compositions of NEPOR species, there are disclosed methods for rationally identifying/designing NEPOR modulating therapeutics. Thus, the present disclosure provides methods for treating neurological insults such as stroke (via enhancement of NEPOR activity) and cancer (via down-regulation of cyto-protective signaling from NEPOR).

  本发明公开了一种新型组织保护性促红细胞生成素（EPO）结合受体蛋白复合物（称为 NEPOR）的分子组成。肿瘤上 NEPOR 成分的存在可使 EPO 影响相关细胞的存活，从而促进肿瘤的发展并对病人的存活产生负面影响。据披露，NEPOR 的存在是患者预后较差的预后生物标志物。因此，所公开的方法用于将肿瘤患者分层为适合（即不存在 NEPOR）或不适合（即存在 NEPOR）使用 EPO、NEPOR 存在）进行 EPO 治疗，包括：(a) 从正在接受或可能接受促红细胞生成素治疗的个体中分离组织样本；(b) 从分离的组织中确定 NEPOR 基因的表达水平（mRNA）和/或 NEPOR 基因产物（蛋白质）的存在；(c) 将 NEPOR 基因表达产物的存在或 NEPOR 蛋白质的存在与促红细胞生成素治疗的生理反应相关联。此外，通过公开 NEPOR 物种的分子组成，还公开了合理鉴定/设计 NEPOR 调节疗法的方法。因此，本公开提供了治疗神经损伤如中风（通过增强 NEPOR 活性）和癌症（通过下调来自 NEPOR 的细胞保护信号）的方法。
• NOVEL TISSUE PROTECTIVE ERYTHROPOIETIN RECEPTOR (NEPOR) AND METHODS OF USE
  申请人：Alepor GMBH & CO. KG

  公开号：EP2109690A1

  公开（公告）日：2009-10-21
• EPH-B4 SPECIFIC SIRNA FOR REDUCING EPO-INDUCED TUMOR CELL GROWTH DURING ANEMIA TREATMENT IN CANCER PATIENTS, TISSUE PROTECTIVE ERYTHROPOIETIN RECEPTOR (NEPOR) AND METHODS OF USE.
  申请人：MOLECULAR HEALTH GmbH

  公开号：EP2109690B1

  公开（公告）日：2012-04-18
• METHODS OF USE OF A NOVEL TISSUE PROTECTIVE ERYTHROPOIETIN RECEPTOR (NEPOR)
  申请人：Molecular Health GmbH

  公开号：EP2435581B1

  公开（公告）日：2017-07-26
• US8357501B2
  申请人：——

  公开号：US8357501B2

  公开（公告）日：2013-01-22