N-{5-[2-(4-chloro-phenylamino)-pyrimidin-4-yl]-4-methyl-thiazol-2-yl}-3-(2-morpholin-4-yl-ethylamino)-propionamide | 693229-28-6

• 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
• 英文名称: N-{5-[2-(4-chloro-phenylamino)-pyrimidin-4-yl]-4-methyl-thiazol-2-yl}-3-(2-morpholin-4-yl-ethylamino)-propionamide
• 英文别名: N-[5-[2-(4-chloroanilino)pyrimidin-4-yl]-4-methyl-1,3-thiazol-2-yl]-3-(2-morpholin-4-ylethylamino)propanamide
• CAS: 693229-28-6
• 化学式: C₂₃H₂₈ClN₇O₂S
• 分子量: 502.04
• InChiKey: HNMSPGQZQNMROI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  34
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  133
• 氢给体数：
  3
• 氢受体数：
  9

反应信息

• 作为产物：
  描述：

  3-bromo-N-{5-[2-(4-chloro-phenylamino)-pyrimidin-4-yl]-4-methyl-thiazol-2-yl}-propionamide 、 N-(2-氨基乙基)吗啉 、 3-amino-N-{5-[2-(4-chloro-phenylamino)-pyrimidin-4-yl]-4-methyl-thiazol-2-yl}-propionamide 、 4-(2-氯乙基)吗啉 以 乙腈 为溶剂， 生成 N-{5-[2-(4-chloro-phenylamino)-pyrimidin-4-yl]-4-methyl-thiazol-2-yl}-3-(2-morpholin-4-yl-ethylamino)-propionamide
  参考文献：
  名称：

  Pyrimidine compounds

  摘要：

  本发明涉及式I的取代嘧啶，其制备方法，含有它们的药物组合物以及它们作为细胞周期依赖性激酶（CDKs）的抑制剂的用途，因此可用于治疗增生性疾病和/或病毒性疾病。

  公开号：

  US07897605B2

文献信息

• [EN] PYRIMIDINE COMPOUNDS<br/>[FR] COMPOSES DE PYRIMIDINE
  申请人：CYCLACEL LTD

  公开号：WO2004043953A1

  公开（公告）日：2004-05-27

  The present invention relates to substituted pyrimidines of formula (I), their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders and/or viral disorders.

  本发明涉及式(I)的取代嘧啶化合物，它们的制备，含有它们的药物组合物，以及它们作为细胞周期依赖性激酶（CDKs）抑制剂的用途，因此可用于治疗增殖性疾病和/或病毒性疾病。
• PYRIMIDINE COMPOUNDS AS CYCLIN-DEPENDENT KINASE INHIBITORS
  申请人：Cyclacel Limited

  公开号：EP1864983A1

  公开（公告）日：2007-12-12

  The present invention relates to substituted pyrimidines of formula (I), their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders and/or viral disorders.

  本发明涉及式（I）的取代嘧啶、它们的制备、含有它们的药物组合物以及它们作为细胞周期蛋白依赖性激酶（CDK）抑制剂的用途，因此它们可用于治疗增殖性疾病和/或病毒性疾病。
• 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。
• PYRIMIDINE COMPOUNDS
  申请人：Cyclacel Limited

  公开号：EP1567522A1

  公开（公告）日：2005-08-31
• 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