N2-[(1S,2R)-2-aminocyclohexyl]-N6-(3-chlorophenyl)-9-ethylpurine-2,6-diamine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并嘧啶类
• 英文名称: N2-[(1S,2R)-2-aminocyclohexyl]-N6-(3-chlorophenyl)-9-ethylpurine-2,6-diamine
• 英文别名: 2-N-[(1S,2R)-2-aminocyclohexyl]-6-N-(3-chlorophenyl)-9-ethylpurine-2,6-diamine
• 化学式: C₁₉H₂₄ClN₇
• 分子量: 385.9
• InChiKey: UTBSBSOBZHXMHI-CABCVRRESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  27
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  93.7
• 氢给体数：
  3
• 氢受体数：
  6

文献信息

• [EN] DUAL CLK/CDK1 INHIBITORS FOR CANCER TREATMENT<br/>[FR] INHIBITEURS DOUBLES DE CLK/CDK1 DESTINÉS AU TRAITEMENT DU CANCER
  申请人：STANFORD RES INST INT

  公开号：WO2018064545A1

  公开（公告）日：2018-04-05

  This disclosure generally relates to dual CLK2/CDK1 inhibitors or more potent and specific CLK inhibitors to target CLK2 and CDKl kinases in the treatment of germ-line mutations of the spliceosome leading to the development of cancers and other human disease. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

  本公开一般涉及双重CLK2/CDK1抑制剂或更强效、更特异的CLK抑制剂，用于治疗导致癌症和其他人类疾病发展的剪接体的生殖细胞系突变。本摘要旨在作为在特定领域进行搜索的扫描工具，不打算限制本发明。
• METHOD FOR THE DIAGNOSIS, PROGNOSIS AND TREATMENT OF BREAST CANCER METASTASIS
  申请人：Fundació Privada Institut de Recerca Biomèdica

  公开号：EP2626431A2

  公开（公告）日：2013-08-14

  The present invention relates to a method for the diagnosis or the prognosis of metastasis in breast cancer which comprises determining if the c-MAF gene is amplified in a primary tumor sample. Likewise, the invention also relates to a method for the diagnosis or the prognosis of metastasis in ER- breast cancer, as well as to a method for determining the tendency to develop bone metastasis with respect to metastasis in other organs, which comprise determining the c-MAF gene expression level. Finally, the invention relates to the use of a c-MAF inhibitor as therapeutic target for treating the ER- breast cancer metastasis.

  本发明涉及一种诊断或预后乳腺癌转移的方法，该方法包括确定原发肿瘤样本中 c-MAF 基因是否扩增。同样，本发明还涉及一种诊断或预后ER-乳腺癌转移的方法，以及一种确定骨转移与其他器官转移倾向的方法，其中包括确定c-MAF基因的表达水平。最后，本发明涉及使用 c-MAF 抑制剂作为治疗 ER- 乳腺癌转移的治疗靶点。
• METHOD FOR THE DIAGNOSIS, PROGNOSIS AND TREATMENT OF CANCER METASTASIS
  申请人：Fundació Institut de Recerca Biomèdica (IRB Barcelona)

  公开号：EP2975138A2

  公开（公告）日：2016-01-20

  This study describes a method to determine the likelihood of the development of metastasis in a subject suffering from cancer, in addition to a method to design a customized therapy in a subject suffering from cancer, in particular breast, colon, lung, kidney and thyroid cancer, based on the determination of the expression level of one or more genes whose expression is modulated by an increase in c-MAF expression. It also describes a method for the identification of marker genes with a propensity for metastatic cancer based on inducing the modulation of the c-MAF expression Finally, the use of PTHLH and PODXL inhibitors and RERG activators in the treatment and/or prevention of the cancer, in particular breast, colon, lung, kidney and thyroid cancer.

  本研究介绍了一种确定癌症患者发生转移的可能性的方法，以及一种为癌症患者（尤其是乳腺癌、结肠癌、肺癌、肾癌和甲状腺癌患者）设计定制疗法的方法，其依据是确定一个或多个基因的表达水平，这些基因的表达受 c-MAF 表达增加的调节。它还描述了一种基于诱导 c-MAF 表达调节来鉴定具有转移性癌症倾向的标记基因的方法。最后，还描述了 PTHLH 和 PODXL 抑制剂以及 RERG 激活剂在治疗和/或预防癌症（尤其是乳腺癌、结肠癌、肺癌、肾癌和甲状腺癌）中的应用。
• METHOD FOR THE DIAGNOSIS, PROGNOSIS AND TREATMENT OF METASTATIC CANCER
  申请人：Fundació Institut de Recerca Biomèdica IRB (Barcelona)

  公开号：EP3272880A2

  公开（公告）日：2018-01-24

  This study describes a method to determine the likelihood of the development of metastasis in a subject suffering from cancer, in addition to a method to design a customized therapy in a subject suffering from cancer, in particular breast, colon, lung, kidney and thyroid cancer, based on the determination of the expression level of one or more genes whose expression is modulated by an increase in c-MAF expression. It also describes a method for the identification of marker genes with a propensity for metastatic cancer based on inducing the modulation of the c-MAF expression Finally, the use of PTHLH and PODXL inhibitors and RERG activators in the treatment and/or prevention of the cancer, in particular breast, colon, lung, kidney and thyroid cancer.

  本研究介绍了一种确定癌症患者发生转移的可能性的方法，以及一种为癌症患者（尤其是乳腺癌、结肠癌、肺癌、肾癌和甲状腺癌患者）设计定制疗法的方法，其依据是确定一个或多个基因的表达水平，这些基因的表达受 c-MAF 表达增加的调节。它还描述了一种基于诱导 c-MAF 表达调节来鉴定具有转移性癌症倾向的标记基因的方法。最后，还描述了 PTHLH 和 PODXL 抑制剂以及 RERG 激活剂在治疗和/或预防癌症（尤其是乳腺癌、结肠癌、肺癌、肾癌和甲状腺癌）中的应用。
• METHOD FOR THE DIAGNOSIS, PROGNOSIS AND TREATMENT OF LUNG CANCER METASTASIS
  申请人：Fundació Institut de Recerca Biomèdica IRB (Barcelona)

  公开号：EP3467124A1

  公开（公告）日：2019-04-10

  The present invention relates to a method for the diagnosis or the prognosis of metastasis in lung cancer which comprises determining if the c-MAF gene is amplified in a primary tumor sample. Likewise, the invention also relates to a method for the diagnosis or the prognosis of metastasis in lung cancer, as well as to a method for determining the tendency to develop bone metastasis with respect to metastasis in other organs, which comprise determining the c-MAF gene expression level. Finally, the invention relates to the use of a c-MAF inhibitor as therapeutic target for treating the lung cancer.

  本发明涉及肺癌转移的诊断或预后方法，该方法包括确定原发肿瘤样本中 c-MAF 基因是否扩增。同样，本发明还涉及一种诊断或预后肺癌转移的方法，以及一种确定相对于其他器官转移的骨转移倾向的方法，该方法包括确定 c-MAF 基因的表达水平。最后，本发明涉及使用 c-MAF 抑制剂作为治疗肺癌的靶点。