2-[[6-[[3-(1H-Imidazol-1-yl)propyl]amino]-2-pyridinyl]amino]-N-[1-(phenylmethyl)-1H-indazol-5-yl]-5-thiazolecarboxamide | 302963-55-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡唑类
• 英文名称: 2-[[6-[[3-(1H-Imidazol-1-yl)propyl]amino]-2-pyridinyl]amino]-N-[1-(phenylmethyl)-1H-indazol-5-yl]-5-thiazolecarboxamide
• 英文别名: N-(1-benzylindazol-5-yl)-2-[[6-(3-imidazol-1-ylpropylamino)pyridin-2-yl]amino]-1,3-thiazole-5-carboxamide
• CAS: 302963-55-9
• 化学式: C₂₉H₂₇N₉OS
• 分子量: 549.659
• InChiKey: SJAPKKCTEGBGNE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.9
• 重原子数：
  40
• 可旋转键数：
  11
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  143
• 氢给体数：
  3
• 氢受体数：
  8

文献信息

• Cyclic protein tyrosine kinase inhibitors
  申请人：——

  公开号：US20040054186A1

  公开（公告）日：2004-03-18

  Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.

  新型环状化合物及其盐类，含有此类化合物的药物组合物，以及使用此类化合物治疗蛋白质酪氨酸激酶相关疾病，如免疫和肿瘤疾病的方法。
• HALOGENATED-HETEROARYL AND OTHER HETEROCYCLIC KINASE INHIBITORS, AND USES THEREOF
  申请人：iOmx Therapeutics AG

  公开号：EP3901151A1

  公开（公告）日：2021-10-27

  The invention relates to kinase inhibitors, in particular inhibitors of protein kinases including the SIK-family CSF1R, ABL/BCR-ABL, SRC, HCK, PDGFR, KIT and/or their mutants. Although structurally similar to dasatinib, the kinase inhibitors of the invention are distinctive; possessing a particular class of halogenated heteroaryls. Such kinase inhibitors can display one or more certain properties distinct to dasatinib and other structurally similar kinase inhibitors. The kinase inhibitors of the invention or pharmaceutical compositions comprising them may be used in the treatment of a disorder or condition, such as a proliferative disorder, for example, a leukaemia or solid tumour. In particular, these and other structurally similar kinase inhibitors may be used in the treatment of a proliferative disorder - such as a mixed phenotype acute leukaemia (MPAL) - characterised by (inter-alia) the presence of MEF2C protein, a human chromosomal translocation at 11q23, and/or a KMT2A fusion oncoprotein. The kinase inhibitors or pharmaceutical compositions disclosed herein may be used topically to modulate skin pigmentation in a subject, for example to impart UV protection and reduce skin cancer risk.

  该发明涉及激酶抑制剂，特别是蛋白激酶的抑制剂，包括SIK家族CSF1R，ABL/BCR-ABL，SRC，HCK，PDGFR，KIT和/或它们的突变体。尽管在结构上类似于达沙替尼，但该发明的激酶抑制剂具有独特之处；具有一类特殊的卤代杂环芳基。这种激酶抑制剂可能表现出与达沙替尼和其他在结构上相似的激酶抑制剂不同的某些性质。该发明的激酶抑制剂或包含它们的药物组合物可用于治疗某种疾病或病况，例如增生性疾病，例如白血病或实体肿瘤。特别是，这些和其他在结构上相似的激酶抑制剂可用于治疗增生性疾病 - 例如混合表型急性白血病（MPAL）- 其特征包括MEF2C蛋白的存在，11q23处的人类染色体易位，和/或KMT2A融合致癌蛋白。本文披露的激酶抑制剂或药物组合物可用于局部调节受试者的皮肤色素沉着，例如赋予UV保护并降低皮肤癌风险。
• Synergistic methods and compositions for treating cancer
  申请人：——

  公开号：US20040209930A1

  公开（公告）日：2004-10-21

  Combination therapies using IGF1R inhibitors in combination with additional kinase inhibitors are described for the synergistic treatment of cancer.

  描述了使用IGF1R抑制剂与其他激酶抑制剂结合的联合疗法，用于癌症的协同治疗。
• HETEROCYCLIC KINASE INHIBITORS AND USES THEREOF
  申请人：iOmx Therapeutics AG

  公开号：EP3643713A1

  公开（公告）日：2020-04-29

  The invention relates to kinase inhibitors, in particular inhibitors of protein kinases including the protein-tyrosine kinases LCK, ABL, SRC, KIT, SIK-family and/or their mutants. Although structurally similar to dasatinib, the kinase inhibitors of the invention can display one or more certain properties distinct to dasatinib. Also, the invention relates to pharmaceutical compositions that comprise one or more of the kinase inhibitors. The kinase inhibitors or pharmaceutical compositions of the invention may be used in the treatment of a disorder or condition, such as a proliferative disorder, for example, a leukaemia or solid tumour. The kinase inhibitors or pharmaceutical compositions may be used in a treatment regimen that corresponds to, is similar to or is distinct from that used with dasatinib for a corresponding disorder, and in particular may be used in a combination treatment regimen together with one or more additional therapeutic agents, such as immune-checkpoint inhibitors.

  本发明涉及激酶抑制剂，特别是蛋白激酶的抑制剂，包括LCK、ABL、SRC、KIT、SIK家族和/或它们的突变体。虽然在结构上类似于达沙替尼，但本发明的激酶抑制剂可以表现出与达沙替尼不同的一种或多种特定性质。此外，本发明涉及包含一种或多种激酶抑制剂的制药组合物。本发明的激酶抑制剂或制药组合物可用于治疗疾病或病况，例如增生性疾病，例如白血病或实体肿瘤。本发明的激酶抑制剂或制药组合物可用于与达沙替尼用于相应疾病的治疗方案相对应、类似或不同的治疗方案中，并且特别可用于与一种或多种额外的治疗药物，例如免疫检查点抑制剂一起使用的联合治疗方案中。
• CYCLIC PROTEIN TYROSINE KINASE INHIBITORS
  申请人：BRISTOL-MYERS SQUIBB COMPANY

  公开号：US20140206691A1

  公开（公告）日：2014-07-24

  Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.

  新型环状化合物及其盐，含有这种化合物的药物组合物，以及使用这种化合物治疗蛋白酪氨酸激酶相关疾病（如免疫和肿瘤疾病）的方法。