N-cyclopropyl-4-{8-[(2-methylpropyl)amino]-6-(quinolin-5-yl)imidazo[1,2-a]pyrazin-3-yl}benzamide | 1382477-96-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: N-cyclopropyl-4-{8-[(2-methylpropyl)amino]-6-(quinolin-5-yl)imidazo[1,2-a]pyrazin-3-yl}benzamide
• 英文别名: MpsBAY2a；N-cyclopropyl-4-[8-(2-methylpropylamino)-6-quinolin-5-ylimidazo[1,2-a]pyrazin-3-yl]benzamide
• CAS: 1382477-96-4
• 化学式: C₂₉H₂₈N₆O
• 分子量: 476.581
• InChiKey: MDYKTGNHXNTATG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.8
• 重原子数：
  36
• 可旋转键数：
  7
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  84.2
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• [EN] COMBINATIONS FOR THE TREATMENT OF CANCER<br/>[FR] COMBINAISONS POUR LE TRAITEMENT DU CANCER
  申请人：BAYER PHARMA AG

  公开号：WO2014020041A1

  公开（公告）日：2014-02-06

  The present invention relates to combinations of at least two compounds A and B, compound A being an inhibitor of Mps-1 kinase, and compound B being an inhibitor of an anti-apoptotic protein of the Bcl-2 family. Another aspect of the present invention relates to the use of such combinations as described supra for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of cancer. Another aspect of the present invention relates to the use of an anti- apoptotic protein from the Bcl-2 family as a sensitizer of cells to Mps-1 inhibitors. Another aspect of the present invention relates to the use of the ratio of pro-apoptotic and anti-apoptotic proteins from the Bcl-2 family in a biological sample as a biomarker for a Mps-1 kinase inhibitor treatment.

  本发明涉及至少两种化合物A和B的组合，其中化合物A是Mps-1激酶的抑制剂，化合物B是Bcl-2家族抗凋亡蛋白的抑制剂。本发明的另一个方面涉及将这种组合用于制备用于治疗或预防疾病的药物，特别是用于癌症治疗。本发明的另一个方面涉及将Bcl-2家族的抗凋亡蛋白用作细胞对Mps-1抑制剂的敏感剂。本发明的另一个方面涉及将Bcl-2家族的促凋亡和抗凋亡蛋白的比例在生物样本中用作Mps-1激酶抑制剂治疗的生物标志物。
• 6 SUBSTITUTED IMIDAZOPYRAZINES FOR USE AS MPS-1 AND TKK INHIBITORS IN THE TREATMENT OF HYPERPROLIFERATIVE DISORDERS
  申请人：Koppitz Marcus

  公开号：US20140187548A1

  公开（公告）日：2014-07-03

  The present invention relates to substituted imidazopyrazine compounds of general formula (I) in which R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the claims, to methods of and intermediates for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

  本发明涉及通式（I）的取代咪唑吡嗪化合物，其中R1、R2、R3、R4和R5如权利要求中所定义，以及制备该化合物的方法和中间体，包括该化合物的药物组合物和组合物，以及用于制造用于治疗或预防疾病的药物组合物的该化合物的用途，特别是用作唯一的代理或与其他活性成分联合使用，用于治疗或预防增生过度和/或血管生成障碍的疾病。
• METHODS AND COMPOSITIONS FOR INCREASING SUSCEPTIBILITY TO RADIATION TREATMENT BY INHIBITING SUPPRESSION OF NUMERICAL CHROMOSOMAL INSTABILITY OF CANCER CELLS
  申请人：Memorial Sloan-Kettering Cancer Center

  公开号：EP3247410A2

  公开（公告）日：2017-11-29
• MEDICAL USES AND METHODS FOR TREATING CANCER USING MONOPOLAR SPINDLE 1 (MPS1) KINASE INHIBITORS
  申请人：THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL

  公开号：US20180112258A1

  公开（公告）日：2018-04-26

  Medical uses and methods are provided for treating cancer using monopolar spindle 1 (MPS1) kinase inhibitors. Methods and uses for selecting MPS1 kinase inhibitors for use in treating cancer in a subject are provided, both in the initial selection of MPS1 kinase inhibitors and for addressing the development of acquired drug resistance that occur in the course of treatment.
• METHODS OF TREATING CANCERS CHARACTERIZED BY A HIGH EXPRESSION LEVEL OF SPINDLE AND KINETOCHORE ASSOCIATED COMPLEX SUBUNIT 3 (SKA3) GENE
  申请人：UNIVERSITY HEALTH NETWORK

  公开号：US20210290624A1

  公开（公告）日：2021-09-23

  Provided herein are methods of treating cancers characterized by a high expression of SKA3 gene, such as: breast cancer, prostate cancer, endometrial cancer, ovarian cancer, brain cancer, skin cancer, thyroid cancer, lung cancer, mesothelioma cancer, bladder cancer, colorectal cancer, liver cancer, melanoma, glioblastoma, leukemia or lymphoma, comprising administering a therapeutically effective amount of a TTK inhibitor, such as: CFI-402257, BAY 1161909, BAY 1217389, AZ-3146, NMS-P715, TC Mps1 12, reversine, Mps1-IN-1, Mps1-IN-2, Mps1-IN-3, MPS BAY1, MPS BAY2a, MPS BAY2b, MPI-0479605, SP600125, S81694/NMS-P153; BOS172722; NTRC 0060-0; NTRC 1501-0; and a pharmaceutically acceptable salt thereof.