N-[1,4-二氢-3-[4-[[4-(2-甲氧基乙基)-1-哌嗪基]甲基]苯基]-4-氧代茚并[1,2-c]吡唑-5-基]-N'-4-吗啉基脲盐酸盐 | 784210-87-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 中文名称: N-[1,4-二氢-3-[4-[[4-(2-甲氧基乙基)-1-哌嗪基]甲基]苯基]-4-氧代茚并[1,2-c]吡唑-5-基]-N'-4-吗啉基脲盐酸盐
• 中文别名: N-[1,4-二氢-3-[4-[[4-(2-甲氧基乙基)-1-哌嗪基]甲基]苯基]-4-氧代茚并[1,2-C]吡唑-5-基]-N'-4-吗啉基脲盐酸盐
• 英文名称: Rgb-286638
• 英文别名: 1-[3-[4-[[4-(2-methoxyethyl)piperazin-1-yl]methyl]phenyl]-4-oxo-1H-indeno[1,2-c]pyrazol-5-yl]-3-morpholin-4-ylurea;dihydrochloride
• CAS: 784210-87-3
• 化学式: C29H37Cl2N7O4
• 分子量: 618.6
• InChiKey: WJVMGQMXUBAAPL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.26
• 重原子数：
  42
• 可旋转键数：
  8
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  115
• 氢给体数：
  5
• 氢受体数：
  8

文献信息

• Inhibitors of cyclin-dependent kinases, compositions and uses related thereto
  申请人：GPC Biotech, Inc.

  公开号：US20040266854A1

  公开（公告）日：2004-12-30

  The invention pertains to novel cyclin dependent kinase inhibitors (cdks) and specifically, but not exclusively, as inhibitors of cdk/cyclin complexes. As described herein, the inhibitors of this invention are capable of inhibiting the cell-cycle machinery and consequently may be useful in modulating cell-cycle progression, ultimately controlling cell growth and differentiation. Such compounds would be useful for treating subjects having disorders associated with excessive cell proliferation.

  这项发明涉及新型细胞周期依赖性激酶抑制剂（cdks），具体而言，但不仅限于作为cdk/cyclin复合物的抑制剂。如本文所述，本发明的抑制剂能够抑制细胞周期机制，因此可能有助于调节细胞周期进程，最终控制细胞生长和分化。这样的化合物对于治疗患有与过度细胞增殖相关的疾病的患者将会很有用。
• Kinase inhibitors for treating cancers
  申请人：GPC Biotech Inc.

  公开号：EP2027853A2

  公开（公告）日：2009-02-25

  The invention pertains to inhibitors of various kinases (e.g. S/T kinases, Tyr kinases, etc.), which inhibitors are previously known as cyclin dependent kinase inhibitors (CDKs). As described herein, the inhibitors of this invention are capable of inhibiting various wild-type and mutant form kinases, including drug resistant forms of mutant kinases. Thus the subject kinase inhibitors are useful in treating a wide range of diseases/conditions associated with abnormal functions/excessive activities of the target kinases, including mutant kinases. The invention further provides methods for treating cancers, tumours and patients which are resistant or refractory to other therapeutic agents. Pharmaceutical compositions and packaged pharmaceuticals with instructions of these inhibitors, and methods of using these inhibitors are also provided.

  本发明涉及各种激酶（如S/T激酶、Tyr激酶等）的抑制剂，这些抑制剂以前称为细胞周期蛋白依赖性激酶抑制剂（CDK）。如本文所述，本发明的抑制剂能够抑制各种野生型和突变型激酶，包括突变型激酶的耐药形式。因此，本发明的激酶抑制剂可用于治疗与靶激酶（包括突变激酶）功能异常/活性过强有关的多种疾病/病症。本发明进一步提供了治疗对其他治疗剂耐药或难治的癌症、肿瘤和患者的方法。本发明还提供了含有这些抑制剂说明的药物组合物和包装药品，以及使用这些抑制剂的方法。
• EP1611136A2
  申请人：——

  公开号：EP1611136A2

  公开（公告）日：2006-01-04
• KINASE INHIBITORS FOR TREATING CANCERS
  申请人：GPC Biotech Inc.

  公开号：EP1763345A2

  公开（公告）日：2007-03-21
• Uses of Kinase Inhibitors and Compositions Thereof
  申请人：Caligiuri Maureen G.

  公开号：US20080146555A1

  公开（公告）日：2008-06-19

  The invention pertains to inhibitors of various kinases (e.g. S/T kinases, Tyr kinases, etc.), which inhibitors are previously known as cyclin dependent kinase inhibitors (CDKs). As described herein, the inhibitors of this invention are capable of inhibiting various wild-type and mutant form kinases, including drug resistant forms of mutant kinases. Thus the subject kinase inhibitors are useful in treating a wide range of diseases/conditions associated with abnormal functions/excessive activities of the target kinases, including mutant kinases. The invention further provides methods for treating cancers, tumors and patients which are resistant or refractory to other therapeutic agents. Pharmaceutical compositions and packaged pharmaceuticals with instructions of these inhibitors, and methods of using these inhibitors are also provided.