2-fluoro-4-(4-methylpiperazin-1-yl)phenol | 1235036-12-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 2-fluoro-4-(4-methylpiperazin-1-yl)phenol
• 英文别名: 2-Fluoro-4-(4-methyl-1-piperazinyl)phenol
• CAS: 1235036-12-0
• 化学式: C₁₁H₁₅FN₂O
• 分子量: 210.251
• InChiKey: GNRWQDOUORMQMO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  26.7
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] SUBSTITUTED PYRAZOLO-QUINAZOLINE DERIVATIVES AS KINASE INHIBITORS<br/>[FR] DÉRIVÉS DE PYRAZOLO-QUINAZOLINE SUBSTITUÉS À TITRE D'INHIBITEURS DE KINASES
  申请人：NERVIANO MEDICAL SCIENCES SRL

  公开号：WO2012080990A1

  公开（公告）日：2012-06-21

  The present invention relates to substituted pyrazolo[4,3-/h]quinazoline compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular PIM kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.

  本发明涉及替代吡唑并[4,3-/h]喹唑啉化合物，其调节蛋白激酶的活性，因此在治疗由失调的蛋白激酶活性引起的疾病方面具有用处，特别是PIM激酶。本发明还提供了制备这些化合物的方法，包括这些化合物的药物组合物，以及利用这些化合物或含有它们的药物组合物治疗疾病的方法。
• SUBSTITUTED PYRAZOLO-QUINAZOLINE DERIVATIVES AS KINASE INHIBITORS
  申请人：Casuscelli Francesco

  公开号：US20120190678A1

  公开（公告）日：2012-07-26

  The present invention relates to substituted pyrazolo[4,3-h]quinazoline compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular PIM kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.

  本发明涉及替代吡唑并[4,3-h]喹唑啉化合物，其调节蛋白激酶的活性，因此在治疗由失调的蛋白激酶活性引起的疾病方面具有用处，特别是PIM激酶。本发明还提供了制备这些化合物的方法，包括这些化合物的药物组合物，以及利用这些化合物或含有它们的药物组合物治疗疾病的方法。
• [EN] HETEROCYCLIC COMPOUNDS AND METHODS OF USE<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES ET LEURS PROCÉDÉS D'UTILISATION
  申请人：GENENTECH INC

  公开号：WO2010080503A1

  公开（公告）日：2010-07-15

  In one aspect, the present invention provides for a compound of Formula I; in which the variable X1a, X1b, X1c, X1d, Q, A, R1, B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.

  在一个方面，本发明提供了一种具有式I的化合物；其中变量X1a、X1b、X1c、X1d、Q、A、R1、B、L、E和下标m和n的含义如本文所述。在另一个方面，本发明提供了包括式I化合物的药物组合物，以及使用式I化合物治疗由Bcl-2抗凋亡蛋白（例如抗凋亡Bcl-xL蛋白）的表达或过度表达所特征的疾病和状况（例如癌症、血小板增多症等）的方法。
• HETEROCYCLIC COMPOUNDS AND METHODS OF USE
  申请人：Baell Jonathan Bayldon

  公开号：US20100210622A1

  公开（公告）日：2010-08-19

  In one aspect, the present invention provides for a compound of Formula I in which the variable X 1a , X 1b , X 1c , X 1d , Q, A, R 1 , B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-x L proteins.

  在一个方面，本发明提供了一种式子为I的化合物，其中变量X1a，X1b，X1c，X1d，Q，A，R1，B，L，E和下标m和n的含义如此处所述。在另一个方面，本发明提供了包含式子I化合物的制药组合物，以及使用式子I化合物治疗由Bcl-2抗凋亡蛋白（例如抗凋亡Bcl-xL蛋白）的表达或过表达所特征的疾病和病状（例如癌症，血小板增多症等）的方法。
• US8232273B2
  申请人：——

  公开号：US8232273B2

  公开（公告）日：2012-07-31