6-bromo-7,8-dihydro-6H-isoquinolin-5-one

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 6-bromo-7,8-dihydro-6H-isoquinolin-5-one
• 化学式: C₉H₈BrNO
• 分子量: 226.073
• InChiKey: RKHPCZOSIHPKOK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  30
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  6-bromo-7,8-dihydro-6H-isoquinolin-5-one 、 氰乙酸乙酯 在 N,N-二异丙基乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 4.0h， 以95%的产率得到cyano-(5-oxo-5,6,7,8-tetrahydro-isoquinolin-6-yl)-acetic acid ethyl ester
  参考文献：
  名称：

  WO2008/65054

  摘要：

  公开号：

文献信息

• TRICYCLIC INHIBITORS OF PRO-MATRIX METALLOPROTEINASE ACTIVATION
  申请人：WANG Aihua

  公开号：US20120129811A1

  公开（公告）日：2012-05-24

  This invention relates to tricycle I and its therapeutic and prophylactic uses, wherein the variables C 1 , C 2 , Z 1 , Z 2 , Q, J, R 1 , and R 3 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.

  本发明涉及三轮车I及其治疗和预防用途，其中变量C1、C2、Z1、Z2、Q、J、R1和R3在规范中定义。治疗和/或预防的疾病包括类风湿性关节炎。
• TRICYCLIC INDOLES AND (4,5-DIHYDRO) INDOLES
  申请人：Vanotti Ermes

  公开号：US20100075998A1

  公开（公告）日：2010-03-25

  The present invention provides tricyclic indoles and (4,5-dihydro) indoles of the formula (I) or a pharmaceutically acceptable salt thereof: wherein the ring A represents a fused pyrazole, pyridine or pyrimidine, means either simple or double carbon-carbon bond and R 1 , R 2 and R 3 are as defined in the specification. Further objects of the invention are a process for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, in particular Cdc7 and AKT kinase activity, like cancer.

  本发明提供了三环吲哚和（4,5-二氢）吲哚的公式（I）或其药学上可接受的盐：其中环A代表融合的吡唑、吡啶或嘧啶，表示单重或双重碳-碳键，R1、R2和R3如规范中所定义。本发明的进一步目标是公式（I）化合物的制备方法，包含它们的制药组合物以及治疗细胞增殖性疾病的方法。事实上，公式（I）化合物在治疗与失调的蛋白激酶活性有关的疾病，特别是Cdc7和AKT激酶活性，如癌症方面非常有用。
• US8207180B2
  申请人：——

  公开号：US8207180B2

  公开（公告）日：2012-06-26
• [EN] TRICYCLIC INDOLES AND (4,5-DIHYDRO) INDOLES<br/>[FR] INDOLES ET 4,5-DIHYDROINDOLES TRICYCLIQUES
  申请人：NERVIANO MEDICAL SCIENCES SRL

  公开号：WO2008065054A1

  公开（公告）日：2008-06-05

  [EN] The present invention provides tricyclic indoles and (4,5-dihydro) indoles of the formula (I) or a pharmaceutically acceptable salt thereof: wherein the ring A represents a fused pyrazole, pyridine or pyrimidine, ----- means either simple or double carbon-carbon bond and R₁, R₂ and R₃ are as defined in the specification. Further objects of the invention are a process for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, in particular Cdc7 and AKT kinase activity, like cancer.
  [FR] La présente invention concerne des indoles et 4,5-dihydroindoles tricycliques de formule (I) ou un sel acceptable du point de vue pharmaceutique de ceux-ci : dans laquelle le cycle A représente un cycle pyrazole, pyridine ou pyrimidine fusionné, - - - représente une liaison carbone-carbone soit simple soit double et R1, R2 et R3 sont tels que définis dans la description. L'invention concerne en outre un procédé pour la préparation des composés de formule (I), des compositions pharmaceutiques comprenant ceux-ci et des procédés servant à traiter des troubles de type prolifération de cellules. En fait, les composés de formule (I) sont utiles, en thérapie, dans le traitement de maladies associées à une activité dérégulée de protéines kinases, en particulier une activité des kinases Cdc7 et AKT, telles que le cancer.
• [EN] TRICYCLIC INHIBITORS OF PRO-MATRIX METALLOPROTEINASE ACTIVATION<br/>[FR] INHIBITEURS TRICYCLIQUES D'ACTIVATION DE MÉTALLOPROTÉINASES PROMATRICIELLES
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2012068211A1

  公开（公告）日：2012-05-24

  This invention relates to tricycle I and its therapeutic and prophylactic uses, wherein the variables C1, C2, Z1, Z2, Q, J, R1, and R3 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.