1-(4-Oxo-1-propyl-3,4-dihydro-phthalazin-6-yl)-3-pyridin-3-yl-urea | 497255-38-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 1-(4-Oxo-1-propyl-3,4-dihydro-phthalazin-6-yl)-3-pyridin-3-yl-urea
• 英文别名: 1-(4-oxo-1-propyl-3H-phthalazin-6-yl)-3-pyridin-3-ylurea
• CAS: 497255-38-6
• 化学式: C₁₇H₁₇N₅O₂
• 分子量: 323.354
• InChiKey: UUJNJFATNAWTII-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  24
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  95.5
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• Amino-phthalazinone derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions containing them
  申请人：PHARMACIA & UPJOHN S.p.A.

  公开号：US20030073692A1

  公开（公告）日：2003-04-17

  Compounds which are amino-phthalazinone derivatives and pharmaceutically acceptable salts thereof, together with pharmaceutical compositions comprising them are disclosed; these compounds or compositions are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases and neurodegenerative disorders.

  本文揭示了一种氨基-邻苯二氮酮衍生物及其药学上可接受的盐，以及包含它们的制药组合物；这些化合物或组合物在治疗由于和/或与蛋白激酶活性改变有关的疾病方面具有用处，例如癌症、细胞增殖性疾病、阿尔茨海默病、病毒感染、自身免疫性疾病和神经退行性疾病。
• Piperazine compounds and pharmaceutical compositions containing them.
  申请人：GLAXO GROUP LIMITED

  公开号：EP1454901A1

  公开（公告）日：2004-09-08

  A composition comprising a compound of formula (I) wherein R represents a halogen atom or a C1-4 alkyl group; R1 represents hydrogen or a C1-4 alkyl group; R2 represents hydrogen, a C1-4 alkyl, C2-6 alkenyl_or a C3-7 cycloalkyl group; or R1 and R2 together with nitrogen and carbon atom to which they are attached respectively represent a 5-6 membered heterocyclic group; R3 represents a trifluoromethyl, a C1-4 alkyl, a C1-4 alkoxy, a trifluoromethoxy or a halogen group; R4 represents hydrogen, a (CH2)qR7 or a (CH2)rCO(CH2)pR7 group; R5 represents hydrogen, a C1-4 alkyl or a COR6 group; R7 represents hydrogen, hydroxy or NR8R9 wherein R8 and R9 represent independently hydrogen or C1-4 alkyl optionally substituted by hydroxy, or by amino; R10 represents hydrogen, a C1-4 alkyl group or R10 together with R2 represents a a C3-7 cycloalkyl group; m is zero or an integer from 1 to 3; n is zero or an integer from 1 to 3; both p and r are independently zero or an integer from 1 to 4; q is an integer from 1 to 4; provided that, when R1 and R2 together with nitrogen and carbon atom to which they are attached respectively represent a 5 to 6 membered heterocyclic group, i) m is 1 or 2; ii) when m is 1, R is not fluorine and iii) when m is 2, the two substituents R are not both fluorine, or pharmaceutically acceptable salts or solvates thereof and a selective serotonin reuptake inhibitor.

  一种包含式 (I) 化合物的组合物 其中 R 代表卤素原子或 C1-4 烷基； R1 代表氢或 C1-4 烷基 R2 代表氢、C1-4 烷基、C2-6 烯基或 C3-7 环烷基；或 R1 和 R2 与它们分别连接的氮原子和碳原子一起代表 5-6 位杂环基团； R3 代表三氟甲基、C1-4 烷基、C1-4 烷氧基、三氟甲氧基或卤素基团； R4 代表氢、(CH2)qR7 或 ( )rCO( )pR7 基团； R5 代表氢、C1-4 烷基或 COR6 基团； R7 代表氢、羟基或 NR8R9，其中 R8 和 R9 独立地代表氢或任选被羟基或氨基取代的 C1-4 烷基； R10 代表氢、C1-4 烷基或 R10 与 R2 一起代表 C3-7 环烷基； m 为零或 1 至 3 的整数； n 为零或 1 至 3 的整数； p 和 r 独立地均为零或 1 至 4 的整数； q 为 1 至 4 的整数；条件是 当 R1 和 R2 与氮原子和它们分别连接的碳原子一起代表 5 至 6 位杂环基团时，i) m 为 1 或 2；ii) 当 m 为 1 时，R 不为氟，iii) 当 m 为 2 时，两个取代基 R 不同时为氟，或其药学上可接受的盐或溶液，以及选择性 5-羟色胺再摄取抑制剂。
• AMINO-PHTHALAZINONE DERIVATIVES ACTIVE AS KINASE INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
  申请人：Pharmacia Italia S.p.A.

  公开号：EP1427708A1

  公开（公告）日：2004-06-16
• AMINO-PHTHALAZINONE DERIVATIVES AS KINASE INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
  申请人：Pfizer Italia S.r.l.

  公开号：EP1427708B1

  公开（公告）日：2008-09-10
• Pharmaceutical compositions comprising tachykinins antagonists and a serotonin reuptake inhibitor.
  申请人：GLAXO GROUP LIMITED

  公开号：EP1454901B1

  公开（公告）日：2008-09-03