N-(3-bromophenyl)-N'-cyano-4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperazine-1-carboximidamide | 1116570-87-6

• 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: N-(3-bromophenyl)-N'-cyano-4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperazine-1-carboximidamide
• 英文别名: N-(3-bromophenyl)-N''-cyano-4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperazine-1-carboximidamide；N'-(3-bromophenyl)-N-cyano-4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperazine-1-carboximidamide
• CAS: 1116570-87-6
• 化学式: C₁₉H₁₉BrN₈
• 分子量: 439.317
• InChiKey: KXDMWKDZFFHEHC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  96.2
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• (7H-PYRROLO [2, 3-D] PYRIMIDIN-4-YL) -PIPERAZINES AS KINASE INHIBITORS FOR THE TREATMENT OF CANCER AND INFLAMMATION
  申请人：Lexicon Pharmaceuticals, Inc.

  公开号：EP2597098A1

  公开（公告）日：2013-05-29

  Inhibitors of LIM kinase 2 of the following formula are disclosed, along with pharmaceutical compositions comprising them and methods of their use, in particular for treatment of inflammatory and cancerous and ocular diseases. X is O or NRA; A is cycloalkyl, aryl or heterocyclyl; RA is hydrogen, cyano, nitro, RA1, SO2RA1 or SO2N(RA1)2; each RB is independently hydrogen or alkyl. The other variables are as defined in the claims.

  本研究公开了下式的 LIM 激酶 2 抑制剂，以及包含这些抑制剂的药物组合物和使用方法，尤其是用于治疗炎症、癌症和眼部疾病的方法。 X 是 O 或 NRA； A 是环烷基、芳基或杂环基； RA 是氢、氰基、硝基、RA1、SO2RA1 或 SO2N(RA1)2 每个 RB 独立地为氢或烷基。 其他变量如权利要求中所定义。
• (7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)-PIPERAZINES AS KINASE INHIBITORS FOR THE TREATMENT OF CANCER AND INFLAMMATION
  申请人：Lexicon Pharmaceuticals, Inc.

  公开号：EP2188289B1

  公开（公告）日：2015-10-28
• [EN] KINASE INHIBITORS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE<br/>[FR] INHIBITEURS DE KINASE, COMPOSITIONS LES CONTENANT ET PROCÉDÉS D'UTILISATION
  申请人：LEXICON PHARMACEUTICALS INC

  公开号：WO2009021169A2

  公开（公告）日：2009-02-12

  Inhibitors of LIM kinase 2 are disclosed, along with pharmaceutical compositions com πsin them and methods of their use. X is O or NRA; Y is O, NRR, or C(RR)2; A is cycloalkyl, aryl or hctcrocyclc; RA is hydrogen, cyano, nitro, RA1, SO2RA1, SO2NRA1, or SO2N(RA1)2;
• [EN] TREATMENT OF DEMENTIA<br/>[FR] TRAITEMENT DE LA DÉMENCE
  申请人：UNIV MACQUARIE

  公开号：WO2021056071A1

  公开（公告）日：2021-04-01

  Provided herein are methods for treating, delaying the onset of, or ameliorating at least one symptom of, dementia associated with -amyloid (A) accumulation, and for improving memory in subjects suffering from dementia associated with A accumulation, comprising administering to subjects in need thereof an effective amount of an inhibitor of LIMK1, wherein the inhibitor comprises a compound of Formula (I) as defined herein, or a pharmaceutically acceptable salt thereof. Also provided are methods for reducing A toxicity in neurons, comprising exposing neurons to an effective amount of an inhibitor of LIMK1, wherein the inhibitor comprises a compound of Formula (I) as defined herein, or a pharmaceutically acceptable salt thereof.
• [EN] TREATMENT OF EXCITOTOXICITY-RELATED CONDITIONS<br/>[FR] TRAITEMENT D'ÉTATS ASSOCIÉS À L'EXCITOTOXICITÉ
  申请人：UNIV MACQUARIE

  公开号：WO2021056072A1

  公开（公告）日：2021-04-01

  Disclosed herein are methods for treating or preventing an excitotoxicity-related condition, optionally a condition associated with seizures and/or resulting from or associated with a cerebral ischemic event, comprising administering to a subject in need an effective amount of an inhibitor of Lim-domain kinase 1 (LIMK1). Also provided are methods for treating or preventing seizures and for reducing excitotoxicity in neurons and/or protecting neurons from excitotoxicity.