4-(5-hydrazinyl-2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-7-yl)morpholine | 1232225-20-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡唑并嘧啶类
• 英文名称: 4-(5-hydrazinyl-2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-7-yl)morpholine
• 英文别名: (7-morpholin-4-yl-2-pyridin-4-yl-pyrazolo[1,5-a]pyrimidin-5-yl)-hydrazine；(7-Morpholin-4-yl-2-pyridin-4-yl-pyrazolo[1,5-a]pyrimidin-5-yl)-hydrazine；(7-morpholin-4-yl-2-pyridin-4-ylpyrazolo[1,5-a]pyrimidin-5-yl)hydrazine
• CAS: 1232225-20-5
• 化学式: C₁₅H₁₇N₇O
• 分子量: 311.346
• InChiKey: FWIDOHNGPXLOPY-UHFFFAOYSA-N

物化性质

• 沸点：
  454.1±55.0 °C(Predicted)
• 密度：
  1.52±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  23
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  93.6
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  4-(5-hydrazinyl-2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-7-yl)morpholine 在 copper(l) iodide 、 氯化铵 、 溶剂黄146 、 L-脯氨酸 作用下， 以 二甲基亚砜 为溶剂， 反应 6.0h， 生成 5-amino-4-bromo-2-(7-morpholino-2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-5-yl)pyridazin-3(2H)-one
  参考文献：
  名称：

  [EN] COMPOUNDS AND COMPOSITIONS THAT INHIBIT PIKFYVE
  [FR] COMPOSÉS ET COMPOSITIONS QUI INHIBENT PIKFYVE

  摘要：

  Pyrazolo[1,5-a]pyrimidines are disclosed. These compounds may be useful in the treatment of neurological disorder, including frontotemporal dementia, chronic traumatic encephalopathy, Alzheimer's disease, limbic-predominant age-related TDP-43 encephalopathy, or frontotemporal lobar degeneration. Further, the invention features a method of inhibiting toxicity in a cell related to a protein TDP-43 or C9orf72. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.

  公开号：

  WO2023107557A1
• 作为产物：
  描述：

  5,7-dichloro-2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidine 在 一水合肼 作用下， 以 1,4-二氧六环 为溶剂， 反应 11.0h， 生成 4-(5-hydrazinyl-2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-7-yl)morpholine
  参考文献：
  名称：

  PYRAZOLO-PYRIMIDINE COMPOUNDS

  摘要：

  本发明已经寻找到多种显示IL-12/IL-23产生抑制活性的化合物，并在此提供了包括该化合物的用于预防或治疗IL-12/IL-23过度产生相关疾病的药物组合物和药剂。

  公开号：

  US20110294781A1

文献信息

• Pyrazolo-pyrimidine compounds
  申请人：Ajinomoto Co., Inc.

  公开号：US08314098B2

  公开（公告）日：2012-11-20

  The present invention has searched for a variety of compounds which show IL-12/IL-23 production-inhibitory activities and herein provides a pharmaceutical composition and an agent for preventing or treating IL-12/IL-23 excess production-related diseases, which comprise the compound.

  本发明已经寻找了多种显示出IL-12/IL-23抑制活性的化合物，并提供了一种制药组合物和一种用于预防或治疗与IL-12/IL-23过度产生相关的疾病的制剂，其中包括该化合物。
• Structure–activity relationship study, target identification, and pharmacological characterization of a small molecular IL-12/23 inhibitor, APY0201
  作者：Nobuhiko Hayakawa、Masatsugu Noguchi、Sen Takeshita、Agung Eviryanti、Yukie Seki、Hikaru Nishio、Ryohei Yokoyama、Misato Noguchi、Manami Shuto、Yoichiro Shima、Kanna Kuribayashi、Shunsuke Kageyama、Hiroyuki Eda、Manabu Suzuki、Tomohisa Hatta、Shun-ichiro Iemura、Tohru Natsume、Itsuya Tanabe、Ryusuke Nakagawa、Makoto Shiozaki、Kuniya Sakurai、Masataka Shoji、Ayatoshi Andou、Takashi Yamamoto

  DOI：10.1016/j.bmc.2014.03.036

  日期：2014.6

  Interleukin-12 (IL-12) and IL-23 are proinflammatory cytokines and therapeutic targets for inflammatory and autoimmune diseases, including inflammatory bowel diseases, psoriasis, rheumatoid arthritis, and multiple sclerosis. We describe the discovery of APY0201, a unique small molecular IL-12/23 production inhibitor, from activated macrophages and monocytes, and demonstrate ameliorated inflammation in an experimental model of colitis. Through a chemical proteomics approach using a highly sensitive direct nanoflow LC-MS/MS system and bait compounds equipped with the FLAG epitope associated regulator of PIKfyve (ArPIKfyve) was detected. Further study identified its associated protein phosphoinositide kinase, FYVE finger-containing (PIKfyve), as the target protein of APY0201, which was characterized as a potent, highly selective, ATP-competitive PIKfyve inhibitor that interrupts the conversion of phosphatidylinositol 3-phosphate (PtdIns3P) to PtdIns(3,5)P-2. These results elucidate the function of PIKfyve kinase in the IL-12/23 production pathway and in IL-12/23-driven inflammatory disease pathologies to provide a compelling rationale for targeting PIKfyve kinase in inflammatory and autoimmune diseases. (C) 2014 Elsevier Ltd. All rights reserved.
• US8314098B2
  申请人：——

  公开号：US8314098B2

  公开（公告）日：2012-11-20
• [EN] PYRAZOLOPYRIMIDINE COMPOUND<br/>[FR] COMPOSÉ DE PYRAZOLOPYRIMIDINE
  申请人：AJINOMOTO KK

  公开号：WO2010074284A1

  公开（公告）日：2010-07-01

  　ＩＬ－１２／ＩＬ－２３産生阻害活性を有する多くのバリエーション化合物を探索し、当該化合物を含有する、医薬組成物、ＩＬ－１２／ＩＬ－２３過剰産生関連疾患の治療又は予防剤を提供する。