N-(1-methyl-1H-pyrazol-3-yl)-6-(pyrazin-2-yloxy)quinazolin-4-yl-amine

• 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: N-(1-methyl-1H-pyrazol-3-yl)-6-(pyrazin-2-yloxy)quinazolin-4-yl-amine
• 英文别名: N-(1-methyl-1H-pyrazol-3-yl)-6-(pyrazin-2-yloxy)quinazolin-4-amine；N-(1-methylpyrazol-3-yl)-6-pyrazin-2-yloxyquinazolin-4-amine
• 化学式: C₁₆H₁₃N₇O
• 分子量: 319.326
• InChiKey: VDNZMIFVFXYAMK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  24
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  90.6
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  2-氯吡嗪 、 6-hydroxy-4-(1-methylpyrazol-3-ylamino)quinazoline 在 potassium tert-butylate 作用下， 以 N,N-二甲基乙酰胺 为溶剂， 生成 N-(1-methyl-1H-pyrazol-3-yl)-6-(pyrazin-2-yloxy)quinazolin-4-yl-amine
  参考文献：
  名称：

  Discovery and structure–activity relationships of a novel class of quinazoline glucokinase activators

  摘要：

  We describe design, syntheses and structure-activity relationships of a novel class of 4,6-disubstituted quinazoline glucokinase activators. Prototype quinazoline leads (4 and 5) were designed based on the X-ray analyses of the previous 2-aminobenzamide lead classes. Modifications of the quinazoline leads led to the identification of a potent GK activator (21d). (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.08.064

文献信息

• Substituted Quinazoline or Pyridopyrimidine Derivative
  申请人：Mitsuya Morihiro

  公开号：US20080032996A1

  公开（公告）日：2008-02-07

  The present invention provides a compound having a glucokinase activating action being useful for prevention or treatment of diabetes mellitus, etc. being represented by the formula (I): X is nitrogen atom, etc.; Y is oxygen atom, etc.; R 1 is an optionally substituted five to six-membered heteroaryl group, etc.; R 2 is hydrogen atom or fluorine atom; and ring A is a monocyclic or bicyclic heteroaryl group which may have a substituent represented by the formula (II)] or a pharmaceutically acceptable salt thereof.

  本发明提供了一种具有激活葡萄糖激酶作用的化合物，该化合物可用于预防或治疗糖尿病等疾病，其表示式为(I)：其中，X为氮原子等；Y为氧原子等；R1为可选取代的五至六元杂环芳基基团等；R2为氢原子或氟原子；环A为单环或双环杂环芳基基团，其可具有由式(II)表示的取代基，或其药学上可接受的盐。
• Substituted quinazoline or pyridopyrimidine derivative
  申请人：Banyu Pharmaceutical Co., Ltd.

  公开号：US07687502B2

  公开（公告）日：2010-03-30

  The present invention provides a compound having a glucokinase activating action being useful for prevention or treatment of diabetes mellitus, etc. being represented by the formula (I): X is nitrogen atom, etc.; Y is oxygen atom, etc.; R1 is an optionally substituted five to six-membered heteroaryl group, etc.; R2 is hydrogen atom or fluorine atom; and ring A is a monocyclic or bicyclic heteroaryl group which may have a substituent represented by the formula (II)] or a pharmaceutically acceptable salt thereof.

  本发明提供了一种具有激活葡萄糖激酶作用的化合物，其表示为式（I）：X为氮原子等；Y为氧原子等；R1为可选取代的五到六元杂环芳基等；R2为氢原子或氟原子；环A为单环或双环杂环芳基，其可以具有由式（II）表示的取代基，或其药学上可接受的盐，用于预防或治疗糖尿病等。
• SUBSTITUTED QUINAZOLINE OR PYRIDOPYRIMIDINE DERIVATIVE
  申请人：BANYU PHARMACEUTICAL CO., LTD.

  公开号：EP1734040A1

  公开（公告）日：2006-12-20

  The present invention provides a compound having a glucokinase activating action being useful for prevention or treatment of diabetes mellitus, etc. being represented by the formula (I): X is nitrogen atom, etc.; Y is oxygen atom, etc.; R1 is an optionally substituted five to six-membered heteroaryl group, etc.; R2 is hydrogen atom or fluorine atom; and ring A is a monocyclic or bicyclic heteroaryl group which may have a substituent represented by the formula (II)] or a pharmaceutically acceptable salt thereof.

  本发明提供了一种具有葡萄糖激酶激活作用的化合物，可用于预防或治疗糖尿病等，由式（I）表示： X为氮原子等；Y为氧原子等；R1为任选取代的五至六元杂芳基等；R2为氢原子或氟原子；环A为单环或双环杂芳基，可具有由式(II)代表的取代基]。 或其药学上可接受的盐。
• US7687502B2
  申请人：——

  公开号：US7687502B2

  公开（公告）日：2010-03-30
• Discovery and structure–activity relationships of a novel class of quinazoline glucokinase activators
  作者：Tomoharu Iino、Yasuhiro Sasaki、Makoto Bamba、Morihiro Mitsuya、Akio Ohno、Kenji Kamata、Hideka Hosaka、Hiroko Maruki、Mayumi Futamura、Riki Yoshimoto、Sumika Ohyama、Kaori Sasaki、Masato Chiba、Norikazu Ohtake、Yasufumi Nagata、Jun-ichi Eiki、Teruyuki Nishimura

  DOI：10.1016/j.bmcl.2009.08.064

  日期：2009.10

  We describe design, syntheses and structure-activity relationships of a novel class of 4,6-disubstituted quinazoline glucokinase activators. Prototype quinazoline leads (4 and 5) were designed based on the X-ray analyses of the previous 2-aminobenzamide lead classes. Modifications of the quinazoline leads led to the identification of a potent GK activator (21d). (C) 2009 Elsevier Ltd. All rights reserved.