1-(2-methylbenzoxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea | 249889-64-3

• 物质功能分类: 生物化工 - 生化试剂 - 激动剂抑制剂
• 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-(2-methylbenzoxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea
• 英文别名: SB 334867；N-(2-methyl-6-benzoxazolyl)-N’-1,5-naphthyridin-4-yl urea；N-(2-methyl-6-benzoxazolyl)-N′-1,5-naphthyridin-4-yl urea；N-(2-methyl-6-benzoxazolyl)-N’-1,5-naphthyridin-4-ylurea；1-(2-methyl-1,3-benzoxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea；N-(2-methyl-6-ben-zoxazolyl)-N'-1,5-naphthyridin-4-yl urea；1-(2-Methylbenzo[d]oxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea
• CAS: 249889-64-3
• 化学式: C₁₇H₁₃N₅O₂
• 分子量: 319.323
• InChiKey: AKMNUCBQGHFICM-UHFFFAOYSA-N

物化性质

• 熔点：
  >235°C (dec.)
• 溶解度：
  可溶于二氯甲烷（少许）、DMSO（少许）

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  24
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  92.9
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  4-羟基-1,5-萘啶 在 2,6-二甲基吡啶 、 叠氮磷酸二苯酯 、 盐酸丙胺 作用下， 生成 1-(2-methylbenzoxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea
  参考文献：
  名称：

  1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor

  摘要：

  This communication reports SARs for the first orexin-1 receptor antagonist series of 1-aryl-3-quifiolin-4-yl and 1-aryl-3-naphthyridin-4-yl ureas. One of these compounds, 31 (5B-334867), has excellent selectivity for the orexin-1 receptor, blood-brain barrier permeability and shows in vivo activity following ip dosing. (C) 2001 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(01)00343-2

文献信息

• 3-AMINOIMIDAZO 1,2-A PYRIDINE DERIVATIVES HAVING AN SGLT1- AND SGLT2-INHIBITING ACTION FOR THE TREATMENT OF TYPE 1 AND TYPE 2 DIABETES
  申请人：Klein Markus

  公开号：US20100305142A1

  公开（公告）日：2010-12-02

  Novel compounds of the formula (I), in which W, T, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 have the meanings indicated in Patent Claim ( 1 ), are suitable as antidiabetics.

  化合物的新颖结构如下（I）式，其中W，T，R1，R2，R3，R4，R5和R6的含义如专利权要求（1）中所示，适用作为抗糖尿病药物。
• Benzimidazole Derivatives
  申请人：Burgdorf Lars Thore

  公开号：US20100016372A1

  公开（公告）日：2010-01-21

  Novel compounds of the formula I (I), in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , R, Q, W, X and Z have the meanings indicated in Patent Claim 1 , are suitable as antidiabetics.

  公式I（I）的新化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，R11，R12，R13，R，Q，W，X和Z的含义如专利权要求书中所示，适用于抗糖尿病药物。
• IMIDAZO 1, 2-A PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF DISEASES SUCH AS DIABETES
  申请人：Klein Markus

  公开号：US20100249151A1

  公开（公告）日：2010-09-30

  Novel compounds of the formula (I), in which W, T, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and X 7 have the meanings indicated in Patent Claim 1 , are suitable as antidiabetics.

  化合物的新颖结构式（I），其中W、T、R1、R2、R3、R4、R5、R6和X7的含义如专利权要求书中所示，适用于抗糖尿病药物。
• ANTIANXIETY DRUGS AND A METHOD OF SCREENING THE SAME
  申请人：Sawai Toru

  公开号：US20070160538A1

  公开（公告）日：2007-07-12

  An anxiolytic drug of the invention comprises an orexin receptor antagonist, a pharmacologically acceptable salt thereof, or a solvate thereof as an active ingredient. A method for screening a compound having an anxiolytic action of the invention comprises a step of using orexin-A.

  本发明的抗焦虑药物包括作为活性成分的食欲素受体拮抗剂、其药理上可接受的盐或其溶剂化物。本发明用于筛选具有抗焦虑作用的化合物的方法包括使用食欲素-A的步骤。
• Substituted N-aryl heterocycles, process for their preparation and their use as medicaments
  申请人：Aventis Pharma Deutschland GmbH

  公开号：US20040220191A1

  公开（公告）日：2004-11-04

  The invention relates to substituted N-aryl heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I 1 in which the radicals have the stated meanings, the N-oxides and the physiologically tolerated salts thereof and process for the preparation thereof are described. The compounds are suitable for example as anorectic agents.

  这项发明涉及取代N-芳基杂环化合物及其生理耐受盐和生理功能衍生物。式I的化合物 1 其中基团具有所述含义，其N-氧化物及其生理耐受盐以及其制备方法被描述。这些化合物例如适用作为厌食剂。