2-(piperidin-4-yloxy)pyrazine | 615576-64-2

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-(piperidin-4-yloxy)pyrazine
• 英文别名: 2-piperidin-4-yloxypyrazine
• CAS: 615576-64-2
• 化学式: C₉H₁₃N₃O
• mdl: MFCD11504921
• 分子量: 179.222
• InChiKey: KFNFTHXHLCBICA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.555
• 拓扑面积：
  47
• 氢给体数：
  1
• 氢受体数：
  4

安全信息

• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  2-(piperidin-4-yloxy)pyrazine 在 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 反应 2.0h， 生成 4-(pyrimidin-2-yloxy)-piperidine-1-carboxylic acid 2-trifluoromethoxy-benzylamide
  参考文献：
  名称：

  Rapid synthesis of an array of trisubstituted urea-based soluble epoxide hydrolase inhibitors facilitated by a novel solid-phase method

  摘要：

  A 270-membered library of trisubstituted ureas was synthesized and evaluated for inhibition of soluble epoxide hydrolase. Library design and reagent selection was guided by the use of a pharmacophore model and synthesis of the array was enabled with a general solid-phase method. This array approach facilitated multi-dimensional SAR around this series and identified functionality responsible for binding affinity, as well as opportunities for modulating the overall in vitro profiles of this class of soluble epoxide hydrolase inhibitors. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.04.078
• 作为产物：
  描述：

  2-(哌啶-4-基氧代)嘧啶 、 N-[3,3-bis(4-fluorophenyl)propyl]-3-(hydroxymethyl)piperidine-1-carboxamide 在 1,8-二氮杂双环[5.4.0]十一碳-7-烯 作用下， 以 N,N-二甲基乙酰胺 为溶剂， 反应 36.0h， 生成 2-(piperidin-4-yloxy)pyrazine
  参考文献：
  名称：

  Rapid synthesis of an array of trisubstituted urea-based soluble epoxide hydrolase inhibitors facilitated by a novel solid-phase method

  摘要：

  A 270-membered library of trisubstituted ureas was synthesized and evaluated for inhibition of soluble epoxide hydrolase. Library design and reagent selection was guided by the use of a pharmacophore model and synthesis of the array was enabled with a general solid-phase method. This array approach facilitated multi-dimensional SAR around this series and identified functionality responsible for binding affinity, as well as opportunities for modulating the overall in vitro profiles of this class of soluble epoxide hydrolase inhibitors. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.04.078

文献信息

• [EN] SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS<br/>[FR] COMPOSÉS DE PYRAZOLO[1,5-A]PYRIDINE SUBSTITUÉS EN TANT QU'INHIBITEURS DE LA KINASE RET
  申请人：ANDREWS STEVEN W

  公开号：WO2018071454A1

  公开（公告）日：2018-04-19

  Provided herein are compounds of the Formula I: (I) or pharmaceutically acceptable salt or solvate thereof, wherein A, B, X1, X2, X3, X4, Ring D, E, Ra, Rb, n and m have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.

  本文提供了Formula I的化合物：(I)或其药用可接受的盐或溶剂，其中A、B、X1、X2、X3、X4、环D、E、Ra、Rb、n和m的含义如规范中所述，它们是RET激酶的抑制剂，并且在治疗和预防可以用RET激酶抑制剂治疗的疾病中非常有用，包括与RET相关的疾病和紊乱。
• Substituted Pyrimidine and Triazine Compounds
  申请人：Schunk Stefan

  公开号：US20100173889A1

  公开（公告）日：2010-07-08

  Substituted pyrimidine and triazine compounds corresponding to formula I wherein R 1 , R 2 , R 3 , R 4a , R 4b , R 5a , R 5b , R 7 , R 8 , R 9a , R 9b , R 10 , R 11 , A, a, b, s, t, V, W 1 , W 2 and W 3 have defined meanings, pharmaceutical compositions comprising such compounds, a process for preparing such compounds, and the use of such compounds and compositions to treat or inhibit pain and/or other disorders or disease states.

  将对应于公式I的嘧啶和三嗪化合物替代为R1、R2、R3、R4a、R4b、R5a、R5b、R7、R8、R9a、R9b、R10、R11、A、a、b、s、t、V、W1、W2和W3具有定义意义，包括这种化合物的药物组合物、制备这种化合物的过程，以及使用这种化合物和组合物来治疗或抑制疼痛和/或其他疾病状态的专利。
• [EN] SUBSTITUTED 2, 4-DIAMINO-QUINOLINE DERIVATIVES FOR USE IN THE TREATMENT OF PROLIFERATIVE DISEASES<br/>[FR] DÉRIVÉS SUBSTITUÉS DE 2, 4-DIAMINO-QUINOLÉINE POUR LEUR UTILISATION DANS LE TRAITEMENT DE MALADIES PROLIFÉRATIVES
  申请人：GENOSCIENCE PHARMA

  公开号：WO2017191599A1

  公开（公告）日：2017-11-09

  This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein which exhibit strong inhibition effects on various cancer cell lines. The compounds disclosed herein are useful for the treatment of proliferative diseases, including neoplastic diseases such as cancer and non- neoplastic disorders such as rheumatoid arthritis. Also disclosed are pharmaceutical compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient and optionally one or more additional therapeutically active agents, including anticancer agents. This application also discloses methods for treating a proliferative disease, including neoplastic diseases such as cancer and non- neoplastic disorders such as rheumatoid arthritis.

  本申请披露了根据通用式（I）定义的化合物，其中所有变量如本文所述，这些化合物对各种癌细胞系表现出强烈的抑制作用。本文披露的化合物对于治疗增生性疾病非常有用，包括肿瘤性疾病如癌症和非肿瘤性疾病如类风湿性关节炎。还披露了含有通用式（I）化合物和至少一种载体、稀释剂或赋形剂以及可选的一种或多种其他治疗活性剂的药物组合物。本申请还披露了治疗增生性疾病的方法，包括肿瘤性疾病如癌症和非肿瘤性疾病如类风湿性关节炎的方法。
• [EN] SULFONAMIDE DERIVATIVES<br/>[FR] DERIVES DE SULFAMIDE
  申请人：CELLTECH R&D LTD

  公开号：WO2003087071A1

  公开（公告）日：2003-10-23

  Sulfonamide derivatives of formula (1) are described wherein X is an O or S atom; Y is an 0 or S atom; A is a group -S02NR1R2; m is zero or the integer 1; n is zero or the integer 1; provided that at least one but not both of m and n are the integer 1; R3 is a hydrogen atom or an alkyl or cycloalkyl group; and the salts, solvates, hydrates, tautomers, isomers, N-oxides thereof. The compounds are potent inhibitors of IMPDH and are of use as immunosuppressants, anti-cancer agents, anti-inflammatory agents, antipsoriatic and anti-viral agents.

  描述了式（1）的磺酰胺衍生物，其中X是O或S原子；Y是0或S原子；A是-S02NR1R2基团；m为零或整数1；n为零或整数1；前提是m和n中至少有一个但不是两个都是整数1；R3是氢原子或烷基或环烷基；以及其盐，溶剂合物，水合物，互变异构体，N-氧化物。这些化合物是IMPDH的有效抑制剂，并可用作免疫抑制剂，抗癌剂，抗炎剂，抗银屑病和抗病毒剂。
• HETEROCYCLIC TRPML1 AGONISTS
  申请人：Libra Therapeutics, Inc.

  公开号：EP3821947A1

  公开（公告）日：2021-05-19

  The invention relates to a compound of formula (I) or a stereoisomer thereof, or a salt of any of the foregoing and to processes for its preparation. The compounds of formula (I) are useful in the treatment TRPML1- mediated disorders or diseases.

  该发明涉及公式(I)的化合物或其立体异构体，或任何上述化合物的盐，以及其制备的过程。公式(I)的化合物在治疗TRPML1介导的疾病或疾病中有用。