5-(4-氟苯基)吡嗪-2-羧酸 | 652979-82-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 中文名称: 5-(4-氟苯基)吡嗪-2-羧酸
• 英文名称: 5-(4-fluorophenyl)-2-pyrazinecarboxylic acid
• 英文别名: 5-(4-Fluorophenyl)pyrazine-2-carboxylic acid
• CAS: 652979-82-3
• 化学式: C₁₁H₇FN₂O₂
• 分子量: 218.187
• InChiKey: UDUYQYBNZRZQIZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  63.1
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  5-(4-氟苯基)吡嗪-2-羧酸 、 2-cyclopropyl-3-methylimidazo[1,2-a]pyridin-6-amine 在 N,N-二异丙基乙胺 、 Methanaminium,N-[(dimethylamino)(3H-1,2,3-triazolo[4,5-b]pyridin-3-yloxy)methylene]-N-methyl-, hexafluorophosphate(1-) 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 16.0h， 生成 N-(2-cyclopropyl-3-methylimidazo[1,2-a]pyridin-6-yl)-5-(4-fluorophenyl)-2-pyrazinecarboxamide
  参考文献：
  名称：

  Discovery of imidazo[1,2-a]pyridines as potent MCH1R antagonists

  摘要：

  A series of imidazo[1,2-a] pyridine derivatives was identified and evaluated for MCH1R binding and antagonistic activity. Introduction of a methyl substituent at the 3-position of imidazo[1,2-a] pyridine provided compounds with a significant improvement in MCH1R affinity. Representative compounds in this series exhibited good potency and brain exposure in rats. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.06.101
• 作为产物：
  描述：

  5-(4-fluorophenyl)-2-pyrazine-carbonitrile 在 硫酸 、 水 作用下， 生成 5-(4-氟苯基)吡嗪-2-羧酸
  参考文献：
  名称：

  EP1657242

  摘要：

  公开号：

文献信息

• Antagonists to melanin-concentrating hormone receptor comprising benzimidazole derivative as active ingredient
  申请人：Moriya Minoru

  公开号：US20050222161A1

  公开（公告）日：2005-10-06

  This invention relates to a benzimidazole derivative of the general formula [I] [wherein B 1 , B 2 , and B 3 represent hydrogen atom or lower alkyl; R 1 and R 2 are same or different and represent lower alkyl, etc.; R 3 and R 4 represent hydrogen atom, etc.; W represents a 3 to 8-membered aromatic or alphatic heterocycle, etc.; and Ar represents a substituted or unsubstituted aromatic heterocycle, etc.] This compound functions as an antagonist to melanin-concentrating hormone receptor and is useful as a drug for central diseases, circulatory diseases and metabolic diseases.

  本发明涉及一种苯并咪唑衍生物，其一般式为[I] [其中B1，B2和B3代表氢原子或低碳基; R1和R2相同或不同，代表低碳基等; R3和R4代表氢原子等; W代表3至8个成员的芳香或脂肪族杂环等; Ar代表取代或未取代的芳香族杂环等] 该化合物作为黑色素浓缩激素受体的拮抗剂，并可用作中枢疾病、循环系统疾病和代谢性疾病的药物。
• Imidazopyridine Derivatives
  申请人：Kishino Hiroyuki

  公开号：US20080200494A1

  公开（公告）日：2008-08-21

  The invention provides imidazopyridine derivatives represented by the general formula [I] [in which R 1 and R 2 may be the same or different and stand for C 1-6 alkyl or the like, R 3 and R 4 stand for hydrogen atom, methyl group or the like, W stands for mono- or bi-cyclic 3- to 8-membered aromatic or aliphatic heterocycle or the like, and Ar stands for optionally substituted aromatic heterocycle or the like]. These compounds act as melanin-concentrating hormone receptor antagonist and are useful as medicines for central nervous system disorders, cardiovascular system disorders and metabolic disorders.

  该发明提供了由通式[I]表示的咪唑吡啶衍生物 [其中R1和R2可能相同或不同，且代表C1-6烷基或类似物，R3和R4代表氢原子，甲基基团或类似物，W代表单环或双环的3-8元芳香或脂肪杂环或类似物，Ar代表可选择取代的芳香杂环或类似物]。这些化合物作为黑色素浓集激素受体拮抗剂，可用于治疗中枢神经系统疾病、心血管系统疾病和代谢性疾病的药物。
• Imidazopyridine derivatives
  申请人：Banyu Pharmaceuticals, Co., Ltd.

  公开号：US07504412B2

  公开（公告）日：2009-03-17

  The invention provides imidazopyridine derivatives represented by the general formula [I] [in which R1 and R2 may be the same or different and stand for C1-6 alkyl or the like, R3 and R4 stand for hydrogen atom, methyl group or the like, W stands for mono- or bi-cyclic 3- to 8-membered aromatic or aliphatic heterocycle or the like, and Ar stands for optionally substituted aromatic heterocycle or the like]. These compounds act as melanin-concentrating hormone receptor antagonist and are useful as medicines for central nervous system disorders, cardiovascular system disorders and metabolic disorders.

  本发明提供了由通式[I]表示的咪唑吡啶衍生物 [其中R1和R2可以相同或不同，代表C1-6烷基或类似物，R3和R4代表氢原子，甲基基团或类似物，W代表单环或双环3-8成员的芳香或脂肪族杂环或类似物，Ar代表可选取代的芳香杂环或类似物]。这些化合物作为黑素浓聚激素受体拮抗剂，并且可用于治疗中枢神经系统疾病、心血管系统疾病和代谢性疾病的药物。
• NOVEL MCH RECEPTOR ANTAGONISTS
  申请人：Beck James Peter

  公开号：US20090170913A1

  公开（公告）日：2009-07-02

  The present invention relates to a melanin concentrating hormone antagonist compound of formula (I); wherein Ar 1 , L 1 , R 1 , q, X, R 2 , R 3 , R 4 , and R 5 are as defined, or a pharmaceutically acceptable salt, solvate, or enantiomer thereof useful in the treatment, prevention or amelioration of symptoms associated with obesity and related diseases.

  本发明涉及一种公式(I)的黑色素浓集激素拮抗剂化合物;其中Ar1，L1，R1，q，X，R2，R3，R4和R5如定义，或其药学上可接受的盐，溶剂合物或对映体，用于治疗，预防或改善与肥胖和相关疾病相关的症状。
• IMIDAZOPYRIDINE DERIVATIVES
  申请人：BANYU PHARMACEUTICAL CO., LTD.

  公开号：EP1657242A1

  公开（公告）日：2006-05-17

  The invention provides imidazopyridine derivatives represented by the general formula [I] [in which R1 and R2 may be the same or different and stand for C1-6 alkyl or the like, R3 and R4 stand for hydrogen atom, methyl group or the like, W stands for mono- or bi-cyclic 3- to 8-membered aromatic or aliphatic heterocycle or the like, and Ar stands for optionally substituted aromatic heterocycle or the like]. These compounds act as melanin-concentrating hormone receptor antagonist and are useful as medicines for central nervous system disorders, cardiovascular system disorders and metabolic disorders.

  本发明提供由通式[I]代表的咪唑吡啶衍生物[其中 R1 和 R2 可以相同或不同，代表 C1-6 烷基或类似物，R3 和 R4 代表氢原子、甲基或类似物，W 代表单环或双环 3 至 8 元芳香族或脂肪族杂环或类似物，Ar 代表任选取代的芳香族杂环或类似物]。这些化合物具有黑色素浓缩激素受体拮抗剂的作用，可作为治疗中枢神经系统疾病、心血管系统疾病和代谢紊乱的药物。