2-cyclopropyl-3-methyl-6-nitroimidazo[1,2-a]pyridine | 845826-84-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡啶类
• 英文名称: 2-cyclopropyl-3-methyl-6-nitroimidazo[1,2-a]pyridine
• CAS: 845826-84-8
• 化学式: C₁₁H₁₁N₃O₂
• 分子量: 217.227
• InChiKey: PEFVNMSRFMQVPW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  63.1
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-cyclopropyl-3-methyl-6-nitroimidazo[1,2-a]pyridine 在 palladium 10% on activated carbon 、 氢气 作用下， 以 甲醇 为溶剂， 反应 2.0h， 生成 2-cyclopropyl-3-methylimidazo[1,2-a]pyridin-6-amine
  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：

  2-氨基-5-硝基吡啶 、 2-溴-1-环丙基-1-丙酮 以 乙醇 为溶剂， 生成 2-cyclopropyl-3-methyl-6-nitroimidazo[1,2-a]pyridine
  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

文献信息

• 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 Compound
  申请人：Sakuraba Shunji

  公开号：US20070249659A1

  公开（公告）日：2007-10-25

  The present invention provides an imidazopyridine compound represented by formula (I), wherein R 1 and R 2 each independently represent a C 1-6 alkyl group et al; R 3 and R 4 each independently represent a hydrogen atom, a methyl et al; Ar 1 is a divalent substituent representing a monocyclic or bicyclic, 3- to 8-membered aromatic or aliphatic heterocyclic group et al; Ar 2 represents an aromatic carbocyclic group, or an aromatic heterocyclic group; W represents —(CH 2 ) m et al, and m indicates an integer of from 0 to 10. This compound acts as a melanin concentrating hormone receptor antagonist, and is useful as treating agents for obesity.

  本发明提供了一种以式（I）表示的咪唑吡啶化合物，其中R1和R2各自独立地表示C1-6烷基等；R3和R4各自独立地表示氢原子、甲基等；Ar1表示一个双价的取代基，该取代基代表一个单环或双环、3-到8-成员的芳香或脂肪族杂环基等；Ar2表示一个芳香碳环基或芳香杂环基；W表示—（CH2）me等，其中m表示从0到10的整数。该化合物作为黑色素浓集激素受体拮抗剂，并且可用作肥胖症的治疗剂。
• 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。
• 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。
• IMIDAZOPYRIDINE COMPOUND
  申请人：BANYU PHARMACEUTICAL CO., LTD.

  公开号：EP1748048A1

  公开（公告）日：2007-01-31

  The present invention provides an imidazopyridine compound represented by formula (I), wherein R1 and R2 each independently represent a C1-6 alkyl group et al; R3 and R4 each independently represent a hydrogen atom, a methyl et al; Ar1 is a divalent substituent representing a monocyclic or bicyclic, 3- to 8-membered aromatic or aliphatic heterocyclic group et al; Ar2 represents an aromatic carbocyclic group, or an aromatic heterocyclic group; W represents -(CH2)m et al, and m indicates an integer of from 0 to 10. This compound acts as a melanin concentrating hormone receptor antagonist, and is useful as treating agents for obesity.

  本发明提供了一种由式（I）代表的咪唑吡啶化合物、 其中 R1 和 R2 各自独立地代表 C1-6 烷基等；R3 和 R4 各自独立地代表氢原子、甲基等；Ar1 是二价取代基，代表单环或双环、3 至 8 元芳香族或脂肪族杂环基等；Ar2 代表芳香族碳环基团或芳香族杂环基团；W 代表-(CH2)m 等，m 表示 0 至 10 的整数。该化合物是一种黑色素浓缩激素受体拮抗剂，可作为肥胖症的治疗药物。