4-Chloro-6-nitro-2-propylquinoline | 538360-65-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 4-Chloro-6-nitro-2-propylquinoline
• CAS: 538360-65-5
• 化学式: C₁₂H₁₁ClN₂O₂
• 分子量: 250.685
• InChiKey: YNBYRQNMTLTTKM-UHFFFAOYSA-N

物化性质

• 沸点：
  364.2±37.0 °C(Predicted)
• 密度：
  1.320±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  58.7
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-Chloro-6-nitro-2-propylquinoline 在 三氯化铁 、 肼 作用下， 以 甲醇 为溶剂， 生成
  参考文献：
  名称：

  4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists

  摘要：

  Structure-activity relationships of a 4-aminoquinoline MCHlR antagonist lead series were explored by synthesis of analogs with modifications at the 2-, 4-, and 6-positions of the original HTS hit. Improvements to the original screening lead included lipophilic groups at the 2-position and biphenyl, cyclohexyl phenyl, and hydrocinnamyl carboxamides at the 6-position. Modifications of the 4-amino group were not well tolerated. (c) 2006 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2006.08.008
• 作为产物：
  描述：

  2-propyl-4-hydroxy-6-nitroquinoline 在 三氯氧磷 作用下， 生成 4-Chloro-6-nitro-2-propylquinoline
  参考文献：
  名称：

  4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists

  摘要：

  Structure-activity relationships of a 4-aminoquinoline MCHlR antagonist lead series were explored by synthesis of analogs with modifications at the 2-, 4-, and 6-positions of the original HTS hit. Improvements to the original screening lead included lipophilic groups at the 2-position and biphenyl, cyclohexyl phenyl, and hydrocinnamyl carboxamides at the 6-position. Modifications of the 4-amino group were not well tolerated. (c) 2006 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2006.08.008

文献信息

• [EN] 4-AMINOQUINOLINE COMPOUNDS<br/>[FR] COMPOSES 4-AMINOQUINOLEINES
  申请人：MERCK & CO INC

  公开号：WO2003045920A1

  公开（公告）日：2003-06-05

  The present invention is concerned with compounds of the general Formula I : and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-1R antagonists. As such, compounds of the present invention are useful for the treatment or prevention of obesity or eating disorders associated with excessive food intake and complications thereof, osteoarthritis, certain cancers, AIDS wasting, cachexia, frailty (particularly in elderly), mental disorders stress, cognitive disorders, sexual function, reproductive function, kidney function, locomotor disorders, attention deficit disorder (ADD), substance abuse disorders and dyskinesias, Huntington s disease, epilepsy, memory function, and spinal muscular atrophy. Compounds of formula I may therefore be used in the treatment of these conditions, and in the manufacture of a medicament useful in treating these conditions. Pharmaceutical formulations comprising one of the compounds of formula (I) as an active ingredient are disclosed, as are processes for preparing these compounds.

  本发明涉及一般式I的化合物及其药学上可接受的盐，这些化合物可用作黑色素浓集激素受体拮抗剂，尤其是MCH-1R拮抗剂。因此，本发明的化合物可用于治疗或预防与过度进食及其并发症相关的肥胖症或进食障碍、骨关节炎、某些癌症、艾滋病消耗症、消瘦、虚弱（尤其是老年人）、心理障碍、压力、认知障碍、性功能、生殖功能、肾功能、运动障碍、注意力缺陷障碍（ADD）、物质滥用障碍和运动障碍、亨廷顿病、癫痫、记忆功能和脊髓肌萎缩症。因此，I式化合物可用于治疗这些疾病，并用于制造用于治疗这些疾病的药物。本发明披露了包含一种I式化合物作为活性成分的制药配方，以及制备这些化合物的过程。
• 4-Aminoquinoline compounds
  申请人：DeVita J. Robert

  公开号：US20050009815A1

  公开（公告）日：2005-01-13

  The present invention is concerned with compounds of the general Formula I: and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-1R antagonists. As such, compounds of the present invention are useful for the treatment or prevention of obesity or eating disorders associated with excessive food intake and complications thereof, osteoarthritis, certain cancers, AIDS wasting, cachexia, frailty (particularly in elderly), mental disorders stress, cognitive disorders, sexual function, reproductive function, kidney function, locomotor disorders, attention deficit disorder (ADD), substance abuse disorders and dyskinesias, Huntington's disease, epilepsy, memory function, and spinal muscular atrophy. Compounds of formula I may therefore be used in the treatment of these conditions, and in the manufacture of a medicament useful in treating these conditions. Pharmaceutical formulations comprising one of the compounds of formula (I) as an active ingredient are disclosed, as are processes for preparing these compounds.

  本发明涉及一般式I的化合物及其药用可接受的盐，其作为黑色素浓集激素受体拮抗剂，特别是MCH-1R拮抗剂，具有用途。因此，本发明的化合物可用于治疗或预防与过度进食及其并发症相关的肥胖症或进食障碍、骨关节炎、某些癌症、艾滋病消耗综合征、恶病质、虚弱（特别是老年人）、心理障碍、压力、认知障碍、性功能、生殖功能、肾功能、运动障碍、注意力缺陷障碍（ADD）、物质滥用障碍和运动障碍、亨廷顿病、癫痫、记忆功能和脊髓肌萎缩症。因此，式I的化合物可用于治疗这些疾病，并用于制造用于治疗这些疾病的药物。本发明还揭示了包含式（I）的化合物作为活性成分的制药配方，以及制备这些化合物的过程。
• 4-AMINOQUINOLINE COMPOUNDS
  申请人：Merck & Co., Inc.

  公开号：EP1451156A1

  公开（公告）日：2004-09-01
• EP1451156A4
  申请人：——

  公开号：EP1451156A4

  公开（公告）日：2005-05-25
• 4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists
  作者：Jinlong Jiang、Peter Lin、Myle Hoang、Lehua Chang、Carina Tan、Scott Feighner、Oksana C. Palyha、Donna L. Hreniuk、Jie Pan、Andreas W. Sailer、Nancy R. Morin、Douglas J. MacNeil、Andrew D. Howard、Lex H.T. Van der Ploeg、Mark T. Goulet、Robert J. DeVita

  DOI：10.1016/j.bmcl.2006.08.008

  日期：2006.10

  Structure-activity relationships of a 4-aminoquinoline MCHlR antagonist lead series were explored by synthesis of analogs with modifications at the 2-, 4-, and 6-positions of the original HTS hit. Improvements to the original screening lead included lipophilic groups at the 2-position and biphenyl, cyclohexyl phenyl, and hydrocinnamyl carboxamides at the 6-position. Modifications of the 4-amino group were not well tolerated. (c) 2006 Elsevier Ltd. All rights reserved.