2,5,7-trichloroquinoline | 577967-74-9

• 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: 2,5,7-trichloroquinoline
• CAS: 577967-74-9
• 化学式: C₉H₄Cl₃N
• 分子量: 232.496
• InChiKey: WEXKNHYUKUGFKP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  12.9
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  1-环丙基哌嗪 、 2,5,7-trichloroquinoline 以 various solvent(s) 为溶剂， 反应 44.0h， 生成 5,7-Dichloro-2-(4-cyclopropyl-piperazin-1-yl)-quinoline
  参考文献：
  名称：

  2-（4-烷基哌嗪-1-基）喹啉是一种新型的无咪唑的组胺H3受体拮抗剂。

  摘要：

  为了确定结构新颖，中央作用的组胺H（3）拮抗剂，准备了一系列的2-（4-烷基哌嗪-1-基）喹啉。取代基的系统变化导致低极性表面积和血脑屏障渗透的适当log P的高效组胺H（3）拮抗剂。

  DOI：

  10.1021/jm040873u
• 作为产物：
  描述：

  5,7-二氯-2-喹啉 在 三氯氧磷 作用下， 反应 2.0h， 以67%的产率得到2,5,7-trichloroquinoline
  参考文献：
  名称：

  2-（4-烷基哌嗪-1-基）喹啉是一种新型的无咪唑的组胺H3受体拮抗剂。

  摘要：

  为了确定结构新颖，中央作用的组胺H（3）拮抗剂，准备了一系列的2-（4-烷基哌嗪-1-基）喹啉。取代基的系统变化导致低极性表面积和血脑屏障渗透的适当log P的高效组胺H（3）拮抗剂。

  DOI：

  10.1021/jm040873u

文献信息

• Novel aryl- and heteroarylpiperazines
  申请人：——

  公开号：US20030236259A1

  公开（公告）日：2003-12-25

  Novel aryl- and heteroarylpiperazines, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.

  新颖的芳基和杂环基哌嗪类化合物，这些化合物作为药物组合物的用途，包含这些化合物的药物组合物，以及利用这些化合物和组合物的治疗方法。这些化合物显示出对组胺H3受体的高度和选择性结合亲和力，表明具有组胺H3受体拮抗、逆激动或激动活性。因此，这些化合物对于治疗与组胺H3受体相关的疾病和紊乱是有用的。
• Novel Aryl- and Heteroarylpiperazines
  申请人：Hohlweg Rolf

  公开号：US20090264435A1

  公开（公告）日：2009-10-22

  Novel aryl- and heteroarylpiperazines, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.

  新型芳基和杂环基哌嗪，这些化合物的药用组合物，包含这些化合物的药用组合物，以及采用这些化合物和组合物的治疗方法。这些化合物表现出高度和选择性的结合亲和力，表明它们具有组胺H3受体拮抗、反向激动或激动活性。因此，这些化合物对于治疗与组胺H3受体相关的疾病和障碍非常有用。
• NOVEL ARYL- AND HETEROARYLPIPERAZINES
  申请人：NOVO NORDISK A/S

  公开号：EP1474401A2

  公开（公告）日：2004-11-10
• [EN] NOVEL ARYL- AND HETEROARYLPIPERAZINES<br/>[FR] NOUVELLES ARYL- ET HETEROARYLPIPERAZINES
  申请人：NOVO NORDISK AS

  公开号：WO2003066604A2

  公开（公告）日：2003-08-14

  Novel aryl- and heteroarylpiperazines, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.
• MULTITARGET NUCLEAR RECEPTOR LIGANDS BASED ON 2-(4-(QUINOLIN-2-YLOXY)PHENOXY)PROPANOIC ACID AND 2-(4-(QUINOXALIN-2-YLOXY)PHENOXY)PROPANOIC ACID FOR THE TREATMENT OF METABOLIC AND LIVER DISEASES
  申请人：[en]CHARLES UNIVERSITY, FACULTY OF PHARMACY IN HRADEC KRALOVE

  公开号：WO2024132001A1

  公开（公告）日：2024-06-27

  1. A compound of general formula (I) wherein L1is either aryl or 6-membered heteroaryl, which optionally further includes a heteroatom selected from N, O, and S; L2is aryl, 5 or 6-membered heteroaryl containing 1 or 2 heteroatoms selected from N, O and S; or C5-C6 cycloalkyl; R1is H or independently selected from the group consisting of C1-C2 alkyl, C1-C2 haloalkyl, wherein each of these substituents may optionally be further substituted by one or more substituents selected from the group consisting of halogen, pseudohalogen, hydroxy, amino, or alkyloxy moieties; R2is H or independently selected from the group consisting of C1-C4 alkyl, C1-C4 haloalkyl, wherein each of these substituents may optionally be further substituted by one or more substituents selected from the group consisting of halogen, pseudohalogen, hydroxy, amino, or alkyloxy moieties; R3is H or independently selected from the group consisting of halogen, pseudohalogen, C1-C2 alkyl, C1-C2 haloalkyl, hydroxy or amino moieties; R4is H or independently selected from the group consisting of halogen, pseudohalogen, C1-C2 alkyl, C1-C2 haloalkyl, methoxy C1-C4 alkyl, thio C1-C4 alkyl, halogen, pseudohalogen, wherein each of these substituents may optionally be further substituted by halogen, pseudohalogen, hydroxy, or amino moiety; R5is H or independently selected from the one or two groups consisting of C1-C4 alkyl, C1-C4 haloalkyl, methoxy C1-C4 alkyl, thio C1-C4 alkyl, halogen, pseudohalogen, wherein each of these substituents may optionally be further substituted by halogen, pseudohalogen, hydroxy, nitro, or amino moiety; R6is H or independently selected from C1-C6 alkyl, C1-C4 haloalkyl, methoxy Cl- C4 alkyl, thio C1-C4 alkyl, wherein each of these substituents may optionally be further substituted by halogen, pseudohalogen, hydroxy, nitro, or amino moiety; Y is O, C, N, or S; and n is 0, 1 or 2, as well as any isomers, including geometric, tautomeric and optical forms, as well as mixtures of isomers, including racemic mixtures, and pharmaceutically acceptable derivatives and solvates thereof, for use, as a compound dually acting on two nuclear receptors in prevention or treatment of conditions which are mediated by the action, or by loss of action, of PPARα, PPARγ or FXR receptors or their endogenous ligands, and/or by excessive stimulation of LXRα.