3-(N-哌嗪-1-基)-6-苯基吡嗪 | 50693-75-9

• 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: 3-(N-哌嗪-1-基)-6-苯基吡嗪
• 中文别名: 3-苯基-6-(哌嗪-1-基)哒嗪
• 英文名称: 3-(N-piperazin-1-yl)-6-phenylpyridazine
• 英文别名: 3-phenyl-6-(1-piperazinyl)pyridazine；3-phenyl-6-piperazin-1-yl-pyridazine；3-Phenyl-6-(piperazin-1-yl)pyridazine；3-phenyl-6-piperazin-1-ylpyridazine
• CAS: 50693-75-9
• 化学式: C₁₄H₁₆N₄
• mdl: MFCD07386473
• 分子量: 240.308
• InChiKey: GSQDWXKOJGHXCX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  41
• 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：

  3-(N-哌嗪-1-基)-6-苯基吡嗪 在 盐酸 、 sodium carbonate 、 potassium iodide 作用下， 以 甲醇 为溶剂， 反应 10.0h， 生成 3-<4-<3-(p-fluorobenzoyl)>-1-propylpiperazin-1-yl>-6-phenylpyridazine
  参考文献：
  名称：

  Pyridazine derivatives XII. Synthesis and antipsychotic-antidepressant activity of some butyrophenone derivatives of 6-phenylpyridazine

  摘要：

  We have synthesized several 3-amino-6-phenyl pyridazines in which the amino substituent is a linear butyrophenone moiety (compounds 8 and 10), a cyclic butyrophenone moiety (compound 3), or a phenylpiperazine fragment (compound 2). Compound 8 potently inhibited [H-3]spiperone binding to striatal D-2 receptors and [H-3]SCH 23390 binding to striatal D-1 receptors (K-i in the nanomolar range but lower than that of haloperidol). Compounds 3, 2 and 10 showed no affinity for dopamine (DA) receptors. Only 2 compounds (3 and 8) inhibited [H-3]ketanserin binding to cortical 5-HT2A receptors; compound 8 strongly inhibited binding with a K-i similar to that of methysergide, while binding was only weakly inhibited by compound 3. The DA and 5-HT2A antagonist. activity of compound 8 was evaluated in vivo and in vitro. The results in standard screening tests indicate that this compound possesses neuroleptic activity. However, in contrast to haloperidol, compound 8 did not modify DA and its metabolite levels in rat striatum, or induce catalepsy. It inhibited serotonin-induced contractions in endothelium-stripped aorta with a pA(2) of 8.26 and did not affect reserpine induced palpebral ptosis, indicating that it does not have antidepressant activity; compound 10, however, showed slight activity in this test.

  DOI：

  10.1016/0223-5234(94)90106-6
• 作为产物：
  描述：

  哌嗪 、 3-氯-6-苯基哒嗪 在 二氯甲烷 、 水 、 magnesium sulfate 作用下， 以 乙腈 为溶剂， 反应 16.0h， 以The title compound was obtained in 99% yield (1.200 g)的产率得到3-(N-哌嗪-1-基)-6-苯基吡嗪
  参考文献：
  名称：

  Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors

  摘要：

  本发明揭示了治疗哺乳动物，尤其是人类SCD介导的疾病或病况的方法，其中该方法包括向需要该药物的哺乳动物内给予化合物(I)的方法，其中化合物(I)的公式如下：其中x、y、G、J、K、L、M、V、R2、R3、R4、R5、R5a、R6、R6a、R7、R7a、R8和R8a在此定义。本发明还揭示了包含化合物(I)的制药组合物。

  公开号：

  US07767677B2

文献信息

• Treatment of affective disorders by the combined action of a nicotinic receptor agonist and a monoaminergic substance
  申请人：——

  公开号：US20040092508A1

  公开（公告）日：2004-05-13

  This invention relates to use of the combined action of a nicotinic acetylcholine receptor agonist and a monoaminergic substance for the treatment of affective disorders, as well as to pharmaceutical compositions comprising these substances and chemical substances for use according to the invention.

  本发明涉及使用尼古丁型乙酰胆碱受体激动剂和单胺类物质的联合作用治疗情感障碍，以及包含这些物质的制药组合物和用于本发明的化学物质。
• Heterocyclic Derivatives and Their Use as Stearoyl-Coa Desaturase Inhibitors
  申请人：Kamboj Rajender

  公开号：US20080096895A1

  公开（公告）日：2008-04-24

  Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, G, J, K, L, M, V R 2 , R 3 , R 4 , R 5 , R 5a , R 6 , R 6a , R 7 , R 7a , R 8 and R 8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

  本文披露了一种治疗哺乳动物（最好是人类）SCD介导的疾病或病症的方法，其中方法包括向需要该方法的哺乳动物施用式（I）的化合物：其中x、y、G、J、K、L、M、V、R2、R3、R4、R5、R5a、R6、R6a、R7、R7a、R8和R8a在本文中有定义。本文还披露了包含式（I）化合物的药物组合物。
• TREATMENT OF AFFECTIVE DISORDERS BY THE COMBINED ACTION OF A NICOTINIC RECEPTOR AGONIST AND A MONOAMINERGIC SUBSTANCE
  申请人：Olsen M. Gunnar

  公开号：US20070265241A1

  公开（公告）日：2007-11-15

  This invention relates to use of the combined action of a nicotinic acetylcholine receptor agonist and a monoaminergic substance for the treatment of affective disorders, as well as to pharmaceutical compositions comprising these substances and chemical substances for use according to the invention.

  本发明涉及使用尼古丁型乙酰胆碱受体激动剂和单胺类物质的联合作用治疗情感障碍，以及包含这些物质的药物组合物和用于本发明的化学物质。
• Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
  申请人：Xenon Pharmaceuticals Inc.

  公开号：US07767677B2

  公开（公告）日：2010-08-03

  Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, G, J, K, L, M, V R2, R3, R4, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

  本发明揭示了治疗哺乳动物，尤其是人类SCD介导的疾病或病况的方法，其中该方法包括向需要该药物的哺乳动物内给予化合物(I)的方法，其中化合物(I)的公式如下：其中x、y、G、J、K、L、M、V、R2、R3、R4、R5、R5a、R6、R6a、R7、R7a、R8和R8a在此定义。本发明还揭示了包含化合物(I)的制药组合物。
• Novel (4-substituted-piperazinyl)pyridazines
  申请人：JANSSEN PHARMACEUTICA N.V.

  公开号：EP0211457A2

  公开（公告）日：1987-02-25

  Novel (4-substituted-piperazinyl)pyridazines of formula wherein R is hydrogen, halo, C1-6alkyloxy, hydroxy or phenyl; m is the integer 2 or 3; R¹, R², R³ and R⁴ are, each independently, hydrogen, or C1-6alkyl; or where R³ and R⁴ are substituted on a different carbon atom, R³ and R⁴ taken together, may form a bivalent radical -CH₂-CH₂-; R⁵ is (aryl)C2-6alkenyl, (aryl)C2-6alkynyl, (aryl)(hydroxy)­C1-6alkyl or (aryl)(oxo)C1-6alkyl; the N-oxide forms, the pharmaceutically acceptable acid addition salts and the possible stereochemically isomeric forms, which compounds are analgesic and antitussive agents; pharmaceutical compositions containing such compounds as an active ingredient and methods of preparing said compounds and pharmaceutical compositions.

  新型 (4-取代哌嗪基)哒嗪，其式如下 其中 R 是氢、卤素、C1-6-烷氧基、羟基或苯基； m 是整数 2 或 3； R¹、R²、R³ 和 R⁴ 各自独立为氢或 C1-6 烷基； 或当 R³ 和 R⁴ 在不同碳原子上被取代时，R³ 和 R⁴ 合在一起可形成二价基 -CH₂-CH₂-； R⁵ 是（芳基）C2-6烯基、（芳基）C2-6炔基、（芳基）（羟基）C1-6烷基或（芳基）（氧代）C1-6烷基； N-氧化物形式、药学上可接受的酸加成盐以及可能的立体化学异构形式，这些化合物是镇痛和止咳剂；含有这些化合物作为活性成分的药物组合物以及制备所述化合物和药物组合物的方法。