N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide | 77746-90-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide
• 英文别名: N-(2,5-diphenylpyrazol-3-yl)benzamide
• CAS: 77746-90-8
• 化学式: C₂₂H₁₇N₃O
• mdl: MFCD00122768
• 分子量: 339.396
• InChiKey: AYVLYDAJDALPHK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  26
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  46.9
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide 在 三氯氧磷 作用下， 以 乙醇 为溶剂， 反应 6.0h， 生成 2-((5-(((dimethylamino)methylene)amino)-1,3-diphenyl-1H-pyrazol-4-yl)methylene)hydrazine-1-carbothioamide
  参考文献：
  名称：

  Simay, A.; Takacs, K.; Horvath, K., Acta Chimica Academiae Scientiarum Hungaricae, 1980, vol. 105, p. 127 - 140

  摘要：

  DOI：
• 作为产物：
  描述：

  苯肼 在 potassium carbonate 作用下， 以 乙醇 、 溶剂黄146 、 丙酮 为溶剂， 反应 3.0h， 生成 N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide
  参考文献：
  名称：

  Simay, A.; Takacs, K.; Horvath, K., Acta Chimica Academiae Scientiarum Hungaricae, 1980, vol. 105, p. 127 - 140

  摘要：

  DOI：

文献信息

• [EN] PYRIDINYLPYRAZOLES FOR USE AS KINASE MODULATORS FOR THE TREATMENT OF CANCER<br/>[FR] PYRIDINYLPYRAZOLES DESTINÉS À ÊTRE UTILISÉS COMME MODULATEURS DE KINASE DANS LE TRAITEMENT DU CANCER
  申请人：SYNOVO GMBH

  公开号：WO2013046041A1

  公开（公告）日：2013-04-04

  Compounds of the substituted pyrazole class of Formula (I) as treatments for cancer are reported. A method of treating cancer in which a compound that inhibits the activity of receptor kinases is described. Said method is effective and can be provided in addition to standard therapies, notably chemotherapy using cytotoxic drugs and other forms of immune therapy including therapeutic vaccines.

  报道了公式（I）的取代吡唑类化合物作为治疗癌症的方法。描述了一种抑制受体激酶活性的化合物治疗癌症的方法。该方法是有效的，并可在标准治疗，特别是使用细胞毒性药物的化疗和其他形式的免疫疗法，包括治疗性疫苗的基础上提供。
• Pyrazole modulators of metabotropic glutamate receptors
  申请人：Lindsley W. Craig

  公开号：US20060281803A1

  公开（公告）日：2006-12-14

  The present invention is directed to compounds which are allosteric modulators of metabotropic glutamate receptors, including the mGluR5 receptor, and which are useful in the treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.

  本发明涉及化合物，它们是代谢性谷氨酸受体的别构调节剂，包括mGluR5受体，并且在治疗与谷氨酸功能障碍和代谢性谷氨酸受体相关的神经和精神障碍以及相关疾病方面有用。该发明还涉及包含这些化合物的制药组合物以及在预防或治疗代谢性谷氨酸受体相关疾病方面使用这些化合物和组合物。
• BENZAMIDE mGluR5 POSITIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING SAME
  申请人：Conn P. Jeffrey

  公开号：US20090042855A1

  公开（公告）日：2009-02-12

  In one aspect, the invention relates to compounds, including phenylethynylbenzamide derivatives, cycloalkylethynylbenzamide derivatives, styrylbenzamide derivatives, 4-(3-phenyl-1,2,4-oxadiazol-5-yl)benzamide derivatives, 4-(pyridinylethynyl)benzamide derivatives, and N 1 -phenylterephthalamide derivatives, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

  本发明涉及化合物，包括苯乙炔基苯甲酰胺衍生物、环烷基乙炔基苯甲酰胺衍生物、苯乙烯基苯甲酰胺衍生物、4-(3-苯基-1,2,4-噁唑-5-基)苯甲酰胺衍生物、4-(吡啶乙炔基)苯甲酰胺衍生物和N1-苯基对苯二甲酰胺衍生物，它们是代谢型谷氨酸受体亚型5 (mGluR5) 的正向变构调节剂；制备这些化合物的合成方法；含有这些化合物的药物组合物；以及使用这些化合物和组合物治疗与谷氨酸功能失调相关的神经和精神障碍的方法。本摘要旨在作为搜索特定领域的扫描工具，不限制本发明。
• Partial mGluR5 antagonists for treatment of anxiety and CNS disorders
  申请人：Conn Jeffrey P.

  公开号：US20070208028A1

  公开（公告）日：2007-09-06

  Provided is a method of treating conditions and disorders for which full mGluR5 antagonists are potentially effective, such as, e.g., anxiety, epilepsy, schizophrenia and other psychotic disorders, Parkinson's disease, addictive disorders, and the like in a subject in need of such treatment, comprising administration to such subject of a therapeutically effective amount of a partial, non-competitive mGluR5 antagonist compound of the invention. Specific examples of partial MgluR5 antagonists provided include those compounds having the formula: wherein: Z is, independently N or —CH—, provided that one, and only one Z is N; R is halogen (e.g., Br, F and the like), alkyl (e.g., methyl), alkenyl (e.g., CH═CH2, aryl (e.g., phenyl), heterocyclic (e.g., thiophenyl).

  提供了一种治疗全mGluR5拮抗剂可能有效的疾病和疾病的方法，例如焦虑、癫痫、精神分裂症和其他精神障碍、帕金森病、成瘾性疾病等，适用于需要此类治疗的患者，包括向该患者施用本发明的部分、非竞争性mGluR5拮抗剂化合物的治疗有效量。所提供的部分MgluR5拮抗剂的具体例子包括具有以下式子的化合物：其中：Z独立地为N或—CH—，但仅有一个Z为N；R为卤素（例如Br、F等）、烷基（例如甲基）、烯基（例如CH═CH2）、芳基（例如苯基）、杂环（例如噻吩基）。
• KINASE MODULATORS FOR THE TREATMENT OF CANCER
  申请人：Synovo GmbH

  公开号：US20140336225A1

  公开（公告）日：2014-11-13

  Compounds of the substituted pyrazole class as treatments for cancer are reported. A method of treating cancer in which a compound that inhibits the activity of receptor kinases. Said method is effective and can be provided in addition to standard therapies, notably chemotherapy using cytotoxic drugs and other forms of immune therapy including therapeutic vaccines.

  报道了替代吡唑类化合物作为治疗癌症的方法。一种治疗癌症的方法是使用抑制受体激酶活性的化合物。该方法是有效的，并可在标准疗法中提供，特别是化疗使用细胞毒药物和其他形式的免疫疗法，包括治疗性疫苗。