1-amino-4,6-dimethyl-1H-pyrimidin-2-ylidene-ammonium 2,4,6-trimethyl-benzenesulfonate | 446839-32-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1-amino-4,6-dimethyl-1H-pyrimidin-2-ylidene-ammonium 2,4,6-trimethyl-benzenesulfonate
• 英文别名: 1-amino-4,6-dimethyl-1H-pyrimidin-2-ylidene-amnnoniunn 2,4,6-trinnethyl-benzenesulfonate；1-amino-4,6-dimethylpyrimidin-2(1H)-iminium 2,4,6-trimethylbenzenesulfonate；4,6-dimethylpyrimidin-1-ium-1,2-diamine;2,4,6-trimethylbenzenesulfonate
• CAS: 446839-32-3
• 化学式: C₆H₁₀N₄*C₉H₁₂O₃S
• 分子量: 338.431
• InChiKey: CUOZHUHTGNEBKK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  23
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  134
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  1-amino-4,6-dimethyl-1H-pyrimidin-2-ylidene-ammonium 2,4,6-trimethyl-benzenesulfonate 、 氯乙酸甲酯 在 sodium hydroxide 作用下， 以 乙醇 为溶剂， 反应 1.0h， 以9%的产率得到2-(chloromethyl)-5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidine
  参考文献：
  名称：

  [EN] HETEROAROMATIC PHENYLIMIDAZOLE DERIVATIVES AS PDE10A ENZYME INHIBITORS
  [FR] DÉRIVÉS HÉTÉROAROMATIQUES DE PHÉNYLIMIDAZOLE EN TANT QU'INHIBITEURS DE L'ENZYME PDE10A

  摘要：

  本发明涉及化合物，这些化合物是PDE10A酶抑制剂。本发明提供了一种药物组合物，包含本发明化合物的治疗有效量和药学上可接受的载体。本发明还提供了制备式I化合物的方法。本发明进一步提供了一种治疗患有神经退行性疾病的主体的方法，包括向该主体施用式I化合物的治疗有效量。本发明还提供了一种治疗患有药物成瘾的主体的方法，包括向该主体施用式I化合物的治疗有效量。本发明进一步提供了一种治疗患有精神疾病的主体的方法，包括向该主体施用式I化合物的治疗有效量。

  公开号：

  WO2011072694A1
• 作为产物：
  描述：

  2-氨基-4,6-二甲基嘧啶 以 甲醇 、 methanol-dichloromethane 、 二氯甲烷 、 水 为溶剂， 生成 1-amino-4,6-dimethyl-1H-pyrimidin-2-ylidene-ammonium 2,4,6-trimethyl-benzenesulfonate
  参考文献：
  名称：

  Method and composition for rejuvinating cells, tissues organs, hair and nails

  摘要：

  在一个实施例中，本发明涉及包含药物组合物的化合物和组合物，其中药物组合物包含这些化合物，并且相关方法解耦蛋白质、脂质、核酸和其他生物材料以及它们的任意组合的糖介导偶联。在另一个实施例中，这些组合物和相关方法在体内具有实用性，用于减少生物体暴露于内部摄入、经皮应用或其他方式的化合物或组合物时，糖介导偶联过程的有害影响。在另一个实施例中，这些组合物和相关方法对器官、细胞和组织的离体处理以及头发、指甲和皮肤的外部处理具有用处，通过改变可变性和增加组织扩散系数来使它们恢复活力。在另一个实施例中，本发明涉及新颖的化合物和药物组合物。

  公开号：

  US20020188015A1

文献信息

• HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF
  申请人：CAMPBELL John Emmerson

  公开号：US20120178748A1

  公开（公告）日：2012-07-12

  Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.

  本文提供了杂环芳基化合物，其合成方法，包含这些化合物的药物组合物，以及它们的使用方法。在一个实施例中，本文提供的化合物可用于治疗、预防和/或管理各种疾病，如中枢神经系统疾病和代谢性疾病，包括但不限于神经系统疾病、精神病、精神分裂症、肥胖症和糖尿病。
• NOVEL PHENYLIMIDAZOLE DERIVATIVES AS PDE10A ENZYME INHIBITORS
  申请人：Ritzén Andreas

  公开号：US20100016303A1

  公开（公告）日：2010-01-21

  This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.

  这项发明涉及一类PDE10A酶抑制剂化合物。该发明提供了一种包含所述发明化合物的治疗有效量和药学可接受载体的药物组合物。本发明还提供了制备式I化合物的方法。本发明还提供了一种治疗患有神经退行性疾病的受试者的方法，包括向受试者投予式I化合物的治疗有效量。本发明还提供了一种治疗患有药物成瘾的受试者的方法，包括向受试者投予式I化合物的治疗有效量。本发明还提供了一种治疗患有精神障碍的受试者的方法，包括向受试者投予式I化合物的治疗有效量。
• [EN] 2-ARYLIMIDAZOLE DERIVATIVES AS PDE10A ENZYME INHIBITORS<br/>[FR] DÉRIVÉS DE 2-ARYLIMIDAZOLE EN TANT QU'INHIBITEURS DE L'ENZYME PDE10A
  申请人：LUNDBECK & CO AS H

  公开号：WO2011072696A1

  公开（公告）日：2011-06-23

  This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula (I). The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I). The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula (I). The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I).

  这项发明涉及一类PDE10A酶抑制剂化合物。该发明提供了一种包含本发明化合物的治疗有效量和药学可接受载体的药物组合物。本发明还提供了制备式(I)化合物的方法。本发明进一步提供了一种治疗神经退行性疾病的方法，包括向患有神经退行性疾病的对象施用式(I)化合物的治疗有效量。本发明还提供了一种治疗药物成瘾的方法，包括向患有药物成瘾的对象施用式(I)化合物的治疗有效量。本发明还提供了一种治疗精神障碍的方法，包括向患有精神障碍的对象施用式(I)化合物的治疗有效量。
• [EN] HETEROAROMATIC ARYL TRIAZOLE DERIVATIVES AS PDE10A ENZYME INHIBITORS<br/>[FR] DÉRIVÉS HÉTÉROAROMATIQUES D'ARYLTRIAZOLE EN TANT QU'INHIBITEURS DE L'ENZYME PDE10A
  申请人：LUNDBECK & CO AS H

  公开号：WO2011072697A1

  公开（公告）日：2011-06-23

  This invention is directed to compounds (Formula 1), which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula (I). The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I). The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula (I). The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I).

  这项发明涉及化合物（式1），其为PDE10A酶抑制剂。该发明提供了一种包括本发明化合物的治疗有效量和药用可接受载体的药物组合物。本发明还提供了制备式（I）化合物的方法。本发明还提供了一种治疗患有神经退行性疾病的受试者的方法，包括向受试者施用化合物式（I）的治疗有效量。本发明还提供了一种治疗患有药物成瘾的受试者的方法，包括向受试者施用化合物式（I）的治疗有效量。本发明还提供了一种治疗患有精神障碍的受试者的方法，包括向受试者施用化合物式（I）的治疗有效量。
• [EN] NOVEL PHENYLIMIDAZOLE DERIVATIVES AS PDE10A ENZYME INHIBITORS<br/>[FR] NOUVEAU DÉRIVÉS DE PHÉNYLIMIDAZOLE CONVENANT COMME INHIBITEURS DE L'ENZYME PDE10A
  申请人：LUNDBECK & CO AS H

  公开号：WO2009152825A1

  公开（公告）日：2009-12-23

  This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective, amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula (I). The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I). The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula (I). The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I).

  该发明涉及一种PDE10A酶抑制剂的化合物。该发明提供了一种包含该发明化合物的治疗有效量和药用可接受载体的药物组合物。本发明还提供了一种制备公式（I）化合物的方法。本发明还提供了一种治疗患有神经退行性疾病的受试者的方法，包括向受试者投与公式（I）化合物的治疗有效量。本发明还提供了一种治疗患有药物成瘾的受试者的方法，包括向受试者投与公式（I）化合物的治疗有效量。本发明还提供了一种治疗患有精神障碍的受试者的方法，包括向受试者投与公式（I）化合物的治疗有效量。