hydroxylamine-O-mesitylenesulfonic acid

• 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: hydroxylamine-O-mesitylenesulfonic acid
• 英文别名: hydroxylamine-2,4,6-Trimethyl-benzenesulfonate；Hydroxylamine;2,4,6-trimethylbenzenesulfonic acid
• 化学式: C₉H₁₂O₃S*H₃NO
• 分子量: 233.288
• InChiKey: YEOPCLNIDCRQKI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.19
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  109
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2-氨基-4,6-二甲基嘧啶 、 1-amino-4,6-dimethyl-1H-pyrimidin-2-ylidene-ammonium 2,4,6-trimethyl-benzenesulfonate 、 hydroxylamine-O-mesitylenesulfonic acid 、 氯乙酸甲酯 在 NaOH 作用下， 以 乙醇 、 二氯甲烷 为溶剂， 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：

  NOVEL PHENYLIMIDAZOLE DERIVATIVE AS PDE10A ENZYME INHIBITOR

  摘要：

  这项发明提供了化合物5,8-二甲基-2-[2-(1-甲基-4-苯基-1H-咪唑-2-基)-乙基]-[1,2,4]噻唑并其药学上可接受的酸盐。

  公开号：

  US20120190685A1
• 作为试剂：
  描述：

  saccharin sodium salt 在 hydroxylamine-O-mesitylenesulfonic acid 作用下， 以 四氢呋喃 、 水 为溶剂， 反应 12.0h， 以82%的产率得到2-aminobenzo[d]isothiazol-3(2H)-one 1,1-dioxide
  参考文献：
  名称：

  N-氨基糖精的合成，结构和性质-人类碳酸酐酶I的选择性抑制剂

  摘要：

  通过将糖精钠盐与羟胺-O-间苯二甲磺酸（MSH）一步直接胺化，可以以高收率制得以前未知的N-氨基糖精，并研究了其反应性。对N-氨基糖精及其衍生物针对h CA同工型进行了测试，并将母体化合物鉴定为h CA I的选择性低微摩尔抑制剂（K i  = 8.8μM）。这些发现为设计提供了有效的配体起点有效的h CA I抑制剂的研发–一种有望治疗视网膜/脑水肿的药物。

  DOI：

  10.1016/j.tetlet.2016.12.005

文献信息

• Imidazole derivatives as PDE10A enzyme inhibitors
  申请人：Kehler Jan

  公开号：US20120129836A1

  公开（公告）日：2012-05-24

  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该发明化合物的治疗有效量和药用载体的药物组合物。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神经退行性疾病的方法，包括向患有神经退行性疾病的受试者施用式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受试者施用式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受试者施用式I化合物的治疗有效量。
• 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] HETEROAROMATIC PHENYLIMIDAZOLE DERIVATIVES AS PDE10A ENZYME INHIBITORS<br/>[FR] DÉRIVÉS HÉTÉROAROMATIQUES DE PHÉNYLIMIDAZOLE EN TANT QU'INHIBITEURS DE L'ENZYME PDE10A
  申请人：LUNDBECK & CO AS H

  公开号：WO2011072694A1

  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.

  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。
• [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。