(1Z)-N'-hydroxy-2-(methylsulfonyl)ethanimidamide

• 分子结构分类: 有机化合物 - 有机硫化合物 - 磺酰类
• 英文名称: (1Z)-N'-hydroxy-2-(methylsulfonyl)ethanimidamide
• 英文别名: N'-hydroxy-2-methylsulfonylethanimidamide
• 化学式: C₃H₈N₂O₃S
• 分子量: 152.174
• InChiKey: PIXITPIFCMHKJZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.2
• 重原子数：
  9
• 可旋转键数：
  2
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  101
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  cis-1-(morpholin-4-ylcarbonyl)-5-[4-(trifluoromethyl)phenyl]piperidine-3-carboxylic acid 、 (1Z)-N'-hydroxy-2-(methylsulfonyl)ethanimidamide 生成 4-({3-(3-Methylsulphonylmethyl-1,2,4-oxadiazol-5-yl)-5-[4-(trifluoromethyl)phenyl]piperidin-1-yl}carbonyl)morpholine
  参考文献：
  名称：

  HETEROARYL-SUBSTITUTED PIPERIDINES

  摘要：

  本发明涉及新型杂环芳基取代哌啶，其制备过程，其用于治疗和/或预防疾病以及用于制备治疗和/或预防疾病的药物，特别是心血管疾病和肿瘤疾病。

  公开号：

  US20090306139A1
• 作为产物：
  描述：

  甲基磺酰乙腈 在 羟胺 作用下， 生成 (1Z)-N'-hydroxy-2-(methylsulfonyl)ethanimidamide
  参考文献：
  名称：

  Pyrrolopyridazine compounds and methods of use thereof for the treatment of proliferative disorders

  摘要：

  揭示了吡咯吡啶并嗪化合物，制备这类化合物的方法，以及它们用于治疗增殖性、炎症性和其他疾病的用途。

  公开号：

  US20040209886A1

文献信息

• [EN] PIPERIDINYLPYRAZOLOPYRIMIDINONES AND THEIR USE<br/>[FR] PIPÉRIDINYLPYRAZOLOPYRIMIDINONES ET LEUR UTILISATION
  申请人：BAYER PHARMA AG

  公开号：WO2016071216A1

  公开（公告）日：2016-05-12

  The present application relates to novel substituted piperidinylpyrazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired hemostatic disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of heavy menstrual bleeding, postpartum hemorrhage, hemorrhagic shock, hemorrhagic cystitis, gastrointestinal hemorrhage, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.

  本申请涉及新型取代哌啶基吡唑吡嘧啶酮，以及它们的制备方法，这些化合物可单独或组合使用于治疗和/或预防疾病的方法中，特别是用于治疗和/或预防患有或不患有基础遗传或获得性止血障碍的患者的急性和复发性出血，其中出血与从重经期出血、产后出血、出血性休克、出血性膀胱炎、胃肠道出血、创伤、手术、移植、中风、肝脏疾病、遗传性血管性水肿、鼻血、以及血液积聚后的滑膜炎和软骨损伤等一组疾病或医疗干预有关。
• 2-Trifluoroacetylthiophene oxadiazoles as potent and selective class II human histone deacetylase inhibitors
  作者：Ester Muraglia、Sergio Altamura、Danila Branca、Ottavia Cecchetti、Federica Ferrigno、Maria Vittoria Orsale、Maria Cecilia Palumbi、Michael Rowley、Rita Scarpelli、Christian Steinkühler、Philip Jones

  DOI：10.1016/j.bmcl.2008.09.076

  日期：2008.12

  class II HDAC inhibitors, with moderate selectivity. Exploration of replacements for the carboxamide with bioisosteric pentatomic heteroaromatic like 1,3,4-oxadiazoles, 1,2,4-oxadiazoles and 1,3-thiazoles, led to the discovery that 2-trifluoroacetylthiophene 1,3,4-oxadiazole derivatives are very potent low nanomolar HDAC4 inhibitors, highly selective over class I HDACs (HDAC 1 and 3), and moderately

  最近已经报道三氟乙酰基噻吩羧酰胺是II类HDAC抑制剂，具有中等选择性。探索用生物等位五原子杂芳族化合物（如1,3,4-恶二唑，1,2,4-恶二唑和1,3-噻唑）替代羧酰胺，导致发现2-三氟乙酰基噻吩1,3,4-恶二唑衍生物是非常有效的低纳摩尔HDAC4抑制剂，对I类HDAC（HDAC 1和3）具有高度选择性，并且在HCT116细胞培养中具有中等稳定性。
• HCV NS5B Inhibitors
  申请人：Bergstrom Carl P.

  公开号：US20070185083A1

  公开（公告）日：2007-08-09

  The invention encompasses compounds of Formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.

  这项发明涵盖了Formula I的化合物，以及使用这些化合物的组合物和方法。这些化合物对丙型肝炎病毒（HCV）具有活性，并可用于治疗感染HCV的人。
• Pyrrolidine oxadiazole-and thiadiazole oxime derivatives being oxytocin receptor antagonists
  申请人：Schwarz Matthias

  公开号：US20060229343A1

  公开（公告）日：2006-10-12

  The present invention is related to pyrrolidine oxadiazole and thiadiazole derivatives for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such pyrrolidine oxadiazole derivatives. Said pyrrolidine derivatives are useful in the treatment and/or prevention of preterm labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including preterm labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation. B is a oxadiazole or thiadiazole group.

  本发明涉及吡咯烷氧噻二唑和噻二唑衍生物，用作药物活性化合物，以及包含此类吡咯烷氧噻二唑衍生物的制药配方。所述吡咯烷衍生物在治疗和/或预防早产、早产和痛经方面具有用途。特别是，本发明涉及显示出 oxytocin 受体的重要调节作用，特别是拮抗剂活性的吡咯烷衍生物。更具体地说，所述化合物在治疗和/或预防由 oxytocin 介导的疾病状态方面具有用途，包括早产、早产和痛经。本发明还涉及新的吡咯烷衍生物以及它们的制备方法。B 是一个氧噻二唑或噻二唑基团。
• Pyrrolidine oxadiazole- and thiadiazole oxime derivatives being oxytocin receptor antagonists
  申请人：Applied Research Systems ARS Holding N.V.

  公开号：US07115639B2

  公开（公告）日：2006-10-03

  The present invention is related to pyrrolidine oxadiazole and thiadiazole derivatives for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such pyrrolidine oxadiazole derivatives. Said pyrrolidine derivatives are useful in the treatment and/or prevention of preterm labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including preterm labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation. (I) B is a oxadiazole or thiadiazole group

  本发明涉及吡咯烷噁唑和噻唑衍生物，用作药物活性化合物，以及含有此类吡咯烷噁唑衍生物的制药配方。所述吡咯烷衍生物在治疗和/或预防早产、早产和痛经方面有用。特别地，本发明涉及显示 oxytocin 受体的显著调节作用，特别是拮抗剂活性的吡咯烷衍生物。更优选地，这些化合物在治疗和/或预防由 oxytocin 介导的疾病状态，包括早产、早产和痛经方面有用。本发明还涉及新型吡咯烷衍生物以及它们的制备方法。(I) B 是噁唑或噻唑基团。