2-ethylbenzyl methanesulfonate | 910777-83-2

• 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: 2-ethylbenzyl methanesulfonate
• 英文别名: (2-Ethylphenyl)methyl methanesulfonate；(2-ethylphenyl)methyl methanesulfonate
• CAS: 910777-83-2
• 化学式: C₁₀H₁₄O₃S
• 分子量: 214.285
• InChiKey: ITVZOLBIGHWGIW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  14
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  51.8
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-ethylbenzyl methanesulfonate 在 sodium hydride 、 一水合肼 作用下， 以 四氢呋喃 、 甲苯 、 mineral oil 为溶剂， 反应 18.08h， 生成 4-(2-ethylphenylmethyl)-1,2-dihydro-5-isopropyl-3H-pyrazol-3-one
  参考文献：
  名称：

  Structure–activity relationship studies of 4-benzyl-1H-pyrazol-3-yl β-d-glucopyranoside derivatives as potent and selective sodium glucose co-transporter 1 (SGLT1) inhibitors with therapeutic activity on postprandial hyperglycemia

  摘要：

  Sodium glucose co-transporter 1 (SGLT1) plays a dominant role in the absorption of glucose in the gut and is considered a promising target in the development of treatments for postprandial hyperglycemia. A series of 4-benzyl-1H-pyrazol-3-yl beta-D-glucopyranoside derivatives have been synthesized, and its inhibitory activity toward SGLTs has been evaluated. By altering the substitution groups at the 5-position of the pyrazole ring, and every position of the phenyl ring, we studied the structure-activity relationship (SAR) profiles and identified a series of potent and selective SGLT1 inhibitors. Representative derivatives showed a dose-dependent suppressing effect on the escalation of blood glucose levels in oral mixed carbohydrate tolerance tests (OCTT) in streptozotocin-nicotinamide-induced diabetic rats (NA-STZ rats). (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2012.09.037
• 作为产物：
  描述：

  邻乙基苯甲醇 、 甲基磺酰氯 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 1.5h， 以600 mg的产率得到2-ethylbenzyl methanesulfonate
  参考文献：
  名称：

  [EN] COMBINATION TREATMENTS COMPRISING ADMINISTRATION OF IMIDAZOPYRAZINONES
  [FR] TRAITEMENTS COMBINÉS COMPRENANT L'ADMINISTRATION D'IMIDAZOPYRAZINONES

  摘要：

  本发明提供了组合治疗方法，包括给予PDE1酶抑制剂和其他在治疗神经退行性疾病（例如阿尔茨海默病、帕金森病或亨廷顿病）方面有用的化合物。本发明的另一方面涉及上述化合物的联合使用，用于治疗神经退行性和/或认知障碍。本发明还提供了包括上述PDE1酶抑制剂和其他在治疗神经退行性疾病方面有用的化合物的药物组合物。

  公开号：

  WO2018078042A1

文献信息

• [EN] IMIDAZOPYRAZINONES AS PDE1 INHIBITORS<br/>[FR] IMIDAZOPYRAZINONES UTILISÉES COMME INHIBITEURS DE PDE1
  申请人：H LUNDBECK AS

  公开号：WO2016174188A1

  公开（公告）日：2016-11-03

  The present invention provides imidazopyrazinones as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.

  本发明提供了咪唑吡嗪酮类化合物作为PDE1抑制剂，并将其用作药物，特别用于治疗神经退行性疾病和精神疾病。
• [EN] COMBINATION TREATMENTS COMPRISING IMIDAZOPYRAZINONES FOR THE TREATMENT OF PSYCHIATRIC AND/OR COGNITIVE DISORDERS<br/>[FR] TRAITEMENTS COMBINÉS COMPRENANT DES IMIDAZOPYRAZINONES POUR LE TRAITEMENT DE TROUBLES PSYCHIATRIQUES ET/OU COGNITIFS
  申请人：H LUNDBECK AS

  公开号：WO2018078038A1

  公开（公告）日：2018-05-03

  The present invention provides combination treatments comprising administration of compounds that are PDE1 enzyme inhibitors and other compounds useful in the treatment of psychiatric and/or cognitive disorders such as for example Attention Deficit Hyperactivity Disorder (ADHD), depression, anxiety, narcolepsy, schizophrenia, cognitive impairment or cognitive impairment associated with schizophrenia (CIAS). Separate aspects of the invention are directed to the combined use of said compounds for the treatment of psychiatric and/or cognitive disorders. The present invention also provides pharmaceutical compositions comprising said PDE1 enzyme inhibitors together with other compounds useful in the treatment of psychiatric and/or cognitive disorders.

  本发明提供了组合治疗方法，包括给予PDE1酶抑制剂和其他在治疗精神和/或认知障碍方面有用的化合物，例如注意力缺陷多动障碍（ADHD）、抑郁症、焦虑症、嗜睡症、精神分裂症、认知障碍或与精神分裂症相关的认知障碍（CIAS）的治疗。该发明的另一方面涉及上述化合物的联合使用以治疗精神和/或认知障碍。本发明还提供了包括上述PDE1酶抑制剂和其他在治疗精神和/或认知障碍方面有用的化合物的药物组合物。
• [EN] COMBINATION TREATMENTS COMPRISING ADMINISTRATION OF IMIDAZOPYRAZINONES<br/>[FR] TRAITEMENTS COMBINÉS COMPRENANT L'ADMINISTRATION D'IMIDAZOPYRAZINONES
  申请人：H LUNDBECK AS

  公开号：WO2018078042A1

  公开（公告）日：2018-05-03

  The present invention provides combination treatments comprising administration of compounds that are PDE1 enzyme inhibitors and other compounds useful in the treatment of neurodegenerative disorders such as for example Alzheimer's Disease, Parkinson's Disease or Huntington's Disease. Separate aspects of the invention are directed to the combined use of said compounds for the treatment of neurodegenerative and/or cognitive disorders. The present invention also provides pharmaceutical compositions comprising said PDE1 enzyme inhibitors together with other compounds useful in the treatment of neurodegenerative disorders.

  本发明提供了组合治疗方法，包括给予PDE1酶抑制剂和其他在治疗神经退行性疾病（例如阿尔茨海默病、帕金森病或亨廷顿病）方面有用的化合物。本发明的另一方面涉及上述化合物的联合使用，用于治疗神经退行性和/或认知障碍。本发明还提供了包括上述PDE1酶抑制剂和其他在治疗神经退行性疾病方面有用的化合物的药物组合物。
• Derivatives of Imidazo [1,2-A] Pyridine Useful as Medicaments For Treating Gastrointestinal Diseases
  申请人：Bamford Mark James

  公开号：US20080255358A1

  公开（公告）日：2008-10-16

  Disclosed are imidazopyridine compounds having the formula:

  揭示了具有以下式子的咪唑吡啶化合物：
• CHIRAL CONTROL
  申请人：WAVE LIFE SCIENCES PTE. LTD.

  公开号：US20150211006A1

  公开（公告）日：2015-07-30

  The present invention relates to chirally controlled oligonucleotides, chirally controlled oligonucleotide compositions, and the method of making and using the same. The invention specifically encompasses the identification of the source of certain problems with prior methodologies for preparing chiral oligonucleotides, including problems that prohibit preparation of fully chirally controlled compositions, particularly compositions comprising a plurality of oligonucleotide types. In some embodiments, the present invention provides chirally controlled oligonucleotide compositions. In some embodiments, the present invention provides methods of making chirally controlled oligonucleotides and chirally controlled oligonucleotide compositions.

  本发明涉及手性控制的寡核苷酸、手性控制的寡核苷酸组合物以及其制备和使用方法。本发明特别涵盖了鉴定以前制备手性寡核苷酸方法中某些问题的来源，包括禁止制备完全手性控制的组合物，特别是包含多种寡核苷酸类型的组合物。在某些实施例中，本发明提供了手性控制的寡核苷酸组合物。在某些实施例中，本发明提供了制备手性控制的寡核苷酸和手性控制的寡核苷酸组合物的方法。