Piperazine, 1-[(aminooxy)acetyl]-4-phenyl- | 398507-80-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: Piperazine, 1-[(aminooxy)acetyl]-4-phenyl-
• 英文别名: 2-aminooxy-1-(4-phenylpiperazin-1-yl)ethanone
• CAS: 398507-80-7
• 化学式: C₁₂H₁₇N₃O₂
• 分子量: 235.28
• InChiKey: BLQSENNYARVVFU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  58.8
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Pharmaceutical uses and synthesis of benzobicyclooctanes
  申请人：Celltech R & D, Inc.

  公开号：US20030069305A1

  公开（公告）日：2003-04-10

  Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-&agr; and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.

  苯并双环辛烷化合物，它们在抑制涉及TNF-α和IL-8的细胞事件以及在一般炎症事件治疗中的用途；多样双环辛烷的组合化合物库以及它们的合成过程，既可以作为库存，也可以作为单个化合物。
• Use of isatin derivatives as ion channel activating agents
  申请人：——

  公开号：US20020016354A1

  公开（公告）日：2002-02-07

  The present invention relates to ion channel activating agents. More particularly, the present invention relates to a particular class of chemical compounds that has proven useful as openers of SK Ca and IK Ca channels. In further aspects, the present invention relates to the use of these SK/IK channel activating agents for the manufacture of medicaments and pharmaceutical compositions comprising the SK/IK channel activating agents. The SK/IK channel activating agents of the invention are useful for the treatment or alleviation of diseases and conditions associated with the SK/IK channels, in particular respiratory diseases such as asthma, cystic fibrosis, chronic obstructive pulmonary disease and rhinorrhea, convulsions, vascular spasms, coronary artery spasms, renal disorders, polycystic kidney disease, bladder spasms, urinary incontinence, bladder outflow obstruction, irritable bowel syndrome, gastrointestinal dysfunction, secretory diarrhea, ischaemia, cerebral ischaemia, ischaemic heart disease, angina pectoris, coronary heart disease, traumatic brain injury, psychosis, anxiety, depression, dementia, memory and attention deficits, Alzheimer's disease, dysmenorrhea, narcolepsy, Reynaud's disease, intermittent claudication, Sjorgren's syndrome, migraine, arrhythmia, hypertension, absence seizures, myotonic muscle dystrophia, xerostomi, diabetes type II, hyperinsulinemia, premature labor, baldness, cancer, and immune suppression.

  本发明涉及离子通道激活剂。更具体地说，本发明涉及一类特定的化合物，已被证明对SKCa和IKCa通道的开放具有用处。在进一步方面，本发明涉及利用这些SK/IK通道激活剂制造药物和包含SK/IK通道激活剂的药物组合物。本发明的SK/IK通道激活剂对于治疗或缓解与SK/IK通道相关的疾病和症状非常有用，特别是呼吸道疾病，如哮喘、囊性纤维化、慢性阻塞性肺疾病和鼻涕，痉挛、血管痉挛、冠状动脉痉挛、肾脏疾病、多囊肾病、膀胱痉挛、尿失禁、膀胱排空阻塞、肠易激综合征、胃肠功能障碍、分泌性腹泻、缺血、脑缺血、缺血性心脏病、心绞痛、冠心病、创伤性脑损伤、精神病、焦虑、抑郁、痴呆、记忆和注意力缺陷、阿尔茨海默病、痛经、嗜睡症、雷诺氏病、间歇性跛行、斯约格伦综合征、偏头痛、心律失常、高血压、缺席性癫痫发作、肌肉肌无力、干燥综合征、2型糖尿病、胰岛素过多症、早产、秃头、癌症和免疫抑制。
• [EN] USE OF ISATIN DERIVATIVES AS ION CHANNEL ACTIVATING AGENTS<br/>[FR] UTILISATION DE DERIVES D'ISATINE EN TANT QU'AGENTS D'ACTIVATION DE CANAUX IONIQUES
  申请人：NEUROSEARCH AS

  公开号：WO2000033834A1

  公开（公告）日：2000-06-15

  The present invention relates to ion channel activating agents. More particularly, the present invention relates to a particular class of chemical compounds that has proven useful as openers of SKCa and IKCa channels. In further aspects, the present invention relates to the use of these SK/IK channel activating agents for the manufacture of medicaments, and pharmaceutical compositions comprising the SK/IK channel activating agents. The SK/IK channel activating agents of the invention are useful for the treatment or alleviation of diseases and conditions associated with the SK/IK channels, in particular respiratory diseases such as asthma, cystic fibrosis, chronic obstructive pulmonary disease and rhinorrhea, convulsions, vascular spasms, coronary artery spasms, renal disorders, polycystic kidney disease, bladder spasms, urinary incontinence, bladder outflow obstruction, irritable bowel syndrome, gastrointestinal dysfunction, secretory diarrhoea, ischaemia, cerebral ischaemia, ischaemic hearth disease, angina pectoris, coronary hearth disease, traumatic brain injury, psychosis, anxiety, depression, dementia, memory and attention deficits, Alzheimer's disease, dysmenorrhea, narcolepsy, Reynaud's disease, intermittent claudication, Sjorgren's syndrome, migraine, arrhythmia, hypertension, absence seizures, myotonic muscle dystrophia, xerostomi, diabetes type II, hyperinsulinemia, premature labour, baldness, cancer, and immune suppression.

  本发明涉及离子通道激活剂。更具体地，本发明涉及一类已被证明对SKCa和IKCa通道具有开放作用的化学化合物。在进一步方面，本发明涉及使用这些SK/IK通道激活剂制造药物，以及包括SK/IK通道激活剂的药物组合物。本发明的SK/IK通道激活剂对于治疗或缓解与SK/IK通道相关的疾病和症状非常有用，特别是呼吸系统疾病，如哮喘、囊性纤维化、慢性阻塞性肺疾病和流涕、惊厥、血管痉挛、冠状动脉痉挛、肾功能障碍、多囊肾病、膀胱痉挛、尿失禁、膀胱出口梗阻、肠易激综合征、胃肠功能障碍、分泌性腹泻、缺血、脑缺血、缺血性心脏病、心绞痛、冠心病、创伤性脑损伤、精神病、焦虑、抑郁症、痴呆、记忆和注意力缺陷、阿尔茨海默病、痛经、嗜睡症、雷诺氏病、间歇性跛行、Sjogren综合征、偏头痛、心律失常、高血压、失神发作、肌肉萎缩症、口干症、2型糖尿病、高胰岛素血症、早产、秃发、癌症和免疫抑制等。
• USE OF ISATIN DERIVATIVES AS ION CHANNEL ACTIVATING AGENTS
  申请人：NEUROSEARCH A/S

  公开号：EP1135123A1

  公开（公告）日：2001-09-26
• US6906046B2
  申请人：——

  公开号：US6906046B2

  公开（公告）日：2005-06-14