Ethanol, 2-[[3-butyl-4-[(2-methylphenyl)amino]-8-quinolinyl]oxy]- | 799765-45-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: Ethanol, 2-[[3-butyl-4-[(2-methylphenyl)amino]-8-quinolinyl]oxy]-
• 英文别名: 2-[3-butyl-4-(2-methylanilino)quinolin-8-yl]oxyethanol
• CAS: 799765-45-0
• 化学式: C₂₂H₂₆N₂O₂
• 分子量: 350.5
• InChiKey: MTUDPDCLKAOLSZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.3
• 重原子数：
  26
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  54.4
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• Nitrosated proton pump inhibitors, compositions and methods of use
  申请人：NitroMed, Inc.

  公开号：US20040024014A1

  公开（公告）日：2004-02-05

  The invention describes novel nitrosated proton pump inhibitor compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated proton pump inhibitor compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated proton pump inhibitor compound, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated proton pump inhibitor compound, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating gastrointestinal disorders; facilitating ulcer healing; decreasing the recurrence of ulcers; improving gastroprotective properties, anti- Helicobacter pylori properties or antacid properties of proton pump inhibitors; decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds; treating bacterial infections and/or viral infections.

  该发明描述了新颖的亚硝化质子泵抑制剂化合物及其药用盐，以及包含至少一种亚硝化质子泵抑制剂化合物的新型组合物，以及可选地，至少一种捐赠、转移或释放一氧化氮、刺激内源性一氧化氮合成、提高内源性内皮源性舒张因子水平或是一氧化氮合酶底物的化合物，和/或至少一种治疗剂。该发明还提供了包含至少一种亚硝化质子泵抑制剂化合物和至少一种捐赠、转移或释放一氧化氮、提高内源性内皮源性舒张因子水平、刺激内源性一氧化氮合成或是一氧化氮合酶底物和/或至少一种治疗剂的新型组合物。该发明还提供了包含至少一种亚硝化质子泵抑制剂化合物，可选地至少一种一氧化氮供体和/或至少一种治疗剂的新型套装。该发明还提供了治疗胃肠道疾病的方法；促进溃疡愈合；减少溃疡复发；改善质子泵抑制剂的胃保护性能、抗幽门螺杆菌性能或抗酸性能；减少或减轻与非甾体类抗炎化合物使用相关的胃肠毒性；治疗细菌感染和/或病毒感染。
• Nitrosated and nitrosylated proton pump inhibitors, compositions and methods of use
  申请人：NitroMed, Inc.

  公开号：US20040266828A1

  公开（公告）日：2004-12-30

  The present invention describes novel nitrosated and/or nitrosylated proton pump inhibitor compounds, and novel compositions comprising at least one proton pump inhibitor compound that is optionally substituted with at least one NO and/or NO 2 group, and, optionally, at least one compound that donates, transfers, or releases nitric oxide, induces the production of endogenous nitric oxide or endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase, and/or at least one nonsteroidal antiinflammatory drug, selective COX-2 inhibitor, antacid, bismuth-containing reagent, acid-degradable antibacterial compound, and mixtures thereof. The present invention also provides methods for treating and/or preventing gastrointestinal disorders; facilitating ulcer healing; decreasing the recurrence of ulcers; improving gastroprotective properties, anti- Helicobacter pylon properties or antacid properties of proton pump inhibitors; decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds; treating Helicobacter pylori and viral infections. The compounds and/or compositions of the present invention can also be provided in the form of a pharmaceutical kit.

  本发明描述了新型的硝化和/或亚硝化质子泵抑制剂化合物，以及包含至少一种质子泵抑制剂化合物的新型组合物，该化合物可以选择地取代至少一个NO和/或NO2基团，并且可以选择地包含至少一种提供、转移或释放一氧化氮、诱导内源性一氧化氮或内皮源性舒张因子产生、刺激内源性一氧化氮合成或是一氧化氮合酶底物的化合物，和/或至少一种非甾体抗炎药、选择性COX-2抑制剂、抗酸剂、含铋试剂、酸降解抗菌化合物及其混合物。本发明还提供了治疗和/或预防胃肠道疾病的方法；促进溃疡愈合；减少溃疡复发；改善质子泵抑制剂的胃保护性能、抗幽门螺杆菌性能或抗酸性能；减少或降低与非甾体抗炎化合物使用相关的胃肠道毒性；治疗幽门螺杆菌和病毒感染。本发明的化合物和/或组合物还可以以药用工具包的形式提供。
• Compositions and methods using proton pump inhibitors
  申请人：Barth Jay

  公开号：US20060024238A1

  公开（公告）日：2006-02-02

  The invention provides methods for treating and preventing gastrointestinal disorders, viral infections, fungal infections, Whipple's disease, sleep disorders, sleep apnea, iron deficiency anemia, asthma, nasal airway resistance, cystic fibrosis, pancreatitis, chemotherapy-induced emesis, radiation-induced injury to the gastrointestinal tract, epilepsy, middle ear infections, obesity, hiatal hernia, anorexia, bulimia, dental decay, post-operative aspiration, migraines and other disorders by administering to a patient a therapeutically effective amount of at least one proton pump inhibitor. In other embodiments, the proton pump inhibitor can be administered with one or more histamine antagonists, antacids, bismuth compounds, anti-viral agents, anti-fungal agents, NSAIDs, steroids, cyclodextrins, cyclodextrin derivatives, and migraine drugs. In other embodiments, the invention provides nasally or transdermally administrable formulations comprising at least one proton pump inhibitor and, optionally, one or more histamine antagonists, antacids, bismuth compounds, anti-viral agents, anti-fungal agents, NSAIDs, steroids, cyclodextrins, cyclodextrin derivatives, and migraine drugs.

  本发明提供了治疗和预防胃肠道疾病、病毒感染、真菌感染、惠普尔氏病、睡眠障碍、睡眠呼吸暂停、缺铁性贫血、哮喘、鼻气道阻力、囊性纤维化、胰腺炎、化疗诱发的呕吐、胃肠道辐射损伤、癫痫、中耳感染、肥胖、食道裂孔疝、厌食症、贪食症、蛀牙、术后吸入、肥胖症的方法、通过向患者施用治疗有效量的至少一种质子泵抑制剂，可治疗胃肠道辐射引起的损伤、癫痫、中耳炎、肥胖症、食道裂孔疝、厌食症、贪食症、蛀牙、术后吸入、偏头痛和其他疾病。在其他实施方案中，质子泵抑制剂可与一种或多种组胺拮抗剂、抗酸剂、铋化合物、抗病毒剂、抗真菌剂、非甾体抗炎药、类固醇、环糊精、环糊精衍生物和偏头痛药物一起施用。在其他实施方案中，本发明提供了可经鼻或经皮给药的制剂，其中包含至少一种质子泵抑制剂，以及可选的一种或多种组胺拮抗剂、抗酸剂、铋化合物、抗病毒剂、抗真菌剂、非甾体抗炎药、类固醇、环糊精、环糊精衍生物和偏头痛药物。
• NITROSATED AND NITROSYLATED PROTON PUMP INHIBITORS, COMPOSITIONS AND METHODS OF USE
  申请人：Nitromed, Inc.

  公开号：EP1154771A1

  公开（公告）日：2001-11-21
• EP1154771A4
  申请人：——

  公开号：EP1154771A4

  公开（公告）日：2005-04-20