Riluzole hydrochloride

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻唑类
• 英文名称: Riluzole hydrochloride
• 英文别名: 2-amino-6-(trifluoromethoxy)benzothiazole hydrochloride；6-(trifluoromethoxy)-1,3-benzothiazol-2-amine;hydrochloride
• 化学式: C₈H₅F₃N₂OS*ClH
• 分子量: 270.663
• InChiKey: QEAOELIJQRYJJS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  76.4
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  利鲁唑 在 盐酸 作用下， 以 甲醇 、 水 为溶剂， 生成 Riluzole hydrochloride
  参考文献：
  名称：

  Synthesis and Biological Evaluation of Amidine, Guanidine, and Thiourea Derivatives of 2-Amino(6-trifluoromethoxy)benzothiazole as Neuroprotective Agents Potentially Useful in Brain Diseases

  摘要：

  A series of amidine, thiourea, and guanidine derivatives of 2-amino-6-(trifluoromethoxy)benzothiazole termed 2, 3, and 4, respectively, and structurally related to riluzole, a neuroprotective drug in many animal models of brain disease, have been synthesized. The biological activity of compounds 2a-e, 3a-f, and 4a,b was preliminarily tested by means of an in vitro protocol of ischemia/reperfusion injury. The results demonstrated that 2c and 3a-d significantly attenuated neuronal injury. Selected for testing of their antioxidant properties, compounds 3a-d were shown to be endowed with a direct ROS scavenging activity. Compounds 3b and 3d were also evaluated for their activity on voltage-dependent Na(+) and Ca(2+) currents in neurons from rat piriform cortex. At 50 mu M, compound 3b inhibited the transient Na(+) Current to a much smaller extent than riluzole, whereas 3d was almost completely ineffective.

  DOI：

  10.1021/jm901375r

文献信息

• METHODS AND COMPOSITIONS FOR TREATING INFECTION
  申请人：UNIVERSITY OF ROCHESTER

  公开号：US20150238473A1

  公开（公告）日：2015-08-27

  Provided herein are compositions and methods for treating or preventing infection.

  本文提供了用于治疗或预防感染的组合物和方法。
• AMIDINE, THIOUREA AND GUANIDINE DERIVATIVES OF 2-AMINOBENZOTHIAZOLES AND AMINOBENZOTHIAZINES FOR THEIR USE AS PHARMACOLOGICAL AGENTS FOR THE TREATMENT OF NEURODEGENERATIVE PATHOLOGIES
  申请人：Anzini Maurizio

  公开号：US20100197670A1

  公开（公告）日：2010-08-05

  Amidine, thiourea and guanidine derivatives of appropriately substituted 2-aminobenzothiazoles, 2-amino-3,1-4H-benzothiazines and 3-amino-1,4-3H-benzothiazines, as understood from formula (I), the related pharmaceutically acceptable salts and solvates thereof: and the use of the products and the corresponding pharmaceutical formulations for the treatment of neurodegenerative pathologies such as cerebral ischemia, neurodegeneration induced by cranial trauma, Alzheimer's disease, Multiple Sclerosis and Amyotrophic Lateral Sclerosis.

  适当取代的2-氨基苯并噻唑、2-氨基-3,1-4H-苯并噻嗪和3-氨基-1,4-3H-苯并噻嗪的脲、硫脲和胍衍生物，如公式（I）所示，相关的药用可接受盐和溶剂合物：以及所述产品和相应的制药配方用于治疗神经退行性病理，如脑缺血、颅脑创伤引起的神经退化、阿尔茨海默病、多发性硬化症和肌萎缩侧索硬化症。
• Amidine, thiourea and guanidine derivatives of 2-aminobenzothiazoles and aminobenzothiazines for their use as pharmacological agents for the treatment of neurodegenerative pathologies
  申请人：Anzini Maurizio

  公开号：US08420634B2

  公开（公告）日：2013-04-16

  Amidine, thiourea and guanidine derivatives of appropriately substituted 2-aminobenzothiazoles, 2-amino-3,1-4H-benzothiazines and 3-amino-1,4-3H-benzothiazines, as understood from formula (I), the related pharmaceutically acceptable salts and solvates thereof: and the use of the products and the corresponding pharmaceutical formulations for the treatment of neurodegenerative pathologies such as cerebral ischemia, neurodegeneration induced by cranial trauma, Alzheimer's disease, Multiple Sclerosis and Amyotrophic Lateral Sclerosis.

  适当取代的2-氨基苯并噻唑、2-氨基-3,1-4H-苯并噻嗪和3-氨基-1,4-3H-苯并噻嗪的脒、硫脲和脲衍生物，如公式(I)所示，相关的药学上可接受的盐和溶剂合物：以及这些产品及其相应的制药配方的用途，用于治疗神经退行性病理，如脑缺血、颅脑外伤引起的神经退行性疾病、阿尔茨海默病、多发性硬化症和肌萎缩侧索硬化症。
• SUR1 inhibitors for therapy
  申请人：University of Maryland, Baltimore

  公开号：EP2719380A2

  公开（公告）日：2014-04-16

  The present invention provides An NCca-ATP inhibitor for use in a method for treating and/or preventing: (i) colitis or inflammatory bowel disease in an individual; or (ii) subarachnoid hemorrhage or an inflammation related medical condition that is arthritis, eczema, psoriasis, atopic dermatitis, psoriatic arthropathy, asthma, autoimmune diseases, chronic inflammation, chronic prostatitis, glomerulonephritis, hypersensitivities, pelvic inflammatory disease, reperfusion injury, vasculitis, allergies, shoulder tendinitis, myocarditis, nephritis, bursitis or myopathy in an individual.

  本发明提供一种 NCca-ATP 抑制剂，用于治疗和/或预防以下疾病的方法中： (i) 结肠炎或炎症性肠病；或 (ii) 蛛网膜下腔出血或与炎症相关的病症，如关节炎、湿疹、银屑病、特应性皮炎、银屑病关节病、哮喘、自身免疫性疾病、慢性炎症、慢性前列腺炎、肾小球肾炎、过敏性疾病、盆腔炎、再灌注损伤、血管炎、过敏症、肩腱炎、心肌炎、肾炎、滑囊炎或肌病。
• OSTEOGENESIS PROMOTER AND USE THEREOF
  申请人：National University Corporation Nagoya University

  公开号：EP2749285A1

  公开（公告）日：2014-07-02

  The purpose of the present invention is to provide an osteogenesis promoter that can be administered locally and systemically and that is suitable for clinical application. Provided is an osteogenesis promoter that contains, as an active ingredient, at least one compound selected from the group consisting of phenazopyridine hydrochloride, riluzole hydrochloride, tranilast, rabeprazole, indoprofen, nabumetone, luteolin, leflunomide, lansoprazole, methiazole, thiabendazole, albendazole, tiaprofenic acid, balsalazide sodium salt, and cyclosporin A, or a pharmaceutically acceptable salt thereof. Preferably, rabeprazole or lansoprazole, which are proton pump inhibitors, is used as an active ingredient.

  本发明的目的是提供一种可局部和全身给药并适合临床应用的成骨促进剂。本发明提供了一种成骨促进剂，它含有至少一种选自由盐酸苯并吡啶、盐酸利鲁唑、氨非司特、雷贝拉唑组成的组的化合物作为活性成分、吲哚布洛芬、萘丁美酮、叶黄素、来氟米特、兰索拉唑、甲噻唑、噻苯达唑、阿苯达唑、噻丙芬酸、巴柳氮钠盐和环孢素 A 或其药学上可接受的盐。最好使用雷贝拉唑或兰索拉唑（质子泵抑制剂）作为活性成分。