1-(2-(1H-imidazol-4-yl)ethyl)piperidine-2,6-dione | 1464897-15-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 1-(2-(1H-imidazol-4-yl)ethyl)piperidine-2,6-dione
• 英文别名: Histamine glutarimide；1-[2-(1H-imidazol-5-yl)ethyl]piperidine-2,6-dione
• CAS: 1464897-15-1
• 化学式: C₁₀H₁₃N₃O₂
• 分子量: 207.232
• InChiKey: DYKZYSKWOHKZMF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.4
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  66.1
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  N-glutarylhistamine 在 乙酸酐 作用下， 以80%的产率得到1-(2-(1H-imidazol-4-yl)ethyl)piperidine-2,6-dione
  参考文献：
  名称：

  US2016/46598

  摘要：

  公开号：

文献信息

• PHARMACEUTICAL COMPOSITION COMPRISING GLUTARIMIDE DERIVATIVES AND USE THEREOF IN THE TREATMENT OF EOSINOPHILIC DISEASES
  申请人：OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU "PHARMENTERPRISES"

  公开号：US20180104230A1

  公开（公告）日：2018-04-19

  The present invention relates to novel biologically active glutarimide derivatives of general formula (I) or a pharmaceutically acceptable salt thereof, their use as a therapeutic agent for the treatment of eosinophilic diseases, preferably of allergic nature, in particular bronchial asthma, allergic rhinitis, polypous rhinosinusopathies, eosinophilic colitis, eosinophilic syndrome, allergic conjunctivitis, atopic dermatitis, Churg-Strauss syndrome, anaphylactic shock, Quincke's edema, eosinophilic vasculitis, eosinophilic esophagitis, eosinophilic gastroenteritis, or fibroses. The invention also relates to pharmaceutical compositions comprising glutarimide derivatives of general formula (I):

  本发明涉及一种新颖的生物活性戊二酰亚胺衍生物，其化学式为(I)或其药学上可接受的盐，其用作治疗嗜酸性疾病的治疗剂，优选为过敏性的嗜酸性疾病，特别是支气管哮喘、过敏性鼻炎、息肉性鼻窦病、嗜酸性结肠炎、嗜酸性综合症、过敏性结膜炎、特应性皮炎、Churg-Strauss综合症、过敏性休克、Quincke水肿、嗜酸性血管炎、嗜酸性食管炎、嗜酸性胃肠炎或纤维化。本发明还涉及包含通式(I)的戊二酰亚胺衍生物的制药组合物。
• Glutarimide Derivatives, Use Thereof, Pharmaceutical Composition Based Thereon and Methods for Producing Glutarimide Derivatives
  申请人：OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU "PHARMENTERPRISES"

  公开号：US20160046598A1

  公开（公告）日：2016-02-18

  The present invention relates to novel biologically active glutarimide derivatives of general formula I or pharmaceutically acceptable salts thereof, their use as an agent for the treatment of upper respiratory tract diseases, pharmaceutical compositions comprising the glutarimide derivatives of general formula I, methods for preparing the glutarimide derivatives of general formula I by heating a dicarboxylic acid monoamide of general formula II with a dehydrating agent.

  本发明涉及一种新颖的生物活性戊二酰亚胺衍生物，其一般式为I或其药学上可接受的盐，其用作治疗上呼吸道疾病的药物，包括一般式I的戊二酰亚胺衍生物的制药组合物，以及通过将一般式II的二羧酸单酰胺与脱水剂加热制备一般式I的戊二酰亚胺衍生物的方法。
• N-ACYLIC AMINOACID DERIVATIVES. METHOD FOR THE PRODUCTION THEREOF, PHARMACOLOGICAL COMPOSITION AND THE USE IN THE FORM OF ANTI-ALLERGIC, ANTI-INFLAMMATORY AND HYPOLIPIDEMIC AGENTS
  申请人：Nebolsin, Vladimir Evgenievich

  公开号：EP1905763A1

  公开（公告）日：2008-04-02

  The present invention relates to N-acyl derivatives of amino acids and pharmaceutically acceptable salts thereof wherein n is 2 or 3; and R1 represents or pharmaceutically acceptable salts thereof, to novel processes for preparing the same, to use thereof as anti-allergic, anti-anaphylactic, anti-inflammatory and hypolipidemic agents as well as to a pharmaceutical composition comprising the indicated compounds in an efficient amount and to a method for treating allergic and inflammatory diseases and lipid metabolism disorders: bronchial asthma, allergic rhinitis, pollinoses, seasonal and year-round rhinitis, allergic pneumonitis, atopic dermatitis, psoriasis, urticaria, allergic (including anaphylactic) reactions to insect stings and medicaments, cold allergy, allergic conjunctivitis, atherosclerosis, obesity, ischemic heart and cerebral disease, myocardial infarction and stroke.

  本发明涉及氨基酸的 N-酰基衍生物及其药学上可接受的盐类 其中 n 是 2 或 3；以及 R1 代表 或其药学上可接受的盐；涉及制备上述物质的新工艺；涉及将上述物质用作抗过敏、抗过敏反应、抗炎症和降血脂药剂；涉及包含有效量的上述化合物的药物组合物；还涉及治疗过敏性和炎症性疾病以及脂质代谢紊乱的方法：支气管哮喘、过敏性鼻炎、花粉症、季节性和全年性鼻炎、过敏性肺炎、特应性皮炎、银屑病、荨麻疹、对昆虫叮咬和药物的过敏反应（包括过敏性反应）、寒冷过敏、过敏性结膜炎、动脉粥样硬化、肥胖、缺血性心脑疾病、心肌梗塞和中风。
• Peptide derivatives or pharmaceutically acceptable salts thereof, method for producing the same, use of said derivatives and pharmaceutical composition
  申请人：Nebolsin, Vladimir Evgenievich

  公开号：EP2229935A1

  公开（公告）日：2010-09-22

  Derivatives of peptides of general formula or pharmaceutically acceptable salts thereof, their use as the agents possessing antioxidant, antiasthmatic, antihypoxic, antiinflammatory, antiviral, antibacterial, lipid-regulating, antitumor, antimetastatic, glucose lowering, adaptogenic and the other kinds of therapeutic effects, a method to produce them, a pharmaceutical composition or a cosmetic agent comprising as an active agent a peptide derivative of formula (I) or pharmaceutically or cosmetically acceptable salts thereof as well as a method of therapy or prevention of diseases.

  通式肽的衍生物 或其药学上可接受的盐，它们作为具有抗氧化、抗通气、抗缺氧、抗炎、抗病毒、抗菌、调节血脂、抗肿瘤、抗转移、降糖、适应性和其他各种治疗效果的制剂的用途，生产它们的方法，包含式 (I) 肽衍生物或其药学上或化妆品学上可接受的盐作为活性剂的药物组合物或化妆品制剂，以及治疗或预防疾病的方法。
• USE OF GLUTARYL HISTAMINE TO TREAT RESPIRATORY TRACT INFECTIONS
  申请人：Ltd. "Valenta-Intellekt"

  公开号：EP2767282A2

  公开（公告）日：2014-08-20

  The invention relates to a medicament for the treatment of respiratory tract diseases selected from the group including rhinosinusitis, sinusitis, tonsillitis, bronchiolitis, pneumonia, and acute respiratory distress syndrome, wherein the medicament comprises glutaryl histamine or a pharmaceutically acceptable salt thereof in an effective amount. The invention also relates to use of glutaryl histamine or a pharmaceutically acceptable salt thereof for manufacture a medicament for the treatment of a respiratory tract disease. The medicament provides potentiating the effectiveness of antibacterial therapy for the treatment of respiratory tract diseases.

  本发明涉及一种用于治疗选自包括鼻炎、鼻窦炎、扁桃体炎、支气管炎、肺炎和急性呼吸窘迫综合征在内的呼吸道疾病的药物，其中该药物包含有效量的谷氨酰组胺或其药学上可接受的盐。本发明还涉及使用戊二酰组胺或其药学上可接受的盐制造治疗呼吸道疾病的药物。该药物可增强治疗呼吸道疾病的抗菌疗法的效果。