1-[2-(1H-benzothiazol-2-yl)ethyl]piperidine-2,6-dione

• 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: 1-[2-(1H-benzothiazol-2-yl)ethyl]piperidine-2,6-dione
• 英文别名: 1-(2-(1,3-benzothiazol-2-yl)ethyl)piperidine-2,6-dione；1-[2-(1,3-Benzothiazol-2-yl)ethyl]piperidine-2,6-dione；1-[2-(1,3-benzothiazol-2-yl)ethyl]piperidine-2,6-dione
• 化学式: C₁₄H₁₄N₂O₂S
• 分子量: 274.343
• InChiKey: KLGNTQYDSRTGOY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  78.5
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  5-{[2-(1,3-benzothiazol-2-yl)ethyl]amino}-5-oxopentanoic acid 在 乙酸酐 作用下， 以 1,4-二氧六环 为溶剂， 反应 3.0h， 以79.9%的产率得到1-[2-(1H-benzothiazol-2-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 Otvetstennostiyu "Pharmenterprises"

  公开号：EP2985282A1

  公开（公告）日：2016-02-17

  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.

  本发明涉及通式Ⅰ的新型生物活性戊二酰亚胺衍生物或其药学上可接受的盐、它们作为治疗上呼吸道疾病的制剂的用途、包含通式Ⅰ的戊二酰亚胺衍生物的药物组合物、通过用脱水剂加热通式Ⅱ的二羧酸单酰胺来制备通式Ⅰ的戊二酰亚胺衍生物的方法。
• PHARMACEUTICAL COMPOSITION CONTAINING GLUTARIMIDE DERIVATIVES, AND APPLICATION THEREOF FOR TREATING EOSINOPHILIC DISEASES
  申请人：Obschestvo S Ogranichennoi Otvetstennostiyu "Pharmenterprises"

  公开号：EP3069720A1

  公开（公告）日：2016-09-21

  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, eosinophylic esophagitis, eosinophilic gastroenteritis, or fibroses. The invention also relates to pharmaceutical compositions comprising glutarimide derivatives of general formula (I):

  本发明涉及通式(I)的新型生物活性戊二酰亚胺衍生物或其药学上可接受的盐，以及它们作为治疗剂用于治疗嗜酸性粒细胞疾病，最好是过敏性疾病，特别是支气管哮喘、过敏性鼻炎、多发性鼻窦炎、嗜酸性粒细胞结肠炎、嗜酸性粒细胞综合征、过敏性结膜炎、特应性皮炎、Churg-Strauss 综合征、过敏性休克、Quincke 水肿、嗜酸性粒细胞血管炎、嗜酸性粒细胞食管炎、嗜酸性粒细胞胃肠炎或纤维瘤。本发明还涉及包含通式（I）戊二酰亚胺衍生物的药物组合物：
• 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：US10196377B2

  公开（公告）日：2019-02-05

  A compound having the following formula: or a pharmaceutically acceptable salt thereof. A medicament or pharmaceutical composition contains the compound. A method of treating a respiratory tract disease includes administering to a patient an effective amount of a compound or a pharmaceutically acceptable salt thereof.

  具有下式的化合物 或其药学上可接受的盐。药物或药物组合物含有该化合物。一种治疗呼吸道疾病的方法包括向患者施用有效量的化合物或其药学上可接受的盐。
• Pharmaceutical composition comprising glutarimide derivatives and use thereof in the treatment of eosinophilic diseases
  申请人：OBSCHESTVO S ORGANICHENNOI OTVETSTVENNOSTIYU “PHARMENTERPRISES”

  公开号：US10220029B2

  公开（公告）日：2019-03-05

  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):

  本发明涉及通式(I)的新型生物活性戊二酰亚胺衍生物或其药学上可接受的盐，以及它们作为治疗剂用于治疗嗜酸性粒细胞疾病，最好是过敏性疾病，特别是支气管哮喘、过敏性鼻炎、多发性鼻窦炎、嗜酸性粒细胞结肠炎、嗜酸性粒细胞综合征、过敏性结膜炎、特应性皮炎、Churg-Strauss 综合征、过敏性休克、Quincke 水肿、嗜酸性粒细胞血管炎、嗜酸性粒细胞食管炎、嗜酸性粒细胞胃肠炎或纤维瘤。本发明还涉及包含通式(I)戊二酰亚胺衍生物的药物组合物：