N'-[3-(dimethylamino)propyl]ethanimidamide

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: N'-[3-(dimethylamino)propyl]ethanimidamide
• 化学式: C₇H₁₇N₃
• 分子量: 143.23
• InChiKey: RQOAIBMORQPIBH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.4
• 重原子数：
  10
• 可旋转键数：
  4
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  41.6
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• MONOCYCLIC B-LACTAM COMPOUND FOR TREATING BACTERIAL INFECTION
  申请人：Medshine Discovery Inc.

  公开号：EP3747883A1

  公开（公告）日：2020-12-09

  Disclosed are a class of new monocyclic β-lactam compounds, an isomer thereof or pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising the compounds, and the use of same in preparing drugs for treating diseases associated with bacterial infection. Specifically disclosed are the compounds as shown in formula (I') and formula (II'), isomers thereof or pharmaceutically acceptable salts thereof.

  公开了一类新的单环 β-内酰胺化合物、其异构体或其药学上可接受的盐、包含这些化合物的药物组合物，以及这些化合物在制备治疗与细菌感染有关的疾病的药物中的用途。具体公开了式(I')和式(II')所示的化合物、其异构体或其药学上可接受的盐。
• Monocyclic β-lactam compound for treating bacterial infection
  申请人：MEDSHINE DISCOVERY INC.

  公开号：US11459323B2

  公开（公告）日：2022-10-04

  Disclosed are a class of new monocyclic β-lactam compounds, an isomer thereof or pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising the compounds, and the use of same in preparing drugs for treating diseases associated with bacterial infection. Specifically disclosed are the compounds as shown in formula (I′) and formula (II′), isomers thereof or pharmaceutically acceptable salts thereof.

  公开了一类新的单环β-内酰胺化合物、其异构体或其药学上可接受的盐、包含这些化合物的药物组合物，以及这些化合物在制备治疗与细菌感染有关的疾病的药物中的用途。具体公开了式(Ⅰ′)和式(Ⅱ′)所示的化合物、其异构体或其药学上可接受的盐。
• Novel formulations of opioid-based treatments of pain comprising substituted 1,4-di-piperidin-4-yl-piperazine derivatives
  申请人：Janssens Eduard Frans

  公开号：US20060128721A1

  公开（公告）日：2006-06-15

  This invention concerns novel formulations for opioid-based treatments of pain and/or nociception comprising opioid analgesics and 1,4-di-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK 1 antagonistic activity, the use of said formulation for the manufacture of a medicament for the prevention and/or treatment of emesis, pain and/or nociception, in particular in opioid-based acute and chronic pain treatments, more in particular in inflammatory, post-operative, emergency room (ER), breakthrough, neuropathic and cancer pain treatments and the use of an NK 1 -receptor antagonist for the manufacture of a medicament for the prevention and/or treatment of respiratory depression in opioid-based treatments of pain. The pharmaceutical formulations according to the invention comprise a pharmaceutically acceptable carrier and, as active ingredients, a therapeutically effective amount of an opioid analgesic and NK 1 -antagonists according to the general Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1. The pharmaceutical composition according to the invention reduces to a large extent a number of unwanted side-effects associated with opioid analgesics, in particular emesis, respiratory depression and tolerance, thereby increasing the total tolerability of said opioids in pain treatment.

  本发明涉及基于阿片类药物治疗疼痛和/或痛觉的新型制剂，包括阿片类镇痛剂和具有神经激肽拮抗活性的 1,4-二哌啶-4-基哌嗪衍生物，特别是 NK 1 拮抗活性，使用所述制剂制造用于预防和/或治疗呕吐、疼痛和/或痛觉的药物，特别是在基于阿片类药物的急性和慢性疼痛治疗中，尤其是在炎症、术后、急诊室（ER）、突破性、神经病理性和癌症疼痛治疗中，以及使用 NK 1 -受体拮抗剂来制造预防和/或治疗以阿片类药物为主的疼痛治疗中的呼吸抑制的药物。 根据本发明的药物制剂包括药学上可接受的载体以及作为活性成分的治疗有效量的阿片类镇痛剂和 NK 1 -拮抗剂的通式（I） 其药学上可接受的酸或碱加成盐、其立体化学异构体形式、其 N-氧化物形式和其原药，其中所有取代基的定义如权利要求 1 所述。根据本发明的药物组合物在很大程度上减少了与阿片类镇痛药相关的一些不希望出现的副作用，特别是呕吐、呼吸抑制和耐受性，从而提高了所述阿片类药物在疼痛治疗中的总体耐受性。
• Substituted 1,4,-di-piperidin-4-yl-piperazine derivatives and their use as neurokinin antagonists
  申请人：Janssens Eduard Frans

  公开号：US20060167008A1

  公开（公告）日：2006-07-27

  The invention concerns substituted 1,4-di-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK 1 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of emesis, anxiety, depression, pain, pancreatitis and IBS. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1. In view of their capability to antagonize the actions of neurokinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P by blocking the NK 1 receptor, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of neurokinin-mediated conditions, such as, for instance CNS disorders, in particular depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, schizoaffective disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions; inflammation; allergic disorders; emesis; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders; vasospastic diseases; fibrosing and collagen diseases; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control.

  本发明涉及具有神经激肽拮抗活性，特别是 NK 1 拮抗活性的取代的 1,4-二哌啶-4-基哌嗪衍生物、它们的制备方法、包含它们的组合物以及它们作为药物的用途，特别是用于治疗呕吐、焦虑、抑郁、疼痛、胰腺炎和肠易激综合征。 根据本发明的化合物可以由通式 (I) 表示 还包括其药学上可接受的酸或碱加成盐、其立体化学异构体形式、其 N-氧化物形式和其原药，其中所有取代基的定义如权利要求 1. 鉴于它们能够通过阻断神经激肽受体来拮抗神经激肽的作用，特别是通过阻断 NK 1 受体来拮抗 P 物质的作用，因此根据本发明的化合物可用作药物，特别是用于预防和治疗神经激肽介导的疾病，例如中枢神经系统疾病，尤其是抑郁症、焦虑症、压力相关疾病、睡眠障碍、认知障碍、人格障碍、精神分裂症、进食障碍、神经退行性疾病、成瘾性疾病、情绪障碍、性功能障碍、疼痛和其他中枢神经系统相关疾病；炎症；过敏性疾病；呕吐；胃肠道疾病，特别是肠易激综合征（IBS）；皮肤疾病；血管痉挛性疾病；纤维化和胶原疾病；与免疫增强或抑制有关的疾病以及风湿性疾病和体重控制。
• SUBSTITUTED 1,4-DI-PIPERIDIN-4-YL-PIPERAZINE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS
  申请人：Janssen Pharmaceutica NV

  公开号：EP1551804B1

  公开（公告）日：2008-12-24