Isoquinoline, 1-(4,5-dihydro-1H-imidazol-2-yl)- | 63656-90-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异喹啉及其衍生物
• 英文名称: Isoquinoline, 1-(4,5-dihydro-1H-imidazol-2-yl)-
• 英文别名: 1-(4,5-dihydro-1H-imidazol-2-yl)isoquinoline
• CAS: 63656-90-6
• 化学式: C₁₂H₁₁N₃
• 分子量: 197.24
• InChiKey: MYTRGMPNAUVEIU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  37.3
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• [EN] IMIDAZOLINE RECEPTOR TYPE 1 LIGANDS FOR USE AS THERAPEUTICS<br/>[FR] LIGANDS DU RÉCEPTEUR AUX IMIDAZOLINES DE TYPE 1 À UTILISER EN TANT QU'AGENTS THÉRAPEUTIQUES
  申请人：RIDEOUT DARRYL

  公开号：WO2016105448A1

  公开（公告）日：2016-06-30

  This disclosure provides compounds and compositions for use as analgesics and for the treatment of various conditions, such as pain, headaches, allodynia, and fibromyalgia. The disclosure also provides compounds that are ligands, and in some embodiments, modulators (e.g., agonists), for the imidazoline receptor type 1.

  本公开提供了作为止痛剂和用于治疗各种病症的化合物和组合物，如疼痛、头痛、触痛和纤维肌痛。本公开还提供了作为嘌呤受体1的配体的化合物，有些实施例中还提供了对其的调节剂（例如，激动剂）。
• [EN] COMPOUNDS FOR USE AS PAIN THERAPEUTICS<br/>[FR] COMPOSÉS DESTINÉS À ÊTRE UTILISÉS EN TANT QU'AGENTS THÉRAPEUTIQUES CONTRE LA DOULEUR
  申请人：LEDERMAN SETH

  公开号：WO2016105449A1

  公开（公告）日：2016-06-30

  This disclosure provides compounds and compositions for use as analgesics and for the treatment of one or more conditions selected from: pain; psychic pain; psychological pain; psychiatric pain; depression; allodynia; fibromyalgia; fibromyalgia-ness; central sensitization; centralization; regional pain syndrome; temporomandibular joint syndrome (TMJ); lower back pain; interstitial cystitis; Gulf War syndrome; visceral pain; phantom limb painj.kidney stones; gout; neuropathic pain; post-herpetic neuralgia; diabetic neuropathy; sickle cell pain; priapism; nociceptive pain; post-operative pain; orthopedic injury pain; bunionectomy; dental extraction; pain after severed spinal cord injury; osteoarthritis; rheumatoid arthritis; Lyme disease; Parkinson's disease; opioid-induced constipation; an opioid withdrawal symptom; pain associated with post-traumatic stress disorder (PTSD); and combinations of any of the foregoing conditions. This disclosure also provides compounds that are ligands, and in some embodiments, modulators (e.g., agonists), for the imidazoline receptor type 1.

  本公开提供了用作镇痛剂和用于治疗以下一种或多种疾病的化合物和组合物：疼痛；心理疼痛；心理疼痛；精神疼痛；抑郁症；痛觉过敏；纤维肌痛；纤维肌痛症；中枢敏感化；中枢化；区域性疼痛综合征；颞下颌关节综合征（TMJ）；腰部疼痛；间质性膀胱炎；海湾战争综合征；内脏疼痛；幻肢疼痛；肾结石；痛风；神经性疼痛；带状疱疹后神经痛；糖尿病性神经病；镰状细胞疼痛；阴茎长时间勃起症；伤害性疼痛；术后疼痛；骨科损伤疼痛；拇外翻术；牙科拔牙；断裂脊髓损伤后疼痛；骨关节炎；类风湿关节炎；莱姆病；帕金森病；阿片类药物引起的便秘；阿片类药物戒断症状；与创伤后应激障碍（PTSD）相关的疼痛；以及上述任何疾病的组合。本公开还提供了作为咪唑啉受体类型1的配体的化合物，有些实施例中是调节剂（例如，激动剂）。
• Pharmaceutical compositions comprising a selective I1 imidazoline receptor agonist and an angiotensin II receptor blocker
  申请人：Baum Dominique

  公开号：US20050143435A1

  公开（公告）日：2005-06-30

  Parmaceutical compositions comprising selective imidazoline receptor agonists combined with angiotensin II receptor blockers, particularly, pharmaceutical compositions comprising Moxonidine and Eprosartan mesylate, as well as the use of such compositions for the treatment of hypertension, especially in hypertensive patients suffering from type II diabetes or susceptible to developing type II diabetes.

  由选择性咪唑啉受体激动剂和血管紧张素 II 受体阻滞剂组成的药物组合物，特别是由莫索尼定和甲磺酸依普沙坦组成的药物组合物，以及使用此类组合物治疗高血压，尤其是治疗患有 II 型糖尿病或易患 II 型糖尿病的高血压患者。
• Method for the treatment of diseases requiring inhibition or a reduction in the activity of pH value-regulating bicarbonate transporter proteins
  申请人：Rupp Heinz

  公开号：US20050165080A1

  公开（公告）日：2005-07-28

  The use of selective imidazoline receptor agonists, such as moxonidine, rilmenidine, LNP-509, S-23515, PMS-812, PMS-847 and BU-98008, and their physiologically compatible acid addition salts in pharmaceutical preparations for the treatment and/or inhibition of functional disorders and/or diseases in larger mammals or humans which require inhibition or reduction of the activity of proteins which regulate the intracellular pH value and which belong to the superfamily of bicarbonate transporters, in particular the treatment or inhibition of clinical conditions of bones which are caused by an undesirable amount of bone resorption, such as osteoporosis; of diseases of the gastrointestinal tract, such as gastric ulcers; and of neuronal and/or neuropsychiatric diseases associated with a pathologically altered (especially increased) neuronal activity, such as depression, Alzheimer's disease, eating disorders and schizophrenia.

  在药物制剂中使用选择性咪唑啉受体激动剂，如莫索尼定、利美尼定、LNP-509、S-23515、PMS-812、PMS-847 和 BU-98008，以及它们与生理相容的酸加成盐，用于治疗和/或抑制大型哺乳动物或人类的功能紊乱和/或疾病，这些疾病需要抑制或降低调节细胞内 pH 值的蛋白质的活性，这些蛋白质属于碳酸氢盐转运体超家族、特别是治疗或抑制因骨吸收量过大而引起的骨骼临床症状，如骨质疏松症；胃肠道疾病，如胃溃疡；以及与神经元活性病理性改变（尤其是增加）有关的神经元和/或神经精神疾病，如抑郁症、阿尔茨海默病、饮食失调症和精神分裂症。
• ARZNEIMITTEL ZUR BEHANDLUNG VON EINE INHIBITION ODER AKTIVITÄTSVERMINDERUNG VON PH-WERT-REGULIERENDEN BIKARBONAT-TRANSPORTER-PROTEINEN ERFORDERNDEN ERKRANGUNGEN
  申请人：Solvay Pharmaceuticals GmbH

  公开号：EP1517688A2

  公开（公告）日：2005-03-30