美立苯旦 | 119322-27-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• 中文名称: 美立苯旦
• 英文名称: 5-methyl-6-<2-(3-pyrazolyl)-5-benzimidazolyl>-2,3,4,5-tetrahydro-pyridazin-3-one
• 英文别名: meribendan；4-methyl-3-[2-(1H-pyrazol-5-yl)-3H-benzimidazol-5-yl]-4,5-dihydro-1H-pyridazin-6-one
• CAS: 119322-27-9
• 化学式: C₁₅H₁₄N₆O
• 分子量: 294.316
• InChiKey: FDWDHUONLKCDBV-UHFFFAOYSA-N

物化性质

• 密度：
  1.59±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  98.8
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  6-(4-苄基氨基-3-硝基苯基)-5-甲基-2,3,4,5-四氢哒嗪-3-酮 在 palladium on activated charcoal 盐酸 、 氢气 、 sodium hydrogensulfite 作用下， 以 甲醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 4.0h， 生成 美立苯旦
  参考文献：
  名称：

  Synthesis and biological activities of meribendan and related heterocyclic benzimidazolo-pyridazinones

  摘要：

  The synthesis of new heterocyclic benzimidazolo-pyridazinones is described. The new compounds were evaluated as inotropic agents with 'calcium-sensitizing' effects. 5-Methyl-6-[2-(3-pyrazolyl)-5-benzimidazolyl]-2,3,4,5-tetrahydro-pyridazin-3-one hydrochloride (meribendan) turned out to be the most interesting compound and was chosen for development as a positive inotrope.

  DOI：

  10.1016/0223-5234(93)90005-y

文献信息

• METHODS FOR THE TREATMENT OF NON-HODGKIN'S LYMPHOMAS USING LENALIDOMIDE, AND GENE AND PROTEIN BIOMARKERS AS A PREDICTOR
  申请人：SCHAFER Peter H.

  公开号：US20110223157A1

  公开（公告）日：2011-09-15

  Methods of treating or managing specific cancers, including non-Hodgkin's lymphoma, by the administration of 3-(4-amino- 1 -oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Methods of using gene and protein biomarkers as a predictor of non-Hodgkin's lymphoma response to treatment with 3-(4-amino- 1 -oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione are also disclosed.

  通过给予3-(4-氨基-1-氧代-1,3-二氢-异吲哚-2-基)-哌啶-2,6-二酮，披露了治疗或管理特定癌症，包括非霍奇金淋巴瘤的方法。还披露了使用基因和蛋白生物标志物作为非霍奇金淋巴瘤对3-(4-氨基-1-氧代-1,3-二氢-异吲哚-2-基)-哌啶-2,6-二酮治疗反应的预测方法。
• Pharmaceutical preparation comprising an active dispersed on a matrix
  申请人：——

  公开号：US20040058896A1

  公开（公告）日：2004-03-25

  The present invention relates to the field of pharmaceutical technology and describes a novel advantageous preparation for an active ingredient. The novel preparation is suitable for producing a large number of pharmaceutical dosage forms. In the new preparation an active ingredient is present essentially uniformly dispersed in an excipient matrix composed of one or more excipients selected from the group of fatty alcohol, triglyceride, partial glyceride and fatty acid ester.

  本发明涉及制药技术领域，描述了一种新的有利的活性成分制备方法。这种新的制备方法适用于生产大量的药物剂型。在这种新的制备方法中，活性成分基本上均匀地分散在由脂肪醇、甘油三酯、部分甘油酯和脂肪酸酯等多种赋形剂中选择的一种或多种赋形剂组成的赋形剂基质中。
• Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases
  申请人：Scaramuzzino, Giovanni

  公开号：EP1336602A1

  公开（公告）日：2003-08-20

  New pharmaceutical compounds of general formula (I): F-(X)q where q is an integer from 1 to 5, preferably 1; -F is chosen among drugs described in the text, -X is chosen among 4 groups -M, -T, -V and -Y as described in the text. The compounds of general formula (I) are nitrate prodrugs which can release nitric oxide in vivo in a controlled and selective way and without hypotensive side effects and for this reason they are useful for the preparation of medicines for prevention and treatment of inflammatory, ischemic, degenerative and proliferative diseases of musculoskeletal, tegumental, respiratory, gastrointestinal, genito-urinary and central nervous systems.

  通式（I）的新药物化合物：F-（X）q，其中q是1到5的整数，最好是1；-F是在文本中描述的药物中选择的，-X是在文本中描述的4个组-M，-T，-V和-Y中选择的。通式（I）的化合物是硝酸盐前药，可以在体内以受控和选择性的方式释放一氧化氮，而不会产生降压副作用，因此它们非常适用于制备用于预防和治疗肌肉骨骼，皮肤，呼吸，消化，泌尿和中枢神经系统的炎症，缺血，退行性和增生性疾病的药物。
• [EN] COMPOSITIONS AND METHODS FOR TREATING METABOLIC DISORDERS<br/>[FR] COMPOSITIONS ET MÉTHODES POUR LE TRAITEMENT DE TROUBLES MÉTABOLIQUES
  申请人：NUSIRT SCIENCES INC

  公开号：WO2018058109A1

  公开（公告）日：2018-03-29

  Methods and compounds useful for reducing, treating, preventing, or sustaining the reduction of a metabolic disease or disorder are provided herein. Also provided herein are compositions and kits for practicing any of the methods described herein.

  本文提供了用于减少、治疗、预防或维持代谢性疾病或紊乱的方法和化合物。本文还提供了用于实施本文中描述的任何方法的组合物和工具包。
• Benzimidazoles
  申请人：Edwards L. Michael

  公开号：US20060014756A1

  公开（公告）日：2006-01-19

  The invention is directed to physiologically active compounds of the general formula (Ix) and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

  本发明涉及一般式（Ix）的生理活性化合物及含有这种化合物的组合物，以及它们的前药、药学上可接受的盐和溶剂化物，还涉及在式（Ix）范围内的新化合物和它们的制备方法。这种化合物和组合物具有有价值的药物性质，特别是抑制激酶的能力。