(R)-4,5-dihydro-5-methyl-6-[4-(2-propyl-3-oxo-1-cyclohexenyl)amino]phenyl-3(2H)-pyridazinone

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (R)-4,5-dihydro-5-methyl-6-[4-(2-propyl-3-oxo-1-cyclohexenyl)amino]phenyl-3(2H)-pyridazinone
• 英文别名: NSP-513；(4R)-4-methyl-3-[4-[(3-oxo-2-propylcyclohexen-1-yl)amino]phenyl]-4,5-dihydro-1H-pyridazin-6-one
• 化学式: C₂₀H₂₅N₃O₂
• 分子量: 339.437
• InChiKey: GWHBUAUGUIYQBO-CYBMUJFWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  25
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  70.6
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• OPTICALLY ACTIVE COMPOUND
  申请人：NIPPON SODA CO., LTD.

  公开号：EP0791584A1

  公开（公告）日：1997-08-27

  The present invention is directed to (R)-(-)-4,5-dihydro-5-methyl-6-[4-[(2-propyl-3-oxo-1-cyclohexenyl)amino]phenyl]-3(2H)-pyridazinone, the crystalline form thereof and a method for manufacturing the said compound and the said crystalline form. The compound of the present invention has excellent inhibitory effect on platelet aggregation while giving less side effect, and therefore, it is useful to utilize the compound as an antithrombotic drug. In addition, the compound of the present invention has bronchodialatic effect as well, and it is therefore useful to utilize the compound for chemotherapy of chronic obstructive lung disease, such as asthma and bronchitis. Moreover, the compound of the present invention is useful for chemotherapy of the diseases relating to the concentration of cAMP in cells, such as hypertension, ulcer, diabetes mellitus and cancer. Again, crystalline form of the said compound is the most suitable form in order to supply stable and homogeneous bulk thereof.

  本发明涉及(R)-(-)-4,5-二氢-5-甲基-6-[4-[(2-丙基-3-氧代-1-环己烯基)氨基]苯基]-3(2H)-哒嗪酮、其结晶形式以及制造上述化合物和上述结晶形式的方法。 本发明的化合物对血小板聚集有很好的抑制作用，同时副作用较小，因此可以用作抗血栓药物。此外，本发明化合物还具有支气管扩张作用，因此可用于慢性阻塞性肺病（如哮喘和支气管炎）的化疗。 此外，本发明化合物还可用于高血压、溃疡、糖尿病和癌症等与细胞中 cAMP 浓度有关的疾病的化疗。 同样，上述化合物的结晶体是最合适的形式，以便提供稳定和均匀的块状物。
• [EN] OPTICALLY ACTIVE COMPOUND<br/>[FR] COMPOSE OPTIQUEMENT ACTIF
  申请人：NIPPON SODA CO., LTD.

  公开号：WO1996015117A1

  公开（公告）日：1996-05-23

  (EN) (R)-(-)-4,5-Dihydro-5-methyl-6-[4-[(2-propyl-3-oxo-1-cyclohexenyl)amino]phenyl]-3(2H)-pyridazinone, its crystals, and a process for producing the same. The compound is reduced in the side effects and has such an excellent effect of controlling platelet agglutination that it is useful as an antithrombotic agent. As it has also a bronchodilatory effect, it is useful for treating chronic obstructive pulmonary diseases such as asthma and bronchitis. Further, it is useful for treating various diseases related to the intracellular cAMP concentration, such as hypertension, ulcer, diabetes and cancer. The crystals of this compound are most suitable for providing a stable homogeneous bulk.(FR) (R)-(-)-4,5-Dihydro-5-méthyl-6-[4-[(2-propyl-3-oxo-1-cyclohexenyl)amino]phényl]-3(2H)-pyridazinone, ses cristaux, et son procédé de production. Le composé présente des effets secondaires réduits et un excellent effet de régulation de l'agglutination plaquettaire utile en tant qu'agent antithrombotique. Etant donné qu'il présente également un effet bronchodilatateur, il est utile dans le traitement de maladies pulmonaires obstructives chroniques telles que l'asthme et la bronchite. Il est également utile dans le traitement de diverses maladies associées à la concentration de cAMP intracellulaire, telles que l'hypertension, l'ulcère, le diabète et le cancer. Les cristaux de ce composé sont particulièrement adaptés à la production d'une masse homogène stable.

  (R)-(-)-4,5-双氢-5-甲基-6-[4-((2-丙基-3-羰基-1-环己烯基)氨基)苯基]-3(2H)-吡咯酮及其晶体及制备该物质的方法。该化合物具有较小的副作用并表现出对血小板聚集 excellent excellent effect of controlling platelet agglutination 良好效果，因此它对抗凝血剂很有用。由于它还具有扩张支气管的作用，因此对于治疗如哮喘和支气管炎等慢性呼 气阻塞性呼吸系统疾病很有用。此外，对细胞内 cAMP 浓度相关的各种疾病也具有良好的效果，例如高血压、溃疡、糖尿病和癌症。该化合物的晶体是最适合提供稳定均相大 规模的。
• EP0791584A4
  申请人：——

  公开号：EP0791584A4

  公开（公告）日：1997-11-19
• SYNERGISTIC COMBINATION COMPRISING ROFLUMILAST AND A PDE-3 INHIBITOR
  申请人：ALTANA Pharma AG

  公开号：EP1176960B1

  公开（公告）日：2004-09-29
• US5856480A
  申请人：——

  公开号：US5856480A

  公开（公告）日：1999-01-05