5-bromo-3-[3-(4-chlorophenyl)-3-hydroxypropoxy]-4-(pyridin-3-ylmethylamino)-1H-pyridazin-6-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 5-bromo-3-[3-(4-chlorophenyl)-3-hydroxypropoxy]-4-(pyridin-3-ylmethylamino)-1H-pyridazin-6-one
• 化学式: C₁₉H₁₈BrClN₄O₃
• 分子量: 465.7
• InChiKey: HZVJNIUTIWSMAC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  28
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  95.8
• 氢给体数：
  3
• 氢受体数：
  6

文献信息

• PYRIDAZINONE DERIVATIVE
  申请人：NISSAN CHEMICAL INDUSTRIES, LIMITED

  公开号：EP0742211A1

  公开（公告）日：1996-11-13

  Pyridazinone derivatives represented by the formula (I) and antiplatelet agents containing them: [wherein R is a hydrogen atom or a C1-C4 alkyl group, X is a hydrogen atom, a chlorine atom or a bromine atom, Ar is a pyridyl group or a phenyl group substituted with OR1 (wherein R1 is a hydrogen atom or a C1-C4 alkyl group) and A wherein A is a hydrogen atom, a halogen atom, a C1-C4 alkyl group or OR2 (wherein R2 is a hydrogen atom or a C1-C4 alkyl group)}, Y is C1-C8 alkylene wherein one carbon atom on the straight chain is substituted with one OR1 group (wherein R1 is the same as defined above), and Z1 and Z2 are independently a hydrogen atom, a halogen atom, a C1-C4 alkyl group or a OR1 group (wherein R1 is the same as defined above)]. These compounds have strong antiplatelet effects, are excellently safe, and can be used as active ingredients of prophylactic and therapeutic drugs for various thrombotic diseases.

  由式(I)代表的哒嗪酮衍生物和含有它们的抗血小板药物： [其中 R 是氢原子或 C1-C4 烷基，X 是氢原子、氯原子或溴原子，Ar 是吡啶基或被 OR1（其中 R1 是氢原子或 C1-C4 烷基）取代的苯基和 A 其中 A 是氢原子、卤素原子、C1-C4 烷基或 OR2（其中 R2 是氢原子或 C1-C4 烷基）}、Y 是 C1-C8 亚烷基，其中直链上的一个碳原子被一个 OR1 基团取代（其中 R1 与上述定义相同），Z1 和 Z2 独立地为氢原子、卤素原子、C1-C4 烷基或 OR1 基团（其中 R1 与上述定义相同）]。 这些化合物具有很强的抗血小板作用，安全性极高，可用作各种血栓性疾病的预防和治疗药物的活性成分。
• Compositions for oral administration containing pyridazinone compounds
  申请人：THE GREEN CROSS CORPORATION

  公开号：EP0860169A2

  公开（公告）日：1998-08-26

  A composition for oral administration which contains a pyridazinone compound of the formula (I) wherein R1, R2 and R3 are each independently a hydrogen atom or a lower alkyl, X is a halogen atom, a cyano or a hydrogen atom, Y is a halogen atom, a trifluoromethyl or a hydrogen atom, and A is a C1-C8 alkylene optionally substituted by hydroxy, or a pharmacologically acceptable salt thereof, and an organic acid. According to the present invention, a composition for oral administration which is stable to heat, light, moisture and the like and which shows improved dissolution and absorption of a pyridazinone compound can be provided.

  一种口服组合物，其中含有式(I)的哒嗪酮化合物 其中 R1、R2 和 R3 各自独立地为氢原子或低级烷基，X 为卤素原子、氰基或氢原子，Y 为卤素原子、三氟甲基或氢原子，A 为任选被羟基取代的 C1-C8 亚烷基或其药理学上可接受的盐，以及有机酸。根据本发明，可以提供一种用于口服的组合物，该组合物对热、光、湿度等稳定，并能改善哒嗪酮化合物的溶解和吸收。
• REMEDIES FOR SPINAL CANAL STENOSIS
  申请人：WELFIDE CORPORATION

  公开号：EP1123704A1

  公开（公告）日：2001-08-16

  A therapeutic agent for spinal canal stenosis is provided, which contains a pyridazinone compound of the formula (I) wherein R1, R2 and R3 are each independently a hydrogen atom or a lower alkyl, X is a halogen atom, a cyano or a hydrogen atom, Y is a halogen atom, a trifluoromethyl or a hydrogen atom, and A is a C1 - C8 alkylene optionally substituted with a hydroxyl, or its pharmacologically acceptable salt.

  本发明提供了一种治疗椎管狭窄的药物，其中含有式（I）的哒嗪酮化合物 其中 R1、R2 和 R3 各自独立地为氢原子或低级烷基，X 为卤素原子、氰基或氢原子，Y 为卤素原子、三氟甲基或氢原子，A 为任选被羟基取代的 C1 - C8 亚烷基或其药理学上可接受的盐。
• REMEDIAL AGENT FOR ERECTILE DYSFUNCTION
  申请人：Nissan Chemical Industries, Ltd.

  公开号：EP1157694A1

  公开（公告）日：2001-11-28

  The present invention provides a remedial agent for erectile dysfunction which comprises a 3(2H)-pyridazinone derivative represented by the formula (I): wherein each symbol is the same as defined in the specification or a pharmaceutically acceptable salt thereof as an active ingredient.

  本发明提供了一种治疗勃起功能障碍的药物，它包括由式(I)代表的3(2H)-哒嗪酮衍生物： 其中各符号与说明书中的定义相同 或其药学上可接受的盐作为活性成分。
• NEUTROPHILIA INHIBITOR
  申请人：Nissan Chemical Industries, Ltd.

  公开号：EP1698339A1

  公开（公告）日：2006-09-06

  To provide an antineutrophilia agent effective for treatment of development and progress of acute infections, collagen diseases (chronic rheumatoid arthritis, Wegener's granulomatosis and Behcet's disease), chronic obstructive pulmonary disease (COPD), chronic bronchitis, pulmonary emphysema, small airway disease, gout, Cushing's syndrome, myelofibrosis, neoplastic neutrophilia, polycythemia vera and diseases caused by administration of steroid drugs. An antineutrophilia agent containing a 3(2H)-pyridazinone compound represented by the formula (I) or a pharmaceutically acceptable salt thereof [wherein each of R1, R2 and R3 is independently a hydrogen atom or a C1-6 alkyl group, X is a halogen atom, cyano or a hydrogen atom, Y is a halogen atom, trifluoromethyl or a hydrogen atom, and A is a C1-8 alkylene which may be substituted with a hydroxyl group].

  提供一种抗中性粒细胞增多剂，有效治疗急性感染、胶原病（慢性类风湿性关节炎、韦格纳肉芽肿病和白塞氏病）、慢性阻塞性肺病（COPD）、慢性支气管炎、肺气肿、小气道疾病、痛风、库欣综合征、骨髓纤维化、肿瘤性中性粒细胞增多症、多发性红细胞症和服用类固醇药物引起的疾病的发展和进展。 一种抗中性粒细胞增多剂，含有由式（I）代表的 3(2H)-哒嗪酮化合物或其药学上可接受的盐[其中 R1、R2 和 R3 各自独立地为氢原子或 C1-6 烷基，X 为卤素原子、氰基或氢原子，Y 为卤素原子、三氟甲基或氢原子，A 为可被羟基取代的 C1-8 亚烷基]。