(4S)-3-[2-(4-methoxyphenyl)-3H-benzimidazol-5-yl]-4-methyl-4,5-dihydro-1H-pyridazin-6-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• 英文名称: (4S)-3-[2-(4-methoxyphenyl)-3H-benzimidazol-5-yl]-4-methyl-4,5-dihydro-1H-pyridazin-6-one
• 化学式: C₁₉H₁₈N₄O₂
• 分子量: 334.4
• InChiKey: GLBJJMFZWDBELO-NSHDSACASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  25
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  79.4
• 氢给体数：
  2
• 氢受体数：
  4

ADMET

代谢

Pimobendan已知的人类代谢物包括3-[2-(4-羟基苯基)-3H-苯并咪唑-5-基]-4-甲基-4,5-二氢-1H-吡啶并[4,3-c]吡唑-6-酮。

Pimobendan has known human metabolites that include 3-[2-(4-Hydroxyphenyl)-3H-benzimidazol-5-yl]-4-methyl-4,5-dihydro-1H-pyridazin-6-one.

来源:NORMAN Suspect List Exchange

文献信息

• Pharmaceutical tablet formulation for the veterinary medical sector, method of production and use thereof
  申请人：BOEHRINGER INGELHEIM VETMEDICA GMBH

  公开号：US10398705B2

  公开（公告）日：2019-09-03

  The invention is directed to a pharmaceutical tablet formulation for the veterinary medical sector containing an instable ACE inhibitor or a pharmaceutically acceptable salt thereof as a first pharmaceutically active substance, and pimobendan or a pharmaceutically acceptable salt thereof as a second pharmaceutically active substance, comprising granules which contain carrier core particles coated with at least one layer wherein the first pharmaceutically active substance is present, the granules being embedded in a tablet matrix wherein the second pharmaceutically active substance is present. It is provided a “fixed-dose-combination” which allows to ease the treatment and administration of the medication, improves the medication compliance by reducing the pill burden to the animal holder and enables the better observation of and adherence to the therapy by decreasing the number of tablets to be administered. The lower number of tablets leads to a lower treatment failure rate, minimizes dosage mistakes and avoids confusions by false dose intake and slower development of resistance.

  本发明涉及一种用于兽医医疗领域的药物片剂制剂，该制剂含有作为第一药物活性物质的不稳定ACE抑制剂或其药学上可接受的盐，以及作为第二药物活性物质的匹莫苯丹或其药学上可接受的盐，该制剂由颗粒组成，颗粒含有涂有至少一层的载体核心颗粒，其中含有第一药物活性物质，颗粒被嵌入片剂基质中，其中含有第二药物活性物质。本发明提供了一种 "固定剂量组合"，可简化治疗和给药，通过减少动物的药片负担来提高用药依从性，并通过减少给药片数来更好地观察和坚持治疗。药片数量的减少可降低治疗失败率，最大程度地减少剂量错误，避免因错误剂量摄入和抗药性发展缓慢而造成的混乱。
• Liquid formulation
  申请人：Luoda Pharma Pty Ltd

  公开号：US10413610B2

  公开（公告）日：2019-09-17

  The invention relates to a liquid formulation comprising propylene glycol and an effective amount of an inodilator, an angiotensin converting enzyme inhibitor, or a combination of an inodilator and an angiotensin converting enzyme inhibitor and to use of the formulation for treating cardiac disease and/or hypertension.

  本发明涉及一种液体制剂，该制剂包含丙二醇和有效量的血管舒张剂、血管紧张素转换酶抑制剂或血管舒张剂和血管紧张素转换酶抑制剂的复方制剂，并涉及使用该制剂治疗心脏病和/或高血压。
• TASTE MASKED PHARMACEUTICAL COMPOSITION
  申请人：Boehringer Ingelheim Vetmedica GmbH

  公开号：EP2741736B1

  公开（公告）日：2017-11-22
• PHARMACEUTICAL TABLET FORMULATION FOR THE VETERINARY MEDICAL SECTOR, METHOD OF PRODUCTION AND USE THEREOF
  申请人：Boehringer Ingelheim Vetmedica GmbH

  公开号：EP2825159B1

  公开（公告）日：2022-06-22
• LIQUID FORMULATION
  申请人：Luoda Pharma Limited

  公开号：EP2849792B1

  公开（公告）日：2020-03-04