6-(2-chlorophenyl)-2-[(4-methylpiperazin-1-yl)methylidene]-8-nitro-4H-imidazo[1,2-a][1,4]benzodiazepin-1-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯二氮卓类
• 英文名称: 6-(2-chlorophenyl)-2-[(4-methylpiperazin-1-yl)methylidene]-8-nitro-4H-imidazo[1,2-a][1,4]benzodiazepin-1-one
• 英文别名: (2E)-6-(2-chlorophenyl)-2-[(4-methylpiperazin-1-yl)methylidene]-8-nitro-4H-imidazo[1,2-a][1,4]benzodiazepin-1-one
• 化学式: C23H21ClN6O3
• 分子量: 464.9
• InChiKey: UTEFBSAVJNEPTR-XMHGGMMESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  33
• 可旋转键数：
  2
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  97.3
• 氢给体数：
  0
• 氢受体数：
  7

文献信息

• Methods and compositions for self-regulated release of active pharmaceutical ingredient
  申请人：Acura Pharmaceuticals, Inc.

  公开号：US10441657B2

  公开（公告）日：2019-10-15

  An abuse deterrent pharmaceutical composition including a pharmaceutically active ingredient; an acid soluble ingredient; and a buffering ingredient; wherein the acid soluble ingredient and the buffering ingredient retard release of the active pharmaceutical ingredient when the composition is ingested in excess of an intended dosage.

  一种抑制滥用的药物组合物，包括一种药用活性成分；一种酸溶性成分；以及一种缓冲成分；其中酸溶性成分和缓冲成分可在组合物摄入量超过预期剂量时延缓活性药物成分的释放。
• Active ingredient release system comprising a plaster containing an active ingredient and at least one active ingredient release regulator
  申请人：Kugelmann Heinrich

  公开号：US20050249792A1

  公开（公告）日：2005-11-10

  An active ingredient release system for the systemic or topical release of an active ingredient into a human or animal organism, including: a) a plaster containing active ingredient, and b) at least one divisible active ingredient release regulator that is impermeable to the active ingredient, or at least one optionally divisible active ingredient release regulator that retards the release of active ingredient and is separate from the plaster, or an optionally divisible active ingredient release regulator that retards the release of active ingredient and is already detachably bonded to the plaster.

  一种将活性成分全身或局部释放到人或动物机体内的活性成分释放系统，包括：a) 含有活性成分的膏药；b) 至少一种可分割的活性成分释放调节剂，该调节剂与活性成分不可渗透，或至少一种可选择分割的活性成分释放调节剂，该调节剂可阻止活性成分的释放并与膏药分离，或一种可选择分割的活性成分释放调节剂，该调节剂可阻止活性成分的释放并已与膏药可分离地粘合在一起。
• Methods and compositions for deterring abuse of orally administered pharmaceutical products
  申请人：Emigh F. James

  公开号：US20060110327A1

  公开（公告）日：2006-05-25

  This invention relates to an abuse deterrent formulation of an oral dosage form of a therapeutically effective amount of any active drug substance that can be subject to abuse combined with a gel forming polymer, a nasal mucosal irritating surfactant and a flushing agent. Such a dosage form is intended to deter abuse of the active drug substance via injection, nasal inhalation or consumption of quantities of the dosage unit exceeding the usual therapeutically effective dose.

  本发明涉及一种阻遏滥用的制剂，它是一种口服剂型，含有治疗有效量的任何可被滥用的活性药物物质，并与凝胶形成聚合物、鼻粘膜刺激性表面活性剂和冲洗剂相结合。这种剂型旨在阻止通过注射、鼻腔吸入或服用超过通常治疗有效剂量的剂量单位滥用活性药物物质。
• GEGEN MISSBRAUCH GESICHERTE DARREICHUNGSFORM
  申请人：Grünenthal GmbH

  公开号：EP1558257B1

  公开（公告）日：2013-12-25
• Gegen Missbrauch gesicherte Darreichungsform
  申请人：Grünenthal GmbH

  公开号：EP1859789B1

  公开（公告）日：2016-02-17