苄啶喹酮 | 1897-89-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 中文名称: 苄啶喹酮
• 英文名称: 2-<β-(2-pyridyl)aethenyl>-3-(2-methylphenyl)-4-chinazolinon
• 英文别名: 2-(2-pyridin-2-yl-vinyl)-3-o-tolyl-3H-quinazolin-4-one；3-(2-Methylphenyl)-2-(2-(2-pyridinyl)ethenyl)-4(3H)-quinazolinone；3-(2-methylphenyl)-2-(2-pyridin-2-ylethenyl)quinazolin-4-one
• CAS: 1897-89-8
• 化学式: C₂₂H₁₇N₃O
• 分子量: 339.396
• InChiKey: MYGZNGAHFWOCLI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  26
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.05
• 拓扑面积：
  45.6
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• Quinazolinone Compounds and Methods of Use Thereof
  申请人：Liu Jifeng

  公开号：US20090130097A1

  公开（公告）日：2009-05-21

  The present invention relates to quinazolinone compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the quinazolinone compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a quinazolinone compound of the present invention

  本发明涉及喹唑啉酮化合物及其制备方法。本发明还涉及包含喹唑啉酮化合物的药物组合物。本发明提供了通过向需要治疗细胞增殖性疾病（如癌症）的受试者施用本发明中的喹唑啉酮化合物的治疗有效量来治疗细胞增殖性疾病的方法。
• Controlled absorption water-soluble pharmaceutically active organic compound formulation for once-daily administration
  申请人：Counts David F.

  公开号：US10463611B2

  公开（公告）日：2019-11-05

  The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a water-soluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound. In some embodiments, the formulation of the invention are designed to extend release of the pharmaceutically active organic compound for about 3 hours to about 8 hours, thereby enabling preparation of an extended release formulation for any pharmaceutically active compound with a half-life of from about 16 hours to about 21 hours.

  本公开提供了一种用于口服的每日一次水溶性药用活性制剂。在某些实施方案中，该组合物包括掺入小颗粒中的水溶性药用活性有机化合物，每个颗粒都有一个水溶性药用活性有机化合物或其可接受盐的核心，该核心与药学上可接受的药物结合聚合物可逆结合。组合物的核心由不溶性透水膜包围，该膜能够延迟其中的药用活性化合物的溶解，并延长药用活性化合物的释放时间。在某些实施方案中，本发明的制剂可将药用活性有机化合物的释放时间延长约 3 小时至约 8 小时，从而能够制备半衰期为约 16 小时至约 21 小时的任何药用活性化合物的缓释制剂。
• Substituted quinazolinones for inhibiting PI3K
  申请人：BIOWAY., INC

  公开号：US10577369B2

  公开（公告）日：2020-03-03

  The present invention relates to novel quinazolinone derivatives inhibiting PI3K; a method for preparing the derivatives; and a pharmaceutical composition for treating hematologic neoplasms or liver diseases, containing the quinazolinone derivatives, wherein the novel quinazolinone derivatives according to the present invention have a beneficial effect in the treatment of hematologic neoplasms or liver diseases. Particularly, the quinazolinone derivatives inhibit PI3Kδ with high selectivity compared to that of a conventional anticancer drug of PI3Kδ inhibitors, thereby significantly reducing immunotoxicity, or simultaneously inhibit PI3Kδ and PI3Kγ, thereby enabling the treatment of autoimmune diseases, and anticancer therapy for blood cancer and the like. These targeted drugs have reduced side effects. The present invention provides a compound represented by Formula 1 or a pharmaceutically acceptable salt thereof, wherein X is —H, halogen, —CH3, or —NH2; and Y is C1-2 linear alkyl or C3-4 cycloalkyl.

  本发明涉及抑制PI3K的新型喹唑啉酮衍生物；制备该衍生物的方法；以及含有该喹唑啉酮衍生物的治疗血液肿瘤或肝脏疾病的药物组合物，其中根据本发明的新型喹唑啉酮衍生物在治疗血液肿瘤或肝脏疾病方面具有有益的效果。特别是，与传统抗癌药物的PI3Kδ抑制剂相比，喹唑啉酮衍生物以高选择性抑制PI3Kδ，从而显著降低免疫毒性，或同时抑制PI3Kδ和PI3Kγ，从而实现自身免疫性疾病的治疗和血癌等的抗癌治疗。这些靶向药物的副作用较小。本发明提供了由式 1 表示的化合物或其药学上可接受的盐，其中 X 是-H、卤素、-CH3 或-NH2；Y 是 C1-2 直链烷基或 C3-4 环烷基。
• NOVEL QUINAZOLINONE DERIVATIVES INHIBITING PI3K AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
  申请人：Bioway., Inc

  公开号：EP3453393B1

  公开（公告）日：2020-09-09