N-{7-methoxy-8-[3-((S)-3-methylmorpholin-4-yl)propoxy]-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl}nicotinamide | 1032568-72-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: N-{7-methoxy-8-[3-((S)-3-methylmorpholin-4-yl)propoxy]-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl}nicotinamide
• 英文别名: N-[7-methoxy-8-[3-[(3S)-3-methylmorpholin-4-yl]propoxy]-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]pyridine-3-carboxamide
• CAS: 1032568-72-1
• 化学式: C₂₅H₃₀N₆O₄
• 分子量: 478.551
• InChiKey: MBTCIYIPCNTFMO-KRWDZBQOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  35
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  101
• 氢给体数：
  1
• 氢受体数：
  8

文献信息

• [EN] COMBINATIONS OF COPANLISIB<br/>[FR] COMBINAISONS DE COPANLISIB
  申请人：BAYER PHARMA AG

  公开号：WO2017157792A1

  公开（公告）日：2017-09-21

  The present invention relates to * combinations of : component A : one or more 2,3-dihydroimidazo[l,2-c]quinazoline compounds of general formula (Al) or (A2) as defined herein, or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; component B : one or more IRAK4-inhibiting compounds of general formula (I) as defined herein, or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; in which optionally some or all of the components are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially. dependently of one another by the oral, intravenous, topical, local installations, intraperitoneal or nasal route; * use of such combinations for the preparation of a medicament for the treatment or prophylaxis of a cancer; and * a kit comprising such a combination.

  本发明涉及以下组合物：组分A：一种或多种2,3-二氢咪唑[1,2-c]喹唑啉化合物，其通式为(Al)或(A2)，如本文所定义，或其生理上可接受的盐、溶剂化合物、水合物或立体异构体；组分B：一种或多种IRAK4抑制剂，其通式为(I)，如本文所定义，或其生理上可接受的盐、溶剂化合物、水合物或立体异构体；其中，可选地，某些或所有组分以制药配方的形式存在，该配方可同时、同时、分别或依次通过口服、静脉注射、局部安装、腹腔注射或鼻路给予；使用这种组合物制备治疗或预防癌症的药物；以及包含这种组合物的试剂盒。
• Substituted 2,3-dihydroimidazo[1,2-c]quinazoline Derivatives Useful for Treating Hyper-Proliferative Disorders and Diseases Associated with Angiogenesis
  申请人：Hentemann Martin

  公开号：US20110083984A1

  公开（公告）日：2011-04-14

  This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.

  该发明涉及一种新型的2,3-二氢咪唑[1,2-c]喹唑啉化合物，以及含有这些化合物的药物组合物，以及用于磷脂酰肌醇-3-激酶（PI3K）抑制和治疗与磷脂酰肌醇-3-激酶（PI3K）活性相关的疾病的这些化合物或组合物的用途，特别是作为单独的药物或与其他活性成分联合使用，用于治疗过度增殖和/或血管生成异常。
• SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS
  申请人：BAYER INTELLECTUAL PROPERTY GmbH

  公开号：US20130261113A1

  公开（公告）日：2013-10-03

  This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.

  本发明涉及新型的2,3-二氢咪唑[1,2-c]喹唑啉化合物，含有这种化合物的药物组合物以及利用这些化合物或组合物进行磷脂酰肌醇-3-激酶（PI3K）抑制和治疗与磷脂酰肌醇-3-激酶（PI3K）活性相关的疾病，特别是作为唯一的活性成分或与其他活性成分组合使用来治疗高增殖和/或血管生成异常。
• COMBINATIONS OF COPANLISIB
  申请人：Bayer Pharma Aktiengesellschaft

  公开号：EP3219329A1

  公开（公告）日：2017-09-20

  The present invention relates to : * combinations of : component A: one or more 2,3-dihydroimidazo[1,2-c]quinazoline compounds of general formula (A1) or (A2) as defined herein, or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof ; component B : one or more IRAK4-inhibiting compounds of general formula (I) as defined herein,or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof ; in which optionally some or all of the components are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially. dependently of one another by the oral, intravenous, topical, local installations, intraperitoneal or nasal route ; * use of such combinations for the preparation of a medicament for the treatment or prophylaxis of a cancer ; and * a kit comprising such a combination.

  本发明涉及： * 以下物质的组合 组分 A：一种或多种本文定义的通式（A1）或（A2）的 2,3-二氢咪唑并[1,2-c]喹唑啉化合物，或其生理学上可接受的盐、溶液、水合物或立体异构体； 成分 B：一种或多种本文定义的通式（I）的 IRAK4 抑制化合物，或其生理学上可接受的盐、溶液、水合物或立体异构体； 其中部分或全部组分可选择以药物制剂的形式存在，该制剂可同时、同时、分别或依次给药。 * 可通过口服、静脉注射、局部外用、局部安装、腹腔注射或鼻腔注射等途径相互依赖地使用； * 使用这种组合物制备治疗或预防癌症的药物；以及 * 包含这种组合物的试剂盒。
• Substituted 2,3-dihydroimidazo[1,2-C]quinazoline-containing combinations
  申请人：BAYER PHARMA AKTIENGESELLSCHAFT

  公开号：US10406162B2

  公开（公告）日：2019-09-10

  The present invention relates to * combinations of: ⋅ component A: one or more 2,3-dihydroimidazo[1,2-c]quinazoline compounds of general formula (A1) or (A2), or a physiologically acceptable salt, solvate, hydrate or ⋅ stereoisomer thereof; ⋅ component B: one or more substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]-triazin-4-amine compounds of general formula (B), or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; ⋅ in which optionally some or all of the components are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially, ⋅ dependently of one another by the oral, intravenous, topical, local installations, ⋅ intraperitoneal or nasal route; * use of such combinations for the preparation of a medicament for the treatment or prophylaxis of a cancer; * a kit comprising such a combination; * use of biomarkers which is the loss of tumor suppressor PTEN or FBXW7, for predicting the sensitivity and/or resistance of a cancer patient to said compound and providing a rationale-based dosage to increase sensitivity and/or to overcome resistance; * a method of determining the loss of tumor suppressor PTEN or FBXW7; and a method for determining perturbations in PIK3CA, PIK3CB, PIK3CD, PIK3CG, PIK3R1, PIK3R2, PIK3R3, PIK3R4, PIK3R5, FGFR1, FGFR2, FGFR3 and/or FGFR4.

  本发明涉及 * 种组合物：⋅ A 组分：一种或多种通式(A1)或(A2)的 2,3-二氢咪唑并[1,2-c]喹唑啉化合物，或其生理上可接受的盐、溶液、水合物或⋅ 立体异构体； ⋅ B 组分一种或多种取代的 5-(1-苯并噻吩-2-基)吡咯并[2,1-f][1,2,4]-三嗪-4-胺通式 (B) 化合物，或其生理上可接受的盐、溶液、水合物或立体异构体；⋅ 其中部分或全部成分可选择以药物制剂的形式存在，可通过口服、静脉注射、局部外用、局部安装、腹膜内或鼻腔途径同时、同时、分别或依次给药；* 使用这种组合物制备治疗或预防癌症的药物； * 包含这种组合物的试剂盒； * 使用肿瘤抑制因子 PTEN 或 FBXW7 缺失的生物标志物，预测癌症患者对所述化合物的敏感性和/或耐药性，并提供合理的剂量以提高敏感性和/或克服耐药性；* 确定肿瘤抑制因子PTEN或FBXW7缺失的方法；以及确定PIK3CA、PIK3CB、PIK3CD、PIK3CG、PIK3R1、PIK3R2、PIK3R3、PIK3R4、PIK3R5、FGFR1、FGFR2、FGFR3和/或FGFR4扰动的方法。