N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]-6-(2-pyrrolidin-1-ylethyl)nicotinamide | 1032568-66-3

• 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-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]-6-(2-pyrrolidin-1-ylethyl)nicotinamide
• 英文别名: N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]-6-(2-pyrrolidin-1-ylethyl)pyridine-3-carboxamide
• CAS: 1032568-66-3
• 化学式: C₃₀H₃₉N₇O₄
• 分子量: 561.684
• InChiKey: OOKZPTFFKVIJEJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  41
• 可旋转键数：
  11
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  104
• 氢给体数：
  1
• 氢受体数：
  9

反应信息

• 作为产物：
  描述：

  6-(2-pyrrolidine-1-yl-ethyl)-nicotinic acid 、 7-methoxy-8-[3-(morpholin-4-yl)propoxy]-2,3-dihydroimidazo[1,2-c]quinazolin-5-amine 在 benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate 、 N,N-二异丙基乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以69%的产率得到N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]-6-(2-pyrrolidin-1-ylethyl)nicotinamide
  参考文献：
  名称：

  WO2008/70150

  摘要：

  公开号：

文献信息

• Combinations of substituted 2,3-dihydroimidazo[1,2-c]quinazolines
  申请人：Bayer Schering Pharma Aktiengesellschaft

  公开号：EP2168582A1

  公开（公告）日：2010-03-31

  The present invention relates to the use of 2,3-dihydroimidazo[1,2-c]quinazoline compounds, and of pharmaceutical compositions containing such compounds, for the treatment or prophylaxis of multiple myeloma, as a sole agent or in combination with other one or more other active ingredients.

  本发明涉及使用2,3-二氢咪唑[1,2-c]喹唑啉化合物，以及含有这种化合物的药物组合物，用于治疗或预防多发性骨髓瘤，作为单一药剂或与其他一个或多个其他活性成分联合使用。
• Use of substituted 2,3-dihydroimidazo[1,2-c]quinazolines for the treatment of myeloma
  申请人：Bayer Schering Pharma Aktiengesellschaft

  公开号：EP2168583A1

  公开（公告）日：2010-03-31

  The present invention relates to the use of 2,3-dihydroimidazo[1,2-c]quinazoline compounds, and of pharmaceutical compositions containing such compounds, for the treatment or prophylaxis of multiple myeloma, as a sole agent or in combination with other one or more other active ingredients.

  本发明涉及使用2,3-二氢咪唑[1,2-c]喹唑啉化合物以及含有这种化合物的药物组合物，用于治疗或预防多发性骨髓瘤，作为唯一药剂或与其他一种或多种其他活性成分联合使用。
• [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。
• [EN] USE OF SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINES<br/>[FR] UTILISATION DE 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINES SUBSTITUÉES
  申请人：BAYER PHARMA AG

  公开号：WO2016142313A1

  公开（公告）日：2016-09-15

  The present invention relates to : - use of a 2,3-dihydroimidazo[1,2-c]quinazoline compound, or of a pharmaceutical composition containing same, as a sole active agent, or of a combination of a) said compound or a pharmaceutical composition containing said compound and b) one or more further active agents, for the preparation of a medicament for the treatment or prophylaxis of endometrial cancer (hereinafter abbreviated to "EC"), particularly 1st line, 2nd line, relapsed, refractory, type I or type II EC, or endometriosis; - combinations of a) said compound and b) one or more further active agents; - a pharmaceutical composition comprising said compound as a sole active agent for the treatment of endometrial cancer (hereinafter abbreviated to "EC"), particularly 1st line, 2nd line, relapsed, refractory, type I or type II EC, or endometriosis; - a pharmaceutical composition comprising a combination of a) said compound and b) one or more further active agents; - 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.

  本发明涉及以下内容：- 使用2,3-二氢咪唑[1,2-c]喹唑啉化合物或含有该化合物的药物组成物作为唯一活性剂，或使用a) 该化合物或含有该化合物的药物组成物和b) 一种或多种进一步的活性剂的组合，用于制备治疗或预防子宫内膜癌（以下简称“EC”），特别是1线、2线、复发、难治、I型或II型EC或子宫内膜异位症的药物；- a) 该化合物和b) 一种或多种进一步的活性剂的组合；- 仅包含该化合物作为唯一活性剂的药物组成物，用于治疗子宫内膜癌（以下简称“EC”），特别是1线、2线、复发、难治、I型或II型EC或子宫内膜异位症；- 包含a) 该化合物和b) 一种或多种进一步的活性剂的药物组成物；- 使用生物标志物，即肿瘤抑制剂PTEN或FBXW7的丧失，来预测癌症患者对该化合物的敏感性和/或抗药性，并提供基于理性的剂量以增加敏感性和/或克服抗药性；- 确定肿瘤抑制剂PTEN或FBXW7的丧失的方法；以及- 确定PIK3CA、PIK3CB、PIK3CD、PIK3CG、PIK3R1、PIK3R2、PIK3R3、PIK3R4、PIK3R5、FGFR1、FGFR2、FGFR3和/或FGFR4扰动的方法。
• Use of substituted 2,3-dihydroimidazo[1,2-C]quinazolines
  申请人：Liu Ningshu

  公开号：US10202385B2

  公开（公告）日：2019-02-12

  The present invention relates to: —use of a 2,3-dihydroimidazo[1,2-c]quinazoline compound, or of a pharmaceutical composition containing same, as a sole active agent, or of a combination of a) said compound or a pharmaceutical composition containing said compound and b) one or more further active agents, for the preparation of a medicament for the treatment or prophylaxis of cancer; —combinations of a) said compound and b) one or more further active agents; —a pharmaceutical composition comprising said compound as a sole active agent for the treatment of breast cancer; —a pharmaceutical composition comprising a combination of a) said compound and b) one or more further active agents; —use of biomarkers involved in the modification of Bel expression, HER family expression and/or activation, PIK3CA signaling and/or loss of PTEN for predicting the sensitivity and/or resistance of a cancer patient to said compound and providing a rationale-based synergistic combination as defined herein to increase sensitivity and/or to overcome resistance; and —a method of determining the level of a component of one or more of Bcl expression, HER family expression and/or activation, PIK3CA signaling and/or loss of PTEN.

  本发明涉及以下内容：-使用2,3-二氢咪唑并[1,2-c]喹唑啉化合物或含有该化合物的药物组合物作为唯一活性成分，或a)该化合物或含有该化合物的药物组合物和b)一个或多个进一步的活性成分的组合，用于制备用于治疗或预防癌症的药物；-a)该化合物和b)一个或多个进一步的活性成分的组合；-仅含有该化合物作为唯一活性成分的药物组合物，用于治疗乳腺癌；-含有a)该化合物和b)一个或多个进一步的活性成分的药物组合物；-使用涉及Bel表达的修饰、HER家族表达和/或激活、PIK3CA信号传导和/或PTEN丧失的生物标志物来预测癌症患者对该化合物的敏感性和/或耐药性，并提供基于理性的协同组合，以增强敏感性和/或克服耐药性；以及-确定Bcl表达、HER家族表达和/或激活、PIK3CA信号传导和/或PTEN的一个或多个组分的水平的方法。