N-[8-({(2R)-3-[(2R,6S)-2,6-dimethylmorpholin-4-yl]-2-hydroxypropyl}oxy)-7-methoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]-2-methylpyridine-3-carboxamide | 1375469-00-3

• 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-[8-({(2R)-3-[(2R,6S)-2,6-dimethylmorpholin-4-yl]-2-hydroxypropyl}oxy)-7-methoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]-2-methylpyridine-3-carboxamide
• 英文别名: N-[8-({(2R)-3-[(2R,65)-26-dimethylmorpholin-4-yl]-2-hydroxypropyl}oxy)-7-methoxy-2,3-dihydroimidazo[1,2-c]guinazolin-5-yl]-2-methylpyridine-3-carboxamide；N-[8-[(2R)-3-[(2S,6R)-2,6-dimethylmorpholin-4-yl]-2-hydroxypropoxy]-7-methoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]-2-methylpyridine-3-carboxamide
• CAS: 1375469-00-3
• 化学式: C₂₇H₃₄N₆O₅
• 分子量: 522.604
• InChiKey: WIDPGDQTRDGSJC-ZIFCJYIRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  38
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  121
• 氢给体数：
  2
• 氢受体数：
  9

文献信息

• [EN] AMINOALCOHOL SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS<br/>[FR] DÉRIVÉS DE 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLÉINE SUBSTITUÉS PAR UN AMINOALCOOL UTILES POUR TRAITER DES TROUBLES HYPERPROLIFÉRATIFS ET DES MALADIES ASSOCIÉES À L'ANGIOGENÈSE
  申请人：BAYER PHARMA AG

  公开号：WO2012062748A1

  公开（公告）日：2012-05-18

  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.

  这项发明涉及新颖的2,3-二氢咪唑[1,2-c]喹唑啉化合物，包含这些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，特别是治疗高增殖和/或血管生成障碍，作为唯一药剂或与其他活性成分组合使用。
• AMINOALCOHOL 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：US20150080374A1

  公开（公告）日：2015-03-19

  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2,3-二氢咪唑[1,2-c]喹唑啉化合物、含有这些化合物的药物组合物以及利用这些化合物或组合物抑制磷脂酰肌醇-3-激酶（PI3K）和治疗与磷脂酰肌醇-3-激酶（PI3K）活性相关的疾病，特别是治疗过度增殖和/或血管生成障碍，作为单一药物或与其他活性成分组合使用。
• US8895549B2
  申请人：——

  公开号：US8895549B2

  公开（公告）日：2014-11-25
• US9902727B2
  申请人：——

  公开号：US9902727B2

  公开（公告）日：2018-02-27
• [EN] COMBINATION OF PI3K-INHIBITORS<br/>[FR] COMBINAISON D'INHIBITEURS DE LA VOIE PI3K
  申请人：BAYER PHARMA AG

  公开号：WO2016087490A1

  公开（公告）日：2016-06-09

  The present invention relates to combinations of at least two components, component A and component B, component A being a PI3K-inhibitor of general formula (I), or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, in particular a physiologically acceptable salt, or a mixture of same, and component B being an anti-hyperproliferative, cytotoxic and/or cytostatic agent selected from : 5-FU, or a prodrug of 5-FU, such as 5'-deoxy-5- fluorouridine, capecitabine, BOF-A2, tegafur, LIFT, or S-1; a platinum-based antineoplastic agent, such as oxaliplatin, cisplatin or carboplatin; and a taxane, such as docetaxel or paclitaxel, or combinations thereof. Another aspect of the present invention relates to the use of such combinations as described supra for the preparation of a medicament for the treatment or prophylaxis of a disease, particurlarly for the treatment of gastric cancer and/or metastases thereof. Another aspect of the present invention relates to methods of predicting the sensitivity of tumor cell growth to inhibition by PI3K inhibitors, methods of selecting and/or treating patients responsive to PI3K inhibitors, and/or their combinations with other therapeutic agents, as well as means (e.g. a kit) to carry out those methods.