2-(1-Aminoethyl)-5-methyl-3-(2-methylphenyl)quinazolin-4-one | 371244-09-6

• 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: 2-(1-Aminoethyl)-5-methyl-3-(2-methylphenyl)quinazolin-4-one
• CAS: 371244-09-6
• 化学式: C₁₈H₁₉N₃O
• 分子量: 293.368
• InChiKey: QHBKIIGWSNSIOR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  58.7
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• [EN] COMPOUNDS, COMPOSITIONALS, AND METHODS FOR TREATING T-CELL ACUTE LYMPHOBLASTIC LEUKEMIA<br/>[FR] COMPOSÉS, COMPOSITIONS ET PROCÉDÉS DE TRAITEMENT DE LA LEUCÉMIE LYMPHOBLASTIQUE AIGUË À LYMPHOCYTES T
  申请人：THE TRUSTEES OF COLUMBIA UNIVERISTY IN THE CITY OF NEW YORK

  公开号：WO2019028055A1

  公开（公告）日：2019-02-07

  In an aspect, the disclosure provides for compounds (II), compositions, and methods of administering the compounds and compositions to a patient in need thereof. In another aspect, the disclosure relates to compounds and compositions for treating cancer, for example, lymphoid leukemia. The disclosure further provides for compounds which inhibit two phosphoinositide 3-kinase (PI3K) isoforms, y and δ, pharmaceutical compositions comprising said compounds, and methods of using said compounds and pharmaceutical compositions for treatment, amelioration, and/or prevention of non-Hodgkin lymphoma.

  在一个方面，该公开提供了化合物（II），组合物以及向需要的患者施用这些化合物和组合物的方法。在另一个方面，该公开涉及用于治疗癌症的化合物和组合物，例如淋巴细胞白血病。该公开进一步提供了抑制两种磷脂酰肌醇3-激酶（PI3K）亚型y和δ的化合物，包括这些化合物的药物组合物，以及使用这些化合物和药物组合物治疗、改善和/或预防非霍奇金淋巴瘤的方法。
• INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA
  申请人：Sadhu Chanchal

  公开号：US20120172591A1

  公开（公告）日：2012-07-05

  Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.

  本发明揭示了抑制磷脂酰肌醇3-激酶δ亚型（PI3Kδ）活性的方法，以及治疗免疫和炎症等疾病的方法，其中PI3Kδ在白细胞功能中发挥作用。优选地，这些方法采用能够选择性地抑制PI3Kδ而不显著抑制其他PI3K亚型活性的活性剂。提供了抑制PI3Kδ活性的化合物，包括选择性抑制PI3Kδ活性的化合物。还提供了使用PI3Kδ抑制剂化合物抑制癌细胞生长或增殖的方法。因此，本发明提供了使用PI3Kδ抑制剂化合物在体外和体内抑制PI3Kδ介导的过程的方法。
• INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA
  申请人：SADHU Chanchal

  公开号：US20100152211A1

  公开（公告）日：2010-06-17

  Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.

  本文公开了抑制磷脂酰肌醇3-激酶δ亚型（PI3Kδ）活性的方法，以及治疗免疫和炎症等疾病的方法，其中PI3Kδ在白细胞功能中发挥作用。最好的方法是使用能够选择性抑制PI3Kδ的活性剂，同时不显著抑制其他PI3K亚型的活性。提供了抑制PI3Kδ活性的化合物，包括选择性抑制PI3Kδ活性的化合物。还提供了使用PI3Kδ抑制剂化合物抑制癌细胞生长或增殖的方法。因此，本发明提供了使用PI3Kδ抑制剂化合物在体外和体内抑制PI3Kδ介导的过程的方法。
• INHIBITORS OF HUMAN PHOSPHATIDYL-INOSITOL 3-KINASE DELTA
  申请人：ICOS Corporation

  公开号：EP3029041A1

  公开（公告）日：2016-06-08

  Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.

  本发明公开了抑制磷脂酰肌醇 3- 激酶δ异构体（PI3Kδ）活性的方法，以及治疗 PI3Kδ 在白细胞功能中发挥作用的疾病（如免疫和炎症紊乱）的方法。优选地，这些方法采用的活性剂可选择性地抑制 PI3Kδ，同时不会明显抑制其他 PI3K 同工酶的活性。提供了抑制 PI3Kδ 活性的化合物，包括选择性抑制 PI3Kδ 活性的化合物。还提供了使用 PI3Kδ 抑制性化合物抑制癌细胞生长或增殖的方法。因此，本发明提供了使用 PI3Kδ 抑制性化合物抑制体外和体内 PI3Kδ 介导过程的方法。
• Inhibitors of human phosphatidylinositol 3-kinase delta
  申请人：ICOS CORPORATION

  公开号：US10010550B2

  公开（公告）日：2018-07-03

  Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.

  本发明公开了抑制磷脂酰肌醇 3- 激酶δ异构体（PI3Kδ）活性的方法，以及治疗 PI3Kδ 在白细胞功能中发挥作用的疾病（如免疫和炎症紊乱）的方法。优选地，这些方法采用的活性剂可选择性地抑制 PI3Kδ，同时不会明显抑制其他 PI3K 同工酶的活性。提供了抑制 PI3Kδ 活性的化合物，包括选择性抑制 PI3Kδ 活性的化合物。还提供了使用 PI3Kδ 抑制性化合物抑制癌细胞生长或增殖的方法。因此，本发明提供了使用 PI3Kδ 抑制性化合物抑制体外和体内 PI3Kδ 介导过程的方法。