1-(6-Fluoro-4-oxo-3-phenylquinazolin-2-yl)ethylcarbamic acid

• 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: 1-(6-Fluoro-4-oxo-3-phenylquinazolin-2-yl)ethylcarbamic acid
• 英文别名: 1-(6-fluoro-4-oxo-3-phenylquinazolin-2-yl)ethylcarbamic acid
• 化学式: C₁₇H₁₄FN₃O₃
• 分子量: 327.31
• InChiKey: IQMNDXQDXLPTOC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  24
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  82
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• [EN] SUBSTITUTED AMINOPYRIMIDINE COMPOUNDS AND METHODS OF USE<br/>[FR] COMPOSÉS D'AMINOPYRIMIDINE SUBSTITUÉS ET PROCÉDÉS D'UTILISATION
  申请人：SUNSHINE LAKE PHARMA CO LTD

  公开号：WO2016149160A1

  公开（公告）日：2016-09-22

  The invention relates to the preparation and use of new aminopyrimidine derivatives as drug candidates in free form or in pharmaceutically acceptable salt form and formulations thereof for the modulation of a disorder or disease which is mediated by the activity of the PI3K enzymes. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of disorders or diseases, such as disorders of immunity and inflammation in which PI3K enzymes play a role in leukocyte function, and hyperproliferative disorders associated with PI3K activity, including but not restricted to leukemias and solid tumors, in mammals, especially humans.

  该发明涉及新的氨基嘧啶衍生物的制备和使用，作为候选药物，可以以自由形式或药用盐形式及其配方用于调节由PI3K酶活性介导的疾病或紊乱。该发明还提供了包含这种化合物的药用合成物和使用这些合成物治疗疾病或紊乱的方法，例如免疫和炎症紊乱，其中PI3K酶在白细胞功能中发挥作用，以及与PI3K活性相关的过度增殖性疾病，包括但不限于白血病和实体肿瘤，在哺乳动物，尤其是人类中。
• PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS
  申请人：GILEAD CALISTOGA LLC

  公开号：US20140179673A1

  公开（公告）日：2014-06-26

  The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), or pharmaceutically acceptable salts thereof, in which R 1 , R 2 , n, R 3 , R 4 , R 5 and R 6 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms, such as PI3Kδ. The present disclosure further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms, such as PI3Kδ.

  本公开提供了式(I)的磷脂酰肌醇3-激酶（PI3K）抑制剂，或其药用盐，其中R1、R2、n、R3、R4、R5和R6如本文所定义。这些化合物可用于治疗由一个或多个PI3K亚型介导的疾病，如PI3Kδ。本公开还提供了包括式(I)化合物或其药用盐的药物组合物，以及使用这些化合物和组合物治疗由一个或多个PI3K亚型介导的疾病的方法，如PI3Kδ。
• PROCESS METHODS FOR PHOSPHATIDYLINOSITOL 3-KINDASE INHIBITORS
  申请人：Gilead Calistoga LLC

  公开号：US20150175605A1

  公开（公告）日：2015-06-25

  A process for the synthesis of quinazolinone containing compounds which may be useful for the treatment of cancer, is hereby disclosed. In addition, compound intermediates relating to these processes are also disclosed.

  本文公开了一种合成含喹唑啉酮类化合物的方法，这些化合物可能对癌症的治疗有用。此外，还公开了与这些方法相关的化合物中间体。
• Process methods for phosphatidylinositol 3-kinase inhibitors
  申请人：GILEAD CALISTOGA LLC

  公开号：US10414737B2

  公开（公告）日：2019-09-17

  A process for the synthesis of quinazolinone containing compounds which may be useful for the treatment of cancer, is hereby disclosed. In addition, compound intermediates relating to these processes are also disclosed.

  本文公开了一种可用于治疗癌症的含喹唑啉酮化合物的合成工艺。 此外，还公开了与这些工艺有关的化合物中间体。
• SUBSTITUTED PYRIMIDINE AMINOALKYL-QUINAZOLONES AS PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS
  申请人：Gilead Calistoga LLC

  公开号：EP2941426B1

  公开（公告）日：2018-06-13