5-Chloro-2-methyl-3-pyridin-2-yl-3H-quinazolin-4-one | 3360-03-0

• 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: 5-Chloro-2-methyl-3-pyridin-2-yl-3H-quinazolin-4-one
• 英文别名: 5-Chloro-2-methyl-3-pyridin-2-ylquinazolin-4-one
• CAS: 3360-03-0
• 化学式: C₁₄H₁₀ClN₃O
• 分子量: 271.706
• InChiKey: SWFSYFRLLWKAGI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  19
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  45.6
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• SUBSTITUTED AMINOPYRIMIDINE COMPOUNDS AND METHODS OF USE
  申请人：Xi Ning

  公开号：US20150087663A1

  公开（公告）日：2015-03-26

  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 limited to leukemias and solid tumors, in mammals, especially humans.

  本发明涉及新的氨基嘧啶衍生物的制备和使用，作为自由形式或药学上可接受的盐形式和制剂，用于调节PI3K酶活性介导的紊乱或疾病。本发明还提供包含这些化合物的药学上可接受的组成物和使用这些组成物治疗哺乳动物，特别是人类中PI3K酶在白细胞功能中发挥作用的免疫和炎症紊乱以及与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瘤的方法。
• HETEROARYL DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING DISEASES ASSOCIATED WITH PI3 KINASES, CONTAINING SAME AS ACTIVE INGREDIENT
  申请人：Korea Research Institute of Chemical Technology

  公开号：EP3312175A1

  公开（公告）日：2018-04-25

  The present invention relates to a heteroaryl derivative or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition for preventing or treating diseases associated with PI3 kinases, containing the same as an active ingredient. The heteroaryl derivative according to the present invention has an excellent effect of selectively inhibiting PI3 kinases, thereby being useful in preventing or treating PI3 kinase diseases such as: cancers such as hematologic malignancy, ovarian cancer, uterine cervical cancer, breast cancer, colorectal cancer, liver cancer, gastric cancer, pancreatic cancer, colon cancer, peritoneal metastatic cancer, skin cancer, bladder cancer, prostate cancer, lung cancer, osteosarcoma, fibrous tumors, and brain tumors; autoimmune diseases such as rheumatoid arthritis, systemic lupus erythematosis, multiple sclerosis, diabetes mellitus, hyperthyroidism, myasthenia, Crohn's disease, ankylosing spondylitis, autoimmune pernicious anemia, and Sjogren's syndrome; and respiratory diseases such as chronic obstructive pulmonary disease (COPD), rhinitis, asthma, chronic bronchitis, chronic pulmonary inflammatory diseases, silicosis, pulmonary sarcoidosis, pleurisy, alveolitis, angitis, pneumatosis, pneumonia, and bronchiectasis.

  本发明涉及一种杂芳基衍生物或其药学上可接受的盐、其制备方法以及一种用于预防或治疗与PI3激酶相关疾病的药物组合物，其中含有杂芳基衍生物或其药学上可接受的盐、其制备方法以及一种用于预防或治疗与PI3激酶相关疾病的药物组合物，其中含有杂芳基衍生物或其药学上可接受的盐作为活性成分。根据本发明的杂芳基衍生物具有很好的选择性抑制 PI3 激酶的效果，因此可用于预防或治疗 PI3 激酶疾病，如癌症，如血液系统恶性肿瘤、卵巢癌、子宫颈癌、乳腺癌、结直肠癌、肝癌、胃癌、胰腺癌、结肠癌、腹膜转移癌、皮肤癌、膀胱癌、前列腺癌、肺癌、骨肉瘤、纤维瘤和脑瘤；自身免疫性疾病，如类风湿性关节炎、系统性红斑狼疮、多发性硬化症、糖尿病、甲状腺机能亢进症、肌无力、克罗恩病、强直性脊柱炎、自身免疫性恶性贫血和 Sjogren 综合征；呼吸系统疾病，如慢性阻塞性肺病（COPD）、鼻炎、哮喘、慢性支气管炎、慢性肺部炎症、矽肺、肺肉瘤病、胸膜炎、肺泡炎、血管炎、肺气肿、肺炎和支气管扩张。
• SUBSTITUTED AMINOPYRIMIDINE COMPOUNDS AS PI3-KINASE INHIBITORS
  申请人：Calitor Sciences, LLC

  公开号：EP3046563B1

  公开（公告）日：2019-05-29
• US9518046B2
  申请人：——

  公开号：US9518046B2

  公开（公告）日：2016-12-13
• US9670194B2
  申请人：——

  公开号：US9670194B2

  公开（公告）日：2017-06-06