2,4-二甲基-5-嘧啶甲腈 | 4450-24-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 中文名称: 2,4-二甲基-5-嘧啶甲腈
• 英文名称: 2,4-Dimethyl-pyrimidin-5-carbonitril
• 英文别名: 2,4-dimethyl-pyrimidine-5-carbonitrile；2,4-Dimethylpyrimidine-5-carbonitrile
• CAS: 4450-24-2
• 化学式: C₇H₇N₃
• mdl: MFCD18377702
• 分子量: 133.153
• InChiKey: MSGZHTWPQMGROE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.285
• 拓扑面积：
  49.6
• 氢给体数：
  0
• 氢受体数：
  3

安全信息

• 海关编码：
  2933599090

文献信息

• PYRAZOLYL-PYRIMIDINE DERIVATIVES AS KINASE INHIBITORS
  申请人：Casuscelli Francesco

  公开号：US20140051708A1

  公开（公告）日：2014-02-20

  The present invention relates to pyrazolyl-pyrimidine derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.

  本发明涉及嘧啶基嘧唑衍生物，其调节蛋白激酶活性，因此在治疗由蛋白激酶活性失调引起的疾病方面具有用处。本发明还提供了制备这些化合物的方法，包括这些化合物的药物组合物，以及利用这些化合物或含有它们的药物组合物治疗疾病的方法。
• [EN] POLYCYCLIC INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7)<br/>[FR] INHIBITEURS POLYCYCLIQUES DE KINASE CYCLINE-DÉPENDANTE 7 (CDK7)
  申请人：DANA FARBER CANCER INST INC

  公开号：WO2015058140A1

  公开（公告）日：2015-04-23

  The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, lymphoma, melanoma, multiple myeloma, breast cancer, Ewing' s sarcoma, osteosarcoma, brain cancer, neuroblastoma, lung cancer), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7), cyclin-dependent kinase 12 (CDK12), or cyclin-dependent kinase 13 (CDK13)), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.

  本发明提供了一种新型化合物的公式（I），以及其药用可接受的盐、溶剂合物、水合物、多晶形态、共晶体、互变异构体、立体异构体、同位素标记衍生物、前药和其组合物。还提供了涉及创新化合物或组合物的方法和试剂盒，用于治疗或预防增殖性疾病（例如，癌症（例如，白血病、淋巴瘤、黑色素瘤、多发性骨髓瘤、乳腺癌、尤因氏肉瘤、骨肉瘤、脑癌、神经母细胞瘤、肺癌）、良性肿瘤、血管生成、炎症性疾病、自身炎症性疾病和自身免疫疾病）的方法和试剂盒。使用本发明的化合物或组合物治疗患有增殖性疾病的对象可能抑制激酶的异常活性，如细胞周期依赖性激酶（CDK）（例如，细胞周期依赖性激酶7（CDK7）、细胞周期依赖性激酶12（CDK12）或细胞周期依赖性激酶13（CDK13）），从而在对象中诱导细胞凋亡和/或抑制转录。
• BENZOXAZEPINES AS INHIBITORS OF mTOR AND METHODS OF THEIR USE AND MANUFACTURE
  申请人：Rice Kenneth

  公开号：US20140018347A1

  公开（公告）日：2014-01-16

  The invention is directed to inhibitors of mTOR and pharmaceutically acceptable salts or solvates thereof, as well as methods of using them. The inhibitors are generally of structural Formula (I) wherein the variables are as defined herein.

  本发明涉及mTOR的抑制剂及其药学上可接受的盐或溶剂，以及使用它们的方法。抑制剂通常具有结构式（I），其中变量如本文所定义。
• POLYCYCLIC INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7)
  申请人：DANA-FARBER CANCER INSTITUTE, INC.

  公开号：US20160264554A1

  公开（公告）日：2016-09-15

  The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma, lung cancer), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7), cyclin-dependent kinase 12 (CDK12), or cyclin-dependent kinase 13 (CDK13)), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.

  本发明提供了公式（I）的新型化合物，以及其药学上可接受的盐，溶剂合物，水合物，多晶形，共晶体，互变异构体，立体异构体，同位素标记衍生物，前药和其组合物。还提供了涉及本发明化合物或组合物的方法和试剂盒，用于治疗或预防主体中的增殖性疾病（例如，癌症（例如，白血病，淋巴瘤，黑色素瘤，多发性骨髓瘤，乳腺癌，尤因肉瘤，骨肉瘤，脑癌，神经母细胞瘤，肺癌），良性肿瘤，血管生成，炎症性疾病，自身炎症性疾病和自身免疫性疾病）。使用本发明化合物或组合物治疗患有增殖性疾病的主体可能抑制激酶的异常活性，例如细胞周期依赖性激酶（CDK）（例如，细胞周期依赖性激酶7（CDK7），细胞周期依赖性激酶12（CDK12）或细胞周期依赖性激酶13（CDK13）），从而在主体中诱导细胞凋亡和/或抑制转录。
• [EN] BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE<br/>[FR] COMPOSÉS BIFONCTIONNELS POUR LA DÉGRADATION DE L'EGFR ET PROCÉDÉS D'UTILISATION ASSOCIÉS
  申请人：BEIGENE LTD

  公开号：WO2022068849A1

  公开（公告）日：2022-04-07

  Disclosed herein are bifunctional compounds formed by conjugating EGFR inhibitor moieties with E3 ligase Ligand moieties, which function to recruit targeted proteins to E3 ubiquitin ligase for degradation of mutant EGFR kinase, and methods of preparation and uses thereof.

  本文披露了一种双功能化合物，由EGFR抑制剂部分与E3连接配体部分结合而成，其功能是将靶向蛋白质招募到E3泛素连接酶降解突变EGFR激酶，并提供了其制备方法和用途。