5-Chloro-7-ethenyl-3-propan-2-ylpyrazolo[1,5-a]pyrimidine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡唑并嘧啶类
• 英文名称: 5-Chloro-7-ethenyl-3-propan-2-ylpyrazolo[1,5-a]pyrimidine
• 英文别名: 5-chloro-7-ethenyl-3-propan-2-ylpyrazolo[1,5-a]pyrimidine
• 化学式: C₁₁H₁₂ClN₃
• 分子量: 221.68
• InChiKey: KXVUSLIIZPLFST-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  30.2
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• [EN] 1 -PHENOXY-3-(ALKYLAMINO)-PROPAN-2-OL DERIVATIVES AS CARM1 INHIBITORS AND USES THEREOF<br/>[FR] DÉRIVÉS DE 1-PHÉNOXY-3-(ALKYLAMINO)-PROPAN-2-OL EN TANT QU'INHIBITEURS DE CARM1 ET LEURS UTILISATIONS
  申请人：EPIZYME INC

  公开号：WO2014144455A1

  公开（公告）日：2014-09-18

  Provided herein are compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, R1, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is an optionally substituted 6,5-bicyclic heteroaryl ring system comprising 2 to 5 nitrogen atoms, inclusive, wherein the point of attachment is provided on the 6-membered ring of the 6,5-bicyclic heteroaryl ring system, and wherein the 6-membered ring is further substituted with a group of formula -L1 -R3, wherein L1 and R3 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.

  本文提供了Formula (I)的化合物及其药学上可接受的盐，以及药物组合物；其中X、R1、R2a、R2b、R2c、R2d的定义如本文所述，Ring HET是一个可选取代的含2到5个氮原子的6,5-双环杂芳基环系统，其中连接点位于6,5-双环杂芳基环系统的6个环上，并且6个环还进一步取代为一个具有式-L1-R3的基团，其中L1和R3的定义如本文所述。本发明的化合物对于抑制CARM1活性是有用的。还描述了利用这些化合物治疗CARM1介导的疾病的方法。
• [EN] INHIBITORS OF CYCLIN-DEPENDENT KINASES<br/>[FR] INHIBITEURS DE KINASES CYCLINE-DÉPENDANTES
  申请人：DANA FARBER CANCER INST INC

  公开号：WO2016160617A2

  公开（公告）日：2016-10-06

  The present invention provides novel compounds of Formula (I), (II), or (III), 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 and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with 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., CDK7, CDK12, or CDK13), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.