2-Fluor-6-methylpurin | 655-37-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并嘧啶类
• 英文名称: 2-Fluor-6-methylpurin
• 英文别名: 2-Fluoro-6-methylpurin；2-fluoro-6-methyl-7(9)H-purine；2-fluoro-6-methyl-7H-purine
• CAS: 655-37-8
• 化学式: C₆H₅FN₄
• 分子量: 152.131
• InChiKey: PVPFGLXLULOCQV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  54.5
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] QUINOLIZINONE DERIVATIVES AS PI3K INHIBITORS<br/>[FR] DÉRIVÉS DE QUINOLIZINONE UTILISÉS COMME INHIBITEURS DE PI3K
  申请人：LUPIN LTD

  公开号：WO2016001855A1

  公开（公告）日：2016-01-07

  Disclosed are compounds of formula (I), their tautomeric forms, stereoisomers, and pharmaceutically acceptable salts thereof, wherein R1 - R4, and n are as defined in the specification, pharmaceutical compositions including a compound, tautomer, stereoisomer, or salt thereof, and methods of treating or preventing diseases or disorders, for example, cancer, that are amenable to treatment or prevention by inhibiting the PI3K enzyme of a subject.

  本发明揭示了公式(I)的化合物及其互变异构体、立体异构体和药学上可接受的盐，其中R1-R4和n如规范所定义，包括一种化合物、互变异构体、立体异构体或其盐的制药组合物，以及治疗或预防疾病或障碍（例如癌症），该疾病或障碍可通过抑制受体内的PI3K酶来进行治疗或预防的方法。
• CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS
  申请人：Ren Pingda

  公开号：US20120245169A1

  公开（公告）日：2012-09-27

  Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.

  本文描述了调节PI3激酶活性的化学实体、含有这些化学实体的制药组合物，以及使用这些化学实体治疗与PI3激酶活性相关的疾病和病状的方法。
• ALKYNYL ALCOHOLS AS KINASE INHIBITORS
  申请人：Chen Guoqing

  公开号：US20110086834A1

  公开（公告）日：2011-04-14

  Selected compounds are effective for prophylaxis and treatment of inflammation and inflammatory disorders, such as NIK-mediated disorders. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, inflammation and the like.

  所选化合物对于预防和治疗炎症和炎症性疾病（如NIK介导的疾病）有效。本发明涵盖新的化合物、类似物、前药和其药学上可接受的盐、制药组合物和预防和治疗涉及炎症等疾病和其他疾病或病症的方法。
• PROCESS FOR PREPARING CERTAIN CHEMICAL ENTITIES
  申请人：Intellikine, LLC

  公开号：EP3150609A1

  公开（公告）日：2017-04-05

  A process for preparing a compound of formula: wherein R3 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, alkoxy, amido, amino, alkoxycarbonyl sulfonamido, halo, cyano, hydroxy or nitro, comprising reacting a compound of formula: with a compound of formula: in the presence of a base. The THP group may be removed with acid to make chemical entities that modulate PI3 kinase activity for treating diseases and conditions associated with PI3 kinase activity and/or formulated into pharmaceutical compositions containing such chemical entities.

  一种制备式化合物的工艺： 其中 R3 为氢、烷基、烯基、炔基、环烷基、杂环烷基、烷氧基、氨基、氨基、烷氧羰基磺酰胺基、卤代、氰基、羟基或硝基，包括将式： 与式 的化合物在碱存在下进行反应。THP基团可以用酸去除，制成调节PI3激酶活性的化学实体，用于治疗与PI3激酶活性相关的疾病和病症，和/或配制成含有此类化学实体的药物组合物。
• A PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION
  申请人：Intellikine, LLC

  公开号：EP3441392A1

  公开（公告）日：2019-02-13

  A pharmaceutical composition for oral administration comprising an effective amount of a compound of Formula V-A2: or a pharmaceutically acceptable salt thereof; wherein B is a moiety of Formula II: Wc is aryl, heteroaryl, heterocycloalkyl, or cycloalkyl; q is an integer of 0 or 1; R1 is hydrogen, alkyl, or halo; R2 is alkyl or halo; R3 is halo; and R9 is alkyl, or heterocycloalkyl; and one or more pharmaceutically acceptable excipients suitable for oral administration. The pharmaceutical composition may contain an effective amount of a second agent such as a chemotherapeutic agent, e.g. a proteasome inhibitor, an alkylating agent or a therapeutic antibody.

  一种口服药物组合物，包含有效量的式 V-A2 化合物： 或其药学上可接受的盐； 其中 B 为式 II 的分子： Wc 是芳基、杂芳基、杂环烷基或环烷基； q 是 0 或 1 的整数； R1 是氢、烷基或卤素； R2 是烷基或卤代 R3 是卤代物；以及 R9 是烷基或杂环烷基； 以及一种或多种适合口服的药学上可接受的赋形剂。药物组合物可含有有效量的第二种药剂，如化疗药，如蛋白酶体抑制剂、烷化剂或治疗性抗体。