7-乙基-7H-嘌呤 | 39253-23-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并嘧啶类
• 中文名称: 7-乙基-7H-嘌呤
• 英文名称: 7-Aethyl-purin
• 英文别名: 9-Ethylpurin；7-Aethyl-7H-purin；7-ethyl-7H-purine；7-Ethyl-7H-purine；7-ethylpurine
• CAS: 39253-23-1
• 化学式: C₇H₈N₄
• 分子量: 148.167
• InChiKey: FFMPFNDGZPBTCQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  43.6
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• [EN] NOVEL PDE INHIBITORS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESSES FOR THEIR PREPARATION<br/>[FR] NOUVEAUX INHIBITEURS DE PHOSPHODIESTÉRASES, COMPOSITIONS PHARMACEUTIQUES LES CONTENANT ET LEURS PROCÉDÉS DE PRÉPARATION
  申请人：MATRIX LAB LTD

  公开号：WO2009147476A1

  公开（公告）日：2009-12-10

  The present invention relates to novel heterocyclic compounds of general formula (I), which are phosphodiesterase inhibitors (PDEs), in particular phosphodiesterase type 4 inhibitors, pharmaceutical compositions containing them, and processes for their preparation. These novel PDEs are useful in treating allergic and inflammatory diseases (such as asthma, COPD, allergic rhinitis, allergic conjunctivitis, respiratory distress syndrome, chronic bronchitis, nephritis, rheumatoid spondylitis, osteoarthritis, atopic dermatitis, eosinophilic granuloma, psoriasis, rheumatoid septic shock, ulcerative colitis, multiple sclerosis, chronic inflammation, Crohn's syndrome and central nervous system(CNS) disorders) and for inhibiting the production of Tumor Necrosis Factor(TNF-α).

  本发明涉及一种新型杂环化合物，其一般式为(I)，它们是磷酸二酯酶抑制剂（PDEs），特别是磷酸二酯酶4型抑制剂，包含它们的制药组合物以及它们的制备方法。这些新型PDEs在治疗过敏和炎症性疾病（如哮喘、慢性阻塞性肺病、过敏性鼻炎、过敏性结膜炎、呼吸窘迫综合征、慢性支气管炎、肾炎、类风湿脊柱炎、骨关节炎、特应性皮炎、嗜酸性肉芽肿、银屑病、类风湿败血症、溃疡性结肠炎、多发性硬化症、慢性炎症、克罗恩综合征和中枢神经系统（CNS）疾病）以及抑制肿瘤坏死因子（TNF-α）的产生方面具有用途。
• ANILINE DERIVATIVES
  申请人：Tokumasu Munetaka

  公开号：US20070066586A1

  公开（公告）日：2007-03-22

  The present invention provides a novel compound having a kininogenase-inhibitory action and its pharmaceutical use. The compounds are represented by the formulas (A), (B), (C), (E) and (H): wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof.

  本发明提供了一种具有激肽原酶抑制作用的新化合物及其药物用途。该化合物由(A)、(B)、(C)、(E)和(H)式表示，其中每个符号如规范所定义，或其药学上可接受的盐。
• METHOD OF MODIFYING NUCLEOTIDE CHAIN
  申请人：MATSUSHITA ELECTRIC INDUSTRIAL CO., LTD.

  公开号：EP1647592A1

  公开（公告）日：2006-04-19

  A method for modifying a nucleotide chain, which includes: allowing a catabolic enzyme specific to a nucleotide sequence containing a specific base such as hypoxanthine (Hx) to act on a nucleotide chain (I) to be modified having the above described nucleotide sequence containing a specific base on the 3'-terminal side thereof; and forming a functional group (for example, an aldehyde group) capable of binding to a desired modifier (for example, NH2R having an amino group) on the 3'-terminus of the nucleotide chain (I); so as to bind the above described modifier to the 3'-terminus of the nucleotide chain. Using a nucleotide chain as a modification target which has a nucleotide sequence containing a specific base acting as an enzyme substrate on its 3'-terminal side, this method enables decomposition of only the above described nucleotide sequence portion, thereby forming a functional group that reacts with a desired modifier and binds thereto. By this method, a nucleotide chain can directly be modified with a modifier, thereby easily labeling or conjugating the nucleotide chain. Further, when immobilization of a nucleotide chain is intended, stable and strong immobilization can be attained using a modifier as a linker.

  一种修饰核苷酸链的方法，包括让对含有特定碱基（如次黄嘌呤（Hx））的核苷酸序列具有特异性的分解酶作用于待修饰的核苷酸链（I），该核苷酸链具有在其 3'- 末端侧含有特定碱基的上述核苷酸序列；并在核苷酸链（I）的 3'末端形成能够与所需修饰剂（例如具有氨基的 NH2R）结合的官能团（例如醛基），从而将上述修饰剂结合到核苷酸链的 3'末端。使用核苷酸链作为修饰靶，该核苷酸链的 3'- 末端含有作为酶底物的特定碱基的核苷酸序列，这种方法可以只分解上述核苷酸序列部分，从而形成与所需修饰剂反应并结合的官能团。通过这种方法，核苷酸链可以直接被修饰剂修饰，从而方便地标记或连接核苷酸链。此外，当需要固定核苷酸链时，使用修饰剂作为连接剂可以实现稳定而牢固的固定。
• Inhibitors of human phosphatidylinositol 3-kinase delta
  申请人：ICOS CORPORATION

  公开号：US10398695B2

  公开（公告）日：2019-09-03

  Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.

  本发明公开了抑制磷脂酰肌醇 3- 激酶δ异构体（PI3Kδ）活性的方法，以及治疗 PI3Kδ 在白细胞功能中发挥作用的疾病（如免疫和炎症紊乱）的方法。优选地，这些方法采用的活性剂可选择性地抑制 PI3Kδ，同时不会明显抑制其他 PI3K 同工酶的活性。提供了抑制 PI3Kδ 活性的化合物，包括选择性抑制 PI3Kδ 活性的化合物。还提供了使用 PI3Kδ 抑制性化合物抑制癌细胞生长或增殖的方法。因此，本发明提供了使用 PI3Kδ 抑制性化合物抑制体外和体内 PI3Kδ 介导过程的方法。
• Identification of genetic modifications
  申请人：WAKE FOREST UNIVERSITY HEALTH SCIENCES

  公开号：US10900071B2

  公开（公告）日：2021-01-26

  Described are methods of detecting modified nucleotide bases in a DNA sample using specific DNA glycosylases to excise target modified bases. DNA molecules are then labeled using a DNA polymerase lacking 3′→5′ exo-nuclease activity and strand displacement activity. The methods can be used to detect epigenetic changes and DNA damage. Provided are methods for diagnosing a disease or condition, determining risk of a disease or condition, identifying appropriate treatment, monitoring effectiveness of treatment, and monitoring side effects of treatment in subjects based on detection of modified bases. Also provided are methods for determining environmental exposure, or an environmental exposure time, of a biological sample containing DNA. Also provided are kits, systems, and devices for performing the described methods.

  描述了利用特定 DNA 糖基化酶切除目标修饰碱基来检测 DNA 样品中修饰核苷酸碱基的方法。然后使用缺乏 3′→5′ 外切核酸酶活性和链置换活性的 DNA 聚合酶标记 DNA 分子。这些方法可用于检测表观遗传变化和 DNA 损伤。所提供的方法可用于诊断疾病或病症、确定疾病或病症的风险、确定适当的治疗方法、监测治疗效果，以及根据对修饰碱基的检测监测治疗对受试者的副作用。还提供了用于确定含有 DNA 的生物样本的环境暴露或环境暴露时间的方法。还提供了用于执行所述方法的试剂盒、系统和装置。