4-hydroxy-3,3-dimethyl-2H,3H,5H-benzo[g]indole-2,5-dione

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 4-hydroxy-3,3-dimethyl-2H,3H,5H-benzo[g]indole-2,5-dione
• 英文别名: 4-hydroxy-3,3-dimethyl-2H-benzo[g]indole-2,5(3H)-dione；BVT-948；BVT.948
• 化学式: C₁₄H₁₁NO₃
• 分子量: 241.246
• InChiKey: BAQXWJQSUXZVIP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.05
• 重原子数：
  18.0
• 可旋转键数：
  0.0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  66.73
• 氢给体数：
  1.0
• 氢受体数：
  3.0

反应信息

• 作为反应物：
  描述：

  4-hydroxy-3,3-dimethyl-2H,3H,5H-benzo[g]indole-2,5-dione 在 potassium carbonate 、 碘甲烷 作用下， 以 甲醇 、 氯仿 为溶剂， 以0.051 mg (50%)的产率得到4-methoxy-3,3-dimethyl-2H,3H,5H-benzo[g]indole-2,5-dione
  参考文献：
  名称：

  Novel compounds

  摘要：

  本发明涉及化合物I、化合物Ia和化合物Ib.1的公式，其中R1、R2、R3、R4、Ra和Rb的每个定义均已在此处定义。本发明还涉及制备过程、使用和包含上述化合物的制药组合物。这些新型化合物在治疗中有用，特别是用于治疗2型糖尿病。

  公开号：

  US20020061921A1
• 作为产物：
  描述：

  2-hydroxy-3,3-dimethyl-5-oxo-3,5-dihydro-2H-benzo[g]indole 1-oxide 在 盐酸 、 对苯醌 作用下， 以 乙醇 、 水 为溶剂， 反应 2.0h， 以0.85 g的产率得到4-hydroxy-3,3-dimethyl-2H,3H,5H-benzo[g]indole-2,5-dione
  参考文献：
  名称：

  4-羟基-3,3-二甲基-2H-苯并[g]吲哚-2,5 （3H）-二酮的合成方法 注意： 申请人在申请日后补交了实验数据，但该数据并未包含在 本授权公告文档中。

  摘要：

  公开号：

  CN112321486B

文献信息

• [EN] RIG-I INNATE IMMUNE RECEPTOR ANTAGONISTS AND METHODS OF USING SAME<br/>[FR] ANTAGONISTES DU RÉCEPTEUR IMMUNITAIRE INNÉ RIG-I ET LEURS PROCÉDÉS D'UTILISATION
  申请人：UNIV YALE

  公开号：WO2021091958A1

  公开（公告）日：2021-05-14

  The present disclosure provides RIG-I antagonists. In certain embodiments, the antagonists of the disclosure can be used to treat or prevent a disease or disorder in a subject.

  本公开提供了RIG-I拮抗剂。在某些实施例中，本公开的拮抗剂可用于治疗或预防受试者的疾病或紊乱。
• Compounds
  申请人：Biovitrum AB

  公开号：US06498182B2

  公开（公告）日：2002-12-24

  The present invention is directed to compounds of formula I, formula Ia, and formula Ib. wherein each of R1, R2, R3, R4, Ra, and Rb has been defined herein. The invention is also directed to a process for the preparation, the use and pharmaceutical compositions comprising the compounds described above. These novel compounds are useful in therapy, particularly for the treatment of type 2 diabetes.

  本发明涉及式I、式Ia和式Ib的化合物，其中R1、R2、R3、R4、Ra和Rb中的每一个已在此处定义。本发明还涉及制备过程、使用和包括上述化合物的制药组合物。这些新化合物在治疗中有用，特别是用于治疗2型糖尿病。
• SYSTEMS, METHODS, AND COMPOSITIONS TO IDENTIFY NEW PROTEIN TARGETS OF A CHEMICAL COMPOUND OR ITS DERIVATIVES
  申请人：CHANG GEEN-DONG

  公开号：US20200333332A1

  公开（公告）日：2020-10-22

  Systems and methods to identify new protein targets of a chemical compound or its derivatives were described. The methods can be used for detection of new binding partners as long as the chemical compound can covalently bind to the protein targets. Once protein targets are resolved, information related to new protein targets can then be used to couple with real-world patient data such as adverse events, efficacy data, and disease correlation data to deduce real-world evidence. Systems collectively with all this information can aide clinical development and use of pharmaceutical drug. Methods are provided for detection of covalently bound phenyl vinyl sulfone (PVS) or its derivatives, and afatinib or its derivatives. Furthermore, generation of antiserum recognizing carrier bound PVS or carrier bound afatinib is described. PRMT1 is described as a new target of PVS and RRM1, RRM2, and NFKB are described as new targets of afatinib.
• COMPOUNDS, COMPOSITIONS, METHODS, AND USES FOR TREATING LEPTIN RESISTANCE, OBESITY, DIABETES MELLITUS AND METABOLIC SYNDROME
  申请人：Hurt Clarence

  公开号：US20210324031A1

  公开（公告）日：2021-10-21

  Novel leptin and leptin-fusion protein-small molecule drug conjugates are disclosed, where conjugation takes place through the use of cleavable and non-cleavable linkers. The small molecules chemically linked to the protein carrier are imported into the specific leptin-responsive target tissue or cell through receptor-mediated endocytosis and released from the carrier protein through enzymatic cleavage of the linker-drug moiety or through lysosomal degradation of the carrier protein. Free drug then act to modify leptin receptor-triggered biochemical pathways that are altered in conditions of leptin-resistance. Drug will correct altered pathway allowing resensitization of receptor signaling. This can greatly aid in the resolution of pathologies either initiated at the onset of leptin resistance or exacerbated by it.
• RIG-I INNATE IMMUNE RECEPTOR ANTAGONISTS AND METHODS OF USING SAME
  申请人：YALE UNIVERSITY

  公开号：US20220395487A1

  公开（公告）日：2022-12-15

  The present disclosure provides certain RIG-I antagonists. In certain embodiments, the antagonists of the disclosure can be used to treat or prevent a disease or disorder in a subject.