2-(tert-Butyl)-5-isopropyl-1H-indole

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 2-(tert-Butyl)-5-isopropyl-1H-indole
• 英文别名: 2-tert-butyl-5-propan-2-yl-1H-indole
• 化学式: C₁₅H₂₁N
• mdl: MFCD05224320
• 分子量: 215.33
• InChiKey: UPZKVRPTJSJUNA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.9
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  15.8
• 氢给体数：
  1
• 氢受体数：
  0

文献信息

• NOVEL COMPOUNDS HAVING ESTROGEN RECEPTOR ALPHA DEGRADATION ACTIVITY AND USES THEREOF
  申请人：ACCUTAR BIOTECHNOLOGY INC.

  公开号：US20200157078A1

  公开（公告）日：2020-05-21

  The present disclosure relates to novel compounds having estrogen receptor alpha degradation activity, pharmaceutical compositions containing such compounds, and their use in prevention and treatment of cancer and related diseases and conditions.

  本公开涉及具有雌激素受体α降解活性的新化合物，包含这些化合物的药物组合物，以及它们在预防和治疗癌症及相关疾病和症状中的应用。
• ZINC SENSORS FOR IN VIVO IMAGING OF BETA-CELL FUNCTION BY MRI
  申请人：The Board of Regents of the University of Texas System

  公开号：US20190031640A1

  公开（公告）日：2019-01-31

  In some aspects, the present disclosure provides gadolinium based sensors which may be used to image zinc ions in vivo. In some embodiments, the compounds show appropriate reactivity with zinc ions while maintaining high relaxivity to achieve improved background relative to other sensors.

  在某些方面，本公开提供了基于钆的传感器，可用于在体内成像锌离子。在某些实施例中，这些化合物与锌离子显示出适当的反应性，同时保持高弛豫度，以实现相对于其他传感器的改善背景。
• HEPATITIS C VIRUS INHIBITORS
  申请人：Qiu Yao-Ling

  公开号：US20120039848A1

  公开（公告）日：2012-02-16

  The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

  本发明揭示了公式（I）的化合物或其药学上可接受的盐、酯或前药，它们能够抑制RNA含量病毒，特别是丙型肝炎病毒（HCV）。因此，本发明的化合物干扰了丙型肝炎病毒的生命周期，并且也可用作抗病毒剂。本发明还涉及包含上述化合物的制药组合物，用于治疗患有HCV感染的受试者。本发明还涉及通过给受试者投予包含本发明化合物的制药组合物来治疗HCV感染的方法。
• ALKYNE COMPOUNDS WITH MCH ANTAGONISTIC ACTIVITY AND MEDICAMENTS COMPRISING THESE COMPOUNDS
  申请人：Stenkamp Dirk

  公开号：US20090069282A1

  公开（公告）日：2009-03-12

  The present invention relates to alkyne compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R 1 and R 2 have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one alkyne according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.

  本发明涉及一般式I的炔化合物，其中A、B、W、X、Y、Z、R1和R2的基团和残基具有权利要求1中给出的含义。本发明还涉及包含至少一种根据本发明的炔烃的制药组合物。鉴于它们的MCH受体拮抗活性，根据本发明的制药组合物适用于治疗代谢性疾病和/或进食障碍，特别是肥胖症、暴食症、厌食症、过度进食和糖尿病。
• Inhibitors of mitochondrial pyruvate dehydrogenase kinase isoforms 1-4 and uses thereof
  申请人：The Board of Regents of the University of Texas System

  公开号：US10167258B2

  公开（公告）日：2019-01-01

  The present disclosure relates to the identification of PDK inhibitors and their use in the treatment of diseases such as diabetes, cardiovascular disease and cancer. The invention relates to the development of robust PDK inhibitors that can be used to improve glucose metabolism and correct metabolic dysfunction in vivo. Based on the unique structural features present in the ATP-binding pocket of PDK2, a single functional-group change was made in a known Hsp90 inhibitor that binds to the corresponding pocket of the latter protein from the GHKL family. This approach efficiently converted the Hsp90 inhibitor to a highly specific inhibitor for all PDK isoforms. These final PDK inhibitors of this series robustly augments PDC activity with reduced phosphorylation in tissues.

  本公开涉及 PDK 抑制剂的鉴定及其在治疗糖尿病、心血管疾病和癌症等疾病中的应用。本发明涉及开发可用于改善葡萄糖代谢和纠正体内代谢功能障碍的强效 PDK 抑制剂。根据 PDK2 的 ATP 结合口袋中存在的独特结构特征，对已知的 Hsp90 抑制剂进行了单官能团改变，使其与 GHKL 家族后一种蛋白质的相应口袋结合。这种方法有效地将 Hsp90 抑制剂转变成了一种针对所有 PDK 同工酶的高度特异性抑制剂。该系列的最后几种 PDK 抑制剂可增强 PDC 的活性，同时降低组织中的磷酸化。