1-Methyl-3,5-di(propan-2-yl)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: 1-Methyl-3,5-di(propan-2-yl)indole
• 英文别名: 1-methyl-3,5-di(propan-2-yl)indole
• 化学式: C₁₅H₂₁N
• 分子量: 215.33
• InChiKey: ZGMGSOAKYBVSHU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 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：
  4.9
• 氢给体数：
  0
• 氢受体数：
  0

文献信息

• [EN] HEMIASTERLIN DERIVATIVES FOR CONJUGATION AND THERAPY<br/>[FR] DÉRIVÉS D'HÉMIASTERLINE POUR CONJUGAISON ET THÉRAPIE
  申请人：SUTRO BIOPHARMA INC

  公开号：WO2016123582A1

  公开（公告）日：2016-08-04

  Provided herein are hemiasterlin derivatives, conjugates thereof, compositions comprising the derivatives or conjugates thereof, methods of producing the derivatives and conjugates thereof, and methods of using the derivatives, conjugates, and compositions for the treatment of cell proliferation. The derivatives, conjugates, and compositions are useful in methods of treatment and prevention of cell proliferation and cancer, methods of detection of cell proliferation and cancer, and methods of diagnosis of cell proliferation and cancer. In an embodiment, the hemiasterlin derivatives are according to Formula 1000: or a pharmaceutically acceptable salt, solvate, or tautomer thereof, wherein Ar, L, W1, W4, W5, SG, and R are as described herein.

  本文提供了半星菱素衍生物，以及与之结合的共轭物，包含这些衍生物或共轭物的组合物，生产这些衍生物和共轭物的方法，以及利用这些衍生物、共轭物和组合物治疗细胞增殖的方法。这些衍生物、共轭物和组合物在治疗和预防细胞增殖和癌症的方法中很有用，也可用于检测细胞增殖和癌症的方法，以及诊断细胞增殖和癌症的方法。在一个实施例中，半星菱素衍生物符合公式1000：或其药用可接受的盐、溶剂化合物或互变异构体，其中Ar、L、W1、W4、W5、SG和R如本文所述。
• HEMIASTERLIN DERIVATIVES FOR CONJUGATION AND THERAPY
  申请人：SUTRO BIOPHARMA, INC.

  公开号：US20160257709A1

  公开（公告）日：2016-09-08

  Provided herein are hemiasterlin derivatives, conjugates thereof, compositions comprising the derivatives or conjugates thereof, methods of producing the derivatives and conjugates thereof, and methods of using the derivatives, conjugates, and compositions for the treatment of cell proliferation. The derivatives, conjugates, and compositions are useful in methods of treatment and prevention of cell proliferation and cancer, methods of detection of cell proliferation and cancer, and methods of diagnosis of cell proliferation and cancer. In an embodiment, the hemiasterlin derivatives are according to Formula 1000: or a pharmaceutically acceptable salt, solvate, or tautomer thereof, wherein Ar, L, W 1 , W 4 , W 5 , SG, and R are as described herein.

  本文提供了半天然菌素衍生物及其共轭物，包含这些衍生物或共轭物的组合物，制备这些衍生物和共轭物的方法，以及使用这些衍生物，共轭物和组合物治疗细胞增殖的方法。这些衍生物，共轭物和组合物在治疗和预防细胞增殖和癌症的方法中有用，用于细胞增殖和癌症的检测方法以及细胞增殖和癌症的诊断方法。在一个实施例中，半天然菌素衍生物如公式1000所示：或其药学上可接受的盐，溶剂或互变异构体，其中Ar，L，W1，W4，W5，SG和R如本文所述。
• Hemiasterlin derivatives for conjugation and therapy
  申请人：SUTRO BIOPHARMA, INC.

  公开号：US10844090B2

  公开（公告）日：2020-11-24

  Provided herein are hemiasterlin derivatives, conjugates thereof, compositions comprising the derivatives or conjugates thereof, methods of producing the derivatives and conjugates thereof, and methods of using the derivatives, conjugates, and compositions for the treatment of cell proliferation. The derivatives, conjugates, and compositions are useful in methods of treatment and prevention of cell proliferation and cancer, methods of detection of cell proliferation and cancer, and methods of diagnosis of cell proliferation and cancer. In an embodiment, the hemiasterlin derivatives are according to Formula 1000: or a pharmaceutically acceptable salt, solvate, or tautomer thereof, wherein Ar, L, W1, W4, W5, SG, and R are as described herein.

  本文提供了半胱氨酸衍生物、其共轭物、包含其衍生物或共轭物的组合物、生产其衍生物和共轭物的方法，以及使用其衍生物、共轭物和组合物治疗细胞增殖的方法。这些衍生物、共轭物和组合物可用于细胞增殖和癌症的治疗和预防方法、细胞增殖和癌症的检测方法以及细胞增殖和癌症的诊断方法。在一个实施方案中，半马斯特林衍生物符合式 1000： 或其药学上可接受的盐、溶液或同系物，其中 Ar、L、W1、W4、W5、SG 和 R 如本文所述。
• US20140256717A1
  申请人：——

  公开号：US20140256717A1

  公开（公告）日：2014-09-11
• MACROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS
  申请人：Fundación Centro Nacional de Investigaciones Oncologicas Carlos III

  公开号：US20160296528A1

  公开（公告）日：2016-10-13

  There is provided compounds of formula I, wherein R1, R 2a , R 2b , R 2c , X, Y, Z, R 3 and ring A/B have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. PI3-K, particularly class I PI3K, PIM family kinase and/or mTOR) is desired and/or required, and particularly in the treatment of cancer. The invention also relates to combinations containing such compounds.