YU 102 | 344591-95-3

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: YU 102
• 英文别名: (2S)-1-(2-acetamidoacetyl)-N-[(2S)-1-[[(2S)-4-methyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]pyrrolidine-2-carboxamide
• CAS: 344591-95-3
• 化学式: C₂₇H₃₈N₄O₆
• 分子量: 514.622
• InChiKey: QWEBSYDRFXZQMF-GHIUXRNCSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  37
• 可旋转键数：
  12
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.59
• 拓扑面积：
  137
• 氢给体数：
  3
• 氢受体数：
  6

文献信息

• FAP-Activated Proteasome Inhibitors for Treating Solid Tumors
  申请人：Trustees of Tufts College

  公开号：US20160346401A1

  公开（公告）日：2016-12-01

  Disclosed are proteasome inhibitors, fibroblast activation protein (FAP)-activated prodrugs of proteasome inhibitors, and pharmaceutically acceptable salts of the inhibitors and prodrugs. Also disclosed are related pharmaceutical compositions, and methods of using the inhibitors and prodrugs and compositions thereof, for example, in treating cancer or other cell proliferative diseases. In vitro and in vivo methods of quantifying the expression of FAP in a biopsy sample and a mammal, respectively, are also disclosed.

  本发明涉及蛋白酶体抑制剂、成纤维细胞激活蛋白（FAP）激活的蛋白酶体抑制剂前药以及药学上可接受的盐。还公开了相关的制药组合物，以及使用抑制剂和前药及其组合物的方法，例如在治疗癌症或其他细胞增殖性疾病方面。还公开了体外和体内方法，用于定量检测活检样品和哺乳动物中FAP的表达。
• FAP-activated proteasome inhibitors for treating solid tumors
  申请人：Trustees of Tufts College

  公开号：US11065339B2

  公开（公告）日：2021-07-20

  Disclosed are proteasome inhibitors, fibroblast activation protein (FAP)-activated prodrugs of proteasome inhibitors, and pharmaceutically acceptable salts of the inhibitors and prodrugs. Also disclosed are related pharmaceutical compositions, and methods of using the inhibitors and prodrugs and compositions thereof, for example, in treating cancer or other cell proliferative diseases. In vitro and in vivo methods of quantifying the expression of FAP in a biopsy sample and a mammal, respectively, are also disclosed.

  公开了蛋白酶体抑制剂、成纤维细胞活化蛋白（FAP）激活的蛋白酶体抑制剂原药，以及这些抑制剂和原药的药学上可接受的盐类。还公开了相关的药物组合物，以及使用这些抑制剂和原药及其组合物的方法，例如治疗癌症或其他细胞增殖性疾病的方法。还公开了分别量化活检样本和哺乳动物中 FAP 表达的体外和体内方法。
• US20140255300A1
  申请人：——

  公开号：US20140255300A1

  公开（公告）日：2014-09-11
• FAP-ACTIVATED PROTEASOME INHIBITORS FOR TREATING SOLID TUMORS
  申请人：Trustees of Tufts College

  公开号：US20190054181A1

  公开（公告）日：2019-02-21

  Disclosed are proteasome inhibitors, fibroblast activation protein (FAP)-activated prodrugs of proteasome inhibitors, and pharmaceutically acceptable salts of the inhibitors and prodrugs. Also disclosed are related pharmaceutical compositions, and methods of using the inhibitors and prodrugs and compositions thereof, for example, in treating cancer or other cell proliferative diseases. In vitro and in vivo methods of quantifying the expression of FAP in a biopsy sample and a mammal, respectively, are also disclosed.
• PROTEASOME INHIBITORS
  申请人：University of Kentucky Research Foundation

  公开号：US20190161516A1

  公开（公告）日：2019-05-30

  Unique epoxyketone compounds useful for inhibiting a proteasome in a cell, pharmaceutical compositions and methods of their use are provided herein.