Z-LLNle-CHO

• 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: Z-LLNle-CHO
• 英文别名: benzyl N-[(2S)-4-methyl-1-[[(2S)-4-methyl-1-oxo-1-[[(2S)-1-oxohexan-2-yl]amino]pentan-2-yl]amino]-1-oxopentan-2-yl]carbamate
• 化学式: C₂₆H₄₁N₃O₅
• 分子量: 475.6
• InChiKey: RNPDUXVFGTULLP-VABKMULXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.9
• 重原子数：
  34
• 可旋转键数：
  16
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  114
• 氢给体数：
  3
• 氢受体数：
  5

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。
• Prophylactic and therapeutic agent for bone diseases comprising di- or tripeptide derivative as active ingredient
  申请人：SUNTORY LIMITED

  公开号：EP0504938A2

  公开（公告）日：1992-09-23

  Use of a compound represented by the following general formula (I): wherein R¹ represents a straight or branched acyl group having 2 to 10 carbon atoms, a branched cyclic or bridged cyclic alkyloxycarbonyl group having 4 to 15 carbon atoms, a substituted or unsubstituted benzyloxycarbonyl group, a 2,2,2-trichloroethyloxycarbonyl group, a 2-(trimethylsilyl)-ethyloxycarbonyl group, a p-toluenesulfonyl group, an o-nitrophenylsulfenyl group, a diphenylphosphonothioyl group, a triphenylmethyl group, a 2-benzoyl-1-methylvinyl group or a 4-phenylbutanoyl group; R² represents a hydrogen atom or forms a phthaloyl group together with R¹; R³ represents an isobutyl group, an n-butyl group or an isopropyl group; R⁴ represents an n-butyl group or an isobutyl group; X represents a direct bond, a methionine residue, a leucine residue or a norleucine residue; and H at the C-terminal means that the carboxyl group is reduced in the form of the aldehyde; as an active ingredient for the preparation of a pharmaceutical composition useful in preventing or treating malignant hypercalcemia, bone Paget's disease or osteoporosis.

  使用以下通式 (I) 所代表的化合物： 其中 R¹ 代表具有 2 至 10 个碳原子的直链或支链酰基、具有 4 至 15 个碳原子的支链环状或桥接环状烷氧基羰基、取代或未取代的苄氧基羰基、2,2、2-三氯乙基氧羰基、2-（三甲基硅基）乙基氧羰基、对甲苯磺酰基、邻硝基苯磺酰基、二苯基膦酰基、三苯基甲基、2-苯甲酰基-1-甲基乙烯基或 4-苯基丁酰基； R² 代表氢原子或与 R¹ 共同形成邻苯二甲酰基； R³ 代表异丁基、正丁基或异丙基； R⁴ 代表一个正丁基或一个异丁基； X 代表直接键、蛋氨酸残基、亮氨酸残基或去甲亮氨酸残基；及 C 末端的 H 表示羧基以醛的形式被还原； 作为制备药物组合物的活性成分，可用于预防或治疗恶性高钙血症、骨髓鞘病或骨质疏松症。
• Human airway stem cells in lung epithelial engineering
  申请人：The General Hospital Corporation

  公开号：US10624992B2

  公开（公告）日：2020-04-21

  Methods of using human airway stem cells in lung epithelial engineering, optionally wherein the cells are contacted with a gamma secretase inhibitor, bioartificial airway organs produced thereby, and the use thereof, e.g., for transplantation. Also methods of treating a bio-artificial matrix with Tenascin-C and/or fibrillin 2.

  在肺上皮工程中使用人气道干细胞的方法，其中细胞可选择与γ分泌酶抑制剂接触，由此产生的生物人工气道器官及其用途，例如用于移植。还包括用Tenascin-C和/或纤维蛋白2处理生物人工基质的方法。
• Treating hearing loss
  申请人：Massachusetts Eye and Ear Infirmary

  公开号：US10898492B2

  公开（公告）日：2021-01-26

  This invention relates to methods for treating hearing loss associated with loss of cochlear hair cells, e.g., caused by noise exposure, using certain gamma secretase inhibitors, in post-neonatal animals, e.g., adolescents and adults.

  本发明涉及使用某些γ分泌酶抑制剂治疗与耳蜗毛细胞缺失有关的听力损失的方法，例如，在新生后动物（如青少年和成年人）中使用这些抑制剂治疗由噪声暴露引起的耳蜗毛细胞缺失。
• 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。