Fmoc-beta,beta-dimethyl-D-Cys(Trt)-OH

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 英文名称: Fmoc-beta,beta-dimethyl-D-Cys(Trt)-OH
• 英文别名: 2-(9H-fluoren-9-ylmethoxycarbonylamino)-3-methyl-3-tritylsulfanylbutanoic acid
• 化学式: C₃₉H₃₅NO₄S
• 分子量: 613.8
• InChiKey: XSGMGAINOILNJR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  8.6
• 重原子数：
  45
• 可旋转键数：
  11
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  101
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• [EN] FLUOROHYDROXYPROLINE DERIVATIVES USEFUL IN THE PREPARATION OF PROTEOLYSIS TARGETED CHIMERAS<br/>[FR] DÉRIVÉS DE FLUOROHYDROXYPROLINE UTILES DANS LA PRÉPARATION DE CHIMÈRES CIBLÉES PAR PROTÉOLYSE
  申请人：UNIV DUNDEE

  公开号：WO2018051107A1

  公开（公告）日：2018-03-22

  There is provided novel small molecule E3 ubiquitin ligase protein binding ligand compounds, and to their utility in PROteolysis Targeted Chimeras (PROTACs), as well as processes for their preparation thereof, and use in medicine. There is particularly provided novel small molecule E3 ubiquitin ligase protein binding inhibitorcompounds based on a fluorohydroxyproline scaffold, to their utility as ligands in synthesizing novel PROTACs, and to synthetic methods therefor.

  提供了新型小分子E3泛素连接酶蛋白结合配体化合物，以及它们在蛋白质降解靶向嵌合物（PROTACs）中的用途，以及其制备的过程，以及在医学中的用途。特别提供了基于氟羟脯氨酸支架的新型小分子E3泛素连接酶蛋白结合抑制剂化合物，以及它们作为配体在合成新型PROTACs中的用途，以及用于此目的的合成方法。
• [EN] SUBSTITUTED ADIPIC ACID AMIDES AND USES THEREOF<br/>[FR] AMIDES DE L'ACIDE ADIPIQUE SUBSTITUÉS ET LEURS UTILISATIONS
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2012125622A1

  公开（公告）日：2012-09-20

  The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein A is a five to eight membered monocyclic or a nine to twelve membered bicyclic heterocyclic ring, as further defined herein; Y is S, CH2, or CH; Z is CH or N; R7 and R9 are hydrogen or (C1-C6)alkyl; R2 is (C1 C6)alkoxy, OH, CN, (C1-C6)alkyl, halogen, or CF3; r and s are 0, 1, or 2; and R1 and R3 are as further defined herein. These compounds are agonists, partial agonists and/or modulators of the NPY4 receptor and may be used for the treatment and prophylaxis of obesity, food intake, and other diseases and conditions modulated by the NPY4 receptor.

  本发明提供了式（I）的化合物或其药学上可接受的盐，其中A是一个五至八元的单环或一个九至十二元的双环杂环环，如本文所进一步定义；Y是S、CH2或CH；Z是CH或N；R7和R9是氢或（C1-C6）烷基；R2是（C1-C6）烷氧基、羟基、氰基、（C1-C6）烷基、卤素或三氟甲基；r和s为0、1或2；R1和R3如本文所进一步定义。这些化合物是NPY4受体的激动剂、部分激动剂和/或调节剂，可用于治疗和预防肥胖、食物摄入和其他由NPY4受体调节的疾病和症状。
• Radioactively Labeled Substance
  申请人：Arano Yasushi

  公开号：US20120065367A1

  公开（公告）日：2012-03-15

  Provided are: a radiolabeled drug, which is efficiently accumulated in a target and has high in vivo stability; and diagnosis and treatment each using the radiolabeled drug. Specifically provided are: a radiolabeled drug showing increased accumulation in a target site, which comprises a complex composed of a ligand that is bound to a compound capable of binding to a target molecule and forms a polycoordinated complex with a metal (e.g., technetium or rhenium) and a radionuclide of the metal; the radiolabeled drug for diagnosis or treatment; a ligand for preparing the radiolabeled drug; a kit that comprises a drug comprising the ligand and a drug comprising a radionuclide of a metal, as separate package units; and a method of increasing accumulation of a radiolabeled drug in a target site, comprising using the above-mentioned radiolabeled drug.

  提供了一种放射标记药物，该药物在靶标中高效积累并具有高体内稳定性；以及使用该放射标记药物进行诊断和治疗。具体提供了以下内容：一种放射标记药物，在靶位点中显示增加积累，包括由与能够结合到靶分子的化合物结合的配体组成的复合物，并与金属（例如锝或铼）形成多配位复合物以及金属的放射性核素；用于诊断或治疗的放射标记药物；用于制备放射标记药物的配体；包括包含配体的药物和包含金属的放射性核素的药物作为单独的包装单元的试剂盒；以及一种增加放射标记药物在靶位点中积累的方法，包括使用上述放射标记药物。
• MACROCYCLIC INHIBITORS OF THE PD-1/PD-L1 AND CD80(B7-1)/PD-L1 PROTEIN/PROTEIN INTERACTIONS
  申请人：Bristol-Myers Squibb Company

  公开号：US20140294898A1

  公开（公告）日：2014-10-02

  The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.

  本公开提供了新型大环肽，其能够抑制PD-1/PD-L1和PD-L1/CD80蛋白质/蛋白质相互作用，因此可用于改善各种疾病，包括癌症和传染性疾病。
• SUBSTITUTED ADIPIC ACID AMIDES AND USES THEREOF
  申请人：Sun Chongqing

  公开号：US20130345123A1

  公开（公告）日：2013-12-26

  The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein A is a five to eight membered monocyclic or a nine to twelve membered bicyclic heterocyclic ring, as further defined herein; Y is S, CH 2 , or CH; Z is CH or N; R 7 and R 9 are hydrogen or (C 1 -C 6 )alkyl; R 2 is (C 1 -C 6 )alkoxy, OH, CN, (C 1 -C 6 )alkyl, halogen, or CF 3 ; r and s are 0, 1, or 2; and R 1 and R 3 are as further defined herein. These compounds are agonists, partial agonists and/or modulators of the NPY4 receptor and may be used for the treatment and prophylaxis of obesity, food intake, and other diseases and conditions modulated by the NPY4 receptor.

  本发明提供了式（I）的化合物或其药学上可接受的盐，其中A是进一步定义的五至八元杂环或九至十二元双环杂环；Y是S，CH2或CH；Z是CH或N；R7和R9是氢或（C1-C6）烷基；R2是（C1-C6）烷氧基，羟基，氰基，（C1-C6）烷基，卤素或CF3；r和s为0、1或2；而R1和R3的定义进一步如下。这些化合物是NPY4受体的激动剂、部分激动剂和/或调节剂，可用于治疗和预防肥胖、食物摄入和其他受NPY4受体调节的疾病和状况。