(2S)-2-[[4-[(2-amino-4-oxo-3H-pteridin-6-yl)methylamino]benzoyl]amino]-6-methyl-5-oxoheptanoic acid

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (2S)-2-[[4-[(2-amino-4-oxo-3H-pteridin-6-yl)methylamino]benzoyl]amino]-6-methyl-5-oxoheptanoic acid
• 化学式: C₂₂H₂₅N₇O₅
• 分子量: 467.5
• InChiKey: XENWHSDXTUGFFE-HNNXBMFYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  34
• 可旋转键数：
  10
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  189
• 氢给体数：
  5
• 氢受体数：
  8

文献信息

• BIOACTIVE CONJUGATE, PREPARATION METHOD THEREFOR AND USE THEREOF
  申请人：SICHUAN KELUN-BIOTECH BIOPHARMACEUTICAL CO., LTD.

  公开号：US20200347075A1

  公开（公告）日：2020-11-05

  The disclosure relates to a bioactive molecule conjugate, preparation methods and use thereof, particularly relates to a novel bioactive molecule conjugate obtained by improving coupling of the drug and the targeting moiety in an ADC or SMDC, as well as its preparation method and use in the manufacture of a medicament for the treatment of a disease associated with an abnormal cell activity.

  该披露涉及一种生物活性分子结合物，其制备方法及用途，特别涉及通过改善药物与靶向基团在ADC或SMDC中的偶联而获得的一种新型生物活性分子结合物，以及其制备方法和用于制造用于治疗与异常细胞活性相关的疾病的药物。
• POLYNUCLEOTIDE CONSTRUCTS HAVING DISULFIDE GROUPS
  申请人：BRADSHAW Curt W.

  公开号：US20160257961A1

  公开（公告）日：2016-09-08

  The invention features polynucleotide constructs containing one or more components (i) containing a disulfide linkage, where each of the one or more components is attached to an internucleotide bridging group or a terminal group of the polynucleotide construct, and each of the one or more components (i) contains one or more bulky groups proximal to the disulfide group. The invention also features polynucleotide constructs containing one or more components (i) containing a disulfide linkage, where each of the one or more components (i) is attached to an internucleotide bridging group or a terminal group of the polynucleotide construct, and each of the one or more components (i) contains at least 4 atoms in a chain between the disulfide linkage and the phosphorus atom of the internucleotide bridging group or the terminal group; and where the chain does not contain a phosphate, an amide, an ester, or an alkenylene. The invention also features methods of delivering a polynucleotide to a cell using the polynucleotide constructs of the invention.

  本发明涉及一种聚核苷酸构建物，其包含一个或多个组分（i），该组分包含一个二硫键，其中每个组分中的一个或多个组分连接到聚核苷酸构建物的核苷酸桥接基团或末端基团上，并且每个组分（i）在二硫键附近包含一个或多个笨重基团。本发明还涉及一种聚核苷酸构建物，其包含一个或多个组分（i），该组分包含一个二硫键，其中每个组分中的一个或多个组分连接到聚核苷酸构建物的核苷酸桥接基团或末端基团上，并且每个组分（i）在二硫键和核苷酸桥接基团或末端基团的磷原子之间的链中至少含有4个原子；并且链中不含有磷酸盐、酰胺、酯或烯基烃。本发明还涉及使用本发明的聚核苷酸构建物向细胞传递聚核苷酸的方法。
• Immunomodulating polynucleotides, antibody conjugates thereof, and methods of their use
  申请人：SOLSTICE BIOLOGICS, LTD.

  公开号：US11203611B2

  公开（公告）日：2021-12-21

  Immunomodulating polynucleotides are disclosed. The immunomodulating polynucleotides may contain 5-modified uridine, 5-modified cytidine, a total of from 6 to 16 nucleotides, and/or one or more abasic spacers and/or internucleoside phosphotriesters. Also disclosed are conjugates containing a targeting moiety and one or more immunomodulating polynucleotides. The immunomodulating polynucleotides and conjugates may further contain one or more auxiliary moieties. Also disclosed are compositions containing the immunomodulating polynucleotides or the conjugates containing one or more stereochemically enriched internucleoside phosphorothioates. Further disclosed are pharmaceutical compositions containing the immunomodulating polynucleotides or the conjugates and methods of their use.

  本发明公开了一种免疫调节聚核苷酸。所述免疫调节聚核苷酸可包含5-修饰的尿苷、5-修饰的胞苷、总计6至16个核苷酸、以及/或一个或多个无嘌呤间隔基团和/或核苷间磷酸三酯。本发明还公开了包含靶向基团和一个或多个免疫调节聚核苷酸的联体。所述免疫调节聚核苷酸和联体还可进一步包含一个或多个辅助基团。本发明还公开了包含免疫调节聚核苷酸或包含一个或多个立体化学富集的核苷间硫代磷酸酯的联体的组合物。此外，本发明还公开了包含免疫调节聚核苷酸或联体的药物组合物以及它们的用途方法。
• COMPOUNDS AND COMPOSITIONS FOR USE IN THE TREATMENT AND PREVENTION OF CANCER AND PRECANCEROUS CONDITIONS, INFLAMMATION-RELATED DISORDERS, PAIN AND FEVER
  申请人：Medicon Pharmaceuticals, Inc.

  公开号：US20140121185A1

  公开（公告）日：2014-05-01

  Novel compounds and pharmaceutical compositions thereof for the treatment and/or prevention of cancer and precancerous conditions, inflammation-related disorders, pain and fever.
• POLYNUCLEOTIDE CONSTRUCTS HAVING BIOREVERSIBLE AND NON-BIOREVERSIBLE GROUPS
  申请人：BRADSHAW Curt W.

  公开号：US20170114341A1

  公开（公告）日：2017-04-27

  The invention features a hybridized polynucleotide construct containing a passenger strand, a guide strand loadable into a RISC complex, and (i) a 3′-terminal or an internucleotide non-bioreversible group in the guide strand; or (ii) a 5′-terminal, a 3′-terminal, or an internucleotide non-bioreversible group in the passenger strand, and a 5′-terminal, a 3′-terminal, or an internucleotide disulfide bioreversible group in the guide strand or the passenger strand. The invention also features methods of delivering a polynucleotide to a cell using the hybridized polynucleotide construct. The invention further features methods of reducing the expression of a polypeptide in a cell using the hybridized polynucleotide construct.