2H-1,4-苯并噻嗪-3(4H)-硫酮,5-氟-4-甲基- | 73449-06-6

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物 - 嘌呤核苷酸
• 中文名称: 2H-1,4-苯并噻嗪-3(4H)-硫酮,5-氟-4-甲基-
• 英文名称: 2'-Deoxy-2'-azidoadenosine triphosphate
• 英文别名: [[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-4-azido-3-hydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate
• CAS: 73449-06-6
• 化学式: C10H15N8O12P3
• 分子量: 532.19
• InChiKey: YEVIXVIVDZWHKS-QYYRPYCUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -4.2
• 重原子数：
  33
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  273
• 氢给体数：
  6
• 氢受体数：
  18

文献信息

• [EN] NUCLEIC ACID CONJUGATES AND USES THEREOF<br/>[FR] CONJUGUÉS DE TYPE ACIDE NUCLÉIQUE ET LEURS UTILISATIONS
  申请人：TRANSLATE BIO MA INC

  公开号：WO2018013525A1

  公开（公告）日：2018-01-18

  Provided herein are conjugates comprising targeting moieties such as sugars, folates and cell-penetrating peptides, which can be used for the improved delivery of agents (e.g., nucleic acids, such as oligonucleotides or mRNAs, or other agents) to cells. The invention provides conjugates and compounds comprising targeting moieties, methods for preparing the same, and intermediates useful in their preparation. In another aspect, the present invention provides formulations (e.g., pharmaceutical compositions) comprising the targetting moiety-containing conjugates and compounds. The present invention also provides methods for delivering agents (e.g., nucleic acids such as oligonucleotides or mRNAs) to a cell, methods for treating and/or preventing a disease or condition in a subject, and methods for modulating gene expression in a cell or a subject. Further, provided herein are kits comprising the conjugates, or formulations thereof; and kits for the preparation of conjugates described herein.

  本文提供了包含靶向基团的共轭物，如糖类、叶酸和穿膜肽，可用于改善药物（例如核酸，如寡核苷酸或mRNA，或其他药物）对细胞的传递。该发明提供了包含靶向基团的共轭物和化合物，以及其制备方法和制备过程中有用的中间体。另一方面，本发明提供了包含靶向基团的共轭物和化合物的配方（例如，药物组合物）。本发明还提供了将药物（例如核酸，如寡核苷酸或mRNA）传递至细胞的方法，用于治疗和/或预防受试者疾病或状况的方法，以及用于调节细胞或受试者基因表达的方法。此外，本文提供了包含这些共轭物或其配方的试剂盒；以及用于制备本文所述共轭物的试剂盒。
• [EN] NOVEL PHOSPHOROUS (V)-BASED REAGENTS, PROCESSES FOR THE PREPARATION THEREOF, AND THEIR USE IN MAKING STEREO-DEFINED ORGANOPHOSHOROUS (V) COMPOUNDS<br/>[FR] NOUVEAUX RÉACTIFS À BASE DE PHOSPHORE (V), LEURS PROCÉDÉS DE PRÉPARATION ET LEUR UTILISATION DANS LA FABRICATION DE COMPOSÉS ORGANOPHOSHOREUX (V) STÉRÉODÉFINIS
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2019200273A1

  公开（公告）日：2019-10-17

  The present invention relates to novel phosphorous (V) (P(V)) reagents, methods for preparing thereof, and methods for preparing organophosphorous (V) compounds by using the novel reagents.

  本发明涉及新型磷（V）（P(V)）试剂，其制备方法以及利用这种新型试剂制备有机磷（V）化合物的方法。
• Metabolic labeling and molecular enhancement of biological materials using bioorthogonal reactions
  申请人：The General Hospital Corporation

  公开号：US20170362266A1

  公开（公告）日：2017-12-21

  The present application provides methods of functionalizing an organ or tissue of a mammal by administering a nutrient (e.g., peracetylated N-azido galactosamine Ac4GalNAz) to the mammal or by culturing an organ or tissue in a bioreactor containing such nutrient. The present application also provides methods of selectively functionalizing extracellular matrix (ECM) of an organ or tissue of a mammal by administering a nutrient (e.g., peracetylated N-azido galactosamine Ac4GalNAz) to the mammal. In some aspects, the present application provides a decellularized scaffold of a mammalian organ or tissue comprising an extracellular matrix, wherein the extracellular matrix of the decellularized scaffold is functionalized with a chemical group that is reactive in a bioorthogonal chemical reaction, such as an azide chemical group. The present application also provides biological prosthetic mesh and mammalian organs and tissues for transplantation prepared according to the methods of the application.

  本申请提供了一种通过向哺乳动物投与营养物质（例如，乙酰化N-叠氮基半乳糖氨酸Ac4GalNAz）或在含有这种营养物质的生物反应器中培养器官或组织来功能化哺乳动物器官或组织的方法。本申请还提供了一种通过向哺乳动物投与营养物质（例如，乙酰化N-叠氮基半乳糖氨酸Ac4GalNAz）来选择性地功能化哺乳动物器官或组织的细胞外基质（ECM）的方法。在某些方面，本申请提供了哺乳动物器官或组织的脱细胞支架，其中脱细胞支架的细胞外基质被功能化为在生物正交化学反应中具有反应性的化学基团，例如叠氮基团。本申请还提供了根据本申请的方法制备的生物义肢网和哺乳动物器官和组织用于移植。
• AMINO ACID PHOSPHORAMIDATE PRONUCLEOTIDES OF 2'-CYANO, AZIDO AND AMINO NUCLEOSIDES FOR THE TREATMENT OF HCV
  申请人：Centre National De La Recherche Scientifique

  公开号：US20160113956A1

  公开（公告）日：2016-04-28

  Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 2′-cyano, azido or amino nucleosides according to Formula 1001 or 2001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form, or polymorphic form thereof, wherein Base, W, R 1 and R 2 are as described herein.

  本文提供了治疗黄病毒科感染，包括丙型肝炎（HCV）感染的化合物、组合物和方法。在某些实施例中，揭示了核苷衍生物的化合物和组合物，可以单独或与其他抗病毒药物联合使用。在某些实施例中，所述化合物是根据公式1001或2001的2'-氰基，偶氮基或氨基核苷衍生物，或其药学上可接受的盐，溶剂化合物，立体异构体，互变异构体或多态形式，其中Base，W，R1和R2如本文所述。
• INDUCTION OF OSTEOGENESIS BY DELIVERING BMP ENCODING RNA
  申请人：Ethris GmbH

  公开号：EP3542825A1

  公开（公告）日：2019-09-25

  The present invention relates to a pharmaceutical composition comprising a polyribonucleotide (RNA) with a sequence which encodes a bone morphogenetic protein (BMP) for use in (i) treating or preventing a bone disease, bone disorder or bone injury; and/or (ii) inducing or enhancing osteogenic differentiation, osteogenesis, ossification, bone regeneration and/or bone morphogenesis in a patient. The present invention also relates to the respective BMP encoding RNAs (BMP RNAs), in particular in its chemically modified form. The present invention also relates to complexes which comprise or are complexed with the BMP RNA, in particular to the respective transfection complexes like lipofection, magnetofection and magnetolipofection complexes. The present invention further relates to a carrier and carrier body to which the RNA or complex has been loaded and to a pharmaceutical composition comprising said carrier or carrier body. The present invention further relates to a matrix or scaffold for sustained mRNA delivery and its application in bone regeneration in vivo, ex vivo and in vitro.

  本发明涉及一种药物组合物，该组合物包含具有编码骨形态发生蛋白（BMP）序列的多核苷酸（RNA），用于(i)治疗或预防骨病、骨紊乱或骨损伤；和/或(ii)诱导或增强患者的成骨分化、成骨、骨化、骨再生和/或骨形态发生。本发明还涉及相应的 BMP 编码 RNA（BMP RNA），特别是其化学修饰形式。本发明还涉及由 BMP RNA 组成或与 BMP RNA 复合的复合物，特别是脂质感染、磁感染和磁脂质感染复合物等转染复合物。本发明还涉及一种载体和载体体，RNA 或复合物已被载入其中，本发明还涉及一种包含所述载体或载体体的药物组合物。本发明还涉及一种用于持续递送 mRNA 的基质或支架及其在体内、体外和体外骨再生中的应用。