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    5′-cyclo-phosphonate modified nucleotides
    65.
    发明授权
    5′-cyclo-phosphonate modified nucleotides 有权

    公开(公告)号：US11078227B2

    公开(公告)日：2021-08-03

    申请号：US16207870

    申请日：2018-12-03

    Applicant: Arrowhead Pharmaceuticals, Inc.

    Inventor： Zhen Li ,  Tao Pei ,  Michael Lawler

    IPC: C07H19/10 ,  C07H21/02 ,  C07H19/16 ,  C07H19/06 ,  C07H19/207 ,  C12N15/113

    Abstract: Described are 5′-cyclo-phosphonate modified nucleotides, and oligonucleotides, such as interference (RNAi) agents, containing 5′-cyclo-phosphonate modified nucleotides. The RNAi agents having either double-stranded or single-stranded oligonucleotides described herein comprising 5′cyclo-phosphonate modified nucleotides are useful in modulating gene expression as well as therapeutic, diagnostic, target validation, and genomic discovery applications. The RNAi agents and single-stranded antisense oligonucleotides comprising 5′-cyclo-phosphonate modified nucleotides are useful in the treatment of diseases or conditions that respond to inhibition of gene expression or activity in a cell, tissue, or organism.

    Synthesis of nucleoside 5′-triphosphates and their derivatives
    66.
    发明授权
    Synthesis of nucleoside 5′-triphosphates and their derivatives 有权

    公开(公告)号：US11072624B2

    公开(公告)日：2021-07-27

    申请号：US13817820

    申请日：2011-08-19

    Applicant: Zhen Huang

    Inventor： Zhen Huang

    IPC: C07H1/04 ,  C07H19/10 ,  C07H19/20 ,  C07H21/00

    Abstract: Disclosed are nucleoside 5′-triphosphates modified at the α, (β, and/or γ phosphate to substitute one or more of the phosphate oxygen atoms with a borano, seleno, and/or thio group. Derivatives and pharmaceutically acceptable salts are also contemplated herein. Also disclosed are processes for preparing nucleoside 5′-triphosphates. Non-limiting, exemplary processes can include first reacting salicyl phosphorochloridite with a pyrophosphate reagent to provide P2, P3-dioxo-P1-(salicyl) cyclotriphosphite, and then reacting P2, P3-dioxo-P1-(salicyl) cyclotriphosphite with a nucleoside, followed by oxidation of the nucleoside-phosphite intermediate and hydrolysis to form the modified nucleoside 5′-triphosphate. Nucleoside 5′-triphosphates can be useful in nucleic acid replication, transcription, and translation. Processes disclosed herein are not limited to nucleoside 5′-triphosphates having a native base moiety, such as 9-adeninyl, 1-cytosinyl, 9-guaninyl, 1-thyminyl, or 1-uracilyl, and are also effective for the preparation of nucleoside 5′-triphosphates having a modified nucleobase or unnatural nucleobase.

    ANTIMICROBIAL COMPOUNDS, COMPOSITIONS, AND USES THEREOF
    68.
    发明申请
    ANTIMICROBIAL COMPOUNDS, COMPOSITIONS, AND USES THEREOF 有权

    公开(公告)号：US20210139522A1

    公开(公告)日：2021-05-13

    申请号：US16492861

    申请日：2018-03-12

    Applicant: Lakewood Amedex, Inc.

    Inventor： Steven A. Kates ,  Randolph B. Sleet ,  Steven Parkinson

    IPC: C07H19/10 ,  A61P31/04

    Abstract: Antimicrobial compounds and compositions of Formulas (I) to (III) and methods of use are disclosed. Another aspect of the present disclosure provides a pharmaceutical composition comprising a compound according to Formula (I) to (III), or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable carriers, excipients, or diluents. Another aspect of the present disclosure provides a method of treating a bacterial infection in a patient in need thereof, the method of comprising administering an effective amount of a compound according to Formula (I) to (III), or a pharmaceutically acceptable salt thereof, to the patient.

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