Process for Preparing Imetelstat
    33.
    发明申请

    公开(公告)号:US20230070069A1

    公开(公告)日:2023-03-09

    申请号:US17718990

    申请日:2022-04-12

    申请人: Geron Corporation

    IPC分类号: C07H1/00

    摘要: The present invention relates to a process for preparing the telomerase inhibitor imetelstat using a 3 steps per cycle solid-phase support bound process comprising the steps of deprotection of the 3′-amino group of the support-bound oligonucleotide, coupling with a 5′-phosphoramidite, and sulfurization with an acyl disulfide, characterized by the absence of an additional capping step in each cycle that is used to prevent unreacted 3′-amino oligonucleotide groups from reacting during subsequent cycles. Imetelstat has formula below.

    Oligonucleotide production method
    38.
    发明授权

    公开(公告)号:US11548910B2

    公开(公告)日:2023-01-10

    申请号:US15776709

    申请日:2016-11-17

    发明人: Yudai Sugawara

    摘要: The invention provides a novel method for producing an oligonucleotide using a nucleoside or oligonucleotide that is easy to isolate and has high storage stability. The oligonucleotide production method includes a step of subjecting a nucleoside or oligonucleotide having a pseudo solid phase-protecting group in at least one location selected from the group consisting of 2′-position, 3′-position, 5′-position and a nucleobase moiety and having a 5′-hydroxyl group or a 3′-hydroxyl group, to H-phosphonation to convert the 5′-hydroxyl group or the 3′-hydroxyl group into an H-phosphonated form.

    Rapid unylinker cleavage
    40.
    发明授权

    公开(公告)号:US11542294B2

    公开(公告)日:2023-01-03

    申请号:US16483148

    申请日:2018-03-22

    IPC分类号: C07H21/00 C07H1/00 C07H1/06

    摘要: Methods for cleaving oligonucleotides from a solid support are described as are methods for synthesizing an oligonucleotide on a solid support and subsequently cleaving the oligonucleotide from the solid support. In the methods, the 3′ nucleoside of the oligonucleotide attached to the solid support is a LNA nucleoside. The method entail treating the bound oligonucleotide with a concentrated ammonium hydroxide solution for about 30 minutes to about 6 hours.