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    AMORPHOUS SOLID SUCCINYLATED 3-(FATTY ACID AMIDO)-2-HYDROXY-1-(PROTECTED HYDROXY)-PROPANE SALTS AND METHODS OF MAKING THE SAME
    4.
    发明申请
    AMORPHOUS SOLID SUCCINYLATED 3-(FATTY ACID AMIDO)-2-HYDROXY-1-(PROTECTED HYDROXY)-PROPANE SALTS AND METHODS OF MAKING THE SAME 有权

    公开(公告)号：US20210147344A1

    公开(公告)日：2021-05-20

    申请号：US17079129

    申请日：2020-10-23

    申请人： Geron Corporation

    发明人： Jennifer E. Albaneze-Walker

    IPC分类号： C07C235/00 ,  C07C231/12

    摘要： Aspects of the disclosure includes methods for preparing an amorphous solid composition of a fatty acid metal salt. In practicing the subject methods according to certain embodiments, a succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane organic salt is contacted with a metal base to produce a succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane metal salt; and the succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane metal salt is precipitated in a solvent to produce an amorphous solid succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane metal salt composition. An amorphous solid succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane lithium salt is also provided.

    Guanine analogs as telomerase substrates and telomere length affectors
    6.
    发明授权
    Guanine analogs as telomerase substrates and telomere length affectors 有权
    鸟嘌呤类似物作为端粒酶底物和端粒长度亲和体

    公开(公告)号：US09593137B2

    公开(公告)日：2017-03-14

    申请号：US14366218

    申请日：2012-12-21

    申请人： Geron Corporation

    发明人： Sergei M. Gryaznov ,  Ronald A. Pruzan ,  Krisztina Pongracz

    IPC分类号： C07D473/18 ,  C07F9/6561

    CPC分类号： C07F9/65616 ,  C07D473/18

    摘要： This invention relates to compounds useful for inhibiting telomere elongation. More specifically, the invention provides nucleotide analogs that are incorporated into telomeres by telomerase thereby inhibiting elongation of telomeres. The compounds are useful in treating cancer and other cell proliferative diseases.

    摘要翻译： 本发明涉及可用于抑制端粒伸长的化合物。 更具体地，本发明提供通过端粒酶掺入端粒中从而抑制端粒伸长的核苷酸类似物。 该化合物可用于治疗癌症和其他细胞增殖性疾病。

    Oligonucleotide Compositions and Methods of Making the Same
    8.
    发明申请
    Oligonucleotide Compositions and Methods of Making the Same 有权
    寡核苷酸组合物及其制备方法

    公开(公告)号：US20150337314A1

    公开(公告)日：2015-11-26

    申请号：US14699902

    申请日：2015-04-29

    申请人： GERON CORPORATION

    发明人： Premchandran H. Ramiya

    IPC分类号： C12N15/113 ,  C07H21/00

    CPC分类号： C07H21/00 ,  C12N15/113 ,  C12N15/1137 ,  C12N2310/113 ,  C12N2310/3145 ,  C12N2310/315 ,  C12N2310/3515 ,  C12P19/34 ,  C12Y207/07049

    摘要： The present disclosure provides a solid phase method of making oligonucleotides via sequential coupling cycles including at least one coupling of a dinucleotide dimer subunit to a free 3′-terminal group of a growing chain. The oligonucleotides include at least two nucleoside subunits joined by a N3′→P5′ phosphoramidate linkage. The method may include the steps of (a) deprotecting the protected 3′ amino group of a terminal nucleoside attached to a solid phase support, said deprotecting forming a free 3′ amino group; (b) contacting the free 3′ amino group with a 3′-protected amino-dinucleotide-5′-phosphoramidite dimer in the presence of a nucleophilic catalyst to form an internucleoside N3′→P5′ phosphoramidite linkage; and (c) oxidizing (e.g., sulfurizing) the linkage. The compositions produced by the subject methods may include a reduced amount of one or more (N−x) oligonucleotide products. Also provided are pharmaceutical compositions including the subject oligonucleotide compositions.

    摘要翻译： 本公开提供了通过连续偶联循环制备寡核苷酸的固相方法，其包括二核苷酸二聚体亚基与生长链的游离3'-端基的至少一个偶联。 寡核苷酸包括通过N 3'→P 5'氨基磷酸酯键连接的至少两个核苷亚基。 该方法可以包括以下步骤：（a）将连接于固相载体上的末端核苷的被保护的3'氨基脱保护，所述去保护形成游离的3'氨基; （b）在亲核催化剂存在下使游离的3'氨基与3'-保护的氨基二核苷酸-5'-亚磷酰胺二聚体接触以形成核苷间N 3'→P 5'亚磷酰胺连接; 和（c）氧化（例如硫化）连接。 通过本发明方法制备的组合物可以包括减少量的一种或多种（N-x）寡核苷酸产物。 还提供了包含本发明的寡核苷酸组合物的药物组合物。