公开(公告)号：US10730904B2

公开(公告)日：2020-08-04

申请号：US16240677

申请日：2019-01-04

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Mitsuru Nonogawa ,  Toshiaki Nagata ,  Hideki Saito ,  Tsuneo Yasuma

IPC: C07H19/207 ,  C07H19/06 ,  C07H19/16 ,  C07H19/067 ,  C07H19/073 ,  C07H21/04 ,  C07H21/00 ,  C07H1/00 ,  C07H19/167

Abstract: In this method, an oligonucleotide represented by formula (II) [wherein Y1, Q, Base, r and r′ are each as defined in claim 1] is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R1, Y, Base, Z, Ar, R2, R3 and n are each as defined in claim 1]. The novel nucleoside monomer compound is a nucleoside, the base moiety of which is substituted with an aromatic-hydrocarbon-ring-carbonyl or -thiocarbonyl group having at least one hydrophobic group. The method can dispense with column-chromatographic purification in every reaction, and enables base elongation not only in the 3′-direction but also in the 5′-direction, thus attaining efficient liquid-phase mass synthesis of an oligonucleotide.

公开(公告)号：US10214555B2

公开(公告)日：2019-02-26

申请号：US14442601

申请日：2013-11-13

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Mitsuru Nonogawa ,  Toshiaki Nagata ,  Hideki Saito ,  Tsuneo Yasuma

IPC: C07H1/00 ,  C07H21/00 ,  C07H21/04 ,  C07H19/06 ,  C07H19/16 ,  C07H19/067 ,  C07H19/073 ,  C07H19/167 ,  C07H19/207

Abstract: In this method, an oligonucleotide is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R1, Y, Base, Z, Ar, R2, R3 and n are each as defined in Claim 1]. The novel nucleoside monomer compound is a nucleoside, the base moiety of which is substituted with an aromatic-hydrocarbon-ring-carbonyl or -thiocarbonyl group having at least one hydrophobic group. The method cars dispense with column-chromatographic purification in every reaction, and enables base elongation not only in the 3′-direction but also in the 5′-direction, thus attaining efficient liquid-phase mass synthesis of an oligonucleotide.