公开(公告)号：EP4194459A1

公开(公告)日：2023-06-14

申请号：EP22206730.8

申请日：2017-06-19

申请人： Shionogi & Co., Ltd

发明人： SHIBAHARA, Setsuya ,  FUKUI, Nobuaki ,  MAKI, Toshikatsu ,  ANAN, Kosuke

IPC分类号： C07D498/14 ,  A61P31/16 ,  A61K31/5383

摘要： The present invention provides a process for preparing a compound of the formula (II):

wherein R 2 is unsubstituted alkyl,
characterized by reacting a compound of the formula (I):

wherein R 1 is hydrogen or a protecting group other than unsubstituted alkyl,
with a compound of the formula: R 2 -OH, wherein R 2 is as defined above, in the presence of a sodium salt and/or a magnesium salt.

公开(公告)号：EP3978024A1

公开(公告)日：2022-04-06

申请号：EP20818583.5

申请日：2020-06-02

申请人： Shionogi & Co., Ltd

发明人： TANINO, Tetsuya ,  SEKIGUCHI, Mitsuaki ,  OCHI, Shunsuke ,  FUKUI, Nobuaki

IPC分类号： A61K47/54 ,  C12N15/11 ,  C07F9/572 ,  A61K31/713

摘要： Provided are production methods capable of controlling quality of a bifurcated lipid-linked oligonucleotide, and intermediates which is useful for the production method, has good stability, and is easy to manage and analyze. Specifically, it is a method for producing a bifurcated lipid-linked oligonucleotide including a step of reacting a compound of formula (II):

wherein Pro 1 to Pro 4 are each independently a protecting group;
Pro 1 and Pro 2 or Pro 3 and Pro 4 may be taken together to form a protecting group;
m, n and p are each independently an integer of 0 to 5; and
Y is a group of a formula: -P(OC 2 H 4 CN)(N(i-Pr) 2 ), or the like, with an oligonucleotide.

公开(公告)号：EP3473629A1

公开(公告)日：2019-04-24

申请号：EP17815337.5

申请日：2017-06-19

申请人： Shionogi & Co., Ltd.

发明人： SHIBAHARA, Setsuya ,  FUKUI, Nobuaki ,  MAKI, Toshikatsu ,  ANAN, Kosuke

IPC分类号： C07D498/14 ,  A61K31/5383 ,  C07B61/00

摘要： The present invention provides a process for preparing a compound of the formula (II):

wherein R 2 is unsubstituted alkyl,
characterized by reacting a compound of the formula (I):

wherein R 1 is hydrogen or a protecting group other than unsubstituted alkyl,
with a compound of the formula: R 2 -OH, wherein R 2 is as defined above, in the presence of a sodium salt and/or a magnesium salt.