公开(公告)号：US20220195437A1

公开(公告)日：2022-06-23

申请号：US17643807

申请日：2021-12-10

Applicant: Eisai R&D Management Co., Ltd.

Inventor： Dae-Shik KIM ,  Hyeong-Wook CHOI ,  Francis G. FANG ,  Yoshinori TAKAHASHI ,  Kenji KIKUTA ,  Hikaru YOSHIMURA ,  Wataru ITANO ,  Toshiki KUROKAWA ,  Ryo DAIRIKI ,  Zhi ZHOU ,  Mingde SHAN

IPC: C12N15/113 ,  A61K31/712 ,  A61P25/28

Abstract: Antisense oligonucleotides are provided. These antisense oligonucleotides are useful in the preparation of gapmers for inhibition of Tau mRNA transcription. Inhibition of Tau mRNA transcription may result in decrease of amounts of Tau protein in a subject, allowing treatment of diseases and disorders related to expression of Tau, including Alzheimer's disease and primary tauopathies.

公开(公告)号：US20210171555A1

公开(公告)日：2021-06-10

申请号：US17082070

申请日：2020-10-28

Applicant: Eisai R&D Management Co., Ltd.

Inventor： Atsushi ENDO ,  Robert T. YU ,  Francis FANG ,  Hyeong Wook CHOI ,  Mingde SHAN

IPC: C07F9/6561 ,  C07H21/00 ,  A61K31/7088 ,  C07F9/6558

Abstract: We provide diastereomerically pure or substantially diastereomerically pure activated phosphoramidochloridate morpholino nucleosides, methods of their preparation, and methods of their use in stereospecific coupling for stereospecific synthesis of diastereomerically pure phosphorodiamidate morpholino oligomers (PMOs).

公开(公告)号：US20240060068A1

公开(公告)日：2024-02-22

申请号：US18256428

申请日：2021-12-10

Applicant: Francis G. FANG ,  Dai-Shik KIM ,  Hyeong Wook CHOI ,  Yoshinori TAKAHASHI ,  Kenji KIKUTA ,  Hikaru KAWASHIMA ,  Toshiki KUROKAWA ,  Tamaki HOSHIKAWA ,  Mingde SHAN ,  John WANG ,  Eisai R&D Management Co., Ltd.

Inventor： Francis G. Fang ,  Dae-Shik Kim ,  Hyeong Wook Choi ,  Yoshinori Takahashi ,  Kenji Kikuta ,  Hikaru Kawashima ,  Wataru Itano ,  Toshiki Kurokawa ,  Tamaki Hoshikawa ,  Mingde SHAN ,  John Wang

IPC: C12N15/113 ,  C07H21/04

CPC classification number: C12N15/113 ,  C07H21/04 ,  C12N2310/341 ,  C12N2310/3233 ,  C12N2310/315

Abstract: Gapmers or pharmaceutically acceptable salt of the gapmers and methods of making the gapmers are provided. The gapmers include a gap region that contains deoxyribonucleosides linked to each other by phosphorothioate bonds, a 5′ wing region positioned at the 5′ end of the gap region that contains morpholino monomers linked to each other by phosphorodiamidate bonds, and a 3′ wing region positioned at the 3′ end of the gap region that contains morpholino monomers linked to each other by phosphorodiamidate bonds. Antisense oligonucleotides are also provided. These antisense oligonucleotides are useful in the preparation of gapmers for inhibition of Tau mRNA transcription.