公开(公告)号：US20160168176A1

公开(公告)日：2016-06-16

申请号：US14904860

申请日：2014-07-18

Applicant: EISAI R&D MANAGEMENT CO., LTD.

Inventor： Keigo Tanaka ,  Takashi Fukuyama ,  Norio Murai ,  Wataru Itano ,  Shinsuke Hirota ,  Daisuke Iida ,  Hiroshi Azuma

IPC: C07F7/22 ,  C07F5/02 ,  C07D495/04 ,  C07D513/04 ,  C07D491/048 ,  C07D493/04

CPC classification number: C07F7/2208 ,  C07D491/048 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04 ,  C07F5/02 ,  C07F5/025 ,  C07F5/027

Abstract: A compound represented by the formula (I) or a salt thereof: wherein a ring Z is a 5 to 6-membered heteroaromatic ring having one or two heteroatoms in the ring; X1 is a hydrogen atom, a hydroxy group, a hydroxy C1-6 alkyl group, —B(OH)2, a boronate ester group, a cyclic boronate ester group, a boranyl group, a cyclic boranyl group, —BF3Mn1, —Sn(R12)(R13)(R14), a leaving group, a carboxy group, a formyl group, or —NR16R17; and X2 is a hydrogen atom or —CO2R18.

Abstract translation: 由式（I）表示的化合物或其盐：其中环Z是环中具有一个或两个杂原子的5至6元杂芳环; X1是氢原子，羟基，羟基C1-6烷基，-B（OH）2，硼酸酯基，环状硼酸酯基，硼烷基，环状硼烷基，-BF3Mn1，-Sn （R 12）（R 13）（R 14），离去基团，羧基，甲酰基或-NR 16 R 17; X 2为氢原子或-CO 2 R 18。

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.

公开(公告)号：US09975910B2

公开(公告)日：2018-05-22

申请号：US14904860

申请日：2014-07-18

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

Inventor： Keigo Tanaka ,  Takashi Fukuyama ,  Norio Murai ,  Wataru Itano ,  Shinsuke Hirota ,  Daisuke Iida ,  Hiroshi Azuma

IPC: C07D491/048 ,  C07F7/22 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04 ,  C07F5/02

CPC classification number: C07F7/2208 ,  C07D491/048 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04 ,  C07F5/02 ,  C07F5/025 ,  C07F5/027

Abstract: A compound represented by the formula (I) or a salt thereof: wherein a ring Z is a 5 to 6-membered heteroaromatic ring having one or two heteroatoms in the ring; X1 is a hydrogen atom, a hydroxy group, a hydroxy C1-6 alkyl group, —B(OH)2, a boronate ester group, a cyclic boronate ester group, a boranyl group, a cyclic boranyl group, —BF3Mn1, —Sn(R12)(R13)(R14), a leaving group, a carboxy group, a formyl group, or —NR16R17; and X2 is a hydrogen atom or —CO2R18.