公开(公告)号：US09458176B2

公开(公告)日：2016-10-04

申请号：US14190356

申请日：2014-02-26

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

Inventor： Mamoru Takaishi ,  Nobuhiro Sato ,  Tomoyuki Shibuguchi ,  Takafumi Motoki ,  Yoshinori Takahashi ,  Takeo Sasaki ,  Alan Braunton

IPC: A61K31/553 ,  C07D498/04

CPC classification number: C07D498/04

Abstract: A compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof works as an mGluR2 antagonist, and is applicable as a therapeutic agent for neurological disorders related to glutamate dysfunction and diseases involving the mGluR2, such as Alzheimer's disease: wherein R is a hydrogen atom, a C1-6 alkyl group or the like, R1 is a C1-6 alkyl group, a C1-6 alkoxy group or the like, R2 is a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or the like, R3 is a hydrogen atom, a C1-6 alkyl group or the like, and R4 is a C1-6 alkyl group or the like.

公开(公告)号：US20200308111A1

公开(公告)日：2020-10-01

申请号：US16897752

申请日：2020-06-10

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

Inventor： Yuta Suzuki ,  Yoshinori Takahashi

IPC: C07D207/16

Abstract: The present invention provides a cationic lipid which is able to be used for nucleic acid delivery to the cytoplasm. A cationic lipid according to the present invention is, for example, a compound represented by formula (1) or a pharmaceutically acceptable salt thereof, wherein L1 and L2 independently represent an alkylene group having 3 to 10 carbon atoms; R1 and R2 independently represent an alkyl group having 4 to 24 carbon atoms or an alkenyl group having 4 to 24 carbon atoms; R3 represents an alkyl group having 1 to 3 carbon atoms; and X1 represents a single bond or CO—O—.

公开(公告)号：US20140243316A1

公开(公告)日：2014-08-28

申请号：US14190356

申请日：2014-02-26

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

Inventor： Mamoru Takaishi ,  Nobuhiro Sato ,  Tomoyuki Shibuguchi ,  Takafumi Motoki ,  Yoshinori Takahashi ,  Takeo Sasaki ,  Alan Braunton

IPC: C07D498/04

CPC classification number: C07D498/04

Abstract: A compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof works as an mGluR2 antagonist, and is applicable as a therapeutic agent for neurological disorders related to glutamate dysfunction and diseases involving the mGluR2, such as Alzheimer's disease: wherein R is a hydrogen atom, a C1-6 alkyl group or the like, R1 is a C1-6 alkyl group, a C1-6 alkoxy group or the like, R2 is a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or the like, R3 is a hydrogen atom, a C1-6 alkyl group or the like, and R4 is a C1-6 alkyl group or the like.

Abstract translation: 由下式（I）表示的化合物或其药学上可接受的盐作为mGluR2拮抗剂起作用，可用作与谷氨酸功能障碍相关的神经障碍和涉及mGluR2的疾病如阿尔茨海默氏病的治疗剂：其中R为 氢原子，C 1-6烷基等，R 1为C 1-6烷基，C 1-6烷氧基等，R 2为卤素原子，C 1-6烷基，C 1-6 烷氧基等，R3是氢原子，C1-6烷基等，R4是C1-6烷基等。

公开(公告)号：US20200216488A1

公开(公告)日：2020-07-09

申请号：US16616693

申请日：2018-06-14

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

Inventor： Yoshinori Takahashi ,  Yuta Suzuki

IPC: C07H21/02 ,  C07H21/04

Abstract: The present invention provides a modified nucleic acid monomer compound having a specific backbone such as 2-ethylglycerol or methoxymethyl-1,3-propanediol backbone instead of a ribose or deoxyribose backbone of a nucleoside, and an oligonucleic acid analogue containing the monomer compound as at least one of building blocks. The oligonucleic acid analogue containing the nucleic acid monomer compound of the present invention allows provision of an oligonucleic acid analogue having excellent biological stability and/or target gene silencing activity.

公开(公告)号：US10526603B1

公开(公告)日：2020-01-07

申请号：US16354916

申请日：2019-03-15

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

Inventor： Yuta Suzuki ,  Sotaro Motoi ,  Yoshinori Takahashi ,  Kazuhiro Tahara

IPC: C12N15/113 ,  A61P7/00

Abstract: Provided is a novel double-stranded ribonucleic acid for suppressing expression of complement C5. A double-stranded ribonucleic acid comprising a combination of sense strand and antisense strand, wherein the combination of the sense strand and antisense strand are selected from the group consisting of combinations: SEQ ID NO: 13/14, SEQ ID NO: 159/160, SEQ ID NO: 115/116, SEQ ID NO: 117/118, SEQ ID NO: 119/120, SEQ ID NO: 121/122, SEQ ID NO: 123/124, SEQ ID NO: 125/126, SEQ ID NO: 127/128, SEQ ID NO: 129/130, SEQ ID NO: 131/132, SEQ ID NO: 133/134, SEQ ID NO: 137/138, SEQ ID NO: 139/140, SEQ ID NO: 141/142, SEQ ID NO: 143/144, SEQ ID NO: 145/146, SEQ ID NO: 147/148, SEQ ID NO: 149/150, SEQ ID NO: 151/152, and SEQ ID NO: 153/154.

公开(公告)号：US20190218180A1

公开(公告)日：2019-07-18

申请号：US16307202

申请日：2017-06-22

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

Inventor： Yuta Suzuki ,  Yoshinori Takahashi

IPC: C07D211/62 ,  C07D209/52 ,  C07D241/04

CPC classification number: C07D211/62 ,  A61K31/7105 ,  A61K47/10 ,  A61K47/18 ,  A61K47/22 ,  A61K47/28 ,  A61K47/44 ,  A61P43/00 ,  C07D209/52 ,  C07D211/36 ,  C07D241/04

Abstract: The present invention provides a cationic lipid which is able to be used for nucleic acid delivery to the cytoplasm. A cationic lipid according to the present invention is, for example, a compound represented by formula (1a) or a pharmaceutically acceptable salt thereof. (In formula (1a), each of L1 and L2 independently represent an alkylene group having 3-10 carbon atoms; each of R1 and R2 independently represent an alkyl group having 4-22 carbon atoms or an alkenyl group having 4-22 carbon atoms; X1 represents a single bond or —CO—O—; and ring P represents one of formulae (P-1) to (P-5).)(In formulae (P-1) to (P-5), R3 represents an alkyl group having 1-3 carbon atoms.)

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：US11208429B2

公开(公告)日：2021-12-28

申请号：US16616693

申请日：2018-06-14

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

Inventor： Yoshinori Takahashi ,  Yuta Suzuki

IPC: C07H21/02 ,  C07H21/04 ,  C07D239/54 ,  C07D239/47 ,  C07D473/34 ,  C07D473/18

Abstract: The present invention provides a modified nucleic acid monomer compound having a specific backbone such as 2-ethylglycerol or methoxymethyl-1,3-propanediol backbone instead of a ribose or deoxyribose backbone of a nucleoside, and an oligonucleic acid analogue containing the monomer compound as at least one of building blocks. The oligonucleic acid analogue containing the nucleic acid monomer compound of the present invention allows provision of an oligonucleic acid analogue having excellent biological stability and/or target gene silencing activity.

公开(公告)号：US10947193B2

公开(公告)日：2021-03-16

申请号：US16897752

申请日：2020-06-10

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

Inventor： Yuta Suzuki ,  Yoshinori Takahashi

IPC: C07D207/16

Abstract: The present invention provides a cationic lipid which is able to be used for nucleic acid delivery to the cytoplasm. A cationic lipid according to the present invention is, for example, a compound represented by formula (1) or a pharmaceutically acceptable salt thereof, wherein L1 and L2 independently represent an alkylene group having 3 to 10 carbon atoms; R1 and R2 independently represent an alkyl group having 4 to 24 carbon atoms or an alkenyl group having 4 to 24 carbon atoms; R3 represents an alkyl group having 1 to 3 carbon atoms; and X1 represents a single bond or CO—O—.