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：US10081598B2

公开(公告)日：2018-09-25

申请号：US15533576

申请日：2015-12-24

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

Inventor： Yuta Suzuki ,  Kenji Hyodo ,  Yohei Tanaka

IPC: A61K31/713 ,  C07D211/62 ,  C12N15/113 ,  C07C229/06 ,  A61K47/10 ,  A61K47/22 ,  A61K47/28 ,  C07C229/12 ,  C12N15/09

CPC classification number: C07D211/62 ,  A61K31/713 ,  A61K47/10 ,  A61K47/22 ,  A61K47/28 ,  C07C229/06 ,  C07C229/12 ,  C12N15/09 ,  C12N15/113 ,  C12N15/1137 ,  C12N2310/14

Abstract: The present invention provides a cationic lipid which can be utilized for nucleic acid delivery into the cytoplasm. The cationic lipid of the present invention is, for example, a compound represented by the following Formula (1) or a pharmaceutically acceptable salt thereof.

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—.

公开(公告)号：US20160326116A1

公开(公告)日：2016-11-10

申请号：US15109512

申请日：2015-01-07

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

Inventor： Yuta Suzuki ,  Kenji Hyodo ,  Yohei Tanaka

IPC: C07D211/62 ,  A61K48/00 ,  C12N15/113 ,  C07D207/16 ,  C07D205/04

CPC classification number: C07D211/62 ,  A61K9/5123 ,  A61K47/22 ,  A61K48/0033 ,  C07D205/04 ,  C07D207/16 ,  C12N15/111 ,  C12N15/1137 ,  C12N2310/14 ,  C12N2320/32

Abstract: The present invention provides a cationic lipid which can be used for nucleic acid delivery to a cytoplasm and which is possible to solve the problem of physical stability of a lipid complex. This cationic lipid is a compound represented by the general formula (3) or a pharmaceutically acceptable salt thereof: wherein, L is an alkyl having 7-12 carbon atoms or an alkenyl having 7-12 carbon atoms, R is an alkyl having 1-2 carbon atoms, and n1 and n2 are independently an integer of 1-3.

Abstract translation: 其中，L是具有7-12个碳原子的烷基或具有7-12个碳原子的烯基，R是具有1-2个碳原子的烷基，n1和n2独立地是1-3的整数。