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：US10786511B2

公开(公告)日：2020-09-29

申请号：US15527375

申请日：2015-11-17

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

Inventor： Heike Keilhack ,  Brett Truitt ,  Yuta Suzuki ,  Tsukasa Murase ,  Futoshi Shikata

IPC: A61K31/5377 ,  A61K9/00 ,  A61K9/20 ,  A61K33/06 ,  A61K9/28

Abstract: The present invention relates to pharmaceutical compositions comprising inhibitor(s) of human histone methyltransferase EZH2, and methods of cancer therapy using the EZH2 inhibitor(s).

公开(公告)号：US20180105493A1

公开(公告)日：2018-04-19

申请号：US15841652

申请日：2017-12-14

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

Inventor： Yuta Suzuki ,  Kenji Hyodo ,  Yohei Tanaka

IPC: C07D211/62 ,  C12N15/113 ,  A61K48/00 ,  A61K47/22 ,  C07D207/16 ,  C07D205/04 ,  A61K9/51 ,  C12N15/11

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.

公开(公告)号：US09873669B2

公开(公告)日：2018-01-23

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 ,  A61K47/22 ,  A61K9/51 ,  C07D205/04 ,  C07D207/16 ,  C12N15/11 ,  A61K48/00 ,  C12N15/113

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.

公开(公告)号：US20250064822A1

公开(公告)日：2025-02-27

申请号：US18941480

申请日：2024-11-08

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

Inventor： Heike Keilhack ,  Brett Truitt ,  Yuta Suzuki ,  Tsukasa Murase ,  Futoshi Shikata

IPC: A61K31/5377 ,  A61K9/00 ,  A61K9/20 ,  A61K9/28 ,  A61P35/00

Abstract: The present invention relates to pharmaceutical compositions comprising inhibitor(s) of human histone methyltransferase EZH2, and methods of cancer therapy using the EZH2 inhibitor(s).

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：US10131633B2

公开(公告)日：2018-11-20

申请号：US15841652

申请日：2017-12-14

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

Inventor： Yuta Suzuki ,  Kenji Hyodo ,  Yohei Tanaka

IPC: C07D207/16 ,  C07D211/62 ,  A61K47/22 ,  A61K9/51 ,  C07D205/04 ,  C12N15/11 ,  A61K48/00 ,  C12N15/113

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.

公开(公告)号：US20170334852A1

公开(公告)日：2017-11-23

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

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：US12168014B2

公开(公告)日：2024-12-17

申请号：US16998144

申请日：2020-08-20

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

Inventor： Heike Keilhack ,  Brett Truitt ,  Yuta Suzuki ,  Tsukasa Murase ,  Futoshi Shikata

IPC: A61K9/20 ,  A61K9/00 ,  A61K9/28 ,  A61K31/5377 ,  A61P35/00

Abstract: The present invention relates to pharmaceutical compositions comprising inhibitor(s) of human histone methyltransferase EZH2, and methods of cancer therapy using the EZH2 inhibitor(s).