公开(公告)号：US20250163095A1

公开(公告)日：2025-05-22

申请号：US18842196

申请日：2023-03-01

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

Inventor： Praveen Kumar VEMULA ,  Hyeong Wook CHOI ,  Francis G. FANG ,  Mingde David SHAN

IPC: C07H19/173 ,  C07F9/6561

Abstract: Bis-protected, activated guanine monomers or pharmaceutically acceptable salts thereof for use in the synthesis of polymorpholino oligonucleotides and methods of making the bis-protected, activated guanine monomers are provided.

公开(公告)号：US20190269692A1

公开(公告)日：2019-09-05

申请号：US16270752

申请日：2019-02-08

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

Inventor： Kevin Wayne KUNTZ ,  Kuan-Chun HUANG ,  Hyeong Wook CHOI ,  Kristen SANDERS ,  Steven MATHIEU ,  Arani CHANDA ,  Francis FANG

IPC: A61K31/5377 ,  C07D405/12

Abstract: Provided herein is N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl (tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′-(morpholinomethyl)-[1,1′-biphenyl]-3-carboxamide hydrobromide. Also provided herein is a particular polymorph form of this compound.

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：US20210137936A1

公开(公告)日：2021-05-13

申请号：US17032432

申请日：2020-09-25

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

Inventor： Kevin Wayne KUNTZ ,  Kuan-Chun HUANG ,  Hyeong Wook CHOI ,  Kristen SANDERS ,  Steven MATHIEU ,  Arani CHANDA ,  Francis FANG

IPC: A61K31/5377 ,  C07D405/12

Abstract: Provided herein is N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl (tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′-(morpholinomethyl)-[1,1′-biphenyl]-3-carboxamide hydrobromide. Also provided herein is a particular polymorph form of this compound.

公开(公告)号：US20210017163A1

公开(公告)日：2021-01-21

申请号：US16891427

申请日：2020-06-03

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

Inventor： Kevin Wayne KUNTZ ,  Hyeong Wook CHOI ,  Steven MATHIEU ,  Kristen SANDERS ,  Arani CHANDA

IPC: C07D405/12 ,  A61K31/5377 ,  C07D413/12

Abstract: Provided herein are novel solid forms of N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl (tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′-(morpholinomethyl)-[1,1′-biphenyl]-3-carboxamide hydrochloride, and related compositions and methods.

公开(公告)号：US20250092392A1

公开(公告)日：2025-03-20

申请号：US18557876

申请日：2022-04-28

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

Inventor： Vinod VATHIPADIEKAL ,  Branko MITASEV ,  Courtney EASLEY-NEAL ,  Hyeong Wook CHOI ,  Francis G. FANG ,  John WANG ,  Praveen VEMULA ,  Jung Hwa LEE

IPC: C12N15/113

Abstract: Novel antisense oligonucleotides that induce Exon-2 skipping in the CD33 gene during pre-mRNA splicing, and their use in the treatment of a neurodegenerative disease, such as Alzheimer's disease, are disclosed.

公开(公告)号：US20180282312A1

公开(公告)日：2018-10-04

申请号：US16000539

申请日：2018-06-05

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

Inventor： Kevin Wayne KUNTZ ,  Hyeong Wook CHOI ,  Steven MATHIEU ,  Kristen SANDERS ,  Arani CHANDA

IPC: C07D405/12 ,  A61K31/5377 ,  C07D413/12

Abstract: Provided herein are novel solid forms of N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl (tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′-(morpholinomethyl)-[1,1′-biphenyl]-3-carboxamide hydrochloride, and related compositions and methods.

公开(公告)号：US20170143729A1

公开(公告)日：2017-05-25

申请号：US15199522

申请日：2016-06-30

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

Inventor： Kevin Wayne KUNTZ ,  Kuan-Chun HUANG ,  Hyeong Wook CHOI ,  Kristen SANDERS ,  Steven MATHIEU ,  Arani CHANDA ,  Frances FANG

IPC: A61K31/5377

CPC classification number: A61K31/5377 ,  C07D405/12

Abstract: Provided herein is N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl (tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′-(morpholinomethyl)-[1,1′-biphenyl]-3-carboxamide hydrobromide. Also provided herein is a particular polymorph form of this compound.