公开(公告)号：US10245269B2

公开(公告)日：2019-04-02

申请号：US15837390

申请日：2017-12-11

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：US20230140327A1

公开(公告)日：2023-05-04

申请号：US17936555

申请日：2022-09-29

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：US11491163B2

公开(公告)日：2022-11-08

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：US10821113B2

公开(公告)日：2020-11-03

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：US10457698B2

公开(公告)日：2019-10-29

申请号：US15750087

申请日：2016-08-05

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

Inventor： Atsushi Endo ,  Robert T. Yu ,  Francis Fang ,  Hyeong Wook Choi ,  Mingde Shan

IPC: C07D413/00 ,  C07F9/6561 ,  C07F9/6558 ,  C07H21/00 ,  A61K31/7088

Abstract: A method of preparation of stereospecific synthesis of diastereomerically pure phosphorodiamidate morpholino oligomers (PMOs) of one of the following general formulas is provided:

公开(公告)号：US20180243316A1

公开(公告)日：2018-08-30

申请号：US15837390

申请日：2017-12-11

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

CPC classification number: A61K31/5377 ,  C07D405/12 ,  Y02A50/401 ,  Y02A50/409 ,  Y02A50/411

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：US20180222932A1

公开(公告)日：2018-08-09

申请号：US15750087

申请日：2016-08-05

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

Inventor： Atsushi Endo ,  Robert T. Yu ,  Francis Fang ,  Hyeong Wook Choi ,  Mingde Shan

IPC: C07F9/6561 ,  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：US12251386B2

公开(公告)日：2025-03-18

申请号：US17936555

申请日：2022-09-29

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：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：US10710987B2

公开(公告)日：2020-07-14

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.