公开(公告)号：US11498916B2

公开(公告)日：2022-11-15

申请号：US16722838

申请日：2019-12-20

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

Inventor： George Moniz ,  Kristen Sanders ,  Arani Chanda ,  Kenshi Yoshida ,  Ming-Hong Hao ,  Dominic Reynolds ,  Sudeep Prajapati ,  Anand Selvaraj ,  Takashi Satoh ,  John Wang

IPC: C07D403/12 ,  C07D239/48 ,  A61K31/505

Abstract: A number of crystalline forms of N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-y1)phenyl)acrylamide are provided. These include a crystalline free base form, a crystalline monohydrochloride salt form, a crystalline dihydrochloride salt form, and a crystalline ethanesulfonate salt form. Methods of making and using crystalline compounds are also provided.

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：US10562888B2

公开(公告)日：2020-02-18

申请号：US15566527

申请日：2016-04-13

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

Inventor： George Moniz ,  Kristen Sanders ,  Arani Chanda ,  Kenshi Yoshida

IPC: C07D403/12 ,  A61K31/505

Abstract: A number of crystalline forms of N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide are provided. These include a crystalline free base form, a crystalline monohydrochloride salt form, a crystalline dihydrochloride salt form, and a crystalline ethanesulfonate salt form. Methods of making and using crystalline compounds are also 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：US20150065503A1

公开(公告)日：2015-03-05

申请号：US14394431

申请日：2013-04-11

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 ,  Frank Fang

IPC: C07D405/12

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.

Abstract translation: 本文提供的是N - （（4,6-二甲基-2-氧代-1,2-二氢吡啶-3-基）甲基）-5-（乙基（四氢-2H-吡喃-4-基）氨基）-4- 甲基-4' - （吗啉代甲基） - [1,1'-联苯] -3-甲酰胺氢溴酸盐。 本文还提供了该化合物的特定多晶型物。

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：US20190100513A1

公开(公告)日：2019-04-04

申请号：US15529798

申请日：2016-11-17

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

Inventor： Gregg F. Keaney ,  John Wang ,  Baudouin Gerard ,  Kenzo Arai ,  Xiang Liu ,  Guo Zhu Zheng ,  Kazunobu Kira ,  Parcharee Tivitmahaisoon ,  Sudeep Prajapati ,  Nicholas C. Gearhart ,  Yoshihiko Kotake ,  Satoshi Nagao ,  Regina Mikie Kanada Sonobe ,  Masayuki Miyano ,  Norio Murai ,  Silvia Buonamici ,  Lihua Yu ,  Eunice Sun Park ,  Betty Chan ,  Peter G. Smith ,  Michael P. Thomas ,  Ermira Pazolli ,  Kian Huat Lim ,  Atsushi Endo ,  Arani Chanda

IPC: C07D405/14 ,  A61P35/02

Abstract: The present disclosure provides a novel solid state form of pladienolide pyridine compounds, compositions comprising at least one such solid state form, and methods of preparation and use and the same. The novel solid state form of pladienolide pyridine compounds may be useful in the treatment of cancer, such as, for example, cancers in which agents that target the spliceosome and mutations therein are known to be useful.

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：US10745387B2

公开(公告)日：2020-08-18

申请号：US15529798

申请日：2016-11-17

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

Inventor： Gregg F. Keaney ,  John Wang ,  Baudouin Gerard ,  Kenzo Arai ,  Xiang Liu ,  Guo Zhu Zheng ,  Kazunobu Kira ,  Parcharee Tivitmahaisoon ,  Sudeep Prajapati ,  Nicholas C. Gearhart ,  Yoshihiko Kotake ,  Satoshi Nagao ,  Regina Mikie Kanada Sonobe ,  Masayuki Miyano ,  Norio Murai ,  Silvia Buonamici ,  Lihua Yu ,  Eunice Sun Park ,  Betty Chan ,  Peter G. Smith ,  Michael P. Thomas ,  Ermira Pazolli ,  Kian Huat Lim ,  Atsushi Endo ,  Arani Chanda

IPC: A61K31/496 ,  C07D295/182 ,  C07D405/14 ,  C07D405/06 ,  A61P35/02

Abstract: The present disclosure provides a novel solid state form of pladienolide pyridine compounds having Formula I, compositions comprising at least one such solid state form, and methods of preparation and use and the same. The novel solid state form of pladienolide pyridine compounds may be useful in the treatment of cancer, such as, for example, cancers in which agents that target the spliceosome and mutations therein are known to be useful.