公开(公告)号：US10851065B2

公开(公告)日：2020-12-01

申请号：US15713107

申请日：2017-09-22

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

Inventor： Mark Bock ,  Ming-Hong Hao ,  Manav Korpal ,  Vijay Kumar Nyavanandi ,  Xiaoling Puyang ,  Susanta Samajdar ,  Peter Gerard Smith ,  John Wang ,  Guo Zhu Zheng ,  Ping Zhu

IPC: A01N43/00 ,  A01N43/46 ,  A61K31/55 ,  C07D231/56 ,  C07D403/12 ,  C07D471/14 ,  C07D403/06 ,  C07D401/06 ,  C07D401/14

Abstract: Disclosed herein are compounds, or pharmaceutically acceptable salts thereof, and methods of using the compounds for treating breast cancer by administration to a subject in need thereof a therapeutically effective amount of the compounds or pharmaceutically acceptable salts thereof. The breast cancer may be an ER-positive breast cancer and/or the subject in need of treatment may express a mutant ER-α protein.

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：US11926619B2

公开(公告)日：2024-03-12

申请号：US17045952

申请日：2019-04-08

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

Inventor： Gregg F. Keaney ,  John Wang ,  Baudouin Gerard ,  Kenzo Arai ,  Xiang Liu ,  Guo Zhu Zheng ,  Kazunobu Kira ,  Lisa A. Marcaurelle ,  Marta Nevalainen ,  Ming-Hong Hao ,  Morgan Welzel O'Shea ,  Parcharee Tivitmahaisoon ,  Sudeep Prajapati ,  Tuoping Luo ,  Nicholas C. Gearhart ,  Jason T. Lowe ,  Yoshihiko Kotake ,  Satoshi Nagao ,  Regina Mikie Kanada Sonobe ,  Masayuki Miyano ,  Norio Murai ,  Andrew Cook ,  Shelby Ellery ,  Atsushi Endo ,  James Palacino ,  Dominic Reynolds

IPC: C07D407/12 ,  A61K31/365 ,  A61K31/4427 ,  A61K31/497 ,  A61K45/06 ,  A61P35/00 ,  C07D313/00 ,  C07D405/12 ,  C07D405/14 ,  C07D407/06 ,  C07D407/14 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08 ,  C07D487/10 ,  C07D491/107

CPC classification number: C07D407/06 ,  A61K45/06 ,  A61P35/00 ,  C07D313/00 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08 ,  C07D487/10 ,  C07D491/107

Abstract: The present disclosure provides novel pladienolide compounds, pharmaceutical compositions containing such compounds, and methods for using the compounds as therapeutic agents. These compounds may be useful in the treatment of cancers, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful. Also provided herein are methods of treating cancers by administering at least one compound disclosed herein and at least one additional therapy.

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：US20190337921A1

公开(公告)日：2019-11-07

申请号：US16349508

申请日：2017-11-22

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

Inventor： Mark Bock ,  Ming-Hong Hao ,  Manav Korpal ,  Vijay Kumar Nyavanandi ,  Xiaoling Puyang ,  Susanta Samajdar ,  Peter Gerard Smith ,  John Wang ,  Guo Zhu Zheng ,  Ping Zhu ,  Lorna Helen Mitchell ,  Nicholas Larsen ,  Nathalie Rioux

IPC: C07D401/06 ,  C07D209/08 ,  C07D401/14 ,  A61P35/00

Abstract: Disclosed herein are compounds, or pharmaceutically acceptable salts thereof, and methods of using the compounds for treating breast cancer by administration to a subject in need thereof a therapeutically effective amount of the compounds or pharmaceutically acceptable salts thereof. The breast cancer may be an ER-positive breast cancer and/or the subject in need of treatment may express a mutant ER-α protein.

公开(公告)号：US09481669B2

公开(公告)日：2016-11-01

申请号：US14710687

申请日：2015-05-13

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

IPC: C07D405/06 ,  C07D405/14 ,  A61K31/496

CPC classification number: C07D405/14 ,  C07D405/06

Abstract: The present invention provides novel pladienolide pyridine compounds, pharmaceutical compositions containing such compounds, and methods for using the compounds as therapeutic agents. These compounds may be useful in the treatment of cancer, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful.

Abstract translation: 本发明提供新颖的扁桃苷内酰吡啶化合物，含有这些化合物的药物组合物，以及使用该化合物作为治疗剂的方法。 这些化合物可用于治疗癌症，特别是癌症，其中靶向剪接体的试剂和其中的突变已知是有用的。

公开(公告)号：US10912774B2

公开(公告)日：2021-02-09

申请号：US16717080

申请日：2019-12-17

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

Inventor： Dominic Reynolds ,  Ming-Hong Hao ,  John Wang ,  Sudeep Prajapati ,  Takashi Satoh ,  Anand Selvaraj

IPC: A61K31/505 ,  A61K31/506 ,  A61K31/5377

Abstract: Provided herein are compounds of Formula I useful as FGFR4 inhibitors, as well as methods of use of the same.

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.

公开(公告)号：US20200255415A1

公开(公告)日：2020-08-13

申请号：US16349479

申请日：2017-11-22

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

Inventor： Mark Bock ,  Ming-Hong Hao ,  Manav Korpal ,  Vijay Kumar Nyavanandi ,  Xiaoling Puyang ,  Susanta Samajdar ,  Peter Gerard Smith ,  John Wang ,  Guo Zhu Zheng ,  Ping Zhu ,  Lorna Helen Mitchell ,  Nicholas Larsen ,  Nathalie Rioux ,  Sudeep Prajapati ,  Dominic Reynolds ,  Morgan O'Shea ,  Thiwanka Samarakoon

IPC: C07D413/14 ,  A61P35/00 ,  C07D231/56 ,  C07D401/10 ,  C07D401/14 ,  C07D401/12 ,  C07D413/12 ,  C07D403/10

Abstract: Disclosed herein are compounds, or pharmaceutically acceptable salts thereof, and methods of using the compounds for treating breast cancer by administration to a subject in need thereof a therapeutically effective amount of the compounds or pharmaceutically acceptable salts thereof. The breast cancer may be an ER-positive breast cancer and/or the subject in need of treatment may express a mutant ER-α protein.

公开(公告)号：US09796683B2

公开(公告)日：2017-10-24

申请号：US15167373

申请日：2016-05-27

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

Inventor： Mark Bock ,  Ming-Hong Hao ,  Manav Korpal ,  Vijay Kumar Nyavanandi ,  Xiaoling Puyang ,  Susanta Samajdar ,  Peter Gerard Smith ,  John Wang ,  Guo Zhu Zheng ,  Ping Zhu

IPC: A01N43/40 ,  A61K31/44 ,  C07D231/56 ,  C07D403/12 ,  C07D471/14 ,  C07D403/06 ,  C07D401/06 ,  C07D401/14

CPC classification number: C07D231/56 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D471/14

Abstract: Disclosed herein are compounds, or pharmaceutically acceptable salts thereof, and methods of using the compounds for treating breast cancer by administration to a subject in need thereof a therapeutically effective amount of the compounds or pharmaceutically acceptable salts thereof. The breast cancer may be an ER-positive breast cancer and/or the subject in need of treatment may express a mutant ER-α protein.