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：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：US11945807B2

公开(公告)日：2024-04-02

申请号：US17661909

申请日：2022-05-03

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

Inventor： Ermira Pazolli ,  Silvia Buonamici ,  Thiwanka Samarakoon ,  Sudeep Prajapati ,  Nathan Fishkin ,  James Palacino ,  Michael Seiler ,  Ping Zhu ,  Andrew Cook ,  Peter Smith ,  Xiang Liu ,  Shelby Ellery ,  Dominic Reynolds ,  Lihua Yu ,  Zhenhua Wu ,  Shouyong Peng ,  Nicholas Calandra ,  Megan Sheehan ,  Yonghong Xiao

IPC: C07D405/12 ,  A61K9/127 ,  A61K9/51 ,  A61K31/365 ,  A61K31/496 ,  A61K39/00 ,  A61K39/395 ,  A61K45/06 ,  A61K47/60 ,  A61K47/68 ,  A61P35/00 ,  C07D313/00 ,  C07D405/06 ,  C07K16/24 ,  C07K16/28 ,  C07K16/30 ,  C07K16/32 ,  C07K16/40 ,  C12Q1/6886 ,  G01N33/50 ,  G01N33/574

CPC classification number: C07D405/12 ,  A61K9/127 ,  A61K9/51 ,  A61K31/365 ,  A61K31/496 ,  A61K39/0011 ,  A61K39/3955 ,  A61K39/39558 ,  A61K45/06 ,  A61K47/60 ,  A61K47/6845 ,  A61K47/6849 ,  A61K47/6851 ,  A61K47/6857 ,  A61K47/6869 ,  A61K47/6871 ,  A61K47/6889 ,  A61P35/00 ,  C07D313/00 ,  C07D405/06 ,  C07K16/24 ,  C07K16/28 ,  C07K16/2803 ,  C07K16/2818 ,  C07K16/2827 ,  C07K16/2896 ,  C07K16/3007 ,  C07K16/3092 ,  C07K16/32 ,  C07K16/40 ,  C12Q1/6886 ,  G01N33/5011 ,  G01N33/574 ,  A61K2039/505 ,  A61K2039/53 ,  A61K2039/545 ,  C07K2317/565 ,  C07K2317/76 ,  C12Q2600/106 ,  G01N2500/10

Abstract: Linker-drug compounds and antibody-drug conjugates that bind to human oncology targets are disclosed. The linker-drug compounds and antibody-drug conjugates comprise a splicing modulator drug moiety. The disclosure further relates to methods and compositions for use in the treatment of neoplastic disorders by administering the antibody-drug conjugates provided herein. In an embodiment, the splicing modulator comprises a pladienolide or a pladienolide derivative.

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：US12172986B2

公开(公告)日：2024-12-24

申请号：US17059635

申请日：2019-05-31

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

Inventor： Ermira Pazolli ,  Silvia Buonamici ,  Thiwanka Samarakoon ,  Sudeep Prajapati ,  Nathan Fishkin ,  James Palacino ,  Michael Seiler ,  Ping Zhu ,  Andrew Cook ,  Peter Smith ,  Xiang Liu ,  Shelby Ellery ,  Dominic Reynolds ,  Lihua Yu ,  Zhenhua Wu ,  Shouyong Peng ,  Nicholas Calandra ,  Megan Sheehan ,  Yonghong Xiao

IPC: C07D405/12 ,  A61K9/127 ,  A61K9/51 ,  A61K31/365 ,  A61K31/496 ,  A61K39/00 ,  A61K39/395 ,  A61K45/06 ,  A61K47/60 ,  A61K47/68 ,  A61P35/00 ,  C07D313/00 ,  C07D405/06 ,  C07K16/24 ,  C07K16/28 ,  C07K16/30 ,  C07K16/32 ,  C07K16/40 ,  C12Q1/6886 ,  G01N33/50 ,  G01N33/574

Abstract: Linker-drug compounds and antibody-drug conjugates that bind to human oncology targets are disclosed. The linker-drug compounds and antibody-drug conjugates comprise a splicing modulator drug moiety. The disclosure further relates to methods and compositions for use in the treatment of neoplastic disorders by administering the antibody-drug conjugates provided herein. In an embodiment, the splicing modulator comprises a pladienolide or a pladienolide derivative.

公开(公告)号：US11679107B2

公开(公告)日：2023-06-20

申请号：US17046528

申请日：2019-04-11

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

Inventor： Andrew Cook ,  Dominic Reynolds ,  Cheng Zhong ,  Ryan Brawn ,  Shelby Ellery ,  Thiwanka Samarakoon ,  Xiang Liu ,  Sudeep Prajapati ,  Megan Sheehan ,  Jason T. Lowe ,  James Palacino

IPC: C07D405/06 ,  A61K31/496 ,  A61P35/00 ,  A61K9/00 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/551 ,  A61K38/19 ,  A61K38/20 ,  A61K38/21 ,  A61K39/395 ,  C07D313/00 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/10 ,  C07D453/02 ,  C07D471/10 ,  C07D487/04 ,  C07D491/107 ,  C07D498/08

CPC classification number: A61K31/496 ,  A61K9/0053 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/551 ,  A61K38/191 ,  A61K38/208 ,  A61K38/2013 ,  A61K38/2066 ,  A61K38/2086 ,  A61K38/217 ,  A61K39/3955 ,  A61P35/00 ,  C07D313/00 ,  C07D405/06 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/10 ,  C07D453/02 ,  C07D471/10 ,  C07D487/04 ,  C07D491/107 ,  C07D498/08 ,  C07B2200/05

Abstract: The present disclosure provides pladienolide compounds, pharmaceutical compositions containing such compounds, and pladienolide compounds for use in methods of medical treatment. 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. Also provided herein are pladienolide compounds for use in methods of treating cancers by administering at least one pladienolide compound disclosed herein and at least one additional therapy

公开(公告)号：US10537571B2

公开(公告)日：2020-01-21

申请号：US15627851

申请日：2017-06-20

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：US20150329528A1

公开(公告)日：2015-11-19

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

IPC: C07D405/14 ,  C07D405/06

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：US11352348B2

公开(公告)日：2022-06-07

申请号：US17247117

申请日：2020-11-30

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

Inventor： Ermira Pazolli ,  Silvia Buonamici ,  Thiwanka Samarakoon ,  Sudeep Prajapati ,  Nathan Fishkin ,  James Palacino ,  Michael Seiler ,  Ping Zhu ,  Andrew Cook ,  Peter Smith ,  Xiang Liu ,  Shelby Ellery ,  Dominic Reynolds ,  Lihua Yu ,  Zhenhua Wu ,  Shouyong Peng ,  Nicholas Calandra ,  Megan Sheehan ,  Yonghong Xiao

IPC: C07D405/12 ,  A61P35/00 ,  A61K47/68 ,  A61K47/60 ,  A61K9/127 ,  A61K9/51 ,  A61K31/365 ,  A61K31/496 ,  A61K39/00 ,  A61K39/395 ,  A61K45/06 ,  C07D313/00 ,  C07D405/06 ,  C07K16/24 ,  C07K16/28 ,  C07K16/30 ,  C07K16/32 ,  C07K16/40 ,  C12Q1/6886 ,  G01N33/50 ,  G01N33/574

Abstract: Linker-drug compounds and antibody-drug conjugates that bind to human oncology targets are disclosed. The linker-drug compounds and antibody-drug conjugates comprise a splicing modulator drug moiety. The disclosure further relates to methods and compositions for use in the treatment of neoplastic disorders by administering the antibody-drug conjugates provided herein. In an embodiment, the splicing modulator comprises a pladienolide or a pladienolide derivative.