公开(公告)号：US20190315754A1

公开(公告)日：2019-10-17

申请号：US16391882

申请日：2019-04-23

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

Inventor： Wanjun Zheng ,  Xiaojie Zhu ,  Hong Du ,  Maarten Postema ,  Yimin Jiang ,  Jing Li ,  Robert Yu ,  Hyeong-wook Choi ,  Jaemoon Lee ,  Frank Fang ,  Daniel Custar

IPC: C07D487/04 ,  C07D519/00 ,  A61P35/00

Abstract: We provide compounds given by Formula I, which is shown in FIG. 3, or pharmaceutically acceptable salts thereof, as well as formulations thereof and methods of use of those compounds and formulations for treatment of cancer.

公开(公告)号：US20190282541A1

公开(公告)日：2019-09-19

申请号：US16318198

申请日：2017-07-20

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

Inventor： Bruce A. LITTLEFIELD ,  Gary HENDLER

IPC: A61K31/357 ,  A61K31/4406 ,  A61K31/565 ,  A61P35/04

Abstract: The invention features methods for treating and preventing cancer (e.g., a hormone sensitive cancer) in a patient in need thereof by administering eribulin (e.g., eribulin mesylate) in combination with a histone deacetylase (HDAC) inhibitor.

公开(公告)号：US20190263927A1

公开(公告)日：2019-08-29

申请号：US16341579

申请日：2017-10-13

Applicant: Merck Sharp & Dohme Corp. ,  Eisai R&D Management Co., Ltd.

Inventor： Martin S. OLIVO

IPC: C07K16/30 ,  A61K31/351 ,  C07K16/28 ,  A61P35/04 ,  A61K9/00

Abstract: The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and eribulin or a pharmaceutically acceptable salt thereof, and the use of the combination therapies for the treatment of urothelial cancer.

公开(公告)号：US10357495B2

公开(公告)日：2019-07-23

申请号：US16239719

申请日：2019-01-04

Applicant: Dermavant Sciences GmbH ,  Eisai R&D Management Co., Ltd.

Inventor： Ambrish Vyas ,  Seiji Takemoto ,  Yoshihiro Akimoto

IPC: A61K31/517 ,  A61K47/06 ,  A61K47/10 ,  A61K47/14 ,  A61P17/06 ,  A61K9/00

Abstract: Embodiments herein are directed to topical formulations of a compound represented by the formula (I), salt, metabolite, prodrug, or hydrate thereof along with a solvent, and a base. The compound is a PDE4 inhibitor and the topical formulations may be used to treat dermatological conditions such as, but not limited to, atopic dermatitis, seborrheic dermatitis, alopecia, contact dermatitis, psoriasis, urticaria, eczema, burns, sunburn, pancreatitis, hepatitis, lichen planus, scleritis, scleroderma, dermatomyositis, itching associated with any of the preceding conditions or a combination thereof.

公开(公告)号：US20190175598A1

公开(公告)日：2019-06-13

申请号：US16324643

申请日：2017-08-23

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

Inventor： Anand Selvaraj ,  Peter Smith

IPC: A61K31/506 ,  A61K31/519 ,  A61P35/00

Abstract: Provided herein is a combination therapy useful for the treatment hepatocellular carcinoma and/or intrahepatic cholangiocarcinoma. The combination comprises an EGFR4 inhibitor and a CDK 4/6 inhibitor.

公开(公告)号：US20190144419A1

公开(公告)日：2019-05-16

申请号：US16096136

申请日：2017-11-27

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

Inventor： Keiko Onuma

IPC: C07D401/06 ,  A61P35/00

Abstract: The present invention provides salts of (E)-N,N-dimethyl-4-((2-((5-((Z)-4,4,4-trifluoro-1-(3-fluoro-1H-indazol-5-yl)-2-phenylbut-1-en-1-yl)pyridin-2-yl)oxy)ethyl)amino)but-2-enamide represented by the formula I and acids, and crystals thereof, possessing a potential to be used as drug substance in pharmaceuticals.

公开(公告)号：US20190071452A1

公开(公告)日：2019-03-07

申请号：US16122116

申请日：2018-09-05

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

Inventor： Yoshiaki Ohashi ,  Yoshihiko Norimine ,  Tamaki Hoshikawa ,  Yu Yoshida ,  Yoshihisa Kobayashi ,  Nobuhiro Sato ,  Koji Hagiwara

IPC: C07D495/22 ,  A61P25/28 ,  A61P25/16

Abstract: The present invention provides compounds represented by formulas (I) to (VI) or pharmaceutically acceptable salts thereof.

公开(公告)号：US10214539B2

公开(公告)日：2019-02-26

申请号：US15787268

申请日：2017-10-18

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

Inventor： Charles E. Chase ,  Atsushi Endo ,  Francis G. Fang ,  Jing Li

IPC: C07D493/20 ,  C07D307/28 ,  C07D307/33 ,  C07D493/08 ,  C07D493/18 ,  C07D493/04 ,  C07D493/22 ,  C07D307/20 ,  C07D307/26 ,  C07D309/16 ,  C07D405/06 ,  C07D405/14

Abstract: Methods of synthesizing intermediates useful for the synthesis of halichondrin B analogs are described.

公开(公告)号：US10131633B2

公开(公告)日：2018-11-20

申请号：US15841652

申请日：2017-12-14

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

Inventor： Yuta Suzuki ,  Kenji Hyodo ,  Yohei Tanaka

IPC: C07D207/16 ,  C07D211/62 ,  A61K47/22 ,  A61K9/51 ,  C07D205/04 ,  C12N15/11 ,  A61K48/00 ,  C12N15/113

Abstract: The present invention provides a cationic lipid which can be used for nucleic acid delivery to a cytoplasm and which is possible to solve the problem of physical stability of a lipid complex. This cationic lipid is a compound represented by the general formula (3) or a pharmaceutically acceptable salt thereof: wherein, L is an alkyl having 7-12 carbon atoms or an alkenyl having 7-12 carbon atoms, R is an alkyl having 1-2 carbon atoms, and n1 and n2 are independently an integer of 1-3.

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.