公开(公告)号：US20140163242A1

公开(公告)日：2014-06-12

申请号：US14096549

申请日：2013-12-04

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

Inventor： Charles E. Chase ,  Francis G. Fang

IPC: C07D493/20 ,  C07D493/10 ,  C07D493/18 ,  C07F7/18

CPC classification number: C07F7/1804 ,  A61K31/341 ,  C07C33/423 ,  C07D307/12 ,  C07D307/28 ,  C07D307/33 ,  C07D317/72 ,  C07D407/06 ,  C07D407/14 ,  C07D493/04 ,  C07D493/08 ,  C07D493/10 ,  C07D493/18 ,  C07D493/20 ,  C07D493/22 ,  C07F7/188 ,  C07H15/26 ,  Y02P20/55

Abstract: Intermediates and methods of their use in the synthesis of analogs of halichondrin B are provided.

Abstract translation: 提供了中间体及其在合成类软绵母B合成中的应用方法。

公开(公告)号：US20140155452A1

公开(公告)日：2014-06-05

申请号：US14173170

申请日：2014-02-05

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

Inventor： Mark Spyvee ,  Takashi Satoh ,  Jonathan Eric Carlson

IPC: C07D231/22

CPC classification number: C07D231/22 ,  C07D231/20

Abstract: The present invention provides compounds of Formula I: along with pharmaceutical compositions containing the same, and methods of use thereof in subjects in need of treatment.

Abstract translation: 本发明提供式I化合物以及含有其的药物组合物及其在需要治疗的受试者中的使用方法。

公开(公告)号：US20140142315A1

公开(公告)日：2014-05-22

申请号：US14165365

申请日：2014-01-27

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

Inventor： Itaru ARIMOTO ,  Satoshi NAGATO ,  Yukiko SUGAYA ,  Yoshio URAWA ,  Koichi ITO ,  Hiroyuki NAKA ,  Takao OMAE ,  Akio KAYANO ,  Katsutoshi NISHIURA

IPC: C07D213/64

CPC classification number: C07D213/64

Abstract: The present inventions provide a method for commercially producing a 1,2-dihydropyridine-2-one compound represented by the following formula (III-a) wherein the ring A represents an optionally substituted 2-pyridyl group, the ring B represents an optionally substituted phenyl group, and the ring C represents an optionally substituted phenyl group. Further, the invention provides crystals of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one and production processes therefore.

Abstract translation: 本发明提供了一种商业生产下式（III-a）表示的1,2-二氢吡啶-2-酮化合物的方法，其中环A表示任选取代的2-吡啶基，环B表示任选取代的 苯基，环C表示任选取代的苯基。 此外，本发明提供3-（2-氰基苯基）-5-（2-吡啶基）-1-苯基-1,2-二氢吡啶-2-酮的晶体及其制备方法。

公开(公告)号：US20130203741A1

公开(公告)日：2013-08-08

申请号：US13804691

申请日：2013-03-14

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

Inventor： Yuichi Suzuki ,  Takafumi Motoki ,  Toshihiko Kaneko ,  Mamoru Takaishi ,  Tasuku Ishida ,  Yoichi Kita ,  Kunitoshi Takeda ,  Noboru Yamamoto ,  Afzal Khan ,  Paschalis Dimopoulos

IPC: A61K31/542

CPC classification number: A61K31/542 ,  C07D279/08 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04

Abstract: A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.

公开(公告)号：US20130197244A1

公开(公告)日：2013-08-01

申请号：US13795308

申请日：2013-03-12

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

Inventor： Branko Mitasev ,  Dae-Shik Kim ,  Huiming Zhang ,  Matthew J. Schnaderbeck ,  Christopher N. Farthing

IPC: C07D307/22

CPC classification number: C07D307/22 ,  C07D498/04 ,  C07D513/04

Abstract: Provided are compounds and methods useful for the preparation of compounds useful as inhibitors of beta-site amyloid precursor protein (APP)-cleaving enzyme.

Abstract translation: 提供了可用于制备可用作β-位淀粉样蛋白前体蛋白（APP）消除酶抑制剂的化合物的化合物和方法。

公开(公告)号：US20130197045A1

公开(公告)日：2013-08-01

申请号：US13752660

申请日：2013-01-29

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

Inventor： Keigo Tanaka ,  Tomoki Nishioka

IPC: C07D413/14

CPC classification number: C07D413/14

Abstract: A compound represented by formula (1-1) or (1-2), or a pharmacologically acceptable salt thereof retains the principal therapeutic effect of sitaxentan and has an improved CYP inhibitory effect: wherein R1 is a halogen atom, etc., R2 is a methyl group, etc., R3 is a C1-6 alkyl group, etc., and M is a group represented by: etc.

Abstract translation: 由式（1-1）或（1-2）表示的化合物或其药理学上可接受的盐保留了西他生坦的主要治疗效果，并且具有改善的CYP抑制作用：其中R1是卤素原子等，R2是 甲基等，R3为C1-6烷基等，M为由...表示的基团。

公开(公告)号：US12226409B2

公开(公告)日：2025-02-18

申请号：US17407742

申请日：2021-08-20

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

Inventor： Toshiyuki Tamai

IPC: A61K31/47 ,  A61K9/48 ,  A61P35/00

Abstract: This disclosure provides methods for treating a hepatocellular carcinoma (e.g., unresectable HCC) with lenvatinib or a pharmaceutically acceptable salt thereof. Also encompassed by the disclosure are dosage regimens described herein of lenvatinib or a pharmaceutically acceptable salt thereof for use in treating hepatocellular carcinoma (e.g., unresectable hepatocellular carcinoma) according to any of the methods described herein. Particularly useful dosages and dose modifications upon the occurrence of an adverse event or events are also disclosed.

公开(公告)号：US20250051322A1

公开(公告)日：2025-02-13

申请号：US18722917

申请日：2023-01-12

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

Inventor： Ikuo Kushida ,  Yoko Ito ,  So Yasui ,  Takashi Fukuyama ,  Nobuaki Sato ,  Taro Asaba

IPC: C07D451/02 ,  A61K31/506

Abstract: Crystals of compounds represented by formula (I) having potential as drug substances for pharmaceuticals, as well as salts of compounds represented by formula (I) and their crystals.

公开(公告)号：US12220398B2

公开(公告)日：2025-02-11

申请号：US15750712

申请日：2016-08-18

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

Inventor： Kiyoshi Okamoto ,  Junji Matsui ,  Corina Dutcus

IPC: A61K31/357 ,  A61K31/47 ,  A61K31/664 ,  A61K31/675 ,  A61P35/00 ,  A61K31/7048

Abstract: A novel tumor therapeutic agent for a combination therapy is disclosed. More specifically, a tumor therapeutic agent used for a combination therapy of lenvatinib, ifosfamide, and etoposide is disclosed.

公开(公告)号：US20240350484A1

公开(公告)日：2024-10-24

申请号：US18645759

申请日：2024-04-25

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

Inventor： Ermira PAZOLLI ,  Silvia BUONAMICI ,  James PALACINO ,  Michael SEILER ,  Ping ZHU ,  Evan BARRY ,  Lihua YU

IPC: A61K31/496 ,  A61K35/17 ,  A61K38/19 ,  A61K38/20 ,  A61K38/21 ,  A61K39/00 ,  A61K39/39 ,  A61K39/395

CPC classification number: A61K31/496 ,  A61K35/17 ,  A61K38/191 ,  A61K38/2013 ,  A61K38/2066 ,  A61K38/208 ,  A61K38/2086 ,  A61K38/217 ,  A61K39/0011 ,  A61K39/39 ,  A61K39/3955 ,  A61K2039/6031 ,  A61K2039/6037 ,  A61K2039/6056 ,  A61K2039/6081

Abstract: This disclosure relates to methods for the treatment of neoplastic disorders by administering Compound 1, or a pharmaceutically acceptably salt thereof, on its own and/or as part of a conjugate or composition, and inducing production of at least one neoantigen.