公开(公告)号：US20180222932A1

公开(公告)日：2018-08-09

申请号：US15750087

申请日：2016-08-05

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

Inventor： Atsushi Endo ,  Robert T. Yu ,  Francis Fang ,  Hyeong Wook Choi ,  Mingde Shan

IPC: C07F9/6561 ,  C07F9/6558

Abstract: We provide diastereomerically pure or substantially diastereomerically pure activated phosphoramidochloridate morpholino nucleosides, methods of their preparation, and methods of their use in stereospecific coupling for stereospecific synthesis of diastereomerically pure phosphorodiamidate morpholino oligomers (PMOs).

公开(公告)号：US20180136216A1

公开(公告)日：2018-05-17

申请号：US15573197

申请日：2016-05-27

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

Inventor： Yasuhiro Funahashi ,  Tadashi Kadowaki

IPC: G01N33/574

CPC classification number: G01N33/57438 ,  G01N2800/52

Abstract: Biomarkers are provided that predict whether a human subject having a renal cell carcinoma is in need of a combination therapy comprising lenvatinib or a pharmaceutically acceptable salt thereof (e.g., lenvatinib mesylate) and everolimus. The biomarkers, compositions, and methods described herein are useful in selecting appropriate treatment modalities for and treating a subject having, suspected of having, or at risk of developing a renal cell carcinoma.

公开(公告)号：US09938288B1

公开(公告)日：2018-04-10

申请号：US15814105

申请日：2017-11-15

Applicant: President and Fellows of Harvard College ,  Eisai R&D Management Co., Ltd.

Inventor： Yoshito Kishi ,  Kazunobu Kira ,  Ken Ito

IPC: C07D498/22 ,  A61K31/357 ,  C07D493/22 ,  A61K39/395

CPC classification number: C07D493/22 ,  A61K31/357 ,  A61K39/3955 ,  A61K2300/00

Abstract: The present invention provides novel Compound (1) having tumor vascular remodeling effect and/or anti-CAF (Cancer Associated Fibroblasts) activity, or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, and a medical uses thereof.

公开(公告)号：US20180057499A1

公开(公告)日：2018-03-01

申请号：US15689481

申请日：2017-08-29

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

Inventor： Richard Clark ,  Tetsuya Kawahara ,  Daisuke Iida ,  Shinsuke Hirota ,  Yasuaki Kamada ,  Toshiyuki Ohfusa ,  Naoki Yoneda ,  Fumiyoshi Matsuura ,  So Yasui

IPC: C07D487/04

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61P17/06 ,  A61P29/00

Abstract: The compounds represented by formulas (I) to (XVIII) or pharmaceutically acceptable salts thereof.

公开(公告)号：US20180044285A1

公开(公告)日：2018-02-15

申请号：US15791814

申请日：2017-10-24

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

Inventor： George Anthony Moniz ,  Annie Zhu Wilcoxen ,  Farid Benayoud ,  Toshiaki Tanaka ,  Keiichi Sorimachi

IPC: C07C309/73 ,  C12P7/22 ,  C07C309/66 ,  C07C303/28 ,  C07C33/50 ,  C07D239/34 ,  C07D401/12 ,  C07C69/16 ,  C07C303/44 ,  C07C29/147

CPC classification number: C07C309/73 ,  C07B2200/07 ,  C07C29/147 ,  C07C69/16 ,  C07C303/28 ,  C07C303/44 ,  C07C309/66 ,  C07C2601/02 ,  C07D239/34 ,  C07D401/12 ,  C12P7/22 ,  C07C33/50

Abstract: The present disclosure provides compounds and methods that are useful for the preparation of compounds useful as orexin-2 receptor antagonists.

公开(公告)号：US20170334852A1

公开(公告)日：2017-11-23

申请号：US15533576

申请日：2015-12-24

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

Inventor： Yuta Suzuki ,  Kenji Hyodo ,  Yohei Tanaka

IPC: C07D211/62 ,  C12N15/113 ,  A61K47/10 ,  A61K31/713 ,  A61K47/22 ,  A61K47/28 ,  C07C229/12

CPC classification number: C07D211/62 ,  A61K31/713 ,  A61K47/10 ,  A61K47/22 ,  A61K47/28 ,  C07C229/06 ,  C07C229/12 ,  C12N15/09 ,  C12N15/113 ,  C12N15/1137 ,  C12N2310/14

Abstract: The present invention provides a cationic lipid which can be utilized for nucleic acid delivery into the cytoplasm. The cationic lipid of the present invention is, for example, a compound represented by the following Formula (1) or a pharmaceutically acceptable salt thereof.

公开(公告)号：US09604993B2

公开(公告)日：2017-03-28

申请号：US14624033

申请日：2015-02-17

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

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

IPC: C07D493/20 ,  A61K31/335 ,  C07D307/28 ,  C07D307/33 ,  C07D493/08 ,  C07D493/18

CPC classification number: C07D493/20 ,  C07D307/20 ,  C07D307/26 ,  C07D307/28 ,  C07D307/33 ,  C07D309/16 ,  C07D405/06 ,  C07D405/14 ,  C07D493/04 ,  C07D493/08 ,  C07D493/18 ,  C07D493/22 ,  Y02P20/55

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

公开(公告)号：US09599621B2

公开(公告)日：2017-03-21

申请号：US14451044

申请日：2014-08-04

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

Inventor： Daniel John O'Shannessy

IPC: G01N33/574 ,  C07K16/28 ,  G01N33/82

CPC classification number: G01N33/82 ,  C07K16/28 ,  C07K2317/34 ,  C07K2317/565 ,  C07K2317/92 ,  G01N33/57407 ,  G01N33/57415 ,  G01N33/57419 ,  G01N33/57423 ,  G01N33/57442 ,  G01N33/57449 ,  G01N33/57484 ,  G01N33/57492 ,  G01N2800/52 ,  G01N2800/56

Abstract: Described herein are antibodies, and antigen-binding fragments thereof, that are specific for folate receptor alpha, related polynucleotides, expression vectors, and cells that express the described antibodies. Also provided are methods of using the described antibodies, and antigen-binding fragments thereof, and related kits. Provided herein are also methods for diagnosing cancers, such as breast cancer, thyroid cancer, colorectal cancer, endometrial cancer, fallopian tube cancer, ovarian cancer, or lung cancer, using the described antibodies, and antigen-binding fragments thereof. The methods involve determining the amount of folate receptor alpha in a sample derived from a subject and comparing this level with the level of folate receptor alpha in a control sample or reference sample.

公开(公告)号：US20170071903A1

公开(公告)日：2017-03-16

申请号：US15123476

申请日：2015-03-02

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

Inventor： Yasuhiro FUNAHASHI ,  Bruce A. Littlefield ,  Toshimitsu UENAKA

IPC: A61K31/357 ,  A61K45/06 ,  A61K31/436

CPC classification number: A61K31/357 ,  A61K31/436 ,  A61K31/675 ,  A61K45/06 ,  A61K2300/00

Abstract: Methods for treating cancer (e.g., breast cancer, lung cancer, pancreatic cancer, primitive neuroectodermal tumors, lung cancer, ovarian cancer, endometrial cancer, pharyngeal cancer, esophageal cancer, and sarcoma) in a subject (such as an human patient) in need thereof by administering eribulin (e.g., eribulin mesylate, i.e., E7389, Halaven) in combination with one or more mammalian target of rapamycin (mTOR) inhibitors (e.g., everolimus, ridaforolimus, and temsirolimus), and kits therefor are provided.

Abstract translation: 在需要的受试者（例如人类患者）中治疗癌症（例如乳腺癌，肺癌，胰腺癌，原始神经外胚层肿瘤，肺癌，卵巢癌，子宫内膜癌，咽癌，食管癌和肉瘤）的方法 通过与一种或多种雷帕霉素（mTOR）抑制剂（例如依维莫司，阿糖胞苷和替西罗莫司）的哺乳动物靶标组合​​施用eribulin（例如，甲磺酸eribulin，即E7389，Halaven）及其试剂盒。

公开(公告)号：US20160347717A1

公开(公告)日：2016-12-01

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: C07D231/56 ,  C07D401/14 ,  C07D403/06 ,  C07D401/06 ,  C07D403/12 ,  C07D471/14

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.

Abstract translation: 本文公开了化合物或其药学上可接受的盐，以及通过向有需要的受试者施用治疗有效量的化合物或其药学上可接受的盐来使用该化合物治疗乳腺癌的方法。 乳腺癌可能是ER阳性乳腺癌，和/或需要治疗的受试者可以表达突变型ER-α蛋白。