公开(公告)号：US09416109B2

公开(公告)日：2016-08-16

申请号：US14379063

申请日：2013-02-14

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

Inventor： George Anthony Moniz ,  Annie Zhu Wilcoxen ,  Farid Benayoud ,  Jaemoon Lee ,  Huiming Zhang ,  Taro Terauchi ,  Ayumi Takemura ,  Yu Yoshida ,  Toshiaki Tanaka ,  Keiichi Sorimachi ,  Yoshimitsu Naoe ,  Yuji Kazuta

IPC: C07D239/34 ,  C07C69/16 ,  C07C309/66 ,  C12P7/22 ,  C07C309/73 ,  C07D401/12 ,  C07C303/28 ,  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.

Abstract translation: 本公开提供了可用于制备可用作食欲素-2受体拮抗剂的化合物的化合物和方法。

公开(公告)号：US09382262B2

公开(公告)日：2016-07-05

申请号：US14577417

申请日：2014-12-19

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

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

IPC: C07D407/06 ,  C07D493/04 ,  C07D405/06 ,  C07D405/12 ,  C07D307/38

CPC classification number: C07F7/1804 ,  C07D307/12 ,  C07D307/38 ,  C07D405/06 ,  C07D405/12 ,  C07D407/06 ,  C07D493/04 ,  Y02P20/55

Abstract: In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate. Exemplary compounds are of formula (I), (II), or (III):

公开(公告)号：US20160176841A1

公开(公告)日：2016-06-23

申请号：US14908164

申请日：2014-10-14

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

Inventor： Roch BOIVIN ,  Hans HANSEN ,  Sally ISHIZAKA ,  Matthew MACKEY ,  Shawn SCHILLER ,  Chikako OGAWA ,  Sridhar NARAYAN ,  Peter BERTINATO ,  Gregory BERGER ,  Atsushi ENDO ,  Robert T. YU ,  Lynn HAWKINS

IPC: C07D401/02 ,  C07D413/14 ,  C07D471/04 ,  C07D401/14 ,  C07D417/14

CPC classification number: C07D401/02 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

Abstract: Embodiments of the disclosure relate to selectively substituted quinoline compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis.

公开(公告)号：US20160045625A1

公开(公告)日：2016-02-18

申请号：US14780665

申请日：2014-04-02

Applicant: EISAI R&D MANAGEMENT CO., LTD. ,  NATIONAL INSTITUTE OF RADIOLOGICAL SCIENCES

Inventor： Norihito Oi ,  Noboru Yamamoto ,  Michiyuki Suzuki ,  Yosuke Nakatani ,  Tetsuya Suhara ,  Meiei Cho ,  Toshimitsu Fukumura ,  Makoto Higuchi ,  Takafumi Minamimoto ,  Jun Maeda ,  Masaki Tokunaga ,  Yuji Nagai

IPC: A61K51/04 ,  C07D401/04

CPC classification number: A61K51/0459 ,  C07D401/04

Abstract: A compound selected from the group consisting of compounds represented by the formulas below or pharmaceutically acceptable salt thereof is useful in PET imaging for AMPA receptor.

Abstract translation: 选自由下式表示的化合物或其药学上可接受的盐的化合物可用于AMPA受体的PET成像。

公开(公告)号：US20160002165A1

公开(公告)日：2016-01-07

申请号：US14768520

申请日：2014-03-10

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

Inventor： Kenshi Yoshida ,  Ikuo Kushida

IPC: C07D211/58 ,  C07C59/50

CPC classification number: C07D211/58 ,  C07C59/50 ,  C07D401/12

Abstract: An organic carboxylic acid salt of 2-[(3S,4R)-1-{[2-chloro-6-(trifluoromethyl)phenyl]methyl}-3-{[1-(cyclohex-1-en-1-ylmethyl) piperidin-4-yl]carbamoyl}-4-methylpyrrolidin-3-yl]acetic acid and a crystal thereof.

Abstract translation: 2 - [（3S，4R）-1 - {[2-氯-6-（三氟甲基）苯基]甲基} -3 - {[1-（环己-1-烯-1-基甲基） 哌啶-4-基]氨基甲酰基} -4-甲基吡咯烷-3-基]乙酸及其结晶。

公开(公告)号：US20150299654A1

公开(公告)日：2015-10-22

申请号：US14703000

申请日：2015-05-04

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

Inventor： Yoshimasa Sakamoto ,  Yuichi Ono ,  Toshio Imai ,  Yasuko Nakagawa

IPC: C12N5/0797 ,  C12Q1/68 ,  G01N33/50 ,  G01N33/68

CPC classification number: C12N5/0623 ,  A61K35/30 ,  C07K16/286 ,  C12Q1/6881 ,  C12Q1/6883 ,  C12Q2600/158 ,  G01N33/5023 ,  G01N33/56966 ,  G01N33/6896 ,  G01N2500/00 ,  G01N2800/2835

Abstract: The present invention relates to polynucleotide probes and antibodies for detecting Lrp4/Corin dopaminergic neuron progenitor cell markers, which enable the efficient separation of dopaminergic neuron progenitor cells; and methods for selecting the progenitor cells by the use thereof.

Abstract translation: 本发明涉及用于检测Lrp4 / Corin多巴胺能神经元祖细胞标记物的多核苷酸探针和抗体，其能够有效分离多巴胺能神经元祖细胞; 以及通过其使用来选择祖细胞的方法。

公开(公告)号：US20150291532A1

公开(公告)日：2015-10-15

申请号：US14438366

申请日：2013-12-19

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

Inventor： Masaharu Gotoda ,  Kenshi Yoshida ,  Nao Shibuguchi

IPC: C07D215/48

CPC classification number: C07D215/48 ,  C07B2200/13

Abstract: The invention provides an amorphous form of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide.

Abstract translation: 本发明提供无定形形式的4-（3-氯-4-（环丙基氨基羰基）氨基苯氧基）-7-甲氧基-6-喹啉甲酰胺。

公开(公告)号：US09133273B2

公开(公告)日：2015-09-15

申请号：US13924433

申请日：2013-06-21

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

Inventor： Toshio Imai ,  James Bradford Kline ,  Tetsu Kawano ,  Luigi Grasso ,  Yoshimasa Sakamoto ,  Jared Spidel ,  Miyuki Nishimura ,  Kenzo Muramoto ,  Tatsuo Horizoe

IPC: C07K16/24 ,  C12N15/13 ,  C12N15/63 ,  A61K39/00

CPC classification number: C07K16/24 ,  A61K2039/505 ,  C07K2317/24 ,  C07K2317/33 ,  C07K2317/34 ,  C07K2317/76 ,  C07K2317/92 ,  G01N33/6863 ,  G01N2333/521

Abstract: The present invention relates to novel humanized, chimeric and murine antibodies that have binding specificity for the human CC chemokine ligand 20 (CCL20). The present invention further relates to heavy chains and light chains of said antibodies. The invention also relates to isolated nucleic acids, recombinant vectors and host cells that comprise a sequence which encodes a heavy chain and/or a light chain of said antibodies, and to a method of preparing said antibodies. The anti-CCL20 antibodies of the invention can be used in therapeutic applications to treat, for example, inflammatory and autoimmune disorders and cancer.

Abstract translation: 本发明涉及对人CC趋化因子配体20（CCL20）具有结合特异性的新型人源化，嵌合和鼠抗体。 本发明还涉及所述抗体的重链和轻链。 本发明还涉及分离的核酸，重组载体和宿主细胞，其包含编码所述抗体的重链和/或轻链的序列，以及制备所述抗体的方法。 本发明的抗CCL20抗体可用于治疗例如炎性和自身免疫性疾病和癌症的治疗应用。

公开(公告)号：US20150225415A1

公开(公告)日：2015-08-13

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 ,  C07D493/18 ,  C07D493/08 ,  C07D307/28 ,  C07D307/33

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：US20150158881A1

公开(公告)日：2015-06-11

申请号：US14562086

申请日：2014-12-05

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

Inventor： Yongbo HU ,  Huiming ZHANG ,  Hiroyuki CHIBA ,  Yuki KOMATSU ,  Bryan M. LEWIS

IPC: C07D493/22

CPC classification number: C07D493/22

Abstract: In general, the present invention features improved methods useful for the synthesis of analogs of halichondrin B, such as eribulin and pharmaceutically acceptable salts thereof (e.g., eribulin mesylate).

Abstract translation: 通常，本发明的特征在于可用于合成软骨素B类似物的改进方法，例如胡椒素及其药学上可接受的盐（例如，甲磺酸eribulin）。