公开(公告)号：US09975910B2

公开(公告)日：2018-05-22

申请号：US14904860

申请日：2014-07-18

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

Inventor： Keigo Tanaka ,  Takashi Fukuyama ,  Norio Murai ,  Wataru Itano ,  Shinsuke Hirota ,  Daisuke Iida ,  Hiroshi Azuma

IPC: C07D491/048 ,  C07F7/22 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04 ,  C07F5/02

CPC classification number: C07F7/2208 ,  C07D491/048 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04 ,  C07F5/02 ,  C07F5/025 ,  C07F5/027

Abstract: A compound represented by the formula (I) or a salt thereof: wherein a ring Z is a 5 to 6-membered heteroaromatic ring having one or two heteroatoms in the ring; X1 is a hydrogen atom, a hydroxy group, a hydroxy C1-6 alkyl group, —B(OH)2, a boronate ester group, a cyclic boronate ester group, a boranyl group, a cyclic boranyl group, —BF3Mn1, —Sn(R12)(R13)(R14), a leaving group, a carboxy group, a formyl group, or —NR16R17; and X2 is a hydrogen atom or —CO2R18.

公开(公告)号：US09738656B2

公开(公告)日：2017-08-22

申请号：US15346912

申请日：2016-11-09

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

Inventor： Toshiki Kurokawa ,  Yu Yoshida ,  Kogyoku Shin ,  Yoshihisa Kobayashi ,  Hironori Fukumoto ,  Kunitoshi Takeda ,  Yoshiaki Ohashi ,  Makoto Kotake ,  Tomoyuki Shibuguchi ,  Toru Watanabe ,  Yoichi Kita ,  Shinsuke Hirota ,  Takashi Fukuyama ,  Yasuaki Kamada

IPC: C07D491/147 ,  C07D491/052

CPC classification number: C07D491/147 ,  C07D491/052

Abstract: Compounds represented by formulae (I) to (XXII) or pharmaceutically acceptable salts thereof:

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：US20210230177A1

公开(公告)日：2021-07-29

申请号：US16628504

申请日：2018-07-06

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

Inventor： Yoshito Kishi ,  Yanran Ai ,  Ning Ye ,  Qiaoyi Wang ,  Kenzo Yahata ,  Kentaro Iso ,  Santhosh Reddy Naini ,  Shuji Yamashita ,  Jihoon Lee ,  Isao Ohashi ,  Takashi Fukuyama

IPC: C07D493/22

Abstract: The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A)

公开(公告)号：US20170137436A1

公开(公告)日：2017-05-18

申请号：US15346912

申请日：2016-11-09

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

Inventor： Toshiki Kurokawa ,  Yu Yoshida ,  Kogyoku Shin ,  Yoshihisa Kobayashi ,  Hironori Fukumoto ,  Kunitoshi Takeda ,  Yoshiaki Ohashi ,  Makoto Kotake ,  Tomoyuki Shibuguchi ,  Toru Watanabe ,  Yoichi Kita ,  Shinsuke Hirota ,  Takashi Fukuyama ,  Yasuaki Kamada

IPC: C07D491/147 ,  C07D491/052

CPC classification number: C07D491/147 ,  C07D491/052

Abstract: Compounds represented by formulae (I) to (XXII) or pharmaceutically acceptable salts thereof:

公开(公告)号：US20230128195A1

公开(公告)日：2023-04-27

申请号：US18058441

申请日：2022-11-23

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

Inventor： Yoshito Kishi ,  Yanran Ai ,  Ning Ye ,  Qiaoyi Wang ,  Kenzo Yahata ,  Kentaro Iso ,  Santhosh Reddy Naini ,  Shuji Yamashita ,  Jihoon Lee ,  Isao Ohashi ,  Takashi Fukuyama

IPC: C07D493/22

Abstract: The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A):

公开(公告)号：US11548898B2

公开(公告)日：2023-01-10

申请号：US16628504

申请日：2018-07-06

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

Inventor： Yoshito Kishi ,  Yanran Ai ,  Ning Ye ,  Qiaoyi Wang ,  Kenzo Yahata ,  Kentaro Iso ,  Santhosh Reddy Naini ,  Shuji Yamashita ,  Jihoon Lee ,  Isao Ohashi ,  Takashi Fukuyama

IPC: C07D493/22

Abstract: The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).

公开(公告)号：US20160168176A1

公开(公告)日：2016-06-16

申请号：US14904860

申请日：2014-07-18

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

Inventor： Keigo Tanaka ,  Takashi Fukuyama ,  Norio Murai ,  Wataru Itano ,  Shinsuke Hirota ,  Daisuke Iida ,  Hiroshi Azuma

IPC: C07F7/22 ,  C07F5/02 ,  C07D495/04 ,  C07D513/04 ,  C07D491/048 ,  C07D493/04

CPC classification number: C07F7/2208 ,  C07D491/048 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04 ,  C07F5/02 ,  C07F5/025 ,  C07F5/027

Abstract: A compound represented by the formula (I) or a salt thereof: wherein a ring Z is a 5 to 6-membered heteroaromatic ring having one or two heteroatoms in the ring; X1 is a hydrogen atom, a hydroxy group, a hydroxy C1-6 alkyl group, —B(OH)2, a boronate ester group, a cyclic boronate ester group, a boranyl group, a cyclic boranyl group, —BF3Mn1, —Sn(R12)(R13)(R14), a leaving group, a carboxy group, a formyl group, or —NR16R17; and X2 is a hydrogen atom or —CO2R18.

Abstract translation: 由式（I）表示的化合物或其盐：其中环Z是环中具有一个或两个杂原子的5至6元杂芳环; X1是氢原子，羟基，羟基C1-6烷基，-B（OH）2，硼酸酯基，环状硼酸酯基，硼烷基，环状硼烷基，-BF3Mn1，-Sn （R 12）（R 13）（R 14），离去基团，羧基，甲酰基或-NR 16 R 17; X 2为氢原子或-CO 2 R 18。