公开(公告)号：US11318212B2

公开(公告)日：2022-05-03

申请号：US16642277

申请日：2018-08-30

申请人： DAIICHI SANKYO COMPANY, LIMITED

发明人： Yoshio Nishi ,  Kohei Sakanishi ,  Shigeru Noguchi ,  Tadahiro Takeda

IPC分类号： A61K47/68 ,  C07C231/12 ,  C07C233/15 ,  C07C233/33 ,  C07C233/54 ,  C07D491/22 ,  C07K5/103 ,  C07K16/00 ,  C07K16/28 ,  C07K16/30 ,  C07K16/32

摘要： A method for producing a compound represented by formula (C) wherein R1 represents an amino group protected with a protecting group, the method comprising a step of subjecting a compound represented by formula (B) wherein R1 represents the same meaning as above, to intramolecular cyclization to convert the compound into the compound represented by formula (C).

公开(公告)号：US11945882B2

公开(公告)日：2024-04-02

申请号：US16642245

申请日：2018-08-30

申请人： DAIICHI SANKYO COMPANY, LIMITED

发明人： Tatsuya Yamaguchi ,  Takashi Kouko ,  Shigeru Noguchi ,  Yohei Yamane ,  Fumikatsu Kondo ,  Takahiro Aoki ,  Tadahiro Takeda ,  Kohei Sakanishi ,  Hitoshi Sato ,  Tsuyoshi Ueda ,  Shinji Matuura ,  Kei Kurahashi ,  Yutaka Kitagawa ,  Tatsuya Nakamura

IPC分类号： C07K1/30 ,  C07K5/10

CPC分类号： C07K5/10 ,  C07B2200/13

摘要： Crystals of the compound represented by formula (1), a method for the production thereof, and a method for producing an antibody-drug conjugate using the crystals.

公开(公告)号：US11173213B2

公开(公告)日：2021-11-16

申请号：US15579512

申请日：2016-06-28

申请人： DAIICHI SANKYO COMPANY, LIMITED

发明人： Shigeru Noguchi ,  Ken Sakurai ,  Daisuke Okajima

IPC分类号： A61K47/68 ,  A61K31/4745 ,  A61K31/40 ,  C07K16/00 ,  A61K39/395 ,  A61K45/00 ,  A61P35/00 ,  A61K31/407 ,  C07K16/32 ,  C07K16/28

摘要： A method for producing an antibody-drug conjugate composition, comprising: (i) a step of reacting an antibody with a reducing agent in a buffer to reduce interchain disulfides, and (ii) a step of reacting drug linker intermediates with the antibody having thiol groups obtained in the step (i), wherein the reaction temperature in the step (i) is −10° C. to 10° C., and the average number of bound drugs in the produced antibody-drug conjugate composition is 3.5 to 4.5, and the content of antibody-drug conjugates in which four drug linkers are bound to heavy-light interchain thiols, in the produced antibody-drug conjugate composition is 50% or more; and an antibody-drug conjugate composition, wherein the content of antibody-drug conjugates wherein the average number of bound drugs is 3.5 to 4.5, and the content of antibody-drug conjugates in which four drug linkers are bound to heavy-light interchain thiols, is 50% or more.