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公开(公告)号：US11584800B2
公开(公告)日：2023-02-21
申请号：US16997613
申请日：2020-08-19
发明人： Hiroyuki Naito , Yusuke Ogitani , Takeshi Masuda , Takashi Nakada , Masao Yoshida , Shinji Ashida , Koji Morita , Hideki Miyazaki , Yuji Kasuya , Ichiro Hayakawa , Yuki Abe
IPC分类号： A61K47/68 , A61K39/395 , A61K31/4745 , A61K39/00 , C07K16/32 , C07D491/22 , C07K16/28 , C07K16/30 , C07D491/052
摘要： As an antitumor drug which is excellent in terms of antitumor effect and safety and has an excellent therapeutic effect, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-HER2 antibody via a linker having a structure represented by the following formula: -L1-L2-LP-NH—(CH2)n1-La-(CH2)n2-C(═O)— wherein the anti-HER2 antibody is connected to the terminal L1, and the antitumor compound is connected to the carbonyl group of the —(CH2)n2-C(═O)— moiety with the nitrogen atom of the amino group at position 1 as the connecting position.
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公开(公告)号：US11261261B2
公开(公告)日：2022-03-01
申请号：US16997613
申请日：2020-08-19
发明人： Hiroyuki Naito , Yusuke Ogitani , Takeshi Masuda , Takashi Nakada , Masao Yoshida , Shinji Ashida , Koji Morita , Hideki Miyazaki , Yuji Kasuya , Ichiro Hayakawa , Yuki Abe
IPC分类号： A61K47/68 , A61K39/395 , A61K31/4745 , A61K39/00 , C07K16/32 , C07D491/22 , C07K16/28 , C07K16/30 , C07D491/052
摘要： As an antitumor drug which is excellent in terms of antitumor effect and safety and has an excellent therapeutic effect, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-HER2 antibody via a linker having a structure represented by the following formula: -L1-L2-LP-NH—(CH2)n1-La-(CH2)n2-C(═O)— wherein the anti-HER2 antibody is connected to the terminal L1, and the antitumor compound is connected to the carbonyl group of the —(CH2)n2-C(═O)— moiety with the nitrogen atom of the amino group at position 1 as the connecting position.
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公开(公告)号：US09872924B2
公开(公告)日：2018-01-23
申请号：US14436458
申请日：2013-10-17
发明人： Hiroyuki Naito , Takashi Nakada , Masao Yoshida , Shinji Ashida , Takeshi Masuda , Hideki Miyazaki , Yuji Kasuya , Yuki Abe , Yusuke Ogitani
CPC分类号： A61K47/6811 , A61K47/6803 , A61K47/6851 , A61K47/6889 , C07K16/00 , C07K16/28 , C07K16/2803 , C07K16/2827 , C07K16/2875 , C07K16/2878 , C07K16/2896 , C07K16/30
摘要： As an antitumor drug which is excellent in terms of antitumor effect and safety, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula (I) is conjugated to an antibody via a linker having a structure represented by the following formula: -L1-L2-LP-NH—(CH2)n1-La-Lb-Lc- or -L1-L2-LP- wherein the antibody is connected to the terminal of L1, the antitumor compound is connected to the terminal of Lc or LP, and any one or two or more of linkers of L1, L2, and LP has a hydrophilic structure.
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公开(公告)号：US10195288B2
公开(公告)日：2019-02-05
申请号：US14435114
申请日：2013-10-10
发明人： Takeshi Masuda , Hiroyuki Naito , Takashi Nakada , Masao Yoshida , Shinji Ashida , Hideki Miyazaki , Yuji Kasuya , Koji Morita , Yuki Abe , Yusuke Ogitani
IPC分类号： A61K47/68 , A61K31/4745 , A61K31/48 , C07K16/30 , C07K16/28
摘要： As an antitumor drug which is excellent in terms of antitumor effect and safety, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an antibody via a linker having a structure represented by the following formula: -L1-L2-LP-NH—(CH2)n1-La-Lb-Lc- wherein the antibody is connected to the terminal of L1, and the antitumor compound is connected to the terminal of Lc with the nitrogen atom of the amino group at position 1 as a connecting position.
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公开(公告)号：US10155821B2
公开(公告)日：2018-12-18
申请号：US15221851
申请日：2016-07-28
发明人： Hiroyuki Naito , Yusuke Ogitani , Takeshi Masuda , Takashi Nakada , Masao Yoshida , Shinji Ashida , Koji Morita , Hideki Miyazaki , Yuji Kasuya , Ichiro Hayakawa , Yuki Abe
IPC分类号： C07K16/32 , A61K31/4745 , A61K47/68 , A61K39/395 , C07K16/28 , A61K47/48 , C07K16/30 , C07D491/22 , C07D491/052
摘要： As an antitumor drug which is excellent in terms of antitumor effect and safety and has an excellent therapeutic effect, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-HER2 antibody via a linker having a structure represented by the following formula: -L1-L2-LP-NH—(CH2)n1-La-(CH2)n2-C(═O)— wherein the anti-HER2 antibody is connected to the terminal L1, and the antitumor compound is connected to the carbonyl group of the —(CH2)n2-C(═O)— moiety with the nitrogen atom of the amino group at position 1 as the connecting position.
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公开(公告)号：US10117952B2
公开(公告)日：2018-11-06
申请号：US14435114
申请日：2013-10-10
发明人： Takeshi Masuda , Hiroyuki Naito , Takashi Nakada , Masao Yoshida , Shinji Ashida , Hideki Miyazaki , Yuji Kasuya , Koji Morita , Yuki Abe , Yusuke Ogitani
IPC分类号： A61K47/68 , A61K31/4745 , A61K31/48 , C07K16/30 , C07K16/28
摘要： As an antitumor drug which is excellent in terms of antitumor effect and safety, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an antibody via a linker having a structure represented by the following formula: -L1-L2-LP-NH—(CH2)n1-La-Lb-Lc- wherein the antibody is connected to the terminal of L1, and the antitumor compound is connected to the terminal of Lc with the nitrogen atom of the amino group at position 1 as a connecting position.
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公开(公告)号：US11633493B2
公开(公告)日：2023-04-25
申请号：US16828279
申请日：2020-03-24
发明人： Takeshi Masuda , Hiroyuki Naito , Takashi Nakada , Masao Yoshida , Shinji Ashida , Hideki Miyazaki , Yuji Kasuya , Koji Morita , Yuki Abe , Yusuke Ogitani
IPC分类号： A61K47/68 , C07K16/28 , A61K31/4745 , A61K31/48 , C07K16/30
摘要： As an antitumor drug which is excellent in terms of antitumor effect and safety, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an antibody via a linker having a structure represented by the following formula: -L1-L2-LF-NH—(CH2)n1-La-Lb-Lc- wherein the antibody is connected to the terminal of L1, and the antitumor compound is connected to the terminal of Lc with the nitrogen atom of the amino group at position 1 as a connecting position.
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公开(公告)号：US11185594B2
公开(公告)日：2021-11-30
申请号：US15302803
申请日：2015-04-06
发明人： Hiroyuki Naito , Takeshi Masuda , Takashi Nakada , Masao Yoshida , Shinji Ashida , Hideki Miyazaki , Yuji Kasuya , Koji Morita , Yusuke Ogitani , Yuki Abe
IPC分类号： A61K47/68 , A61K31/4745 , C07K7/06 , C07K16/32 , A61K39/395 , C07K16/30
摘要： As an antitumor drug which is excellent in terms of antitumor effect and safety and has an excellent therapeutic effect, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-HER2 antibody via a linker having a structure represented by the formula: L1-L2-LP-NH—(CH2)n1-La-Lb-Lc or -L1-L2-LP- wherein the anti-HER2 antibody is connected to the terminal L1, and the antitumor compound is connected to the terminal Lc or LP with the nitrogen atom of the amino group at position 1 as the connecting position.
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公开(公告)号：US10729782B2
公开(公告)日：2020-08-04
申请号：US15821697
申请日：2017-11-22
发明人： Hiroyuki Naito , Takashi Nakada , Masao Yoshida , Shinji Ashida , Takeshi Masuda , Hideki Miyazaki , Yuji Kasuya , Yuki Abe , Yusuke Ogitani
摘要： As an antitumor drug which is excellent in terms of antitumor effect and safety, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula (I) is conjugated to an antibody via a linker having a structure represented by the following formula: -L1-L2-LP-NH—(CH2)n1-La-Lb-Lc- or -L1-L2-LP- wherein the antibody is connected to the terminal of L1, the antitumor compound is connected to the terminal of Lc or LP, and any one or two or more of linkers of L1, L2, and LP has a hydrophilic structure.
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公开(公告)号：US20190008981A1
公开(公告)日：2019-01-10
申请号：US16142354
申请日：2018-09-26
发明人： Takeshi Masuda , Hiroyuki Naito , Takashi Nakada , Masao Yoshida , Shinji Ashida , Hideki Miyazaki , Yuji Kasuya , Koji Morita , Yuki Abe , Yusuke Ogitani
IPC分类号： A61K47/68 , C07K16/28 , C07K16/30 , A61K31/4745 , A61K31/48
摘要： As an antitumor drug which is excellent in terms of antitumor effect and safety, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an antibody via a linker having a structure represented by the following formula: -L1-L2-LP-NH—(CH2)n1-La-Lb-Lc- wherein the antibody is connected to the terminal of L1, and the antitumor compound is connected to the terminal of Lc with the nitrogen atom of the amino group at position 1 as a connecting position.
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