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公开(公告)号：EP3101032B1
公开(公告)日：2019-01-16
申请号：EP15743738.5
申请日：2015-01-28
发明人： NAITO, Hiroyuki , OGITANI, Yusuke , MASUDA, Takeshi , NAKADA, Takashi , YOSHIDA, Masao , ASHIDA, Shinji , MORITA, Koji , MIYAZAKI, Hideki , KASUYA, Yuji , HAYAKAWA, Ichiro , ABE, Yuki
IPC分类号： C07K16/28 , A61K31/4745 , A61K39/395 , A61P35/00 , C07D491/052
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公开(公告)号：EP4212552A1
公开(公告)日：2023-07-19
申请号：EP22198821.5
申请日：2015-01-28
发明人： NAITO, Hiroyuki , OGITANI, Yusuke , MASUDA, Takeshi , NAKADA, Takashi , YOSHIDA, Masao , ASHIDA, Shinji , MORITA, Koji , MIYAZAKI, Hideki , KASUYA, Yuji , HAYAKAWA, Ichiro , ABE, Yuki
IPC分类号： C07K16/28 , A61K31/4745 , A61K39/395 , A61P35/00 , 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: -L 1 -L 2 -L P -NH-(CH 2 )n 1 -L a -(CH 2 )n 2 -C(=O)- wherein the anti-HER2 antibody is connected to the terminal L 1 , and the antitumor compound is connected to the carbonyl group of the -(CH 2 )n 2 -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：EP3973995A1
公开(公告)日：2022-03-30
申请号：EP21187152.0
申请日：2015-01-28
发明人： NAITO, Hiroyuki , OGITANI, Yusuke , MASUDA, Takeshi , NAKADA, Takashi , YOSHIDA, Masao , ASHIDA, Shinji , MORITA, Koji , MIYAZAKI, Hideki , KASUYA, Yuji , HAYAKAWA, Ichiro , ABE, Yuki
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: ―L 1 ―L 2 ―L P ―NH― (CH 2 ) n 1 ―L a ― (CH 2 ) n 2 ― C(=O)― wherein the anti-HER2 antibody is connected to the terminal L 1 , and the antitumor compound is connected to the carbonyl group of the - (CH 2 )n 2 ―C(=0) ― 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：EP3632471A1
公开(公告)日：2020-04-08
申请号：EP19206764.3
申请日：2013-10-10
发明人： MASUDA, Takeshi , NAITO, Hiroyuki , NAKADA, Takashi , YOSHIDA, Masao , ASHIDA, Shinji , MIYAZAKI, Hideki , KASUYA, Yuji , MORITA, Koji , ABE, Yuki , OGITANI, Yusuke
IPC分类号： A61K47/68
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 anti-B7-H3 antibody via a linker having a structure represented by the following formula: -L 1 -L 2 -L P -NH-(CH 2 )n 1 -L a -L b -L c - wherein the antibody is connected to the terminal of L 1 , and the antitumor compound is connected to the terminal of L c with the nitrogen atom of the amino group at position 1 as a connecting position.
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公开(公告)号：EP3101032A1
公开(公告)日：2016-12-07
申请号：EP15743738.5
申请日：2015-01-28
发明人： NAITO, Hiroyuki , OGITANI, Yusuke , MASUDA, Takeshi , NAKADA, Takashi , YOSHIDA, Masao , ASHIDA, Shinji , MORITA, Koji , MIYAZAKI, Hideki , KASUYA, Yuji , HAYAKAWA, Ichiro , ABE, Yuki
IPC分类号： C07K16/28 , A61K31/4745 , A61K39/395 , A61P35/00 , C07D491/052
CPC分类号： C07K16/32 , A61K31/4745 , A61K39/395 , A61K47/6803 , A61K47/6849 , A61K47/6851 , A61K47/6855 , A61K47/6857 , A61K47/6859 , A61K47/6869 , A61K2039/505 , A61K2039/545 , C07D491/052 , C07D491/22 , C07K16/28 , C07K16/30 , C07K16/3015 , C07K16/3023 , C07K16/303 , C07K16/3046 , C07K16/3069 , C07K2317/24 , C07K2317/73
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: -L 1 -L 2 -L P -NH- (CH 2 ) n 1 -L a -(CH 2 )n 2 -C(=O)- wherein the anti-HER2 antibody is connected to the terminal L 1 , and the antitumor compound is connected to the carbonyl group of the -(CH 2 )n 2 -C(=O)-moiety with the nitrogen atom of the amino group at position 1 as the connecting position.
摘要翻译： 作为抗肿瘤效果和安全性优异并且具有优异治疗效果的抗肿瘤药物，提供了抗体 - 药物偶联物，其中由下式表示的抗肿瘤化合物通过接头与抗HER2抗体缀合 具有由下式表示的结构：-L 1 -L 2 -LP -NH-（CH 2）n 1 -L a - （CH 2）n 2 -C（= O） - 其中抗HER2抗体是 连接到末端L 1，并且将抗肿瘤化合物与位置1处氨基的氮原子连接到 - （CH 2）n 2 -C（= O） - 基团的羰基作为连接位置。
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公开(公告)号：EP2907824A1
公开(公告)日：2015-08-19
申请号：EP13845596.9
申请日：2013-10-10
发明人： MASUDA, Takeshi , NAITO, Hiroyuki , NAKADA, Takashi , YOSHIDA, Masao , ASHIDA, Shinji , MIYAZAKI, Hideki , KASUYA, Yuji , MORITA, Koji , ABE, Yuki , OGITANI, Yusuke
IPC分类号： C07K16/28 , A61K39/395 , A61P35/00 , A61K31/4745 , A61K31/48
CPC分类号： A61K47/6803 , A61K31/4745 , A61K31/48 , C07K16/2803 , C07K16/2827 , C07K16/2851 , C07K16/2875 , C07K16/2878 , C07K16/30 , C07K2317/30 , C07K2317/77
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: -L 1 -L 2 -L P -NH-(CH 2 )n 1 -L a -L b -L c -wherein the antibody is connected to the terminal of L 1 , and the antitumor compound is connected to the terminal of L c with the nitrogen atom of the amino group at position 1 as a connecting position.
摘要翻译： 作为在抗肿瘤效果和安全性方面优异的抗肿瘤药物，提供了抗体 - 药物偶联物，其中由下式表示的抗肿瘤化合物通过具有由下式表示的结构的接头与抗体缀合： -L 1 -L 2 -LP -NH-（CH 2）n 1 -L a -L b -L c - 其中抗体连接到L 1的末端，并且抗肿瘤化合物连接到L的末端 c，位置1处的氨基的氮原子作为连接位置。
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公开(公告)号：EP3342785A1
公开(公告)日：2018-07-04
申请号：EP18152381.2
申请日：2013-10-10
发明人： MASUDA, Takeshi , NAITO, Hiroyuki , NAKADA, Takashi , YOSHIDA, Masao , ASHIDA, Shinji , MIYAZAKI, Hideki , KASUYA, Yuji , MORITA, Koji , ABE, Yuki , OGITANI, Yusuke
IPC分类号： C07K16/28 , A61K39/395 , A61P35/00 , A61K31/4745 , A61K31/48 , A61K47/68
摘要： As an intermediate compound for preparing an antibody-drug conjugate in which an antitumor compound is conjugated to an antibody via a linker having a structure represented by the following formula: -L 1 -L 2 -L P -NH-(CH 2 )n 1 -L a -L b -L c - wherein the antibody is connected to the terminal of L 1 , and the antitumor compound is connected to the terminal of L c with the nitrogen atom of the amino group at position 1 as a connecting position, provided is N-[6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanoyl]glycylglycyl-L-phenylalanyl-N-[(carboxymethoxy)methyl]glycinamide represented by the following formula:
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8.发明公开ANTIBODY-DRUG CONJUGATE PRODUCED BY BINDING THROUGH LINKER HAVING HYDROPHILIC STRUCTURE 审中-公开通过结合与亲水结构的左MADE抗体 - 药物偶联
公开(公告)号：EP2910573A1
公开(公告)日：2015-08-26
申请号：EP13847461.4
申请日：2013-10-17
发明人： NAITO, Hiroyuki , NAKADA, Takashi , YOSHIDA, Masao , ASHIDA, Shinji , MASUDA, Takeshi , MIYAZAKI, Hideki , KASUYA, Yuji , ABE, Yuki , OGITANI, Yusuke
IPC分类号： C07K16/28 , A61K39/395 , A61P35/00 , A61K31/4745 , A61K31/48
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: -L 1 -L 2 -L P -NH-(CH 2 )n 1 -L a -L b -L c - or -L 1 -L 2 -L P - wherein the antibody is connected to the terminal of L 1 , the antitumor compound is connected to the terminal of L c or L P , and any one or two or more of linkers of L 1 , L 2 , and L P has a hydrophilic structure.
摘要翻译： 作为抗肿瘤药物全部具有优异的抗肿瘤效果和安全性方面的，提供对抗体 - 药物偶联物，在其中抗肿瘤由下式（I）表示的化合物在抗体经由具有由表示的结构的左缀合到 下式：-L 1 -L 2 -LP -NH-（CH 2）n的-L 1 -L一个-L b C - 或-L 1 -L 2 -LP - 其中所述抗体连接至L的终端 1，抗肿瘤化合物被连接到L C或LP的终端，以及任意一个或两个或更多个L 1，L 2的连接基的，和LP具有亲水结构。
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公开(公告)号：EP2910573B1
公开(公告)日：2020-02-19
申请号：EP13847461.4
申请日：2013-10-17
发明人： NAITO, Hiroyuki , NAKADA, Takashi , YOSHIDA, Masao , ASHIDA, Shinji , MASUDA, Takeshi , MIYAZAKI, Hideki , KASUYA, Yuji , ABE, Yuki , OGITANI, Yusuke
IPC分类号： C07K16/28 , A61K39/395 , A61P35/00 , A61K31/4745 , A61K31/48 , C07K16/00 , C07K16/30 , A61K47/68
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公开(公告)号：EP2907824B1
公开(公告)日：2018-04-11
申请号：EP13845596.9
申请日：2013-10-10
发明人： MASUDA, Takeshi , NAITO, Hiroyuki , NAKADA, Takashi , YOSHIDA, Masao , ASHIDA, Shinji , MIYAZAKI, Hideki , KASUYA, Yuji , MORITA, Koji , ABE, Yuki , OGITANI, Yusuke
IPC分类号： C07K16/28 , A61K39/395 , A61P35/00 , A61K31/4745 , A61K31/48 , A61K47/50
CPC分类号： A61K47/6803 , A61K31/4745 , A61K31/48 , C07K16/2803 , C07K16/2827 , C07K16/2851 , C07K16/2875 , C07K16/2878 , C07K16/30 , C07K2317/30 , C07K2317/77
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: -L 1 -L 2 -L P -NH-(CH 2 )n 1 -L a -L b -L c -wherein the antibody is connected to the terminal of L 1 , and the antitumor compound is connected to the terminal of L c with the nitrogen atom of the amino group at position 1 as a connecting position.
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