Daiichi Sankyo Company, Limited

Shinji Ashida

Takeshi Masuda

Takashi Nakada

Hideki Miyazaki

Hiroyuki Naito

Masao Yoshida

Yuji Kasuya

Yuki Abe

Yusuke Ogitani

Koji Morita

Ichiro Hayakawa

Narihiro Toda

Mitsuhiro Iwamoto

Kensuke Nakamura

Hiroaki Uchida

Yusuke Ota

Daisuke Okajima

Hirofumi Hamada

Tomoko Terauchi

Masaki Meguro

Fuminao Doi

Naoya Harada

Takahiro Katagiri

Rieko Takano

Takeshi Shida

Mami Yamazaki

The present invention provides a novel antibody-pyrrolodiazepine derivative and a novel antibody-pyrrolodiazepine derivative conjugate using the same, and a novel CLDN6 and/or CLDN9 antibody.

Methods of treating a tumor by administering a claudin-6 (CLDN6) or CLDN9 antibody-pyrrolobenzodiazepine derivative conjugate

Provided are novel antibody-pyrrolodiazepine derivative and novel antibody-pyrrolodiazepine derivative conjugates, as well as methods of using the same, and a novel CLDN6 and/or CLDN9 antibody. The disclosed compounds are of the class of alkyl benzene sulfonyl ureas, useful as oral anti-diabetics, and include substituted benzo[e]pyrrolo[1,2-α][1,4]diazepine.

Antibody-drug conjugates comprising substituted benzo[e]pyrrolo[1,2-a][1,4]diazepines

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-L-L-NH—(CH)n-L-L-L- wherein the antibody is connected to the terminal of L, and the antitumor compound is connected to the terminal of Lwith the nitrogen atom of the amino group at position 1 as a connecting position.

Antibody-drug conjugate

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-L-L-NH&#x2014;(CH)n-L-(CH)n-C(&#x2550;O)&#x2014; wherein the anti-HER2 antibody is connected to the terminal L, and the antitumor compound is connected to the carbonyl group of the &#x2014;(CH)n-C(&#x2550;O)&#x2014; moiety with the nitrogen atom of the amino group at position 1 as the connecting position

Method for treating cancer comprising administration of anti-HER2 antibody-drug conjugate

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-L-L-NH&#x2014;(CH)n-L-L-L- wherein the antibody is connected to the terminal of L, and the antitumor compound is connected to the terminal of Lwith the nitrogen atom of the amino group at position 1 as a connecting position.

A novel antibody-pyrrolodiazepine derivative and a novel antibody-pyrrolodiazepine derivative conjugate using the same, comprising substituted benzo[e]pyrrolo[1,2-a][1,4]diazepines represented by the [Formula 24], [Formula 25], [Formula 26], and/or [Formula 27].

Antibody-drug conjugates comprising substituted benzo[e]pyrrolo[1,2-&#x3b1;][1,4]diazepines

Antibody-pyrrolobenzodiazepine derivative conjugate and method of use thereof for treating a tumor

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-L-L-NH&#x2014;(CH)n-L-(CH)n-C(&#x2550;O)&#x2014; wherein the anti-HER2 antibody is connected to the terminal L, and the antitumor compound is connected to the carbonyl group of the &#x2014;(CH)n-C(&#x2550;O)&#x2014; moiety with the nitrogen atom of the amino group at position 1 as the connecting position. 

Method of treating cancer comprising administration of anti-HER2 antibody-drug conjugate

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: L-L-L-NH&#x2014;(CH)n-L-L-Lor -L-L-L- wherein the anti-HER2 antibody is connected to the terminal L, and the antitumor compound is connected to the terminal Lor Lwith the nitrogen atom of the amino group at position 1 as the connecting position. 

(Anti-HER2 antibody)-drug conjugate

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-L-L-NH&#x2014;(CH)n-L-L-L- or -L-L-L- wherein the antibody is connected to the terminal of L, the antitumor compound is connected to the terminal of Lor L, and any one or two or more of linkers of L, L, and Lhas a hydrophilic structure.

Antibody-drug conjugate produced by binding through linker having hydrophilic structure

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-L-L-NH&#x2014;(CH)-L-L-L-wherein the antibody is connected to the terminal of L, and the antitumor compound is connected to the terminal of Lwith the nitrogen atom of the amino group at position 1 as a connecting position.

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Tokyo, Japan

Shinji Ashida