US 9,808,537 B2
Antibody-drug conjugate
Takeshi Masuda, Tokyo (JP); Hiroyuki Naito, Tokyo (JP); Takashi Nakada, Tokyo (JP); Masao Yoshida, Tokyo (JP); Shinji Ashida, Tokyo (JP); Hideki Miyazaki, Tokyo (JP); Yuji Kasuya, Tokyo (JP); Koji Morita, Tokyo (JP); Yuki Abe, Tokyo (JP); and Yusuke Ogitani, Tokyo (JP)
Assigned to Daiichi Sankyo Company, Limited, Tokyo (JP)
Filed by Daiichi Sankyo Company, Limited, Tokyo (JP)
Filed on Jun. 13, 2016, as Appl. No. 15/180,203.
Application 15/180,203 is a continuation of application No. 14/435,114, previously published as PCT/JP2013/006069, filed on Oct. 10, 2013.
Claims priority of application No. 2012-225887 (JP), filed on Oct. 11, 2012.
Prior Publication US 2016/0279259 A1, Sep. 29, 2016
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 47/50 (2017.01); C07D 491/052 (2006.01); A61K 47/48 (2006.01); A61K 31/4745 (2006.01); A61K 31/48 (2006.01); C07K 16/30 (2006.01); C07K 16/28 (2006.01)
CPC A61K 47/48715 (2013.01) [A61K 31/4745 (2013.01); A61K 31/48 (2013.01); C07K 16/2803 (2013.01); C07K 16/2827 (2013.01); C07K 16/2851 (2013.01); C07K 16/2875 (2013.01); C07K 16/2878 (2013.01); C07K 16/30 (2013.01); C07K 2317/30 (2013.01); C07K 2317/77 (2013.01)] 18 Claims
 
1. An antibody-drug conjugate, comprising a linker that is connected to an antibody, having the following formula:
-(Succinimid-3-yl-N)—CH2CH2CH2CH2CH2—C(═O)-GGFG-NH—CH2—O—CH2—C(═O)—
and an antitumor compound that is connected to the linker, wherein -(Succinimid-3-yl-N)— has a structure having the following formula:

OG Complex Work Unit Drawing
which is connected to the antibody at position 3 thereof and is connected to a methylene group in the linker containing this structure on the nitrogen atom at position 1, and the antitumor compound is connected to the carbon atom of the carbonyl group within the —NH—CH2—O—CH2—C(═O)— moiety.