US 9,808,537 B2Granted

Antibody-drug conjugate

AssigneeDaiichi Sankyo Company, Limited

InventorsTakeshi Masuda, Hiroyuki Naito, Takashi Nakada, Masao Yoshida, Shinji Ashida, Hideki Miyazaki, Yuji Kasuya, Koji Morita, Yuki Abe, Yusuke Ogitani

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Abstract

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.

Claims18

Dependent claims

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:
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.

Dependencies are inferred from the claim text.

Facts

Application: 15/180,203Filed 13 Jun 2016 · continuation
Priority: JP 2012-22588711 Oct 2012
Published: US 2016/0279259 A129 Sep 2016
Granted: 7 Nov 2017
Term ends: Not estimatedThe source records don’t support an estimate.

Classification22 codes

A61K 31/4745
Ortho- or peri-condensed with heterocyclic ring systems: condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
A61K 31/48
Quinolines; Isoquinolines: ergoline derivatives, e.g. lysergic acid, ergotamine
A61K 47/68037
Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates: the drug being a camptothecin [CPT] or derivatives
A61K 47/6849
The modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site: the antibody targeting a receptor, a cell…

Family

PCT/JP2013/006069Parent of this continuation · filed 10 Oct 2013
US 2016/0279259 A1Pre-grant publication · published 29 Sep 2016
Application14/435,114Parent of this continuation
US 10,117,952 B2Related patent
US 10,195,288 B2Related patent
US 2015/0297748 A1Published application
US 9,808,537 B2This patent

From the US filing history. Foreign family members aren’t listed.