	US 12,274,745 B2
	Conjugate of CAPRIN-1 antibody linked to immune activator for cancer treatment
Fumiyoshi Okano, Kamakura (JP); and Takanori Saito, Kamakura (JP)
Assigned to TORAY INDUSTRIES, INC., Tokyo (JP)
Appl. No. 16/344,689
Filed by TORAY INDUSTRIES, INC., Tokyo (JP)
PCT Filed Oct. 27, 2017, PCT No. PCT/JP2017/038986 § 371(c)(1), (2) Date Apr. 24, 2019, PCT Pub. No. WO2018/079740, PCT Pub. Date May 3, 2018.
Claims priority of application No. 2016-211376 (JP), filed on Oct. 28, 2016.
Prior Publication US 2020/0054762 A1, Feb. 20, 2020
Int. Cl. C07K 16/46 (2006.01); A61K 31/4745 (2006.01); A61K 39/39 (2006.01); A61K 39/395 (2006.01); A61K 47/68 (2017.01); A61P 35/02 (2006.01)

CPC A61K 39/39 (2013.01) [A61K 31/4745 (2013.01); A61K 39/3955 (2013.01); A61K 47/6803 (2017.08); A61K 47/6849 (2017.08); A61P 35/02 (2018.01)]

11 Claims

1. A conjugate of an antibody linked to an immune activator,

wherein the antibody or the fragment thereof has immunological reactivity with a CAPRIN-1 protein of any of even-numbered SEQ ID NOs among SEQ ID NO: 2 to 30, wherein the immune activator is an imidazoquinoline compound which is a TLR7- or TLR8-binding ligand or agonist, and

wherein the antibody is linked to the immune activator via a linker;

wherein said imidazoqjuinoline compound is 4-amino-2-(ethoxymethyl)-a,a-dimethyl-1H-imidazo[r4,5-c]quinoline-1-ethanol or 1-(2(2-aminoethoxy)-2-methylpropyl)-2-(ethoxymethyl)-1H-imidazo[4,5-c˜quinolin-4-amine; and

wherein said linker is maleimidocaproyl-valine-citrulline-p-aminobenzyloxycarbonyl (MC-val-Cit-PAB) or succinimidyl 4-(N-maleimidomethyl)cyclohexane-1-carboxylate (SMCC).