US 11,918,656 B2
Antibody-drug-conjugate and its use for the treatment of cancer
Ian Rilatt, Castres (FR); Michel Perez, Castres (FR); and Marie Lamothe, Montredon Labessonnie (FR)
Assigned to PIERRE FABRE MEDICAMENT, Boulogne-Billancourt (FR)
Filed by PIERRE FABRE MEDICAMENT, Boulogne-Billancourt (FR)
Filed on Nov. 15, 2021, as Appl. No. 17/454,931.
Application 16/385,597 is a division of application No. 15/306,404, granted, now 10,314,921, issued on Jun. 11, 2019, previously published as PCT/EP2015/059052, filed on Apr. 27, 2015.
Application 17/454,931 is a continuation of application No. 16/385,597, filed on Apr. 16, 2019, granted, now 11,219,693.
Claims priority of application No. 14305621 (EP), filed on Apr. 25, 2014.
Prior Publication US 2022/0105195 A1, Apr. 7, 2022
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 47/68 (2017.01); A61P 35/00 (2006.01)
CPC A61K 47/6803 (2017.08) [A61K 47/6855 (2017.08); A61K 47/6857 (2017.08); A61K 47/6859 (2017.08); A61K 47/6863 (2017.08); A61K 47/6865 (2017.08); A61K 47/6867 (2017.08); A61K 47/6869 (2017.08); A61P 35/00 (2018.01)] 11 Claims
 
1. A method for treating a cancer selected from the group consisting of breast cancer, lung cancer, and kidney carcinoma, in a person in need thereof, wherein the method comprises administering to said person a therapeutically effective amount of a compound of the following formula:

OG Complex Work Unit Chemistry
or a pharmaceutically acceptable salt thereof,
wherein:
R1 is H or OH,
R2 is a (C1-C6)alkyl, COOH, COO—(C1-C6)alkyl or thiazolyl group,
R3 is H or a (C1-C6)alkyl group, and
H-A- is:
a group of formula Het-Alk-, wherein Alk is a (C1-C8)alkanediyl group and is linked to NR3, and Het is a heterocycle optionally substituted by a (C1-C6)alkyl group and containing at least one nitrogen atom linked to a hydrogen atom, or
a group of formula H-Aa-Ab-, wherein Aa is O or NR9 with R9 being H or (C1-C6)alkyl, and Ab is linked to NR3 and is:
a (C1-C8)alkanediyl group,
a —(CH2CH2X1)a1(CH2CH2X2)a2(CH2CH2X3)a3(CH2CH2X4)a4CH2CH2— group with X1, X2, X3 and X4 each independently of one another being O or NR8; a1, a2, a3 and a4 each independently of one another being 0 or 1; and R8 being H or a (C1-C6)alkyl group, or
an aryl-(C1-C8)alkanediyl or heterocycle-(C1-C8)alkanediyl group, said group being optionally substituted by a (C1-C6)alkyl group, the aryl or heterocycle moiety being linked to Aa and the (C1-C8)alkanediyl moiety being linked to NR3.