	US 12,187,708 B2
	Near-infrared cyanine dyes and conjugates thereof
Francesco Blasi, Rivarolo Canavese (IT); Federica Buonsanti, Turin (IT); Federico Crivellin, Grugliasco (IT); Andrea Ferraris, Genoa (IT); Laura Orio, Turin (IT); Lorena Pizzuto, San Francesco al Campo (IT); Roberta Napolitano, Albiano d'Ivrea (IT); and Giovanni Valbusa, Stresa (IT)
Assigned to BRACCO IMAGING S.P.A., Milan (IT)
Filed by BRACCO IMAGING S.P.A., Milan (IT)
Filed on Nov. 10, 2023, as Appl. No. 18/388,604.
Application 18/388,604 is a continuation of application No. 18/010,905, previously published as PCT/EP2021/066920, filed on Jun. 22, 2021.
Claims priority of application No. 20181771 (EP), filed on Jun. 23, 2020.
Prior Publication US 2024/0083880 A1, Mar. 14, 2024
This patent is subject to a terminal disclaimer.
Int. Cl. C07D 403/10 (2006.01); C07D 403/14 (2006.01); C09B 23/01 (2006.01)

CPC C07D 403/10 (2013.01) [C07D 403/14 (2013.01); C09B 23/0066 (2013.01); C09B 23/0075 (2013.01)]

9 Claims

1. A compound of formula (II)

wherein

X is direct bond or —O—;

Y is a group selected from linear or branched C₁-C₆alkyl, C₃-C₇cycloalkyl and heterocyclyl, substituted by at least two hydroxyl groups;

R1 is linear or branched C₁-C₆alkyl substituted by a group selected from —SO₃H, —COOH, —CONH₂and —COO—C₁-C₆alkyl;

R4 is linear or branched C₁-C₆alkyl substituted by a group selected from —SO₃H, —COOH and —CONH—(S)_m-T, wherein

S is a spacer;

T is a targeting moiety interacting with an integrin receptor and comprising the sequence Arg-Gly-Asp; and

m is an integer equal to 0 or 1; and

R5 is selected from hydrogen, —SO₃H, a linear or branched C₁-C₆alkyl substituted by —COOH or —CONH—Y, and a group CONH—(S)_m-T, wherein Y, S, T and m are defined above;

and wherein at least one between R4 and R5 is linear or branched C₁-C₆alkyl substituted by CONH—(S)_m-T,

or a stereoisomer or pharmaceutically acceptable salt thereof.