US 12,747,224 B2 · Fibroblast activation protein ligands for targeted delivery applications

Abstract

The present invention relates to ligands of Fibroblast Activation Protein (FAP) for the active delivery of various payloads (e.g. cytotoxic drugs, radionuclides, fluorophores, proteins and immunomodulators) at the site of disease. In particular, the present invention relates to the development of FAP ligands for targeting applications, in particular diagnostic methods and/or methods for therapy or surgery in relation to a disease or disorder, such as cancer, inflammation or another disease characterized by overexpression of FAP.

Claims6

Dependent claims

A compound having one the following structures, its individual diastereoisomers, its hydrates, its solvates, its crystal forms, its individual tautomers or a pharmaceutically acceptable salt thereof:

#
Structure
1
2
3
4
5
6
7
8
9
10
11
12
13
14
15
18
21
26
27
30
31
34
34a
35
36
37
37a
38
39
40
41
42
43
43a
44
45
46
47
48
49
50
51
52
53
54
55
56
57
58 58a 58b 58c 58d 58e 58f
R derived from AA:
Glycine Alanine Valine Isoleucine Proline Arginine
59 59a 59b 59c
R H CH3 CH3
R‘ H H CH3
60 60a 60b 60c
R H CH3 CH3
R‘ H H CH3
64
65
66
67
68

61 more elements

Dependencies are inferred from the claim text.

Facts

Application

17/799,611Filed 12 Feb 2021

Priority

EP 2015703612 Feb 2020

Published

US 2023/0147962 A111 May 2023

Granted

29 Sep 2026

Term ends

Not estimatedThe source records don’t support an estimate.

Classification21 codes

C07D 401/12
Containing two hetero rings: linked by a chain containing hetero atoms as chain links
C07D 401/14
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a…:…
A61K 47/545
The modifying agent being an organic compound: heterocyclic compounds
A61K 47/55
The modifying agent being an organic compound: the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire…

Fibroblast activation protein ligands for targeted delivery applications

Life of this patent

Fibroblast activation protein ligands for targeted delivery applications

Life of this patent

Abstract

Claims6