Back to results
US 2026/0061084 A1Published application
Fibroblast activation protein (fap) inhibitors, fap conjugates, and diagnostic and therapeutic uses thereof
AssigneesNuclidium AG, University of Basel
InventorsLeila JAAFAR-THIEL, Melpomeni FANI, Jacopo MILLUL, Francesco DE ROSE
Life of this patent
Estimating the term…
Abstract
The present disclosure relates to the field of fibroblast activation protein (FAP) inhibitors, conjugates comprising the novel FAP inhibitors, including radiotracers, for the imaging, diagnosis and treatment of conditions characterized by overexpression of FAP.
Claims33
A compound, wherein the compound is of Formula I:
- wherein:
- R1 is Ra;
- R2 and R3 are each Ra or together form a C2-9 heterocycle with the nitrogen atoms to which they are attached;
- R4 is H or an amine protecting group;
- Ra, independently for each occurrence, is selected from H, C1-10 alkyl, C2-10 alkenyl, C3-10 alkynyl, C3-10 cycloalkyl, C6-10 aryl, C2-9 heterocyclyl, or C5-9 heteroaryl, optionally substituted by one or more substituents selected from —OH, —OR′, ═O, ═S, —SH, —SR′, —NH2, —NHR′, —N(R′)2, —NHCOR′, —NR′COR′, halogen, —CN, —CO2H, —CO2R′, —CHO, —COR′, —CONH2, —CONHR′, —CON(R′)2, —NO2, —OP(O)(OH)2, —SO3H, —SO3R′, —SOR′, and —SO2R′, wherein R′, independently for each occurrence, is C1-10 alkyl or C3-10 cycloalkyl;
- n is an integer from 1 to 20;
- and
- m is an integer from 1 to 20;
- or is a pharmaceutically acceptable salt thereof.
6 more elements
(canceled)
-54. (canceled)
(canceled)
(canceled)
-65. (canceled)
-70. (canceled)
-140. (canceled)
Dependencies are inferred from the claim text.