LABELED COMPOUNDS AND METHODS OF IMAGING, DIAGNOSING CARTILAGE DISORDERS AND DISEASES, AND MONITORING CARTILAGE HEALTH USING LABELED AND UNLABELED COMPOUNDS

摘要

Novel labeled compounds and metabolites thereof are disclosed, as well as pharmaceutical compositions including the compounds, and methods of using the labeled and unlabeled compounds, and specifically, 2-Amino-5-guanidino-pentanoic acid (3-{4-[3-(2-amino-5-guanidino-pentanoylamino)-propyl]-piperazin-1-yl}-propyl)-amide and metabolites thereof, for imaging, detecting and assessing disorders and diseases, such as arthritis and, more specifically, osteoarthritis by tracking proteoglycan and glycosaminoglycan content of cartilage. Also, pharmaceutical compositions comprising labeled and/or unlabeled 1,4-Bis(3-aminopropyl)piperazine are disclosed and methods of using the same.

主权项

1. A method of imaging comprising:
administering to a subject in need thereof a therapeutically effective amount of a labeled or unlabeled compound of formula I:
Y-M-X-L-A-L′-X′-M′-Y′  (I) or a pharmaceutically acceptable salt thereof, wherein: A is a substituted or unsubstituted aromatic or non-aromatic, carbocyclic or heterocyclic ring or a linear moiety; L and L′ are the same or different and are linkers; X and X′ are the same or different and are absent or are a functional group that attaches the linker L to M and linker L′ to M′, respectively; M and M′ are the same or different and are absent or is a linker that attaches X to Y and X′ to Y′, respectively; and Y and Y′ are the same or different and are a moiety containing one or more cationic atoms or groups or one or more groups that become cationic under physiological conditions; and obtaining an image.