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US 10,471,162 B2Granted
Collagen targeted imaging probes
AssigneeThe General Hospital Corporation
InventorsPauline Desogere, Peter Caravan
Life of this patent
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Abstract
Disclosed herein are collagen-targeted imaging agents for positron emission tomography and related imaging methods using the collagen-targeted imaging agents. The collagen-targeted imaging agent is a cyclic polypeptide comprising a cyclic main body, wherein the cyclic main body comprises at least one S—S bond; at least two branches, wherein each of the at least two branches comprises at least three amino acids; and a linker, wherein the linker is capable of linking an imaging reporter.
Claims31
A cyclic polypeptide of formula (I):
- wherein R1 is selected from the group consisting of lysine (K), tyrosine (Y), glutamic acid (E), aspartic acid (D), arginine (R) and leucine (L);
- wherein R2 is selected from the group consisting of -glycine (G)-tryptophan (W) and -glycine (G)-lysine (K)[glycine (G)];
- wherein R3 is selected from the group consisting of leucine (L) and phenylalanine (F);
- wherein R4 is selected from the group consisting of tyrosine (Y) and 2-Nal (2-naphthylalanine);
- wherein R5 is selected from the group consisting of glycine (G) and BIP (L-4,4′-biphenylalanine);
- wherein R6 is selected from the group consisting of threonine (T) and tyrosine (Y);
- and
- wherein the cyclic polypeptide further comprises a linker that is capable of linking an imaging reporter;
- or
- a cyclic polypeptide of formula (I):
- wherein:
- R1 is lysine (K)-NODAGA,
- R2 is NODAGA-glycine (G)-lysine (K)[glycine (G)-NODAGA],
- R3 is leucine (L),
- R4 is tyrosine (Y),
- R5 is 4,4-biphenylalanine (BIP), and
- R6 is threonine (T), and
- wherein the cyclic polypeptide comprises an imaging reporter;
- or
- a cyclic peptide of formula (I):
- wherein:
- R1 is tyrosine (Y),
- R2 is NODAGA-glycine (G)-glutamine(Q),
- R3 is leucine (L),
- R4 is tyrosine (Y),
- R5 is glycine (G), and
- R6 is threonine (T), and
- wherein the cyclic polypeptide comprises an imaging reporter;
- or
- a cyclic peptide of formula (I):
- wherein:
- R1 is aspartic acid (D),
- R2 is NODAGA-glycine (G)-glutamine(Q),
- R3 is leucine (L),
- R4 is 2-naphthylalanine (2-Nal),
- R5 is glycine (G), and
- R6 is threonine (T), and
- wherein the cyclic polypeptide comprises an imaging reporter;
- or
- a cyclic polypeptide of formula (I):
- wherein:
- R1 is arginine (R),
- R2 is NODAGA-glycine (G)-glutamine(Q),
- R3 is phenylalanine (F),
- R4 is tyrosine (Y),
- R5 is glycine (G), and
- R6 is threonine (T), and
- wherein the cyclic polypeptide comprises an imaging reporter;
- or
- a cyclic polypeptide of formula (I):
- wherein:
- R1 is leucine (L),
- R2 is NODAGA-glycine (G)-glutamine(Q),
- R3 is leucine (L),
- R4 is tyrosine (Y),
- R5 is glycine (G), and
- R6 is tyrosine (Y), and
- wherein the cyclic polypeptide comprises an imaging reporter;
- or
- a cyclic polypeptide of formula (I):
- wherein:
- R1 is glutamic acid (E),
- R2 is NODAGA-glycine (G)-glutamine(Q),
- R3 is leucine (L),
- R4 is tyrosine (Y),
- R5 is 4,4-biphenylalanine (BIP), and
- R6 is threonine (T), and
- wherein the cyclic polypeptide comprises an imaging reporter.
65 more elements
A compound having the following structure:
- or pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.