Patent ID: 8815213
Filing Date: 2014-08-26
Classification: A61K,A61P,C07D

Abstract:
1. A method for diagnosis and visualization of tumor necrotic domains by minimally invasive imaging of tumors, said method comprising: (i) administering to a subject suspected of having a tumor with necrotic domains a conjugate of an RGD-containing peptide or a non-peptidic compound that mimics a peptide and has the RGD motif and a photosensitizer; (ii) imaging the subject at least 24-48 hours after said administration; and (iii) diagnosing the presence or absence of said tumor necrotic domains, wherein said photosensitizer is a chlorophyll or bacteriochlorophyll of the formula II: wherein M represents 2H or an atom selected from the group consisting of Mg, Pd, Pt, Co, Ni, Sn, Cu, Zn, Mn, In, Eu, Fe, Au, Al, Gd, Dy, Er, Yb, Lu, Ga, Y, Rh, Ru, Si, Ge, Cr, Mo, P, Re, Tc and Ti and isotopes and radio-isotopes thereof; R Y is O or S; R R′ R (a) H; (b) C (c) C (d) C (e) C (f) C (g) C (h) a residue of an amino acid, an RGD-containing peptide or a non-peptidic compound that mimics a peptide and has the RGD motif, a protein, a monosaccharide, an oligosaccharide, a polysaccharide; or a polydentate ligand and its chelating complexes with metals; R R A m is 0 or 1; Hal is a halogen selected from fluoro, chloro, bromo or iodo; the dotted line at positions 7-8 represents an optional double bond; and pharmaceutically acceptable salts and optical isomers thereof; wherein said carbocyclic moiety is a saturated or partially unsaturated monocyclic or polycyclic compound containing only carbon atoms in the ring(s); said heterocyclic moiety or said heterocyclyl is a radical derived from a mono- or poly-cyclic heteroaromatic ring containing one to three O, S and/or N heteroatoms, selected from the group consisting of pyrrolyl, furyl, thienyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, pyridyl, quinolinyl, pyrimidinyl, 1,3,4-triazinyl, 1,2,3-triazinyl, 1,3,5-triazinyl, benzofuryl, isobenzofuryl, indolyl, imidazo[1,2-a]pyridyl, benzimidazolyl, benzthiazolyl and benzoxazolyl; and wherein said carbocyclic and heterocyclic moieties are optionally substituted by one or more radicals selected from the group consisting of halogen, C and wherein said chlorophyll or bacteriochlorophyll contains at least one RGD-containing peptide or a non-peptidic compound that mimics a peptide and has the RGD motif.