US 2014/0154181 A1 · RGD-CONTAINING PEPTIDOMIMETICS AND USES THEREOF

Abstract

The invention provides RGD-containing cyclic peptidomimetics; conjugates of said peptidomimetics and a moiety of a payload selected from fluorescent probes, photosensitizers, chelating agents, or cytotoxic agents; and pharmaceutical compositions comprising these conjugates. The conjugates of the invention are useful both for diagnostic purposes and treatment of various diseases, disorders and conditions. More specifically, conjugates comprising fluorescent probes can be used for diagnostic purposes, e.g., visualization of organs and tissues, and diagnosis of tumors; conjugates comprising photosensitizers can be used for photodynamic therapy of both tumors and nonneoplastic tissues; conjugates comprising chelating agents can be used in radioimaging or radiotherapy; and conjugates comprising cytotoxic agents can be used for targeted chemotherapy.

Claims17

Dependent claims

An arginine-glycine-aspartic acid (RGD)-containing cyclic peptidomimetic of the general formula II:

wherein
A1 is a natural or non-natural amino acid residue bearing either an amino or carboxyl group on its side chain, linked via its α- or side chain carboxyl group to the α-amino group of the arginine residue and via its α- or side chain amino group to the backbone C═O;
A2 is a natural or non-natural amino acid residue linked via its α-amino group to the backbone C═O and via its α-carboxyl group to the α- or side chain amino group of A3;
and
A3 is a natural or non-natural amino acid residue bearing an amino group on its side chain and amidated at its C-terminus, linked via one of its α- or side chain amino group to the carboxyl group of A2 and via another of its α- or side chain amino group to the α-carboxyl group of the aspartic acid residue.

2 more elements

Dependencies are inferred from the claim text.

Facts

Application

14/175,302Filed 7 Feb 2014

Priority

23 Oct 2008

Published

5 Jun 2014

Term ends

Not estimatedThe source records don’t support an estimate.

Classification12 codes

C07K 7/64
Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof: cyclic peptides containing only normal peptide links
A61K 47/64
The modifying agent being a protein, peptide or polyamino acid: drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying…
A61K 49/0056
Characterised by the carrier molecule carrying the fluorescent agent: peptides, proteins, polyamino acids
A61P 3/04
Drugs for disorders of the metabolism: anorexiants; Antiobesity agents

Family

Application61/107,952Us provisional application · filed 23 Oct 2008

Application13/125,371Division · filed 29 Jun 2011

Application14/175,302Division

US 2011/0250144 A1Published application

US 8,673,270 B2Related patent

US 9,119,885 B2Related patent

US 2014/0154181 A1This patent

From the US filing history. Foreign family members aren’t listed.

Rgd-containing peptidomimetics and uses thereof

Life of this patent

Rgd-containing peptidomimetics and uses thereof

Life of this patent

Abstract

Claims17