US 10,238,758 B2 · Radiolabeled alpha-melanocyte stimulating hormone hybrid peptide for melanoma targeting

Abstract

The present invention is directed to novel non-invasive diagnostic tools/compounds to image cancers, especially, melanoma, including metastatic melanoma in vivo. The present compounds exhibit enhanced uptake in cancerous cells and tissue, suggesting favorable selective activity of compounds according to the present invention, which can be used as effective therapeutic agents against melanoma, including metastatic melanoma. The compounds according to the present invention represent an advance in the diagnosis and treatment of melanoma, including metastatic melanoma using non-invasive molecular imaging techniques. The novel probes of the present invention are useful to initiate therapy for melanoma as well as monitor patients' response to chemotherapy treatments and other interventions or therapies used in the treatment of melanoma/metastatic melanoma. Compounds according to the present invention may be used as diagnostic and therapeutic tools for a number of conditions and diseases states, especially melanoma.

Claims19

Dependent claims

A compound according to the chemical structure:

Where Q, V and W are each independently an amino acid unit selected from the group consisting of glutamic acid and aspartic acid;
R is an amino acid unit selected from the group consisting of valine, threonine, leucine, and isoleucine;
X is an amino acid residue selected from the group consisting of alanine, valine, threonine, leucine, isoleucine and serine;
Y is an amino acid residue selected from the group consisting of aspartic acid and glutamic acid;
L is alanine or a linker group according to the structure:
p is an integer from 0 to 20;
k is an integer from 1 to 10;
i is 1 or 2;
s is 0, 1 or 2;
and
M is a radioisotope, or
a pharmaceutically acceptable salt thereof.

9 more elements

Dependencies are inferred from the claim text.

Facts

Application

15/261,890Filed 10 Sep 2016 · continuation

Priority

29 Sep 2011

Published

US 2017/0087259 A130 Mar 2017

Granted

26 Mar 2019

Term ends

Not estimatedThe source records don’t support an estimate.

Classification7 codes

A61K 51/086
Peptides, e.g. proteins , carriers being peptides, polyamino acids, proteins: the peptide being alphaMSH, alpha melanocyte stimulating hormone
A61K 38/17
Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof: from animals; from humans
A61K 51/082
Peptides, e.g. proteins , carriers being peptides, polyamino acids, proteins: the peptide being a RGD-containing peptide
C07K 7/56
With at least one abnormal peptide link in the ring: the cyclisation not occurring through 2,4-diamino-butanoic acid

Family

Application61/540,814Us provisional application · filed 29 Sep 2011

Application13/617,042Parent of this continuation · filed 14 Sep 2012

US 2017/0087259 A1Pre-grant publication · published 30 Mar 2017

US 9,463,255 B1Parent of this continuation

US 10,238,758 B2This patent

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

Radiolabeled alpha-melanocyte stimulating hormone hybrid peptide for melanoma targeting

Life of this patent

Radiolabeled alpha-melanocyte stimulating hormone hybrid peptide for melanoma targeting

Life of this patent

Abstract

Claims19