US 11,027,029 B2 · Peptide thiourea derivative, radioisotope labeled compound containing same, and pharmaceutical composition containing same as active ingredient for treating or diagnosing prostate cancer

Abstract

The present invention relates to a peptide thiourea derivative, a pharmaceutically acceptable salt thereof, a radioisotope labeled compound comprising the same, and a pharmaceutical composition for treating or diagnosing prostate cancer comprising the same as an active ingredient. The peptide thiourea derivative of the present invention is excellent in stability in human serum when it is administered in vivo and not only binds well to PSMA expressed in prostate cancer but also inhibits excellently PSMA at a low concentration. Besides, the derivative of the invention has a high water-solubility and can be excreted through the kidney not through the bile passage so that a clear image of the tumor region of prostate cancer can be obtained. Therefore, the derivative of the present invention can be effectively used as a pharmaceutical composition for treating and diagnosing prostate cancer.

Claims12

Dependent claims

A compound represented by formula 1 below or a pharmaceutically acceptable salt of the same:

wherein
X is single bond;
n is an integer of 3;
Y is —N(CH2COOH)(CH2)aCH2CH2—,
m is an integer of 1 or 2;
and
a, b and c are independently an integer of 0 or 1.

4 more elements

Dependencies are inferred from the claim text.

Facts

Application

15/774,632Filed 9 Nov 2016

Priority

KR 10-2015-01565369 Nov 2015

Published

US 2018/0339071 A129 Nov 2018

Granted

8 Jun 2021

Term ends

Not estimatedThe source records don’t support an estimate.

Classification16 codes

A61K 51/044
Heterocyclic compounds: having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
A61K 31/41
Having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins: having five-membered rings with two or more ring hetero atoms, at least…
A61K 51/0402
Organic compounds: carboxylic acid carriers, fatty acids
A61K 51/0482
Complexes or complex-forming compounds, i.e. wherein a radioactive metal is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group:…

Peptide thiourea derivative, radioisotope labeled compound containing same, and pharmaceutical composition containing same as active ingredient for treating or diagnosing prostate cancer

Life of this patent

Peptide thiourea derivative, radioisotope labeled compound containing same, and pharmaceutical composition containing same as active ingredient for treating or diagnosing prostate cancer

Life of this patent

Abstract

Claims12