# US 11,077,217 B2 · Radioactive labeling method for neuropeptide Y derivative compound and medicine for multi-type breast cancer therapy thereof

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- Number: US 11,077,217 B2
- Document ID: US11077217B2
- Status: Granted
- Kind: B2
- Application number: 16/215,647
- Filed: 2018-12-11
- Published: 2020-07-30
- Granted: 2021-08-03
- Earliest claimed: 2018-12-11
- Assignees: Institute of Nuclear Energy Research Atomic Energy Council, Executive Yuan
- Applicants: Ming-Hsin Li; Su-Jung Chen; Ming-Wei Chen; Yuan-Ruei Huang; Shih-Ying Lee; Chun-Fang Feng; Sheng-Nan Lo; Chih-Hsien Chang
- Inventors: Ming-Hsin Li; Su-Jung Chen; Ming-Wei Chen; Yuan-Ruei Huang; Shih-Ying Lee; Chun-Fang Feng; Sheng-Nan Lo; Chih-Hsien Chang
- Web page: https://patentgrep.com/patent/US11077217B2

## CPC

- A61K 47/64: Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent (peptidic linkers A61K47/65)
- A61K 51/088: {conjugates with carriers being peptides, polyamino acids or proteins (antibodies A61K51/10)}
- A61K 41/0095: {Boron neutron capture therapy, i.e. BNCT, e.g. using boronated porphyrins}
- A61K 51/0482: {chelates from cyclic ligands, e.g. DOTA}
- A61K 51/0497: {conjugates with a carrier being an organic compounds}
- A61K 51/065: {conjugates with carriers being macromolecules}
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

The present invention provides a radioactive labeling method for neuropeptide Y (NPY) compound and a mammalian diagnostic radioactive targeting medicine with NPY peptide being modified at position 27th to 36th, and after binding with the chelating agent and labeling the radiation nucleus 66Ga67Ga68Ga177Lu or 111In to provide a radioactive targeting medicine for multi-type breast cancer diagnosis and treatment.

## Claims

### Claim 1

A neuropeptide Y (NPY) derivative compound of Formula 1,
wherein R1 is a metal chelating agent;
EB*is Evans Blue or Evans Blue-lysine;
R2 is a first linker selected from the group consisting of 1 to 10 amino acids and 4 to 10 polyethylene glycol (PEG);
R2′ is a second linker selected from the group consisting of 1 to 10 amino acids and 4 to 10 polyethylene glycol (PEG);
B1 is C4H11B10O3 or S10B12H11; and
NPY derivative is selected from the group consisting of SEQ ID NO. 1, SEQ ID NO. 2, and SEO ID NO. 3.

### Claim 2 (depends on 1)

The neuropeptide Y (NPY) derivative compound of claim 1, wherein the metal chelating agent R1 is DOTA, NOTA, or DTPA.

### Claim 3 (depends on 1)

The neuropeptide Y (NPY) derivative compound of claim 1, wherein the boron-containing molecule B1 at NH2 side is bonded with an amino acid K (Lys).

### Claim 4 (depends on 1)

The neuropeptide Y (NPY) derivative compound of claim 1, wherein EB* is Evans Blue-lysine-.

### Claim 5 (depends on 1)

The neuropeptide Y (NPY) derivative compound of claim 1, wherein NPY derivative is SEQ ID NO. 1 or SEQ ID NO. 2.

### Claim 6 (depends on 1)

The neuropeptide Y (NPY) derivative compound of claim 1, wherein the NPY derivative is SEQ ID NO. 3.

### Claim 7 (depends on 1)

The neuropeptide Y (NPY) derivative compound of claim 1, wherein the NPY derivative compound is DOTA-EB*-GSG-K(C4H11B10O3)-GK(C4H11B10O3) SEQ ID NO. 3 or DOTA-EB*-GSG-K(S10B12H11)-GK(S10B12H11) SEQ ID NO. 3.

### Claim 8 (depends on 1, 2, 3, 4, 5, 6, 7)

A method of for radioactive labeling of the neuropeptide Y (NPY) derivative compound of claim 1, 2, 3, 4, 5, 6 or 7, comprising:
dissolving an amount of the NPY derivative compound in solution;
mixing said NPY derivative compound solution with a radioactive isotope selected from the group consisting of 111In, 68Ga and 177Lu;
wherein said NPY derivative compound is labeled with said radioactive isotope.

### Claim 9 (depends on 8)

The method of claim 8, wherein the amount of NPY derivative compound is from 30μ to 100 μg.