# US 2020/0399314 A1 · Il-2alpha receptor subunit binding compounds

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- Number: US 2020/0399314 A1
- Document ID: US20200399314A1
- Status: Published application
- Kind: A1
- Application number: 16/890,749
- Filed: 2020-06-02
- Published: 2020-12-24
- Earliest claimed: 2019-06-03
- Assignees: Medikine, Inc.
- Applicants: Medikine, Inc.
- Inventors: WILLIAM J. DOWER; MICHAEL C. NEEDELS; RONALD W. BARRETT; ALICE V. BAKKER; STEVEN E. CWIRLA
- Web page: https://patentgrep.com/patent/US20200399314A1

## CPC

- C07K 7/08: having 12 to 20 amino acids (gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68)
- C07K 14/55: IL-2
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- 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

Peptidyl IL-2Rα ligands and compounds comprising the IL-2Rα ligands are disclosed. The IL-2Rα ligands and compounds such as synthetic monomers, homodimers, or heteromers and recombinant fusion proteins comprising the IL-2Rα ligands can be used as targeting or imaging agents, as diagnostics or to treat cancers and autoimmune diseases.

## Claims

### Claim 1

An IL-2Rα ligand, wherein,
the IL-2Rα ligand bind to the human IL-2Rα subunit with an IC50 of less than 100 μM; and
the IL-2Rα ligand comprises an amino acid sequence selected from any one of SEQ ID NOS: 4, 9, 24, 31, 44, 50, 67, 79, 100, 112, 135, 144, 154, 172, 180, 203, 210, 219, 234, 250, and 418:
SEQ ID NO: 4
F L H W P V Y F C Q V M
SEQ ID NO: 9
F I P W D E Y F K Q V L
SEQ ID NO: 24
F V H C T L L G C W S G
SEQ ID NO: 31
W V I C S A V G C R P F
SEQ ID NO: 44
H V I C S V N G G C R G
SEQ ID NO: 50
E Q F C L V S D P M A C W S L
SEQ ID NO: 67
R R F C L R S E P A A C W F V
SEQ ID NO: 79
S K C V Y D Y N F G T C I F
SEQ ID NO: 100
S L N C K T R P G L R W C T W T
SEQ ID NO: 112
A W E C L F L P G H R G C S L F
SEQ ID NO: 135
R Q F C L V S P G Y E D C W F V
SEQ ID NO: 144
S A C Q L K W D E G W T C L F
SEQ ID NO: 154
R G C S L V W S G S W E C I F
SEQ ID NO: 172
G C T L S W N Q G W W H C V
SEQ ID NO: 180
A R C S L H H T G S R Y E C I F
SEQ ID NO: 203
T C R L K R S G P N S W E C I
SEQ ID NO: 210
V R C R L A R P G L T W E C L S
SEQ ID NO: 219
Q L C P W S D P G S W G P C P L
SEQ ID NO: 234
G C Q L V W Q D D S Y M C F Y
SEQ ID NO: 250
W C I G Q P L F R Q G S C K
SEQ ID NO: 418
F V P W D V Y F S Q I L G G

### Claim 2 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand comprises the amino acid sequence of SEQ ID NO: 4.

### Claim 3 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand comprises the amino acid sequence of SEQ ID NO: 9.

### Claim 4 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand comprises the amino acid sequence of SEQ ID NO: 24.

### Claim 5 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand comprises the amino acid sequence of SEQ ID NO: 31.

### Claim 6 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand comprises the amino acid sequence of SEQ ID NO: 44.

### Claim 7 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand comprises the amino acid sequence of SEQ ID NO: 50.

### Claim 8 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand comprises the amino acid sequence of SEQ ID NO: 67.

### Claim 9 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand comprises the amino acid sequence of SEQ ID NO: 79.

### Claim 10 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand comprises the amino acid sequence of SEQ ID NO: 100.

### Claim 11 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand comprises the amino acid sequence of SEQ ID NO: 112.

### Claim 12 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand comprises the amino acid sequence of SEQ ID NO: 135.

### Claim 13 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand comprises the amino acid sequence of SEQ ID NO: 144.

### Claim 14 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand comprises the amino acid sequence of SEQ ID NO: 154.

### Claim 15 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand comprises the amino acid sequence of SEQ ID NO: 172.

### Claim 16 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand comprises the amino acid sequence of SEQ ID NO: 180.

### Claim 17 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand comprises the amino acid sequence of SEQ ID NO: 203.

### Claim 18 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand comprises the amino acid sequence of SEQ ID NO: 210.

### Claim 19 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand comprises the amino acid sequence of SEQ ID NO: 219.

### Claim 20 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand comprises the amino acid sequence of SEQ ID NO: 234.

### Claim 21 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand comprises the amino acid sequence of SEQ ID. NO: 250.

### Claim 22 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand comprises the amino acid sequence of SEQ ID. NO: 418.

### Claim 23 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand has a greater than 70% sequence similarity to any one of SEQ ID NOS: 4, 9, 24, 31, 44, 50, 67, 79, 100, 112, 135, 144, 154, 172, 180, 203, 210, 219, 234, 250, and 418.

### Claim 24 (depends on 1)

The IL-2Rα ligand of claim 1, wherein the IL-2Rα ligand comprises a truncated IL-2Rα ligand of any one of SEQ ID NOS: 4, 9, 24, 31, 44, 50, 67, 79, 100, 112, 135, 144, 154, 172, 180, 203, 210, 219, 234, 250, and 418, in which from 1 to 3 amino acids is removed from the N-terminus, the C-terminus, or from both the N-terminus and the C-terminus.

### Claim 25 (depends on 1)

A compound comprising at least one IL-2Rα ligand of claim 1.

### Claim 26 (depends on 25)

The compound of claim 25, wherein the compound is selected from a peptide, a conjugate, and a fusion protein.

### Claim 27 (depends on 1)

A pharmaceutical composition comprising the IL-2Rα ligand of claim 1.

### Claim 28 (depends on 26)

A pharmaceutical composition comprising the compound of claim 26.