# US 10,246,446 B2 · Blockers of the growth hormone receptor in disease prevention and treatment

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- Number: US 10,246,446 B2
- Document ID: US10246446B2
- Status: Granted
- Kind: B2
- Application number: 14/913,130
- Filed: 2016-02-12
- Published: 2017-11-30
- Granted: 2019-04-02
- Earliest claimed: 2015-02-12
- Assignees: University of Southern California
- Applicants: University of Southern California
- Inventors: Valter D. Longo; Priya Balasubramanian; Nouri Neamati; Min Wei
- Web page: https://patentgrep.com/patent/US10246446B2

## CPC

- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- C07D 413/12: linked by a chain containing hetero atoms as chain links
- A61K 31/4245: Oxadiazoles
- A61K 31/55: having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 35/00: Antineoplastic agents
- C07D 307/68: Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D 405/06: linked by a carbon chain containing only aliphatic carbon atoms
- C07D 405/12: linked by a chain containing hetero atoms as chain links
- C07D 405/14: containing three or more hetero rings
- C07K 16/26: against hormones {; against hormone releasing or inhibiting factors}
- C07K 16/2869: {against hormone receptors (for antibodies against neuromediator receptors C07K16/286)}
- A61K 2039/505: {comprising antibodies}
- C07K 2317/21: from primates, e.g. man
- C07K 2317/33: Crossreactivity, e.g. for species or epitope, or lack of said crossreactivity
- C07K 2317/34: Identification of a linear epitope shorter than 20 amino acid residues or of a conformational epitope defined by amino acid residues
- C07K 2317/75: Agonist effect on antigen
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- 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)
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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)

## Abstract

Compounds and methods for treating diseases or conditions affected by the activity or expression of genes/proteins related to human GH, GHR, STAT5, SOCS, IGF-1, insulin are provided. Monoclonal antibodies for treating diseases or conditions related to growth hormone and growth hormone receptor activity are also provided.

## Claims

### Claim 1

A compound having formula I:
or a pharmaceutically acceptable salt thereof;
wherein:
R1 is NO2, SO3H, NH2, or halogen, and
R2 is hydrogen, NO2, SO3H, NH2, or C1-8 alkyl, or halogen.

### Claim 2

A compound having formula II:
or a pharmaceutically acceptable salt thereof;
wherein:
R1 is hydrogen, C1-8 alkyl, or halogen, and
R2 is C1-8 alkyl, or halogen.

### Claim 3

A method inhibiting GH induced phosphorylation STAT5, the method comprising:
administering to a subject a therapeutically effective amount of a compound selected from the group consisting of:
and combinations thereof and pharmaceutically acceptable salts thereof;
wherein:
R1 is hydrogen, NO2, SO3H, NH3, C1-8 alkyl, or halogen, and
R2 is hydrogen, NO2, SO3H, NH3, C1-8 alkyl, or halogen.

### Claim 4 (depends on 3)

The method of claim 3 wherein the compound is selected from the group consisting of:
and
combinations thereof, and pharmaceutically acceptable salts thereof.

### Claim 5 (depends on 1)

The compound of claim 1 wherein R1 is NO2 or SO3H and R2 is hydrogen or C1-8 alkyl.

### Claim 6 (depends on 1)

The compound of claim 1 wherein R1 is NH2 or halogen and R2 is hydrogen or C1-8 alkyl.

### Claim 7 (depends on 3)

The method of claim 3 wherein is hydrogen.

### Claim 8 (depends on 3)

The method of claim 3 wherein R2 is hydrogen.

### Claim 9 (depends on 3)

The method of claim 3 wherein the compound is selected from the group consisting of:
and pharmaceutically acceptable salts thereof.

### Claim 10 (depends on 3)

The method of claim 3 wherein the compound is selected from the group consisting of:
and pharmaceutically acceptable salts thereof.

### Claim 11 (depends on 3)

The method of claim 3 wherein the compound is selected from the group consisting of:
and pharmaceutically acceptable salts thereof.