# US 10,766,941 B2 · Glycoprotein hormone long-acting superagonists

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- Number: US 10,766,941 B2
- Document ID: US10766941B2
- Status: Granted
- Kind: B2
- Application number: 14/831,124
- Filed: 2015-08-20
- Published: 2016-03-17
- Granted: 2020-09-08
- Earliest claimed: 2012-07-30
- Assignees: Trophogen, Inc.
- Applicants: Trophogen Inc.
- Inventors: Mariusz Szkudlinski; Bruce D. Weintraub
- Web page: https://patentgrep.com/patent/US10766941B2

## CPC

- C07K 14/59: Follicle-stimulating hormone [FSH]; Chorionic gonadotropins, e.g.hCG [human chorionic gonadotropin]; Luteinising hormone [LH]; Thyroid-stimulating hormone [TSH]
- A61P 5/00: Drugs for disorders of the endocrine system
- A61P 5/06: of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
- A61P 5/24: of the sex hormones
- A61P 15/08: for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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

This invention provides long-acting, superactive analogs of glycoprotein hormones demonstrating enhanced bioactivity both in vitro and in vivo as compared to wild type counterparts. The analogs are particularly useful for treating subjects showing low receptor expression or poor receptor responsiveness, and for the treatment of any condition associated with glycoprotein hormone activity.

## Claims

### Claim 1

A modified bovine alpha subunit polypeptide comprising SEQ ID NO:7.

### Claim 2 (depends on 1)

A modified glycoprotein hormone whose polypeptide sequences consist of the alpha subunit polypeptide of claim 1 and the wild-type beta subunit of bovine follicle-stimulating hormone (FSH).

### Claim 3 (depends on 2)

A method of stimulating a follicle-stimulating hormone (FSH) receptor in a bovine, comprising administering the modified glycoprotein hormone of claim 2 to said bovine.

### Claim 4 (depends on 2)

A method for stimulating ovulation in a bovine, comprising administering the modified glycoprotein hormone of claim 2 to said bovine.

### Claim 5 (depends on 3, 4)

The method of claim 3 or claim 4, wherein said modified glycoprotein hormone is administered in a single dose of 60 micrograms.

### Claim 6 (depends on 3, 4)

The method of claim 3 or claim 4, wherein said modified glycoprotein hormone is administered in a first dose of 40 micrograms followed by a second dose of 20 micrograms.