# US 2013/0252884 A1 · Fgf21 analogues and derivatives

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- Number: US 2013/0252884 A1
- Document ID: US20130252884A1
- Status: Published application
- Kind: A1
- Application number: 13/702,122
- Filed: 2011-06-06
- Published: 2013-09-26
- Earliest claimed: 2009-06-11
- Assignees: Novo Nordisk A/S
- Inventors: Patrick William Garibay; Helle Woeldike; Xujia Zhang; Henning Thoegersen; Peter Kresten Nielsen; Birgitte Andersen; Jishu Wang; Kristian Sass Bak-Jensen; Tina Moeller Tagmose
- Web page: https://patentgrep.com/patent/US20130252884A1

## CPC

- C07K 14/50: Fibroblast growth factor [FGF]
- A61K 38/1825: {Fibroblast growth factor [FGF]}
- A61K 38/26: Glucagons
- A61K 47/543: {Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine}
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61K 2300/00: Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Novel analogues of Fibroblast Growth Factor 21 (FGF21), derivatives thereof having a modifying moiety covalently attached thereto, and pharmaceutical use of these analogues and derivatives, in particular, for the treatment of diabetes, dyslipidemia, obesity, cardiovascular diseases, metabolic syndrome, and/or Non Alcoholic Fatty Liver Disease (NAFLD) are described.

## Claims

### Claim at position 1

1-15. (canceled)

### Claim 16

An FGF21 analogue comprising -1A, L166F, M168L, G174V, and Y179F.

### Claim 17 (depends on 16)

The FGF21 analogue of claim 16, wherein said FGF21 analogue further comprises at least one of the following: one or more of the amino acid substitutions/exchanges selected from the group consisting of 71C, 121Q, 173A and des181, up to four additional mutations, or at least one of the amino acids at positions 179 and 180 is not present in said FGF21 analogue.

### Claim 18 (depends on 17)

The FGF21 analogue of claim 17, wherein said FGF21 analogue comprises Cys at position 71.

### Claim 19 (depends on 18)

A derivative of the FGF21 analogue according to claim 18, wherein said derivative comprises a group of the general formula HOOC—(CH2)n—CONH—CH(COOH)—CH2—CH2—CONH—(CH2CH2O)m—CH2—CONH—(CH2CH2O)p—CH2—CONH—(CH2)q—NHCO—CH2— (modifying moiety) covalently attached to the sulphur atom in the mercapto group present in the cysteine residue at position 71, wherein n is an integer in the range of 10-20, m is an integer in the range of 1-3, p is an integer in the range of 1-3, and q is an integer in the range of 2-4.

### Claim 20 (depends on 19)

The derivative according to claim 19, wherein n is 14.

### Claim 21 (depends on 19)

The derivative according to claim 19, wherein n is 16.

### Claim 22 (depends on 19)

The derivative according to claim 19, wherein n is 18.

### Claim 23 (depends on 19)

The derivative according to claim 19, wherein q is 2.

### Claim 24 (depends on 19)

The derivative according to claim 19, wherein q is 3.

### Claim 25 (depends on 19)

The derivative according to claim 19, wherein q is 4.

### Claim 26 (depends on 16)

A pharmaceutical composition comprising the FGF21 analogue according to claim 16 and a pharmaceutically acceptable carrier.

### Claim 27 (depends on 17)

A pharmaceutical composition comprising the FGF21 analogue according to claim 17 and a pharmaceutically acceptable carrier.

### Claim 28 (depends on 18)

A pharmaceutical composition comprising the FGF21 analogue according to claim 18 and a pharmaceutically acceptable carrier.

### Claim 29 (depends on 19)

A pharmaceutical composition comprising the FGF21 analogue according to claim 19 and a pharmaceutically acceptable carrier.

### Claim 30 (depends on 16)

A method for treating or preventing diabetes, dyslipidemia, obesity, cardiovascular diseases, metabolic syndrome, or Non Alcoholic Fatty Liver Disease (NAFLD), comprising administering to a subject in need thereof a therapeutically effective amount of the FGF21 analogue according to claim 16.

### Claim 31 (depends on 17)

A method for treating or preventing diabetes, dyslipidemia, obesity, cardiovascular diseases, metabolic syndrome, or Non Alcoholic Fatty Liver Disease (NAFLD), comprising administering to a subject in need thereof a therapeutically effective amount of the FGF21 analogue according to claim 17.

### Claim 32 (depends on 18)

A method for treating or preventing diabetes, dyslipidemia, obesity, cardiovascular diseases, metabolic syndrome, or Non Alcoholic Fatty Liver Disease (NAFLD), comprising administering to a subject in need thereof a therapeutically effective amount of the FGF21 analogue according to claim 18.

### Claim 33 (depends on 19)

A method for treating or preventing diabetes, dyslipidemia, obesity, cardiovascular diseases, metabolic syndrome, or Non Alcoholic Fatty Liver Disease (NAFLD), comprising administering to a subject in need thereof a therapeutically effective amount of the FGF21 analogue according to claim 19.