# US 9,040,660 B2 · Long-acting gastrin derivatives

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- Number: US 9,040,660 B2
- Document ID: US9040660B2
- Status: Granted
- Kind: B2
- Application number: 13/642,184
- Filed: 2011-04-19
- Published: 2013-03-07
- Granted: 2015-05-26
- Earliest claimed: 2010-04-20
- Assignees: Novo Nordisk A/S
- Applicants: Jacob Kofoed; Carsten Engaard Stidsen; Frantisek Hubalek; Flemming S. Nielsen; Henning Thoegersen; Johannes Fels; Rikke Bjerring Andersen; Janos Tibor Kodra
- Inventors: Jacob Kofoed; Carsten Engaard Stidsen; Frantisek Hubalek; Flemming S. Nielsen; Henning Thoegersen; Johannes Fels; Rikke Bjerring Andersen; Janos Tibor Kodra
- Web page: https://patentgrep.com/patent/US9040660B2

## CPC

- C07K 14/595: Gastrins; Cholecystokinins [CCK]
- A61K 38/22: Hormones (derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin A61K38/33, e.g. corticotropin A61K38/35)
- A61K 38/2207: {Gastrins; Cholecystokinins [CCK]}
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 9/04: Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
- A61P 9/12: Antihypertensives
- C07K 14/00: Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to gastrin derivatives comprising gastrin or an analogue or fragment thereof and a derivatisation group and therapeutic use thereof.

## Claims

### Claim 1

A gastrin derivative comprising:
gastrin-17 or an analogue thereof, wherein the analogue is selected from the group consisting of [Leu15] gastrin-17,[Lys3, Leu15] gastrin-17, [Lys8, Leu15] gastrin-17, and [Lys14, Leu15] gastrin-17; and
a derivatisation group comprising a C12-22 acyl group, wherein said derivatisation group is {2-(2-{2-[2-(2-{2-[4-Carboxy-4-(17-carboxyheptadecanoylamino)butyrylamino]ethoxy}-ethoxy)acetylamino]-ethoxy}ethoxy)acetyl}, and wherein said derivatisation group is attached to a position selected from the group consisting of the N-terminal amino group, position 3, 8, and 14 of gastrin-17 or an analogue thereof.

### Claim 2 (depends on 1)

The gastrin derivative of claim 1, wherein said gastrin derivative is N-alpha-{2-(2-{2-[2-(2-{2-[4-Carboxy-4-(17-carboxyheptadecanoylamino)butyrylamino]ethoxy}-ethoxy)acetylamino]-ethoxy}ethoxy)acetyl}gastrin- 17.

### Claim 3 (depends on 1)

The gastrin derivative of claim 1, wherein said gastrin derivative is N-alpha-{2-(2-{2-[2-(2-{2-[4-Carboxy-4-(17-carboxyheptadecanoylamino)butyrylamino]ethoxy}-ethoxy)acetylamino]-ethoxy}ethoxy)acetyl} [Leu15] gastrin-17 (1-17).