# US 9,085,643 B2 · Biologically active complex and its preparation

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- Number: US 9,085,643 B2
- Document ID: US9085643B2
- Status: Granted
- Kind: B2
- Application number: 13/988,878
- Filed: 2011-11-24
- Published: 2014-02-20
- Granted: 2015-07-21
- Earliest claimed: 2010-11-24
- Assignees: Hamlet Pharma AB
- Applicants: Catharina Svanborg; Kenneth Hun Mok; Maria Trulsson; Ann-Kristin Mossberg; Petter Storm; Chin Shing Ho
- Inventors: Catharina Svanborg; Kenneth Hun Mok; Maria Trulsson; Ann-Kristin Mossberg; Petter Storm; Chin Shing Ho
- Web page: https://patentgrep.com/patent/US9085643B2

## CPC

- C07K 14/00: Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K 31/201: having one or two double bonds, e.g. oleic, linoleic acids
- A61K 38/16: Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof {(enzyme inhibitors A61K38/005)}
- A61P 35/00: Antineoplastic agents
- C07K 14/76: Albumins
- C12Q 1/18: Testing for antimicrobial activity of a material
- G01N 33/5011: {for testing antineoplastic activity}
- G01N 33/6872: {Intracellular protein regulatory factors and their receptors, e.g. including ion channels}
- 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
- C12Q: MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS (immunoassay G01N33/53); COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)

## Abstract

A biologically active complex comprising either a polypeptide having the sequence of a variant of a naturally occurring protein, wherein said polypeptide is at least partially unfolded as compared to the said naturally occurring protein; or a peptide of up to 50 amino acids, for instance a fragment of the naturally occurring protein or a variant thereof; and a pharmaceutically acceptable salt of a fatty acid or lipid. The complexes of the invention demonstrate a novel mode of action, that gives rise to opportunities for the development of further active agents and screening methods.

## Claims

### Claim 1

A biologically active complex comprising a peptide comprising the sequence KQFTKXELSQLLKDIDGYGGIALPELIXTMFHTSGYDTQA (SEQ ID NO: 3), wherein X is an amino acid residue other than cysteine and the peptide is up to 50 amino acids in length, and a pharmaceutically acceptable salt of a fatty acid or lipid.

### Claim 2 (depends on 1)

The biologically active complex of claim 1, wherein the peptide comprises the sequence KQFTKAELSQLLKDIDGYGGIALPELIATMFHTSGYDTQA (SEQ ID NO: 5).

### Claim 3 (depends on 1)

The biologically active complex of claim 1, wherein the salt of the fatty acid or lipid is a sodium or potassium salt.

### Claim 4 (depends on 1)

The biologically active complex of claim 1, wherein the salt of the fatty acid or lipid is a salt of oleic acid.

### Claim 5 (depends on 1)

The biologically active complex of claim 1, which further comprises a secondary reagent.

### Claim 6 (depends on 1)

A pharmaceutical composition comprising the biologically active complex of claim 1 and a pharmaceutically acceptable carrier.

### Claim 7

A method for preparing a biologically active complex comprising a peptide comprising SEQ ID NO: 3, wherein the peptide is up to 50 amino acids in length, and a pharmaceutically acceptable salt of a fatty acid or lipid, wherein the method comprises mixing together the peptide and the salt of a fatty acid or lipid.

### Claim 8

A method for treating a cancer selected from the group consisting of skin papilloma, bladder cancer, glioblastoma, lung cancer, kidney cancer, ovarian cancer, and lymphoma, the method comprising administering to a patient in need thereof a biologically active complex comprising a peptide comprising SEQ ID NO: 3, wherein the peptide is up to 50 amino acids in length, and a fatty acid or lipid salt, or a pharmaceutical composition comprising the biologically active complex.

### Claim 9 (depends on 8)

The method of claim 8, wherein the peptide comprises SEQ ID NO: 5.

### Claim 10 (depends on 8)

The method of claim 8, wherein the fatty acid or lipid salt is an oleate salt.

### Claim 11

A kit comprising a peptide comprising SEQ ID NO: 3, wherein the peptide is up to 50 amino acids in length, and a pharmaceutically acceptable salt of a fatty acid or lipid.

### Claim 12 (depends on 11)

The kit of claim 11, wherein the peptide comprises SEQ ID NO: 5.

### Claim 13 (depends on 11)

The kit of claim 11, wherein the salt of the fatty acid or lipid is a salt of oleic acid.

### Claim 14

A peptide consisting of SEQ ID NO: 3.

### Claim 15 (depends on 14)

The peptide of claim 14, wherein the peptide consists of SEQ ID NO:5.
