# US 2013/0156725 A1 · Random pentapolymer for treatment of autoimmune diseases

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- Number: US 2013/0156725 A1
- Document ID: US20130156725A1
- Status: Published application
- Kind: A1
- Application number: 13/764,460
- Filed: 2013-02-11
- Published: 2013-06-20
- Earliest claimed: 2011-04-21
- Assignees: Mapi Pharma Ltd.
- Inventors: Ehud MAROM; Shai RUBNOV
- Web page: https://patentgrep.com/patent/US20130156725A1

## CPC

- C08G 69/10: Alpha-amino-carboxylic acids {(polysuccinimides C08G73/1092)}
- A61K 31/785: Polymers containing nitrogen
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- C07K 14/001: {by chemical synthesis}
- 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)
- C08G: MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
- 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
- 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

The present invention relates to a synthetic polypeptide which is a random linear pentapolymer comprising alanine, glutamic acid, lysine, tyrosine and phenylalanine and use thereof in treating autoimmune diseases, in particular multiple sclerosis.

## Claims

### Claim at position 1

1-26. (canceled)

### Claim 27

A pentapolymer or a salt thereof, which is a linear random copolymer of alanine, glutamic acid, lysine, tyrosine and phenylalanine.

### Claim 28 (depends on 27)

The pentapolymer according to claim 27, containing from about 15 to about 120 amino acids.

### Claim 29 (depends on 28)

The pentapolymer according to claim 28, having an average molecular weight of about 2,000 to about 20,000 Da.

### Claim 30 (depends on 29)

The pentapolymer according to claim 29, having an average molecular weight of about 5,000 to about 15,000 Da.

### Claim 31 (depends on 27)

The pentapolymer according to claim 27, comprising L amino acids, D-amino acids or a mixture of L- and D-amino acids.

### Claim 32 (depends on 27)

The pentapolymer according to claim 27, wherein the amino acids are in molar ratio of: from about 2.0 to about 3.2 alanine; from about 1.4 to about 2.0 glutamic acid; from about 4.4 to about 4.6 lysine; from about 0.9 to about 1.1 tyrosine; and from about 0.8 to about 1.2 phenylalanine.

### Claim 33 (depends on 27)

The pentapolymer according to claim 27, wherein the molar ratio of alanine to glutamic acid to lysine to tyrosine to phenylalanine is about 2.5:1.9:4.5:1.0:0.9, respectively.

### Claim 34 (depends on 27)

A pharmaceutical composition comprising a therapeutically effective amount of the pentapolymer according to claim 27 and a pharmaceutically acceptable carrier.

### Claim 35 (depends on 34)

The pharmaceutical composition according to claim 34, suitable for parenteral administration by subcutaneous (SC), intravenous (IV), intramuscular (IM), intradermal (ID), or intraperitoneal (IP) injection.

### Claim 36 (depends on 27)

A long acting pharmaceutical composition comprising a therapeutically effective amount of the pentapolymer according to claim 27 in a depot form suitable for administration at a medically acceptable location in a subject in need thereof.

### Claim 37 (depends on 36)

The long acting pharmaceutical composition according to claim 36, further comprising a pharmaceutically acceptable biodegradable or non-biodegradable carrier selected from PLGA, PLA, PGA, polycaprolactone, polyhydroxybutyrate, polyorthoesters, polyalkaneanhydrides, gelatin, collagen, oxidized cellulose, and polyphosphazene.

### Claim 38 (depends on 27)

A method of treating an autoimmune disease comprising administering to a subject in need thereof an effective amount of the pentapolymer according to claim 27.

### Claim 39 (depends on 38)

The method according to claim 38, wherein the autoimmune disease is multiple sclerosis.

### Claim 40 (depends on 39)

The method according to claim 39, wherein the pentapolymer is administered to reduce the frequency of relapses in patients with Relapsing-Remitting Multiple Sclerosis (RRMS).

### Claim 41 (depends on 38)

The method according to claim 38, wherein the pentapolymer is incorporated into a long lasting composition in a depot form suitable for administration at a medically acceptable location in the subject.

### Claim 42 (depends on 38)

The method according to claim 38, comprising administering the pentapolymer in combination with at least one additional active agent.
