# US 7,465,708 B2 · Branched cationic copolymers and methods for antimicrobial use

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- Number: US 7,465,708 B2
- Document ID: US7465708B2
- Status: Granted
- Kind: B2
- Application number: 10/535,991
- Filed: 2003-11-25
- Published: 2006-12-14
- Granted: 2008-12-16
- Earliest claimed: 2002-11-25
- Inventors: A. James Mixson
- Web page: https://patentgrep.com/patent/US7465708B2

## CPC

- C08G 69/10: Alpha-amino-carboxylic acids {(polysuccinimides C08G73/1092)}
- C07K 7/08: having 12 to 20 amino acids (gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68)
- 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
- 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)

## Abstract

The invention provides a branched copolymer for the treatment of bacterial, fungal, and viral infections. The branched copolymer is characterized as having (i) at least 10 amino acids, (ii) at least 10% of the amino acids are histidine, (iii) at least 10% of the amino acids are non-histidine, (iv) said branched polymer comprising one or more backbones, (v) one or more terminal branches, and (vi) optionally, one or more non-terminal branches.

## Claims

### Claim 1

A method for treating bacteria, fungal, or viral infections comprising administering a branched polymer with a backbone of 1 or more amino acid residues and at least one branch with at least 10 amino acid residues, wherein at least 38% of the amino acid residues are histidine and at least 10% of the amino acid residues are non-histidine.

### Claim 2 (depends on 1)

The method of claim 1, wherein at least 50% of the amino acids of said branched polymer are histidines.

### Claim 3 (depends on 1)

The method of claim 1, wherein at least 70% of the amino acids of said branched polymer are histidines.

### Claim 4 (depends on 1)

The method of claim 1, wherein at least 20% of non-histidine amino acid residues are amino acids which carry a positive charge at physiological pH.

### Claim 5 (depends on 4)

The method of claim 4, wherein the positively charged non-histidine amino acid residues are lysines.

### Claim 6 (depends on 1)

The method of claim 1, wherein said branched polymer comprises a subsegment of amino acid residues selected from the group consisting of:
K-H-K-H-K-H-K-G-K-H-K-H-K (SEQ ID NO: 1),
K-H-K-H-K-H-K-G-K-H-K-H-K-H-K (SEQ ID NO: 2),
K-H-K-H-K-H-K-H-K-G-K-H-K-H-K-H-K-H-K (SEQ ID NO: 3),
K-H-K-H-K-H-K-H-K-G-K-H-K-H-K-H-K-H-K-G-K-H-K-H-K-H-K-H-K (SEQ ID NO: 4),
K-H-K-H-H-K-H-H-K-H-H-K-H-H-K-H-H-K-H-K (SEQ ID NO: 5),
K-K-H-H-H-K-H-H-H-K-K-H-H-H-K-H-H-H-K-K (SEQ ID NO: 6),
K-H-H-H-K-H-H-H-K-H-H-H-K-H-H-H-K (SEQ ID NO: 7),
end-to-end repeats of one or more of the above sequences, and
the reverse of any of the above sequences.

### Claim 7 (depends on 6)

The method of claim 6, wherein said branched polymer is selected from the group consisting of:
[K-H-K-H-H-K-H-H-K-H-H-K-H-H-K-H-H-K-H-K]4 K3 (SEQ ID NO: 12),
[K-H-H-H-K-H-H-H-K-H-H-H-K-H-H-H-K]4 K3 (SEQ ID NO: 13).

### Claim 8 (depends on 1)

The method of claim 1, comprising administering the branched polymer with at least one delivery component.

### Claim 9 (depends on 8)

The method of claim 8, wherein the delivery component comprises a lipid.

### Claim 10 (depends on 1)

The method of claim 1, wherein the infection is septic shock.

### Claim 11 (depends on 1)

The method of claim 1, further comprising administering an additive therapeutic infectious agent selected from the group consisting of antibiotics and/or nucleic acids; and-optionally a delivery component.

### Claim 12 (depends on 11)

The method of claim 11, wherein the additive therapeutic infectious agent comprises RNAi nucleic acid that targets viral infections.

### Claim 13 (depends on 1)

The method of claim 1, wherein the infection is local or systemic.

### Claim 14 (depends on 1)

The method of claim 1, wherein the infection is a fungal infection.

### Claim 15 (depends on 1)

The method of claim 1, wherein the backbone of the branched polymer consists entirely of lysine residues.