# US 11,306,313 B2 · Peptide, complex of peptide and siRNA, and methods of use thereof

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- Number: US 11,306,313 B2
- Document ID: US11306313B2
- Status: Granted
- Kind: B2
- Application number: 16/751,783
- Filed: 2020-01-24
- Published: 2020-06-18
- Granted: 2022-04-19
- Earliest claimed: 2013-12-18
- Assignees: Positec Power Tools (Suzhou) Co., Ltd.; Pu Chen
- Applicants: Positec Power Tools (Suzhou) Co., Ltd; Pu Chen
- Inventors: Pu Chen; Dafeng Chu; Baoling Chen; Wen Xu; Ran Pan
- Web page: https://patentgrep.com/patent/US11306313B2

## CPC

- C12N 15/113: Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; {Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing (when used in plants C12N15/8218)}
- A61K 9/5169: {Proteins, e.g. albumin, gelatin}
- A61K 31/713: Double-stranded nucleic acids or oligonucleotides
- A61K 47/42: Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein (oligopeptides having up to five amino acids {A61K47/183}; polyamino acids A61K47/34)
- A61K 47/64: Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent (peptidic linkers A61K47/65)
- A61P 35/00: Antineoplastic agents
- C07K 14/47: from mammals
- C12N 15/111: {General methods applicable to biologically active non-coding nucleic acids}
- C12N 15/87: Introduction of foreign genetic material using processes not otherwise provided for, e.g. co-transformation
- C12N 2310/14: interfering nucleic acids [NA]
- C12N 2310/3513: Protein; Peptide
- C12N 2320/32: Special delivery means, e.g. tissue-specific
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- 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
- 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

A series of peptides and a peptide-siRNA complex are disclosed, wherein the peptide based complex effectively enhances delivery of siRNA molecules into the cells and release of siRNA in the cell, and improves siRNA mediated gene silencing efficiency of cellular targets. Pharmaceutical compositions that include the complex, as well as a use of the complex in the gene therapy field, are also disclosed.

## Claims

### Claim 1

A peptide having the sequence CH3(CH2)16CONH—B—CONH2, wherein B is SEQ ID NO:4 or 5.

### Claim 2

A complex comprising:
a cargo molecule; and
a peptide having the sequence CH3(CH2)16CONH—B—CONH2, wherein B is SEQ ID NO:4 or 5.

### Claim 3 (depends on 2)

The complex according to claim 2, wherein the cargo molecule and the peptide are coupled non-covalently.

### Claim 4 (depends on 2)

The complex according to claim 2, wherein the particle size of the complex is in a range of from 20 nm to 999 nm.

### Claim 5 (depends on 2)

The complex according to claim 2, wherein the cargo molecule is a nucleic acid.

### Claim 6 (depends on 5)

The complex according to claim 5, wherein the nucleic acid is a short interfering RNA (siRNA).

### Claim 7 (depends on 6)

The complex according to claim 6, wherein the siRNA is complexed with the peptide at a molar ratio within a range of from 1:1 to 80:1.

### Claim 8 (depends on 6)

The complex according to claim 6, wherein the siRNA is complexed with the peptide at a molar ratio of 20:1.

### Claim 9 (depends on 6)

The complex according to claim 6, wherein the siRNA is complexed with the peptide at a molar ratio of 40:1.

### Claim 10 (depends on 6)

The complex according to claim 6, wherein the siRNA is complexed with the peptide at a molar ratio of 60:1.

### Claim 11

A pharmaceutical composition containing a complex comprising:
a cargo molecule; and
a peptide having the sequence CH3(CH2)16CONH—B—CONH2, wherein B is SEQ ID NO:4 or 5.

### Claim 12

A kit used to deliver drugs to a patient, wherein the kit comprises:
a pharmaceutical composition comprising a complex comprising:
a cargo molecule; and
a peptide having the sequence CH3(CH2)16CONH—B—CONH2, wherein B is SEQ ID NO:4 or 5;
one or more electrolytes;
one or more buffers;
a delivery device; and
a container adapted to mix one or more other agents together.

### Claim 13 (depends on 12)

The kit according to claim 12, wherein the cargo molecule and the peptide are coupled non-covalently.

### Claim 14 (depends on 12)

The kit according to claim 12, wherein the particle size of the complex is in a range of from 20 nm to 999 nm.

### Claim 15 (depends on 12)

The kit according to claim 12, wherein the cargo molecule is a nucleic acid.

### Claim 16 (depends on 15)

The kit according to claim 15, wherein the nucleic acid is a short interfering RNA (siRNA).

### Claim 17 (depends on 16)

The kit according to claim 16, wherein the siRNA is complexed with the peptide at a molar ratio within a range of from 1:1 to 80:1.

### Claim 18 (depends on 16)

The kit according to claim 16, wherein the siRNA is complexed with the peptide at a molar ratio in a range of from 20:1 to 60:1.

### Claim 19 (depends on 16)

The kit according to claim 16, wherein the siRNA is complexed with the peptide at a molar ratio of 20:1 or 40:1.

### Claim 20 (depends on 11)

A method, comprising:
delivering the pharmaceutical composition of claim 11 to a patient.