# US 12,595,486 B2 · Aptamers for personal health care applications

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- Number: US 12,595,486 B2
- Document ID: US12595486B2
- Status: Granted
- Kind: B2
- Application number: 18/065,739
- Filed: 2022-12-14
- Published: 2023-09-14
- Granted: 2026-04-07
- Earliest claimed: 2021-12-14
- Assignees: The Procter & Gamble Company
- Applicants: The Procter & Gamble Company
- Inventors: Juan Esteban Velasquez; Spencer Christopher Rupard; Amy Violet Trejo; Adam Michael Pitz; Kelly Lee Schmeichel; Erin Nicole Swigart; Gregory Allen Penner; Hilda Andamiche Namanja-Magliano; Matthew Scott Wagner
- Web page: https://patentgrep.com/patent/US12595486B2

## CPC

- C12N 15/115: Aptamers, i.e. nucleic acids binding a target molecule specifically and with high affinity without hybridising therewith {; Nucleic acids binding to non-nucleic acids, e.g. aptamers}
- A61K 31/711: Natural deoxyribonucleic acids, i.e. containing only 2'-deoxyriboses attached to adenine, guanine, cytosine or thymine and having 3'-5' phosphodiester links
- A61K 31/712: Nucleic acids or oligonucleotides having modified sugars, i.e. other than ribose or 2'-deoxyribose
- A61K 31/7125: Nucleic acids or oligonucleotides having modified internucleoside linkage, i.e. other than 3'-5' phosphodiesters
- A61K 31/713: Double-stranded nucleic acids or oligonucleotides
- A61P 31/16: for influenza or rhinoviruses
- C12N 2310/16: Aptamers
- C12N 2310/31: of the backbone
- C12N 2310/317: with an inverted bond, e.g. a cap structure
- C12N 2310/32: of the sugar
- C12N 2310/33: of the base
- C12N 2310/344: Position-specific modifications, e.g. on every purine, at the 3'-end
- C12N 2310/351: Conjugate
- C12N 2310/531: Stem-loop; Hairpin
- C12N 2320/31: Combination therapy
- 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

## Abstract

An aptamer composition is disclosed which has one or more oligonucleotides that include at least one of deoxyribonucleotides, ribonucleotides, derivatives of deoxyribonucleotides, derivatives of ribonucleotides, or mixtures thereof. The aptamer composition has a binding affinity for one or more cellular membrane glycoproteins selected from the group consisting of: intercellular adhesion molecule 1 (ICAM-1), low-density lipoprotein receptor (LDLR) family members, and cadherin-related family member 3 (CDHR3), preferably intercellular adhesion molecule 1 (ICAM-1), and is configured to reduce the binding of one or more human rhinoviruses to the intercellular adhesion molecule 1 (ICAM-1).

## Claims

### Claim 1

Aptamer composition comprising at least one oligonucleotide consisting of: deoxyribonucleotides, ribonucleotides, derivatives of deoxyribonucleotides, derivatives of ribonucleotides, or mixtures thereof, wherein the aptamer composition has a binding affinity for intercellular adhesion molecule 1 (ICAM-1) and wherein the aptamer composition is configured to reduce the binding of one or more human rhinoviruses to the intercellular adhesion molecule 1 (ICAM-1) and
wherein the aptamer composition comprises at least one oligonucleotide forming a secondary structure from a 5′-end to a 3′-end comprising at least a 5′-dangling end, a stem, a hairpin loop, and a 3′-dangling end, wherein the stem is formed between the hairpin loop and the dangling end(s); and
wherein the secondary structure comprises at least the structural sequence 5′-EEEYYSSSSYSSSSYHHHHYYYYYYYYSYYYYYEEEE-3′ (Structure I), wherein H represents a nucleotide located in the hairpin loop, S represents a nucleotide located in the stem, E represents a nucleotide located in a dangling end, and Y represents a nucleotide being absent or H, S, E or I, wherein I represent an internal loop.

### Claim 2 (depends on 1)

The aptamer composition of claim 1, wherein the hairpin loop comprises at least 5 nucleotides.

### Claim 3 (depends on 2)

The aptamer composition of claim 2, wherein the hairpin loop comprises a purine base.

### Claim 4 (depends on 2)

The aptamer composition of claim 2, wherein, the hairpin loop comprises at least three pyrimidine bases.

### Claim 5 (depends on 1)

The aptamer composition of claim 1, wherein the last nucleotide in the stem adjacent to the hairpin loop is a purine base.

### Claim 6 (depends on 1)

The aptamer composition of claim 1, wherein the last nucleotide in the stem adjacent to the 3′-dangling end is a purine base.

### Claim 7 (depends on 1)

The aptamer composition of claim 1, wherein the last 4 nucleotides of the 3′-dangling end are purine bases.

### Claim 8 (depends on 1)

The aptamer composition of claim 1, wherein the 5′-dangling end comprises from 4 to 15 nucleotides.

### Claim 9 (depends on 1)

The aptamer composition of claim 1 comprising an internal loop, a 1st stem and a 2nd stem, wherein the internal loop comprises from 1 to 10 nucleotides and is located between the 1st stem and the 2nd stem.

### Claim 10 (depends on 1)

The aptamer composition of claim 1 wherein the stem adjacent to the dangling ends comprises at least 3 base pairs.

### Claim 11 (depends on 1)

The aptamer composition of claim 1, wherein the stem adjacent to the 3′-dangling end comprises the motif guanine-cytosine-thymine (GCT).

### Claim 12 (depends on 1)

The aptamer composition of claim 1, wherein the stem adjacent to the 5′-dangling end comprises the motif thymine-cytosine-adenine (TCA).

### Claim 13 (depends on 1)

The aptamer composition of claim 1, wherein the at least one oligonucleotide comprises a length from 30 to 60 nucleotides.

### Claim 14 (depends on 1)

The aptamer composition of claim 1, wherein the at least one oligonucleotide is truncated from parent oligonucleotides selected from the group consisting of SEQ ID NO: 1 to SEQ ID NO: 200.

### Claim 15 (depends on 14)

The aptamer composition of claim 14, wherein the at least one oligonucleotide is truncated from parent oligonucleotides comprising SEQ ID NO: 2, SEQ ID NO: 4, SEQ ID NO: 5 and SEQ ID NO: 8, or SEQ ID NO: 102, SEQ ID NO: 104, SEQ ID NO: 105, SEQ ID NO: 108, or mixtures thereof.

### Claim 16 (depends on 1)

The aptamer composition of claim 1, wherein the at least one oligonucleotide comprises natural and non-natural nucleobases, wherein the non-natural nucleobases comprise hypoxanthine, xanthine, 7-methylguanine, 5,6-dihydrouracil, 5-5-methylcytosine, 5-hydroxymethylcytosine, thiouracil, 1-methylhypoxanthine, 6-methylisoquinoline-1-thione-2-yl, 3-methoxy-2-naphthyl, 5-propynyluracil-1-yl, 5-methylcytosin-1-yl, 2-aminoadenin-9-yl, 7-deaza-7-iodoadenin-9-yl, 7-deaza-7-propynyl-2-aminoadenin-9-yl, phenoxazinyl, phenoxazinyl-G-clam, or mixtures thereof.

### Claim 17 (depends on 1)

The aptamer composition of claim 1, where the derivatives of ribonucleotides or the derivatives of deoxyribonucleotides comprise locked oligonucleotides, peptide oligonucleotides, glycol oligonucleotides, threose oligonucleotides, hexitol oligonucleotides, altritol oligonucleotides, butyl oligonucleotides, L-ribonucleotides, arabino oligonucleotides, 2′-fluoroarabino oligonucleotides, cyclohexene oligonucleotides, phosphorodiamidate morpholino oligonucleotides, or mixtures thereof.

### Claim 18 (depends on 1)

The aptamer composition of claim 1, wherein at least one pyrimidine nucleotide of the at least one oligonucleotide is fluorinated at the 2′ position of the pentose group.

### Claim 19

Personal health care composition comprising an aptamer composition comprising at least one oligonucleotide consisting of: deoxyribonucleotides, ribonucleotides, derivatives of deoxyribonucleotides, derivatives of ribonucleotides, and mixtures thereof,
wherein the aptamer composition has a binding affinity for intercellular adhesion molecule 1 (ICAM-1) and wherein the aptamer is configured to reduce the binding of one or more human rhinoviruses to the intercellular adhesion molecule 1 (ICAM-1), and
wherein the aptamer composition comprises at least one oligonucleotide forming a secondary structure from a 5′-end to a 3′-end comprising at least a 5′-dangling end, a stem, a hairpin loop, and a 3′-dangling end; and
wherein the secondary structure comprises at least the structural sequence 5′-EEEYYSSSSYSSSSYHHHHYYYYYYYYSYYYYYEEEE-3′ (Structure I), wherein H represents a nucleotide located in the hairpin loop, S represents a nucleotide located in the stem, E represents a nucleotide located in a dangling end, and Y represents a nucleotide being absent or H, S, E or I, wherein I represent an internal loop.

### Claim 20 (depends on 19)

The personal health care composition of claim 19 comprising at least one oligonucleotide showing at least 80% nucleotide identity to the sequences comprising SEQ ID NO: 237, SEQ ID NO: 238, SEQ ID NO: 239, SEQ ID NO: 240, SEQ ID NO: 241, SEQ ID NO: 242, SEQ ID NO: 243, SEQ ID NO: 244, SEQ ID NO: 245, SEQ ID NO: 246, or mixtures thereof.

### Claim 21

Method of inhibiting human rhinovirus infection by inhibiting binding of the human rhinovirus to the intercellular adhesion molecule 1 (ICAM-1) of epithelial cells comprising applying an aptamer composition comprising at least one oligonucleotide consisting of: deoxyribonucleotides, ribonucleotides, derivatives of deoxyribonucleotides, derivatives of ribonucleotides, or mixtures thereof,
wherein the aptamer composition has a binding affinity for intercellular adhesion molecule 1 (ICAM-1) and wherein the aptamer is configured to reduce the binding of one or more human rhinoviruses to the intercellular adhesion molecule 1 (ICAM-1), and
wherein the aptamer composition comprises at least one oligonucleotide forming a secondary structure from a 5′-end to a 3′-end comprising at least a 5′-dangling end, a stem, a hairpin loop, and a 3′-dangling end; and
wherein the secondary structure comprises at least the structural sequence 5′-EEEYYSSSSYSSSSYHHHHYYYYYYYYSYYYYYEEEE-3′ (Structure I), wherein H represents a nucleotide located in the hairpin loop, S represents a nucleotide located in the stem, E represents a nucleotide located in the dangling end, and Y represents a nucleotide being absent or H, S, E or I, wherein I represent an internal loop.

### Claim 22 (depends on 21)

Method of claim 21, wherein the epithelial cells are cells of the upper respiratory tract and the aptamer composition is delivered by spraying.