# US 11,739,054 B2 · Methods and compositions for substance use disorder vaccine formulations and uses thereof

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- Number: US 11,739,054 B2
- Document ID: US11739054B2
- Status: Granted
- Kind: B2
- Application number: 17/129,712
- Filed: 2020-12-21
- Published: 2021-04-15
- Granted: 2023-08-29
- Earliest claimed: 2017-06-11
- Assignees: Molecular Express, Inc.
- Applicants: Molecular Express, Inc.
- Inventors: Kim Janda; Sam On Ho; Gary Fujii
- Web page: https://patentgrep.com/patent/US11739054B2

## CPC

- C07C 233/54: having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of a saturated carbon skeleton
- A61K 39/0013: {Therapeutic immunisation against small organic molecules, e.g. cocaine, nicotine}
- A61K 39/385: Haptens or antigens, bound to carriers
- A61P 25/30: for treating abuse or dependence
- A61P 37/04: Immunostimulants
- A61K 2039/55505: {Inorganic adjuvants}
- A61K 2039/55555: {Liposomes; Vesicles, e.g. nanoparticles; Spheres, e.g. nanospheres; Polymers}
- A61K 2039/55561: {CpG containing adjuvants; Oligonucleotide containing adjuvants}
- A61K 2039/6012: {Haptens, e.g. di- or trinitrophenyl (DNP, TNP)}
- A61K 2039/6037: {Bacterial toxins, e.g. diphteria toxoid [DT], tetanus toxoid [TT]}
- A61K 2039/627: {characterised by the linker}
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- 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

The present invention relates to vaccine compositions for treatment of substance use disorders, methods for the manufacture thereof, and methods for the use thereof to treat an animal. These compositions comprise a hapten conjugated via a linker to a protein scaffold and mixed with a particulate carrier and at least one immunostimulatory adjuvant molecule.

## Claims

### Claim 1

A method of stimulating an immune response to methamphetamine, comprising:
immunizing an animal by administering to the animal a conjugate comprising one or more compounds having a general formula:
wherein
R1 is —(O—CH2—CH2)p—, wherein p is 1 to 6, or R1 is an optionally substituted C1-6 alkyl, wherein substitution(s) are independently selected from the group consisting of —NO2, —NH2, —OH, ═O, —COOR′ where R′ is H or lower alkyl, —CH2OH, and —CONH2,
R2 is peptide of m amino acid residues, an alkylene oxide of m alkylene oxide monomers, or (CH2)m, where m=2 to 6; and
R3 is selected from the group consisting of a protected or unprotected maleimide, alkyl halide, aryl halide, alpha-haloacyl, pyridyl disulfide, aldehyde, ketone, carboxyl, thiol, thioester, disulfide, N-hydroxy-succinimide, or cyclic thiolactone,
or salts thereof, wherein the one or more compounds or salts thereof are covalently bound through R3 on the compound(s) to a corresponding coupling site on a protein, polypeptide, detectable label, nucleic acid, or solid phase to provide the conjugate.

### Claim 2 (depends on 1)

A method according to claim 1, wherein the animal is a human.

### Claim 3 (depends on 1)

A method according to claim 1, further comprising co-administering one or more immunostimulatory adjuvant molecules with the conjugate.

### Claim 4 (depends on 3)

A method according to claim 3, wherein the animal is a human.

### Claim 5 (depends on 1)

A method according to claim 1, wherein R2 is -Gly-Gly-, -Gly-Ala-, -Ala-Gly-, -Pro-Gly-, -Gly-Pro-, -Ala-Ala-, -Ala-Pro-, or -Pro-Ala-.

### Claim 6 (depends on 1)

A method according to claim 1, wherein the compound has the structure

### Claim 7 (depends on 1)

A method according to claim 1, wherein the compound has the structure

### Claim 8 (depends on 1)

A method according to claim 1, wherein the protein, polypeptide, detectable label, nucleic acid, or solid phase is selected from the group consisting of a hapten carrier protein comprising a T-helper epitope, an enzyme, a fluorophore, biotin, avidin, streptavidin, digoxigenin, maltose, oligohistidine, 2,4-dintrobenzene, phenylarsenate, a metal, a fluorescent or colored microsphere.

### Claim 9 (depends on 8)

A method according to according to claim 8, wherein said protein is selected from the group consisting of keyhole limpet hemocyanin, bovine serum albumin, thyroglobulin, thioredoxin, ovalbumin, lysozyme, diphtheria antigen DT, diphtheria antigen CRM197 and tetanus toxoid.