# US 2023/0053338 A1 · Pro-inflammatory and anti-cancer functions of toll-like receptor 4 antagonists

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- Number: US 2023/0053338 A1
- Document ID: US20230053338A1
- Status: Published application
- Kind: A1
- Application number: 17/739,953
- Filed: 2022-05-09
- Published: 2023-02-23
- Earliest claimed: 2015-01-12
- Assignees: Children’s Medical Center Corporation
- Applicants: Children`s Medical Center Corporation
- Inventors: Jonathan C. Kagan
- Web page: https://patentgrep.com/patent/US20230053338A1

## CPC

- A61K 39/39: characterised by the immunostimulating additives, e.g. chemical adjuvants
- A61P 31/04: Antibacterial agents
- A61P 31/14: for RNA viruses
- A61P 31/16: for influenza or rhinoviruses
- A61P 31/18: for HIV
- A61P 31/20: for DNA viruses
- A61P 31/22: for herpes viruses
- A61P 33/00: Antiparasitic agents
- A61P 33/04: Amoebicides
- A61P 33/06: Antimalarials
- A61P 39/00: General protective or antinoxious agents
- A61K 2039/55511: {Organic adjuvants}
- A61K 2039/55516: {Proteins; Peptides}
- A61K 2039/55561: {CpG containing adjuvants; Oligonucleotide containing adjuvants}
- A61K 2039/55566: {Emulsions, e.g. Freund's adjuvant, MF59}
- A61K 2039/55572: {Lipopolysaccharides; Lipid A; Monophosphoryl lipid A}
- A61K 2039/57: {characterised by the type of response, e.g. Th1, Th2}
- A61K 2039/575: {humoral response}
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- 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
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

The present invention provides methods and compositions for specific activation of inflammatory responses in dendritic cells (DCs). 1-palmitoyl-2-arachidonyl-sn-glycero phosphorylcholine (PAPC) and its oxidized variant (oxPAPC) were identified to promote DC-mediated immunity, and are provided as adjuvants in immunostimulatory compositions, including vaccines.

## Claims

### Claim at position 1

-25. (canceled)

### Claim 26

A pharmaceutical composition comprising:
(i) a TLR4 agonist, a TLR2 agonist, and/or a TLR9 agonist; (ii) an oxidated 1-palmitoyl-2-arachidonyl-sn-glycero-3-phosphorylcholine (oxPAPC) species; and (iii) a cancer immunogen.

### Claim 27 (depends on 26)

The pharmaceutical composition of claim 26, wherein the TLR4 agonist is LPS.

### Claim 28 (depends on 26)

The pharmaceutical composition of claim 26, wherein the TLR4 agonist is monophosphoryl lipid A (MPLA).

### Claim 29 (depends on 26)

The pharmaceutical composition of claim 26, wherein the TLR2 agonist is Pam3CSK.

### Claim 30 (depends on 26)

The pharmaceutical composition of claim 26, wherein the TLR2 agonist is Pam2CSK.

### Claim 31 (depends on 26)

The pharmaceutical composition of claim 26, wherein the TLR9 agonist is CpG.

### Claim 32 (depends on 26)

The pharmaceutical composition of claim 26, wherein the oxPAPC species is 2-[[(2R)-2-[(E)-7-carboxy-5-hydroxyhept-6-enoyl]oxy-3-hexadecanoyloxypropoxy]-hydroxyphosphoryl]oxyethyl-trimethylazanium (HOdiA-PC).

### Claim 33 (depends on 26)

The pharmaceutical composition of claim 26, wherein the oxPAPC species is [(2R)-2-[(E)-7-carboxy-5-oxohept-6-enoyl]oxy-3-hexadecanoyloxypropyl] 2-(trimethylazaniumyl)ethyl phosphate (KOdiA-PC),

### Claim 34 (depends on 26)

The pharmaceutical composition of claim 26, wherein the oxPAPC species is 1-palmitoyl-2-(5-hydroxy-8-oxo-octenoyl)-sn-glycero-3-phosphorylcholine (HOOA-PC).

### Claim 35 (depends on 26)

The pharmaceutical composition of claim 26, wherein the oxPAPC species is 2-[[(2R)-2-[(E)-5,8-dioxooct-6-enoyl]oxy-3-hexadecanoyloxypropoxy]-hydroxyphosphoryl]oxyethyl-trimethylazanium (KOOA-PC).

### Claim 36 (depends on 26)

The pharmaceutical composition of claim 26, wherein the oxPAPC species is (1-palmitoyl-2-(5,6 epoxyisoprostanoyl)-sn-glycero-3-phosphocholine) (PEIPC).

### Claim 37 (depends on 26)

The pharmaceutical composition of claim 26, wherein the cancer is selected from the group consisting of sarcoma, lymphoma, leukemia, carcinoma, melanoma, and astrocytoma.

### Claim 38 (depends on 37)

The pharmaceutical composition of claim 37, wherein the carcinoma is selected from carcinoma of the breast, carcinoma of the prostate, ovarian carcinoma, carcinoma of the cervix, colon carcinoma, carcinoma of the lung, and combinations thereof.

### Claim 39 (depends on 38)

The pharmaceutical composition of claim 38, wherein the astrocytoma is glioblastoma.