# US 12,758,555 B2 · Pharmaceutical formulations

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 12,758,555 B2
- Document ID: US12758555B2
- Status: Granted
- Kind: B2
- Application number: 18/458,436
- Filed: 2023-08-30
- Published: 2024-03-21
- Granted: 2026-10-13
- Earliest claimed: 2022-08-31
- Assignees: AstraZeneca AB
- Applicants: Astrazeneca AB
- Inventors: Wanding Deng; Ying Fan
- Web page: https://patentgrep.com/patent/US12758555B2

## CPC

- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 9/2009: {Inorganic compounds}
- A61K 9/2013: {Organic compounds, e.g. phospholipids, fats}
- A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/2826: {Sugars or sugar alcohols, e.g. sucrose; Derivatives thereof}
- A61K 9/284: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone}
- A61K 9/2866: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/04: Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
- A61P 11/00: Drugs for disorders of the respiratory system
- 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

A pharmaceutical formulation which comprises Compound 1, one or more pharmaceutical fillers, one or more pharmaceutical disintegrants, and one or more pharmaceutical lubricant.

## Claims

### Claim 1

A pharmaceutical formulation comprising Compound 1, or a pharmaceutically acceptable salt thereof, mannitol, microcrystalline cellulose, croscarmellose sodium, and magnesium stearate, wherein Compound 1 is 1-{2-[(1R)-1-aminoethyl]-4-chlorobenzyl}-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo [3,2-d]pyrimidin-4-one
wherein Compound 1 is present at about 2.5% w/w, the mannitol is present at about 55% w/w, the microcrystalline cellulose is present at about 36.5% w/w, the croscarmellose sodium is present at about 4% w/w, and the magnesium stearate is present at about 2% w/w, wherein the weight percentages are based on the total weight of the pharmaceutical formulation.

### Claim 2 (depends on 1)

The pharmaceutical formulation of claim 1 wherein the mannitol has an average mean particle diameter of about 100 μm.

### Claim 3 (depends on 1)

The pharmaceutical formulation of claim 1, wherein the microcrystalline cellulose has a median particle size of about 100 μm.

### Claim 4 (depends on 1)

The pharmaceutical formulation of claim 1 comprising 2.5 mg of Compound 1.

### Claim 5 (depends on 1)

The pharmaceutical formulation of claim 1 comprising 5 mg of Compound 1.

### Claim 6 (depends on 1)

The pharmaceutical formulation of claim 1 wherein the pharmaceutical formulation is a tablet.

### Claim 7 (depends on 6)

The pharmaceutical formulation of claim 6, wherein the tablet further comprises a film-coating.

### Claim 8 (depends on 7)

The pharmaceutical formulation of claim 7 wherein the film-coating comprises a polymer, wherein the polymer is hydroxypropyl methylcellulose (HPMC), hydroxypropyl cellulose (HPC), polyvinylpyrrolidone (PVP), polyvinylpolypyrrolidone (PVPP), or mixtures thereof.

### Claim 9 (depends on 8)

The pharmaceutical formulation of claim 8 wherein the film-coating comprises HPMC.

### Claim 10 (depends on 7)

The pharmaceutical formulation of claim 7 wherein the film-coating is present at about 2.5-3.5% w/w of the coated tablet.

### Claim 11 (depends on 1)

A method of treating, or reducing a risk of, a disease or condition in which inhibition of the enzyme MPO is beneficial which comprises administering to a person suffering from or at risk of, said disease or condition, a pharmaceutical formulation of claim 1.

### Claim 12 (depends on 11)

The method according to claim 11, wherein said disease or condition is heart failure, heart failure with reduced ejection fraction, heart failure with preserved ejection fraction, non-alcoholic steatohepatitis (NASH), or chronic obstructive pulmonary disease (COPD).

### Claim 13 (depends on 1)

The pharmaceutical formulation of claim 1 comprising between 1 mg and 10 mg of Compound 1.

### Claim 14 (depends on 1)

The pharmaceutical formulation of claim 1 comprising 10 mg of Compound 1.