# US 10,945,950 B2 · Liquid inhalation formulation comprising RPL554

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- Number: US 10,945,950 B2
- Document ID: US10945950B2
- Status: Granted
- Kind: B2
- Application number: 15/927,517
- Filed: 2018-03-21
- Published: 2018-12-27
- Granted: 2021-03-16
- Earliest claimed: 2014-09-15
- Assignees: Verona Pharma PLC
- Applicants: Verona Pharma PLC
- Inventors: Peter Lionel Spargo; Edward James French; Phillip A. Haywood
- Web page: https://patentgrep.com/patent/US10945950B2

## CPC

- A61K 9/0078: {for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions}
- A61K 31/495: having six-membered rings with two {or more} nitrogen atoms as the only ring heteroatoms, e.g. piperazine {or tetrazines}(A61K31/48 takes precedence {; with three nitrogen atoms A61K31/53})
- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 47/02: Inorganic compounds
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/02: Nasal agents, e.g. decongestants
- A61P 11/06: Antiasthmatics
- A61P 11/08: Bronchodilators
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/06: Antipsoriatics
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 27/02: Ophthalmic agents
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- A61P 37/02: Immunomodulators
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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

The present invention relates to a liquid pharmaceutical composition suitable for administration by inhalation which comprises a diluent and a suspension of particles of 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one (RPL554) or a pharmaceutically acceptable salt thereof. Also described is a liquid pharmaceutical composition according to the invention for use in the treatment of the human or animal body.

## Claims

### Claim 1

A liquid pharmaceutical composition suitable for administration by inhalation comprising a diluent and a suspension of particles of 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one (RPL554) or a pharmaceutically acceptable salt thereof,
wherein the composition comprises a phosphate buffer at a concentration of less than about 5 mg/mL;
wherein the particles of RPL554 have a particle size distribution with a Dv50 (median particle size by volume) value of from about 0.2 μm to about 5 μm,
wherein the concentration of particles of RPL554 in the liquid pharmaceutical composition is from about 0.1 mg/mL to about 6 mg/mL.

### Claim 2 (depends on 1)

A liquid pharmaceutical composition according to claim 1, wherein the composition does not comprise a phosphate buffer.

### Claim 3 (depends on 2)

A liquid pharmaceutical composition according to claim 2, wherein the composition does not comprise a buffer.

### Claim 4 (depends on 1)

A liquid pharmaceutical composition according to claim 1, wherein the particles of RPL554 have a particle size distribution with a Dv50 value of from about 0.7 μm to about 2.5 μm.

### Claim 5 (depends on 1)

A liquid pharmaceutical composition according to claim 1, wherein the composition further comprises one or more surfactants.

### Claim 6 (depends on 5)

A liquid pharmaceutical composition according to claim 5, wherein the one or more surfactants are selected from one or more non-ionic surfactants.

### Claim 7 (depends on 5)

A liquid pharmaceutical composition according to claim 5, wherein the one or more surfactants are selected from polyoxyethylene glycol sorbitan alkyl esters and sorbitan alkyl esters.

### Claim 8 (depends on 1)

A liquid pharmaceutical composition according to claim 1, wherein the composition further comprises a tonicity adjuster.

### Claim 9 (depends on 1)

A liquid pharmaceutical composition according to claim 1, wherein the tonicity adjuster is sodium chloride.

### Claim 10 (depends on 1)

A liquid pharmaceutical composition according to claim 1, wherein the diluent is water.

### Claim 11 (depends on 1)

A liquid pharmaceutical composition according to claim 1, wherein composition is suitable for administration by nebulizer.

### Claim 12 (depends on 1)

A nebulizer comprising a composition according to claim 1.