# US 12,213,975 B2 · PDE9 inhibitors for treating sickle cell disease

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- Number: US 12,213,975 B2
- Document ID: US12213975B2
- Status: Granted
- Kind: B2
- Application number: 17/186,442
- Filed: 2021-02-26
- Published: 2021-06-17
- Granted: 2025-02-04
- Earliest claimed: 2018-08-31
- Assignees: Cardurion Pharmaceuticals, LLC
- Applicants: Cardurion Pharmaceuticals, Inc.
- Inventors: Edward George Calamai; Deborah Lynn Leithead Dobbins; Michael Paul Dehart; James McArthur; Shi Yin Foo
- Web page: https://patentgrep.com/patent/US12213975B2

## CPC

- A61K 31/506: not condensed and containing further heterocyclic rings
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/2009: {Inorganic compounds}
- A61K 9/2013: {Organic compounds, e.g. phospholipids, fats}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/2059: {Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin}
- A61K 9/284: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone}
- A61K 31/17: having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine (isoureas, isothioureas A61K31/155; sulfonylureas A61K31/64)
- A61K 31/4985: Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
- A61P 7/00: Drugs for disorders of the blood or the extracellular fluid
- A61P 7/06: Antianaemics
- C07D 487/04: Ortho-condensed systems
- 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
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

The present disclosure relates to PDE9 inhibitors, pharmaceutical compositions comprising the PDE9 inhibitors, and methods of using the PDE9 pharmaceutical compositions for the treatment of sickle cell disease (SCD).

## Claims

### Claim 1

An oral tablet composition, comprising:
50 mg 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl) pyrrolidin-3-yl]-3-tetrahydropyran-4-yl-7H-imidazo[1,5-a]pyrazin-8-one (Compound 1),
about 20%, about 30%, or about 40% by weight microcrystalline cellulose (MCC),
about 1% by weight colloidal silicon dioxide, and
about 0.8% by weight magnesium stearate.

### Claim 2 (depends on 1)

The oral tablet composition of claim 1, comprising from 20% to 40% by weight Compound 1.

### Claim 3 (depends on 1)

The oral tablet composition of claim 1, further comprising one or more solid carriers.

### Claim 4 (depends on 3)

The oral tablet composition of claim 3, wherein the one or more solid carriers comprise lactose.

### Claim 5 (depends on 1)

The oral tablet composition of claim 1, wherein Compound 1 is present as a monohydrate.

### Claim 6 (depends on 1)

The oral tablet composition of claim 1, wherein Compound 1 is present as a monohydrate polymorph.

### Claim 7

An oral tablet composition, comprising:
50 mg 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl) pyrrolidin-3-yl]-3-tetrahydropyran-4-yl-7H-imidazo[1,5-a]pyrazin-8-one (Compound 1),
about 20% or about 30% by weight microcrystalline cellulose (MCC),
about 1% by weight colloidal silicon dioxide,
about 0.8% by weight magnesium stearate, and
one or more solid carriers comprising lactose.