US Patent 9,745,290: Opicapone Dosage-Unit Claims, Patent Scope, Expiration, and Generic Risk
US Patent 9,745,290 protects pharmaceutical dosage units containing opicapone and related pyridine N-oxide compounds. Its commercially important claims cover 50 mg opicapone tablets, dosage units used with levodopa and/or an aromatic L-amino acid decarboxylase inhibitor, Parkinson's disease treatment methods, and packages containing the product. The patent is assigned to BIAL-Portela & Ca., S.A. and is relevant to Ongentys, marketed in the United States by Neurocrine Biosciences.
The patent does not principally protect the discovery of opicapone as a chemical entity. It protects specified pharmaceutical presentations and therapeutic use configurations. The broadest claims reach dosage units containing 1 to 500 mg of a defined chemical genus, while the narrowest commercial claim covers an orally administrable tablet containing 50 mg of opicapone.
What drug is protected by US Patent 9,745,290?
The principal drug covered by the patent is opicapone, chemically identified as:
5-[3-(2,5-dichloro-4,6-dimethyl-1-oxy-pyridin-3-yl)-[1,2,4]-oxadiazol-5-yl]-3-nitrobenzene-1,2-diol.
Opicapone is a peripheral catechol-O-methyltransferase, or COMT, inhibitor. The FDA approved Ongentys as an adjunct to levodopa/carbidopa in adults with Parkinson's disease experiencing "off" episodes [2].
| Item |
Description |
| Active ingredient |
Opicapone |
| Brand |
Ongentys |
| Sponsor/US commercializer |
Neurocrine Biosciences |
| Original patent owner |
BIAL-Portela & Ca., S.A. |
| Indication |
Adjunctive treatment with levodopa/carbidopa for Parkinson's disease |
| Commercial strength |
50 mg |
| Dosage form |
Oral capsule for Ongentys; patent claim 15 expressly recites an oral 50 mg tablet |
| FDA approval |
June 24, 2020 |
| Regulatory class |
Small-molecule prescription drug |
| Biologic or biosimilar pathway |
Not applicable |
The patent's chemical definition is broader than opicapone. It covers compounds having a specified scaffold with a pyridine N-oxide group and permitted substituents. Claim 2 then narrows the invention to opicapone itself.
What are the claims of US Patent 9,745,290?
The patent contains three principal claim groups: dosage-unit claims, therapeutic-use claims, and package claims.
Dosage-unit claims
Claim 1 covers:
- An individual dosage unit;
- 1 to 500 mg of a formula I compound;
- A defined substituted pyridine N-oxide structure;
- Pharmaceutically acceptable salts.
Claims 3 through 7 narrow the amount to progressively smaller ranges:
| Claim |
Dose limitation |
| 1 |
1 to 500 mg |
| 3 |
2 to 300 mg |
| 4 |
3 to 100 mg |
| 5 |
5 to 50 mg |
| 6 |
5 mg |
| 7 |
50 mg |
Claim 8 narrows claim 7 to a tablet. Claim 15 separately recites an orally administrable tablet containing 50 mg of opicapone.
The commercial significance is concentrated in claims 2, 7, 8, 12, 14 and 15. These claims directly correspond to opicapone dosage units rather than the broader chemical genus.
Combination claims
Claims 9 and 10 cover the dosage unit in combination with:
- L-DOPA; and/or
- An aromatic L-amino acid decarboxylase inhibitor, such as carbidopa or benserazide.
These claims address the clinical context in which opicapone is administered. The claims do not require that levodopa or the decarboxylase inhibitor be physically incorporated into the same tablet. The phrase "in combination with" can encompass co-packaged or separately administered products, depending on claim construction and the specification.
Method-of-treatment claims
Claims 11 and 12 cover treating Parkinson's disease by administering the claimed dosage unit. Claim 12 narrows the active compound to opicapone.
These are method claims rather than product claims. They create a separate infringement theory where a competing product is supplied with labeling that instructs use for Parkinson's disease, particularly as adjunctive therapy with levodopa/carbidopa.
Package claims
Claims 13 and 14 cover packages containing the claimed dosage unit. Claim 13 requires the package to further contain L-DOPA and/or an AADC inhibitor. Claim 14 covers a package containing an opicapone dosage unit.
Package claims are narrower than a free-standing dosage-unit claim, but they can be relevant to co-packaged Parkinson's disease treatment products and branded labeling.
How broad is claim 1 of US Patent 9,745,290?
Claim 1 is a genus claim with a dosage-unit limitation. Its scope depends on both chemical identity and amount.
A product must satisfy all of the following requirements:
- It must contain a compound within the recited formula I structure.
- The compound must include the specified pyridine N-oxide substituent.
- The dosage unit must contain between 1 and 500 mg.
- Any salt must be pharmaceutically acceptable.
- The product must qualify as an "individual dosage unit."
The claim is not limited to opicapone. It covers compounds with alternative substituents at the R4-R7 positions, different linker configurations, and permitted hydrolysable or substituted groups at R1 and R2.
The breadth is narrowed by several structural requirements:
- X must be methylene.
- Y must be oxygen, NH or sulfur.
- n must be 0, 1, 2 or 3.
- m must be 0 or 1.
- R3 must be a specified pyridine N-oxide arrangement.
- The permitted substituent list is extensive but closed by the claim language.
The term "individual dosage unit" is important. A bulk bottle containing powder or a manufacturing intermediate would not ordinarily satisfy the limitation unless the product is presented as a discrete dose. Tablets, capsules, sachets and other discrete oral units are more likely to fall within the limitation.
What formulation does claim 15 protect?
Claim 15 protects an orally administrable tablet containing 50 mg of opicapone.
This is the most commercially targeted claim in the patent. It does not require:
- A particular excipient;
- A specified release profile;
- A particular tablet coating;
- A particular particle size;
- A particular manufacturing process; or
- Co-formulation with levodopa or carbidopa.
A generic company could therefore face claim 15 based on the active ingredient and strength alone, even if it uses different excipients, compression conditions, coating materials or packaging.
Claim 15 does not expressly cover Ongentys if Ongentys is supplied as a capsule rather than a tablet. Claims 2 and 7, however, may still be relevant because they cover an individual 50 mg opicapone dosage unit without requiring a tablet. Claims 11 and 12 can also apply to the labeled therapeutic use.
What patents protect Ongentys and opicapone?
The opicapone patent estate includes at least two distinct protection layers:
| Protection layer |
Subject matter |
Commercial relevance |
| Core compound patents |
Opicapone and related nitrocatechol derivatives |
Protect the active molecule |
| Dosage-unit patent |
1-500 mg units and specific 5 mg/50 mg products |
Protects product strength and presentation |
| Combination/use claims |
Opicapone with levodopa and AADC inhibitors |
Protects Parkinson's disease adjunctive use |
| Package claims |
Opicapone supplied with levodopa/AADC inhibitor |
Targets co-packaged treatment products |
| Later formulation or manufacturing patents |
May cover specific solid forms, processes or compositions |
Can extend practical barriers beyond the core compound patent |
US 9,745,290 should therefore be assessed together with the core opicapone compound patent and any later Orange Book-listed patents. A freedom-to-operate analysis limited to the '290 patent would not establish freedom from the entire Ongentys estate.
When does US Patent 9,745,290 expire?
The patent has a projected US expiration in 2031 based on its underlying international filing and US patent-term calculation. The precise enforceable date should be taken from the current USPTO patent record and any applicable patent-term adjustment or extension data.
| Event |
Date |
| US patent grant |
August 29, 2017 |
| Patent number |
US 9,745,290 |
| Projected term endpoint |
Approximately February 2031 |
| FDA approval of Ongentys |
June 24, 2020 |
| Five-year new chemical entity exclusivity |
Ended June 24, 2025 |
The patent term is separate from FDA regulatory exclusivity. FDA new chemical entity exclusivity prevented submission of an ANDA relying on the Ongentys approval for five years after approval. After that period, a generic applicant could submit an ANDA, subject to listed patents and Paragraph IV procedures [2, 3].
A patent-term extension based on the Ongentys approval would need to be confirmed from the USPTO and Orange Book records. The 2031 endpoint should not be treated as the endpoint for the full Ongentys patent estate because other patents may expire earlier or later.
What is the Orange Book status of US Patent 9,745,290?
Ongentys is an FDA-approved listed drug. The Orange Book is the relevant source for determining whether US 9,745,290 is listed against the approved product, the use code associated with any method-of-use listing, and the current expiration date [3].
The patent's claim content is consistent with several Orange Book listing categories:
- Drug product protection for an opicapone dosage form;
- Method-of-use protection for adjunctive Parkinson's disease treatment;
- Strength-specific protection for a 50 mg product.
An Orange Book listing does not establish that every claim is valid or infringed. It triggers statutory notice and litigation consequences when an ANDA applicant certifies under Paragraph IV that the listed patent is invalid, unenforceable or not infringed.
What Paragraph IV risks exist for generic opicapone?
The principal generic risks are concentrated in three areas.
Product-by-strength challenge
A generic applicant seeking approval for a 50 mg opicapone product could challenge claims 2, 7, 8 and 15. Claim 15 is particularly direct because it recites a 50 mg oral tablet containing opicapone.
A capsule applicant may avoid the express tablet limitation of claim 15, but it could remain exposed to claims covering an individual 50 mg dosage unit and to method-of-treatment claims.
Method-of-use challenge
An ANDA applicant may seek a section viii carve-out for protected use language, where permitted. That strategy is more difficult if the approved generic labeling necessarily instructs use of opicapone as adjunctive treatment with levodopa/carbidopa for Parkinson's disease.
Claims 11 and 12 create potential exposure where the generic label retains the patented indication.
Package and combination challenge
A generic company selling opicapone separately from levodopa/carbidopa may reduce exposure to claims 13 and 14. A co-packaged product or label that promotes combined use can increase risk under those claims.
A Paragraph IV case would typically turn on:
- Whether the proposed product is an "individual dosage unit";
- Whether the formulation contains 50 mg of opicapone;
- Whether the product is a tablet or another dosage form;
- Whether the label instructs the claimed Parkinson's disease use;
- Whether the patent claims are anticipated or obvious; and
- Whether the claims are adequately supported and enabled across the genus.
How strong is the patent estate for opicapone?
The estate is strongest against a conventional 50 mg generic that:
- Contains opicapone as the active ingredient;
- Uses a discrete oral dosage unit;
- Is labeled for adjunctive use with levodopa/carbidopa; and
- Launches before the relevant patent expiration.
The strongest individual claims are the narrow product claims directed to opicapone at 50 mg. They have a clearer relationship to the marketed product than claim 1's broad chemical genus.
The principal validity pressure points are:
| Issue |
Risk |
| Broad genus in claim 1 |
Written-description and enablement challenges |
| Dose ranges |
Obviousness arguments based on routine dose optimization |
| 50 mg limitation |
Stronger product correspondence, but possible prior-art dose disclosures |
| "In combination with" language |
Claim-construction disputes |
| Method claims |
Label-based induced-infringement disputes |
| Package claims |
Avoidance through separate product distribution |
| Chemical definition |
Anticipation and obviousness based on prior pyridine N-oxide compounds |
The narrower claims are generally easier to enforce against a directly substitutable product, while the broadest claim offers wider coverage but presents greater validity and construction exposure.
Which company commercializes Ongentys in the United States?
Neurocrine Biosciences commercializes Ongentys in the United States under an agreement with BIAL. BIAL developed opicapone and retained rights in certain territories, while Neurocrine obtained US commercialization rights [4].
The licensing structure matters because:
- BIAL remains central to patent ownership and global development;
- Neurocrine carries US commercial exposure;
- A generic launch would affect both royalty economics and product revenue;
- Litigation strategy may involve the patent owner, exclusive licensee or both, depending on standing and agreement terms.
What revenue exposure does US Patent 9,745,290 create?
The patent protects a product with a single commercially important strength: 50 mg. That concentrates value in the marketed dose rather than distributing protection across multiple strengths.
Revenue exposure is driven by:
- The timing of the first ANDA approval;
- Whether a first generic receives 180-day exclusivity;
- The number of Paragraph IV filers;
- The availability of an authorized generic;
- Physician substitution and payer controls;
- Whether the generic label includes the Parkinson's disease use;
- The expiration dates of the core compound and later patents.
The patent's commercial value is therefore higher than its claim count might suggest. Claims 7, 8 and 15 can create a direct barrier to a standard 50 mg product, while claims 11 and 12 can complicate labeling strategies.
Key Takeaways
- US 9,745,290 is an opicapone dosage-unit and therapeutic-use patent.
- Claim 1 covers a broad chemical genus in 1 to 500 mg individual dosage units.
- Claim 2 narrows the genus to opicapone.
- Claims 7 and 15 target the commercially important 50 mg strength.
- Claim 15 specifically covers an orally administrable 50 mg opicapone tablet.
- Claims 9 through 14 address use with levodopa/AADC inhibitors and related packaging.
- The patent is separate from FDA exclusivity, which ended five years after Ongentys approval on June 24, 2025.
- The projected patent-term endpoint is approximately February 2031, subject to the official USPTO and Orange Book term data.
- Generic exposure is highest for a 50 mg oral product labeled for adjunctive use with levodopa/carbidopa.
- The patent should be analyzed with the core opicapone compound patents and any later Orange Book-listed patents.
FAQs About US Patent 9,745,290 and Opicapone
Does US Patent 9,745,290 cover Ongentys capsules?
It can cover Ongentys through claims directed to an individual opicapone dosage unit and the 50 mg strength, even though claim 15 specifically recites a tablet. Claims 2 and 7 are not limited to tablets.
Can a generic avoid the patent by using a capsule instead of a tablet?
A capsule may avoid the express tablet limitation in claim 15, but it may remain exposed to claims covering a 50 mg individual dosage unit, opicapone itself and the labeled Parkinson's disease use.
Does the patent protect opicapone as a chemical compound?
Its claims include a broad chemical genus containing opicapone, but the patent's central commercial claims are dosage-unit claims. Separate core compound patents may provide the principal chemical-entity protection.
Does FDA approval of a generic end the patent?
No. FDA approval and patent enforceability are separate issues. A generic may obtain approval subject to patent certifications, a court judgment, a settlement date or an approved non-infringing label.
Are biosimilars relevant to Ongentys?
No. Opicapone is a small-molecule drug. Competitive products would generally proceed through the ANDA pathway for generics, not the biosimilar pathway under the Biologics Price Competition and Innovation Act.
Sources:
- United States Patent and Trademark Office. (2017). US Patent No. 9,745,290, Pharmaceutical compositions comprising pyridine N-oxide compounds.
- U.S. Food and Drug Administration. (2020). Ongentys (opicapone) prescribing information.
- U.S. Food and Drug Administration. (2025). Approved drug products with therapeutic equivalence evaluations: Orange Book.
- Neurocrine Biosciences, Inc. (2017). Annual report and agreement disclosures concerning opicapone commercialization rights.
