United States Patent 7,250,419: Ticagrelor Claims, Scope, Expiration, and Patent Landscape

U.S. Patent No. 7,250,419 covers ticagrelor, the active pharmaceutical ingredient in Brilinta. The patent claims the specific stereochemically defined compound, its pharmaceutically acceptable salts, pharmaceutical compositions, and cardiovascular treatment methods involving myocardial infarction, thrombotic stroke, transient ischemic attacks, angina, and platelet-aggregation inhibition. The patent does not claim a broad chemical genus, a specific dosage regimen, a delivery device, or a manufacturing process.

The patent’s principal commercial claim was the compound claim covering ticagrelor itself. That core U.S. patent has expired. Later AstraZeneca patents, including crystalline-form and formulation-related patents, created additional barriers to generic entry after expiration of the compound patent.

What drug does U.S. Patent 7,250,419 protect?

U.S. 7,250,419 protects ticagrelor, also known as AZD6140. Ticagrelor is a reversible, orally active P2Y12 platelet receptor antagonist marketed by AstraZeneca as Brilinta in the United States and Brilique in certain other markets.

The claimed molecule is chemically identified as:

A triazolotriazine derivative;
Substituted with a 3,4-difluorophenylcyclopropylamino group;
Containing a propylthio substituent;
Fused or linked to a substituted cyclopentane diol;
Containing a 2-hydroxyethoxy substituent;
Defined by specific absolute and relative stereochemistry.

The claim language corresponds to ticagrelor rather than to a broad class of P2Y12 inhibitors such as clopidogrel, prasugrel, cangrelor, or elinogrel.

Chemical identity and commercial name

Item	Description
Active ingredient	Ticagrelor
Development code	AZD6140
Brand	Brilinta in the United States; Brilique in some markets
Drug class	Reversible P2Y12 platelet receptor antagonist
Dosage forms	Immediate-release oral tablets
Principal indication	Reduction of thrombotic cardiovascular events
Sponsor and originator	AstraZeneca
Regulatory pathway	New drug application, small-molecule product

What are the claims of U.S. Patent 7,250,419?

The 14 claims divide into four categories: the active compound, pharmaceutical compositions, cardiovascular treatment methods, and platelet-aggregation inhibition.

Claims	Subject matter	Scope
1	Compound and pharmaceutically acceptable salts	Ticagrelor and salts
2	Specific compound	Ticagrelor free form
3-4	Pharmaceutical compositions	Ticagrelor with diluent, adjuvant, or carrier
5-12	Treatment methods	Myocardial infarction, thrombotic stroke, TIA, and stable or unstable angina
13-14	Antiplatelet method	Inhibition of platelet aggregation

Claims 1 and 2: compound protection

Claim 1 covers the specified ticagrelor stereoisomer and pharmaceutically acceptable salts. This is the broadest and commercially most important claim in the patent because it reaches the active ingredient independent of tablet strength, excipient system, packaging, or particular disease indication.

Claim 2 repeats the specific compound without the express salt language. It is narrower than claim 1 in that it is directed to the compound itself rather than the compound and its pharmaceutically acceptable salts.

The supplied text contains apparent drafting or transcription errors in claim 2, including mismatched brackets and placement of the cyclopropyl substituent. The intended subject matter is nevertheless identifiable as the same ticagrelor molecule recited in claim 1.

Claims 3 and 4: pharmaceutical compositions

Claims 3 and 4 cover compositions containing the claimed compound with a pharmaceutically acceptable diluent, adjuvant, or carrier.

These claims are composition claims, but they are not narrow formulation claims in the modern patent-landscape sense. They do not require:

A particular tablet composition;
A specified excipient;
A dissolution profile;
A particle-size distribution;
A polymorphic form;
A coating system;
A dosage strength;
A sustained-release or immediate-release limitation.

A generic tablet containing ticagrelor would therefore present a potential issue under these claims if the claims remained enforceable and the generic product contained the claimed active ingredient in a pharmaceutical composition.

Claims 5 through 12: cardiovascular treatment methods

Claims 5 through 12 cover administering ticagrelor to treat:

Myocardial infarction;
Thrombotic stroke;
Transient ischemic attacks;
Stable angina;
Unstable angina.

The claims require administration of a therapeutically effective amount to a person suffering from the specified condition. They do not recite a dosage, treatment duration, loading dose, maintenance dose, concomitant aspirin use, or treatment window.

These claims are method-of-treatment claims rather than product claims. In an ANDA setting, their practical enforcement depends on the proposed labeling, the statutory certification, and whether the generic labeling actively encourages the patented use.

How broad is the scope of U.S. Patent 7,250,419?

The compound claims are narrow in chemical breadth but broad in commercial effect.

The patent does not cover all P2Y12 antagonists. It covers one defined molecular entity and its pharmaceutically acceptable salts. Because the claimed compound is the active ingredient in Brilinta, the claim operates as a product-level barrier against ordinary ticagrelor substitution while enforceable.

The patent does not require:

A specific therapeutic indication for claims 1 and 2;
A specific formulation for claims 1 and 2;
A particular salt for claim 1;
A particular manufacturing route;
A particular crystalline form;
A particular dose;
A particular patient population.

Claim construction issues

Potential claim-construction issues include:

Stereochemical identity. The claim uses detailed stereochemical descriptors. A material with a different stereoisomeric configuration would not literally satisfy the compound claim, although infringement could raise doctrine-of-equivalents issues.
Salt coverage. Claim 1 expressly includes pharmaceutically acceptable salts. Claim 2 is directed to the specified compound.
Chemical naming defects. Errors in punctuation or bracket placement would normally be assessed against the issued patent, prosecution history, specification, and skilled-person interpretation.
Free compound versus solid-state form. The claims do not expressly require a particular polymorph or crystalline form.
Therapeutic scope. The treatment claims are limited to named cardiovascular conditions and platelet aggregation inhibition.

When did U.S. Patent 7,250,419 expire?

U.S. Patent 7,250,419 issued on July 31, 2007. Its ordinary patent term ran from the applicable U.S. filing date and was subject to any applicable patent-term adjustment or extension.

Public patent and Orange Book records identify the patent as having reached the end of its ordinary enforceable term in 2021. Pediatric exclusivity, where applicable to the approved product, is regulatory exclusivity and does not extend the patent claims themselves. The patent is therefore not the principal current barrier to an ordinary ticagrelor ANDA.

Milestone	Date or status
U.S. patent issuance	July 31, 2007
Covered active ingredient	Ticagrelor
Principal commercial product	Brilinta
Core compound patent term	Ended in 2021
Current role	Historical core product patent; no longer the principal live compound barrier

The exact enforceability analysis should distinguish patent expiration from FDA exclusivity. A patent can expire while FDA exclusivity, pediatric exclusivity, or later patents remain relevant.

What is the Orange Book status of ticagrelor?

Brilinta is an FDA-approved small-molecule drug listed in the Orange Book. Orange Book listings for ticagrelor have included the original compound patent and later patents directed to additional aspects of the product, including solid-state or formulation subject matter.

The original compound patent was the most significant Orange Book listing because it reached ticagrelor as an active ingredient. Later listings generally have narrower scope and may depend on:

The physical form supplied;
The formulation used;
The dosage form;
The approved labeling;
The asserted patent’s statutory listing basis.

Orange Book status does not itself determine infringement. It informs the ANDA certification process under the Hatch-Waxman Act.

Which companies have challenged ticagrelor patents?

Generic-drug companies have challenged Brilinta patents through ANDA litigation and Paragraph IV certifications. Publicly reported challengers have included companies such as:

Apotex;
Mylan;
Zydus;
Alembic;
Other generic applicants identified in federal district-court and FDA records.

The relevant legal dispute is not limited to U.S. Patent 7,250,419. After expiration of the compound patent, litigation risk shifted toward later patents covering crystalline forms, formulations, or related product attributes.

The key litigation questions are typically:

Whether the ANDA product contains the claimed ticagrelor form;
Whether the proposed product practices a formulation claim;
Whether a later patent is valid and enforceable;
Whether the generic applicant’s Paragraph IV notice creates a statutory infringement action;
Whether a settlement permits an earlier launch.

What are Paragraph IV risks for generic ticagrelor?

A Paragraph IV certification asserts that an Orange Book-listed patent is invalid, unenforceable, or will not be infringed by the proposed generic product.

For ticagrelor, the risk profile has changed over time:

Patent category	Historical risk	Current significance
Core ticagrelor compound patent	Very high before expiration	Low after expiration
Pharmaceutically acceptable salt claims	High while core patent was active	Limited after core expiration
General composition claims	Moderate to high	Depends on patent term and formulation
Crystalline-form patents	Potentially significant	Product-form dependent
Formulation patents	Potentially significant	Depends on ANDA composition
Method-of-use patents	Label-dependent	Depends on proposed labeling

An ANDA applicant could challenge an expired compound patent without facing a meaningful remaining injunction risk from that patent. A later live patent can still delay launch if it is listed and successfully asserted.

What formulation and solid-state patents affect ticagrelor?

U.S. Patent 7,250,419 is not a detailed formulation patent. Its composition claims use broad pharmaceutical-composition language and do not specify the commercial Brilinta tablet architecture.

The later ticagrelor patent landscape has included patents directed to solid-state forms and related product attributes. U.S. Patent No. 8,618,088 is commonly associated with AstraZeneca’s later ticagrelor patent estate and has been relevant to generic challenges involving Brilinta. Its commercial importance is distinct from the expired 7,250,419 compound patent because a solid-state patent can affect a generic product even after the underlying molecule becomes off-patent.

A solid-state patent may cover:

A crystalline polymorph;
A hydrate or solvate;
X-ray powder diffraction characteristics;
Thermal behavior;
Stability properties;
A process that produces the claimed form.

A generic applicant may attempt to avoid such claims by using a different physical form, although that strategy must remain compatible with bioequivalence, manufacturability, stability, and FDA requirements.

How strong is the patent estate for ticagrelor?

The estate was strongest during the period when the compound patent and later secondary patents overlapped. Its strength can be assessed across four dimensions.

Product coverage

The original compound claim provided direct coverage of ticagrelor. This was the strongest form of protection because it did not depend on a particular indication or formulation.

Secondary patent coverage

Later solid-state and formulation patents could extend practical barriers beyond expiration of the compound patent. Their strength depends on claim validity, written-description support, enablement, claim breadth, and whether the generic product practices the claimed form or formulation.

Regulatory leverage

Orange Book listing creates a structured Hatch-Waxman process. A Paragraph IV challenge can trigger patent litigation and, for an eligible first applicant, a 180-day generic exclusivity period. The regulatory effect depends on the patent’s listing status and whether a statutory stay is available.

Commercial leverage

Brilinta had substantial cardiovascular-market exposure. AstraZeneca reported Brilinta sales of approximately $1.3 billion in 2023, making generic entry commercially material even after expiration of the core compound patent. [4]

Are biosimilar risks relevant to ticagrelor?

No. Ticagrelor is a chemically synthesized small molecule, not a biologic. Biosimilar litigation under the Public Health Service Act is not the relevant pathway.

Competitive entry proceeds through the abbreviated new drug application system. The central regulatory issues are:

Bioequivalence;
Pharmaceutical equivalence;
Labeling;
Patent certifications;
Orange Book-listed patents;
Manufacturing and quality compliance.

The relevant competitors are generic manufacturers, not biosimilar developers.

What generic launch scenarios exist for ticagrelor?

Scenario 1: Unrestricted launch after core-patent expiration

This scenario applies where the generic applicant avoids or defeats all relevant live secondary patents. The applicant can market ticagrelor after satisfying FDA approval requirements.

Scenario 2: Launch after settlement

A generic applicant may settle Paragraph IV litigation with AstraZeneca. The settlement may establish an agreed launch date, an authorized-generic arrangement, or other commercial terms. The precise terms depend on the individual agreement and antitrust review.

Scenario 3: At-risk launch

A generic company may launch before final resolution of all patent disputes. This exposes the company to damages, injunctive relief, and market disruption if the asserted patent is later upheld.

Scenario 4: Formulation or solid-state redesign

A generic applicant may use a non-infringing physical form or formulation. This reduces patent risk but can create development, stability, scale-up, and bioequivalence risks.

How does U.S. Patent 7,250,419 compare with competing antiplatelet patents?

Drug	Active ingredient	Patent type	Commercial status
Brilinta	Ticagrelor	Compound, formulation, solid-state, method patents	Core compound protection expired; secondary estate historically relevant
Plavix	Clopidogrel	Compound and stereochemical protection	Generic competition established
Effient	Prasugrel	Compound and method patents	Generic competition established
Aggrastat	Tirofiban	Compound and formulation protection	Mature product
Kengreal	Cangrelor	Compound, formulation, and method protection	Intravenous P2Y12 product

Ticagrelor’s original patent position was commercially stronger than a pure method-of-use estate because U.S. 7,250,419 claimed the active compound itself. That direct product claim reduced the importance of label design during the principal patent term.

What manufacturing and intellectual-property barriers remain?

The expired compound patent does not eliminate all development barriers. Generic manufacturers must still address:

Control of ticagrelor polymorphic form;
Impurity and degradation-product specifications;
Particle-size control;
Tablet dissolution;
Chemical stability;
Bioequivalence;
Scale-up reproducibility;
Supply of key intermediates;
Freedom to operate under later process patents;
Compliance with current good manufacturing practice requirements.

Process patents are distinct from the claims of U.S. 7,250,419. That patent does not claim a manufacturing method in the supplied claim set. A generic manufacturer could avoid infringement of this patent while remaining exposed to separate process or solid-state patents.

Key Takeaways

U.S. Patent 7,250,419 covers ticagrelor, the active ingredient in Brilinta.
Claims 1 and 2 are compound claims; claim 1 also covers pharmaceutically acceptable salts.
Claims 3 and 4 cover broad pharmaceutical compositions containing ticagrelor.
Claims 5 through 12 cover treatment of myocardial infarction, thrombotic stroke, transient ischemic attacks, and stable or unstable angina.
Claims 13 and 14 cover inhibition of platelet aggregation.
The patent does not claim a broad P2Y12 antagonist genus, a specific dose, a particular tablet formulation, a polymorph, or a manufacturing process.
The core compound patent expired in 2021.
Current generic risk depends primarily on later Orange Book-listed patents, including solid-state and formulation patents, rather than on U.S. 7,250,419 alone.
Ticagrelor is a small molecule, so generic ANDA litigation applies; biosimilar law does not.
Generic entry can proceed through ordinary launch, settlement-based launch, at-risk launch, or a redesigned-formulation strategy.

FAQs About U.S. Patent 7,250,419 and Ticagrelor

Does U.S. Patent 7,250,419 cover Brilinta tablets specifically?

No. The compound claims cover ticagrelor itself. The composition claims cover pharmaceutical compositions containing the compound but do not recite the complete commercial Brilinta tablet formulation.

Does the patent cover all ticagrelor salts?

Claim 1 covers the claimed ticagrelor compound and pharmaceutically acceptable salts. The salt must correspond to the claimed compound and satisfy the pharmaceutical-acceptability limitation.

Can a generic launch after expiration of U.S. 7,250,419?

Not necessarily. Expiration of the core compound patent removes that patent as a barrier, but later Orange Book patents may still affect launch depending on their validity, enforceability, claim scope, and relationship to the proposed generic product.

Is ticagrelor subject to biosimilar competition?

No. Ticagrelor is a chemically synthesized small molecule. The relevant competitors are ANDA-approved generics.

Do the treatment claims prevent all generic ticagrelor sales?

No. Method claims depend on the patented use and the generic labeling or conduct. They do not function in the same manner as a claim directed to the active compound itself.

References

United States Patent and Trademark Office. (2007). U.S. Patent No. 7,250,419: Triazolotriazine compounds. U.S. Department of Commerce. https://patents.google.com/patent/US7250419B2/en
U.S. Food and Drug Administration. (2024). Orange Book: Approved drug products with therapeutic equivalence evaluations. https://www.accessdata.fda.gov/scripts/cder/ob/
U.S. Food and Drug Administration. (2024). Brilinta prescribing information. AstraZeneca Pharmaceuticals LP. https://www.accessdata.fda.gov/drugsatfda_docs/label/
AstraZeneca PLC. (2023). Annual report and Form 20-F 2023. https://www.astrazeneca.com/investor-relations/annual-reports.html
United States Patent and Trademark Office. (2013). U.S. Patent No. 8,618,088. U.S. Department of Commerce. https://patents.google.com/patent/US8618088B2/en

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1135391	⤷ Start Trial	C300485	Netherlands	⤷ Start Trial
European Patent Office	1135391	⤷ Start Trial	CA 2011 00013	Denmark	⤷ Start Trial
European Patent Office	1135391	⤷ Start Trial	PA2011004	Lithuania	⤷ Start Trial
European Patent Office	1135391	⤷ Start Trial	91819	Luxembourg	⤷ Start Trial
European Patent Office	1135391	⤷ Start Trial	PA2011004,C1135391	Lithuania	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 7,250,419

Summary for Patent: 7,250,419