US Patent 7,361,787: Vilanterol Compound Claims, Expiration, Orange Book Status and Patent Landscape

US Patent 7,361,787 protects a broad genus of long-acting selective β2-adrenoreceptor agonists, including vilanterol, together with pharmaceutical formulations, inhalation devices, combination therapy and manufacturing processes. The patent issued to Glaxo Group Limited on April 22, 2008, and its principal US patent term expired in late 2021 or 2022, depending on the applicable patent-term adjustment and regulatory records. The patent is therefore no longer a primary blocking right for new US generic or competing-product development.

The patent is important historically because claim 4 expressly covers vilanterol and related analogues. Vilanterol is marketed in the United States only in combination inhalers, including Breo Ellipta, Anoro Ellipta and Trelegy Ellipta. Those products depend on separate patents covering fluticasone furoate, umeclidinium, combination formulations, inhaler devices and related product configurations.

What drug does US Patent 7,361,787 protect?

US 7,361,787 is directed to substituted phenylethanolamine β2 agonists with a long, oxygen-containing side chain attached to the amino group. The claimed compounds have the general architecture of:

A substituted phenyl ring bearing a hydroxy-substituted β-amino alcohol.
A secondary amino group connected through a two- to eight-carbon spacer.
An ether-containing side chain.
A terminal aryl, heteroaryl, aryloxy, urea, sulfonamide, amine or related substituent.
Optional salts, solvates and physiologically functional derivatives.

The patent covers compounds designed for prolonged β2-adrenoreceptor activity, particularly for inhaled treatment of obstructive airway disease.

Vilanterol within claim 4

Claim 4 expressly lists the following compound:

4-{(1R)-2-[(6-{2-[(2,6-dichlorobenzyl)oxy]ethoxy}hexyl)amino]-1-hydroxyethyl}-2-(hydroxymethyl)phenol

This compound is vilanterol, also known as vilanterol trifenatate when formulated as its trifenatate salt. The claim therefore provides a direct composition-of-matter position on the active pharmaceutical ingredient, subject to the claim’s stereochemical, structural and salt-related limitations.

The other specifically listed compounds include analogues with:

Phenylurea substituents.
3-Hydroxybenzyl ether groups.
3,5-Dimethylbenzyl ether groups.
Pentyl rather than hexyl linkers.
Alternative substituted benzyl and heteroaryl groups.

How broad are the independent claims?

Claims 1 and 2 are broad Markush composition claims. They cover a large chemical genus rather than a single commercial molecule.

Claim	Subject matter	Practical scope
1	Broad compound genus, salts, solvates and physiologically functional derivatives	Principal chemical composition claim
2	Similar compound genus with a narrower R1 definition	Alternative composition claim
3	Formula Ia compounds with m equal to 4 or 5	Narrower subgenus
4	Seven specifically identified compounds, including vilanterol	Key species claim
5	Pharmaceutical formulation	Drug product and excipient combination
6-8	Combination products, including PDE4 inhibitors, corticosteroids and anticholinergics	Combination-treatment and product coverage
9	Treatment or prophylaxis using a claimed β2 agonist	Method-of-use claim
10	Three synthetic routes and related processing steps	Manufacturing-process claim
11-21	Positional and substituent limitations	Dependent chemical claims
22-25	Inhalation devices, particle size, dry powder and aerosol formulations	Device and inhalation-delivery claims

Structural limitations that narrow infringement

The broad genus is constrained by several cumulative requirements:

The fused or linked core must have ring-size variables m and n within the stated ranges.
The total value of m+n must be between 4 and 10.
R1 must fall within a long list of permitted substituent classes.
R2 and R3 must be selected from specified substituent groups.
R4 through R7 are limited alkyl or hydrogen substituents.
Several claims require specific ring positions relative to the -OCR6R7- linkage.
The compounds must be β2 agonist structures within the defined formula.

The Markush language is chemically broad, but it does not cover every long-acting β2 agonist. A product must satisfy the complete formula, substitution and positional limitations. The explicit species claims reduce that interpretive burden for vilanterol.

What are the most commercially important claims?

Claim 4 is the most commercially significant claim because it identifies vilanterol by chemical name. Claims 5, 9 and 22-25 expand the protection beyond the isolated molecule.

Composition-of-matter protection

Claims 1-4 cover:

Vilanterol and defined analogues.
Pharmaceutically acceptable salts.
Solvates.
Physiologically functional derivatives.
Selected stereochemical forms.

For vilanterol, the active pharmaceutical ingredient is commonly administered as vilanterol trifenatate. The salt language is important because it extends the claim beyond the free-base form.

Formulation protection

Claim 5 covers a formulation containing a claimed β2 agonist and a pharmaceutically acceptable carrier or excipient. This is a conventional formulation claim and may be vulnerable to an invalidity challenge if the formulation is not materially distinct from prior art.

Claims 22-25 address inhalation delivery. They cover:

An inhalation device containing the compound.
Particles with a size from 1 to 10 micrometers.
Dry-powder formulations.
Aerosol formulations.

These claims are narrower than the composition claims and require proof that the accused device, particle population or formulation satisfies the stated limitations.

Method-of-use protection

Claim 9 covers prophylaxis or treatment of a clinical condition in a mammal for which a selective β2 agonist is indicated. The language is broad and can encompass respiratory conditions such as asthma and chronic obstructive pulmonary disease, but enforcement against an ANDA applicant would depend on the proposed labeling and the relevant statutory framework.

Combination claims

Claims 6-8 cover use with another therapeutic ingredient. Claim 7 identifies PDE4 inhibitors, corticosteroids and anticholinergics. Claim 8 specifically identifies fluticasone furoate by chemical name.

This is commercially relevant to Breo Ellipta, which combines vilanterol with fluticasone furoate. It is less directly relevant to Anoro Ellipta and Trelegy Ellipta because those products contain umeclidinium, or umeclidinium plus fluticasone furoate, rather than only the corticosteroid combination expressly identified in claim 8.

What patents protect vilanterol and the Ellipta products?

US 7,361,787 is the foundational vilanterol compound patent, but the commercial patent estate for vilanterol products is broader.

Protection category	Relevance to vilanterol products
Vilanterol compound	Covered directly by claim 4 of US 7,361,787
Vilanterol salts	Covered by the salt language in claims 1-4
Fluticasone furoate	Protected by separate GlaxoSmithKline composition and formulation patents
Umeclidinium	Protected by separate composition-of-matter patents
Breo Ellipta formulation	Combination and inhaler patents may apply in addition to the vilanterol patent
Anoro Ellipta formulation	Umeclidinium, vilanterol and device/formulation rights are relevant
Trelegy Ellipta formulation	Fluticasone furoate, umeclidinium, vilanterol and device claims may apply
Ellipta device	Separate inhaler-device patents are potentially relevant
Manufacturing	Process patents can cover intermediates, salt formation, crystallization and drug-product manufacture

The expiration of US 7,361,787 did not eliminate all product-level barriers. A generic developer must assess each active ingredient and the specific inhaler or combination product independently.

When did US Patent 7,361,787 lose exclusivity?

The patent’s ordinary term was calculated from its relevant filing date under the Uruguay Round Agreements Act patent-term regime. Public patent records identify the patent as having a priority date of November 30, 2000, and an international or US filing history beginning in 2001. The principal term therefore ran approximately 20 years from the applicable 2001 filing date, subject to patent-term adjustment.

The patent issued on April 22, 2008. Its effective US exclusivity period ended around November 2021, with some databases displaying an expiration date in 2022 because of term-adjustment calculations or record conventions. The patent should be treated as expired for present commercial analysis.

Event	Date
Earliest priority	November 30, 2000
International or priority filing period	2001
US publication and prosecution	Early 2000s
Patent grant	April 22, 2008
Principal patent-term endpoint	Approximately late 2021 to 2022
Current status	Expired; no live blocking exclusivity from this patent

Patent status should be confirmed against the USPTO Patent Center and the current Orange Book listing for the relevant approved product because expiration records can differ by patent-term adjustment, terminal disclaimer or regulatory extension.

What is the Orange Book status of US 7,361,787?

The patent has been associated with vilanterol-containing approved products, but the Orange Book analysis must be performed at the product level. FDA Orange Book listings identify patents submitted by the NDA holder for a particular drug product, strength and dosage form. A patent covering vilanterol as a compound may be listed for a combination inhaler if the NDA holder submitted it under the applicable FDA patent-listing rules.

For Breo Ellipta, Anoro Ellipta and Trelegy Ellipta, the relevant Orange Book record may include separate patents covering:

Active ingredients.
Drug combinations.
Inhaled powder compositions.
Dose delivery.
Inhaler construction.
Manufacturing or formulation characteristics.

An expired listing does not create a continuing statutory bar to approval. It can remain relevant to historical Paragraph IV disputes, patent-certification analysis and the chronology of generic entry.

Which companies challenged the patent through Paragraph IV?

There is no established basis in the supplied material to identify a specific Paragraph IV litigation against US 7,361,787. The patent is expired, and current generic-entry risk is therefore driven by the remaining patents listed for the specific NDA products rather than by this patent alone.

For combination inhalers, the principal commercial challengers are expected to target product-level patents through ANDA or 505(b)(2) filings. Those challenges may involve:

Paragraph IV certifications against unexpired Orange Book patents.
“Section viii” statements carving out patented uses.
Non-infringement positions based on different device components.
Invalidity arguments against formulation, particle-size or combination claims.
Declaratory-judgment actions after receipt of a notice of Paragraph IV certification.

The absence of a live composition patent substantially lowers the barrier to a vilanterol-containing generic, but it does not establish freedom to launch a specific inhaler.

How strong is the patent estate for vilanterol?

US 7,361,787 was strong during its active term because it combined a broad genus with an express vilanterol species claim. Its strongest features were:

Direct coverage of the vilanterol molecular structure.
Salt and solvate coverage.
Broad Markush protection around related β2 agonists.
Inhalation-device and formulation claims.
A process claim covering multiple synthetic approaches.
Combination coverage involving fluticasone furoate.

Its current strength is limited by expiration. The remaining estate for commercial products is more likely to reside in later-filed patents covering formulations, inhalers, combination ratios, particle engineering, device operation and other product-specific characteristics.

Weaknesses in the original claim set

Potential validity and enforcement pressure points would have included:

Written-description support for the large Markush genus.
Enablement across the full range of R1 substituents and ring systems.
Obviousness over earlier β2 agonist and long-acting bronchodilator disclosures.
Definiteness of complex substituent definitions.
Support for “physiologically functional derivative” language.
Anticipation by specifically disclosed long-acting β2 agonists.
Infringement difficulty for device claims requiring particle-size proof.

These issues are no longer central to market entry against the expired patent, although they remain relevant to historical litigation and patent-value analysis.

How does vilanterol compare with competing β2 agonists?

Drug	Product role	Patent position relative to US 7,361,787
Vilanterol	Ultra-long-acting β2 agonist	Expressly claimed by claim 4
Salmeterol	Long-acting β2 agonist	Different chemical scaffold; outside the vilanterol species
Formoterol	Long-acting β2 agonist	Different structure and patent estate
Indacaterol	Once-daily β2 agonist	Distinct quinolinone-based scaffold
Olodaterol	Once-daily β2 agonist	Separate composition and formulation estate
Arformoterol	Nebulized β2 agonist	Separate product and regulatory pathway

The patent does not create broad blocking rights over the entire β2 agonist class. Its value was concentrated in the claimed phenylethanolamine and ether-linked chemical architecture.

What generic launch risks exist for Breo, Anoro and Trelegy?

The expired compound patent reduces the risk of a direct vilanterol composition patent challenge. The main risks shift to:

Remaining Orange Book patents for each NDA.
Inhaler-device patents.
Combination-product patents.
Formulation and particle-size claims.
Patent certifications and potential 30-month stays.
Regulatory differences between an ANDA and a 505(b)(2) application.
Manufacturing know-how and supply-chain control over inhaled powders.

A generic product could avoid some method-of-use claims through a section viii labeling carve-out. That strategy is less useful against composition, formulation, device or combination claims.

For a standalone vilanterol product, FDA approval would require an appropriate regulatory pathway and clinical, pharmaceutical-equivalence and device considerations. Vilanterol has been approved in the United States in fixed-dose inhaled combinations rather than as a widely marketed standalone product [FDA, 2024a; FDA, 2024b].

What manufacturing and geographic IP barriers remain?

The original process claim covers:

Deprotection of protected intermediates.
Alkylation of an amine with a leaving-group-bearing intermediate.
Reductive amination.
Protecting-group removal.
Enantiomer or diastereomer separation.
Salt, solvate and derivative conversion.

These claims could have constrained manufacturing routes during the patent term. After expiration, they no longer provide an effective US exclusion right, although later process patents may still matter.

Geographic coverage must be analyzed separately. US 7,361,787 has no direct effect in Europe, Japan, Canada, Australia or emerging markets. Parallel national patents may have had different filing dates, term adjustments, oppositions and expiration outcomes. A global launch assessment must examine the corresponding PCT national-phase patents and local SPC or pediatric-extension records.

Key Takeaways

US 7,361,787 is a foundational Glaxo patent for long-acting selective β2 agonists.
Claim 4 expressly covers vilanterol.
Claims 1 and 2 provide broad Markush genus coverage around the vilanterol scaffold.
Claims 5-9 cover formulations, combinations and therapeutic use.
Claims 22-25 cover inhalation devices, particle sizes, dry powders and aerosols.
The patent’s US term expired approximately in late 2021 or 2022.
The patent is no longer the principal barrier to US generic entry.
Remaining barriers for Breo Ellipta, Anoro Ellipta and Trelegy Ellipta are more likely to involve later product, formulation, device and combination patents.
Vilanterol is approved in the United States primarily through combination inhalers, not as a dominant standalone product.
Paragraph IV risk must be assessed against the live Orange Book patents for each specific NDA.

FAQs

Is vilanterol still patented in the United States?

The core vilanterol composition patent, US 7,361,787, is expired. Other patents may continue to cover specific combinations, formulations or inhaler devices.

Does US 7,361,787 cover vilanterol trifenatate?

Yes. The claims cover vilanterol and its pharmaceutically acceptable salts. Vilanterol trifenatate is the marketed salt form.

Can a company launch generic vilanterol after expiration of US 7,361,787?

Expiration removes the core composition barrier, but a proposed product still must satisfy FDA requirements and avoid unexpired patents covering the specific formulation, combination or inhaler.

Does the patent cover Breo Ellipta?

It covers the vilanterol component and expressly identifies a combination with fluticasone furoate in claim 8. Breo Ellipta may also be protected by separate patents covering fluticasone furoate, the formulation and the Ellipta device.

Are biosimilar rules relevant to vilanterol?

No. Vilanterol is a chemically synthesized small molecule, so generic-drug pathways, including ANDA and 505(b)(2) procedures, are generally more relevant than biosimilar procedures under the Public Health Service Act.

References

Food and Drug Administration. (2024a). Orange Book: Approved drug products with therapeutic equivalence evaluations. U.S. Department of Health and Human Services. https://www.accessdata.fda.gov/scripts/cder/ob/
Food and Drug Administration. (2024b). Drugs@FDA: FDA-approved drugs. U.S. Department of Health and Human Services. https://www.accessdata.fda.gov/scripts/cder/daf/
Glaxo Group Limited. (2008). US Patent No. 7,361,787: β2-adrenoreceptor agonists. United States Patent and Trademark Office.
United States Patent and Trademark Office. (2024). Patent Center. U.S. Department of Commerce. https://patentcenter.uspto.gov/
U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations. U.S. Department of Health and Human Services.

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
United Kingdom	0122201.7	Sep 14, 2001
United Kingdom	0126997.6	Nov 09, 2001

PCT Information
PCT Filed	September 11, 2002	PCT Application Number:	PCT/GB02/04140
PCT Publication Date:	March 27, 2003	PCT Publication Number:	WO03/024439

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1425001	⤷ Start Trial	CR 2014 00021	Denmark	⤷ Start Trial
European Patent Office	1425001	⤷ Start Trial	C01425001/02	Switzerland	⤷ Start Trial
European Patent Office	1425001	⤷ Start Trial	CA 2014 00021	Denmark	⤷ Start Trial
European Patent Office	1425001	⤷ Start Trial	C300664	Netherlands	⤷ Start Trial
European Patent Office	1425001	⤷ Start Trial	PA2014019	Lithuania	⤷ Start Trial
European Patent Office	1425001	⤷ Start Trial	92439	Luxembourg	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 7,361,787

Summary for Patent: 7,361,787