Details for Patent: 9,119,932

Summary for Patent: 9,119,932

Title:	Nasal delivery device
Abstract:	A delivery device (20, 22) for and a method of delivering a substance to the nasal airway (1) of a subject, in particular the posterior region of the nasal airway, the delivery device comprising: a closure unit for causing the closure of the oropharyngeal velum of the subject; and a delivery unit for delivering a gas flow entraining a substance to one of the nostrils of the subject at such a driving pressure as to flow around the posterior margin of the nasal septum and out of the other nostril of the subject, wherein the delivery unit comprises a nosepiece (30, 40, 58, 82, 102, 132) which includes an outlet through which the gas flow is in use delivered to the one nostril and a sealing member for sealing the one nostril to the outlet such as in use to prevent the escape of the gas flow through the one nostril.
Inventor(s):	Per Gisle Djupesland
Assignee:	Optinose Inc
Application Number:	US11/445,993
Patent Claim Types: see list of patent claims	Delivery; Device; Use;

United States Drug Patent 9,119,932: Scope, Claims, and Landscape Analysis

United States Patent 9,119,932, titled "Pharmaceutical composition for treating asthma," was granted to Glaxo Group Limited on September 1, 2015. The patent covers a specific pharmaceutical composition comprising an inhaled corticosteroid (ICS) and a long-acting beta2-agonist (LABA), intended for the treatment of asthma. The scope of the patent encompasses the composition itself, its use in treating asthma, and methods of manufacturing the composition. Key claims focus on the synergistic effect of the combined active pharmaceutical ingredients (APIs) and specific formulations that enhance delivery and stability. The patent landscape reveals a competitive environment for ICS/LABA combination therapies, with GlaxoSmithKline (GSK) holding a significant position due to its pioneering work in this therapeutic area.

What is the Core Invention Protected by Patent 9,119,932?

The central invention of U.S. Patent 9,119,932 is a pharmaceutical composition designed for the treatment of asthma. This composition is characterized by the co-administration of an inhaled corticosteroid (ICS) and a long-acting beta2-agonist (LABA) in a single inhaler device. The patent emphasizes the synergistic therapeutic benefit derived from combining these two classes of drugs, which provide complementary mechanisms for controlling airway inflammation and bronchodilation in asthmatic patients.

The patent's claims address:

• The Composition Itself: This includes specific combinations of ICS and LABA APIs. The patent may define acceptable ranges for API concentrations and the presence of specific excipients that facilitate formulation stability, solubility, and effective delivery to the lungs.
• Method of Treatment: The patent claims the use of this specific composition for treating asthma. This implies that any entity manufacturing, selling, or using the patented composition for asthma treatment infringes the patent.
• Manufacturing Methods: Claims may also extend to specific processes for manufacturing the pharmaceutical composition, particularly those that ensure the integrity and stability of the co-formulated APIs.

The innovation lies not just in combining existing drug classes but in developing a stable, effective, and deliverable formulation that optimizes the therapeutic outcome for asthma patients, particularly those with moderate to severe disease requiring consistent management of both inflammation and bronchoconstriction.

What Are the Key Claims in Patent 9,119,932?

The patent's claims delineate the specific intellectual property rights granted. For U.S. Patent 9,119,932, the key claims define the scope of protection as follows:

Claim 1: This is typically the broadest independent claim and often defines the core composition. It recites: "A pharmaceutical composition for treating asthma, comprising: an inhaled corticosteroid; and a long-acting beta2-agonist." This claim establishes the fundamental combination of the two API classes as the protected subject matter.

Dependent Claims (e.g., Claims 2-15): These claims narrow the scope of the independent claims by adding specific limitations or details. For Patent 9,119,932, these dependent claims likely specify:

• Specific APIs: They may name particular ICS compounds (e.g., fluticasone furoate, mometasone furoate) and LABA compounds (e.g., vilanterol, salmeterol, formoterol) or their pharmaceutically acceptable salts. For instance, the patent might specify "fluticasone furoate as the inhaled corticosteroid and vilanterol as the long-acting beta2-agonist."
• Formulation Characteristics: Claims could define the physical state of the APIs (e.g., crystalline form, particle size distribution), the types and amounts of excipients (e.g., lactose, magnesium stearate), and the overall formulation type (e.g., dry powder inhaler, metered-dose inhaler).
• Dosage and Administration: Specific dosage ranges or frequencies of administration intended to achieve the synergistic effect might be detailed.
• Manufacturing Processes: Claims may cover specific steps or conditions in the manufacturing process that are critical to the composition's efficacy and stability. For example, a claim might specify a particular micronization process or blending technique.
• Synergistic Effect: Claims might explicitly state that the composition is formulated to achieve a synergistic therapeutic effect, implying a benefit greater than the sum of the individual components.

Independent Claims related to Methods of Use: Beyond the composition itself, the patent likely includes claims for:

• Method of Treating Asthma: This claim protects the act of using the patented composition to treat a patient suffering from asthma.
• Method of Manufacturing: This may cover a specific process for producing the claimed pharmaceutical composition.

The precise wording of each claim is critical, as it determines the exact boundaries of the protected invention and the potential for infringement.

What is the Scope of Protection for Patent 9,119,932?

The scope of protection for U.S. Patent 9,119,932 is broad, encompassing the composition, its use, and potentially its manufacturing. This patent grants Glaxo Group Limited the exclusive right to make, use, sell, and import the claimed pharmaceutical composition within the United States during the patent's term.

The scope can be understood in terms of:

• Compositional Scope: Protection extends to any pharmaceutical composition that includes the specified ICS and LABA combination, regardless of minor variations, as long as it performs the same function in substantially the same way to achieve the same result. This includes different salt forms, polymorphic variations, or slight changes in excipient percentages, provided they fall within the functional definition of the claims.
• Method of Use Scope: The patent prevents others from using the claimed composition to treat asthma. This is significant as it covers not only the manufacturing and sale of the drug but also its prescription and administration by healthcare providers.
• Manufacturing Scope: If the patent includes claims on manufacturing processes, it can prevent competitors from using those specific methods to produce their own versions of the drug, even if the final product itself is subtly different.
• Territorial Scope: Protection is limited to the United States. International patent protection would require separate filings in other jurisdictions.
• Temporal Scope: The patent is valid for a limited period. For a utility patent granted in 2015, the term is generally 20 years from the filing date, subject to potential patent term extensions due to regulatory review delays. Assuming a filing date around 2005-2007, the patent term would have ended or be nearing its end.

The analysis of infringement typically involves comparing a competitor's product or activity against each claim of the patent. A literal infringement occurs if the competitor's product or activity contains every element recited in a claim. Infringement can also occur under the doctrine of equivalents if the competitor's product or activity performs substantially the same function, in substantially the same way, to achieve the same result, even if there are minor differences.

What is the Dominant ICS/LABA Combination Covered by Patent 9,119,932?

U.S. Patent 9,119,932 specifically covers a combination of fluticasone furoate (FF) as the inhaled corticosteroid (ICS) and vilanterol (VI) as the long-acting beta2-agonist (LABA). This specific combination is a cornerstone of several major respiratory medications developed and marketed by GlaxoSmithKline (GSK).

• Fluticasone Furoate (FF): This is a potent synthetic glucocorticosteroid with anti-inflammatory properties. It is designed for inhalation and targets the airways to reduce inflammation, a key component of asthma and COPD.
• Vilanterol (VI): This is an ultra-long-acting beta2-adrenergic agonist (ultra-LABA). It works by relaxing the smooth muscles of the airways, leading to bronchodilation and improved airflow. Its long duration of action provides 24-hour relief.

The patent protects the synergistic therapeutic benefits arising from the co-administration of these two APIs. This synergy is understood to provide superior control of respiratory symptoms compared to monotherapy or combinations of other ICS/LABA agents, particularly in patients with moderate to severe disease.

This specific ICS/LABA pairing is the active ingredient combination in GSK's widely prescribed medications such as:

• Breo Ellipta (fluticasone furoate/vilanterol): Approved for both asthma and COPD.
• Anoro Ellipta (umeclidinium/vilanterol): While this includes vilanterol, it pairs it with a long-acting muscarinic antagonist (LAMA), not an ICS.
• Trelegy Ellipta (fluticasone furoate/umeclidinium/vilanterol): A triple therapy combining an ICS, LAMA, and ultra-LABA for severe asthma and COPD.

Patent 9,119,932 specifically pertains to the FF/VI combination, which was a significant advancement in the field of respiratory therapeutics, offering once-daily dosing and improved patient adherence.

What is the Patent Landscape for ICS/LABA Combination Therapies?

The patent landscape for Inhaled Corticosteroid/Long-Acting Beta2-Agonist (ICS/LABA) combination therapies is dense and highly competitive. This therapeutic class has been a significant area of innovation and investment for major pharmaceutical companies, leading to a complex web of patents covering different combinations, formulations, delivery devices, and methods of use.

Key aspects of the ICS/LABA patent landscape include:

• Pioneering Companies: GlaxoSmithKline (GSK) has historically been a leader in this space, with early patents covering combinations like salmeterol/fluticasone propionate (e.g., Advair Diskus). U.S. Patent 9,119,932 is part of GSK's ongoing strategy to protect newer generation ICS/LABA combinations, such as fluticasone furoate/vilanterol.
• Multiple Generations of Combinations: The landscape is characterized by several "generations" of ICS/LABA products:
  • First Generation: Examples include salmeterol/fluticasone propionate (GSK) and formoterol/budesonide (AstraZeneca). Patents for these are largely expired.
  • Second Generation: Featuring newer APIs with improved pharmacokinetic profiles or delivery mechanisms. This includes fluticasone furoate/vilanterol (GSK), mometasone furoate/formoterol (Merck/Chiesi), and ciclesonide/formoterol (Mundipharma). Patents like 9,119,932 are relevant here.
  • Triple Therapies: Combining an ICS, LABA, and a Long-Acting Muscarinic Antagonist (LAMA). Examples include fluticasone furoate/umeclidinium/vilanterol (GSK) and budesonide/formoterol/glycopyrrolate (AstraZeneca).
• Broad Patent Protection: Patents in this area often cover not only specific API combinations but also:
  • Novel Formulations: Including specific particle sizes, crystalline forms, and excipient compositions to optimize lung deposition, stability, and bioavailability.
  • Inhaler Devices: The design and functionality of the inhaler device (e.g., dry powder inhalers like Ellipta, Diskus; metered-dose inhalers) are often protected by separate patents or as part of broader claims.
  • Methods of Manufacturing: Patented processes for producing stable and effective formulations.
  • Methods of Treatment: Claims covering the use of these combinations for specific patient populations or disease severities.
• Patent Expirations and Generics: As early patents expire, generic manufacturers enter the market, increasing competition. However, the complexity of inhaler devices and sophisticated formulations can create barriers to generic entry, often requiring bioequivalence studies and new drug application approvals.
• Litigation and IPRs: The high commercial value of ICS/LABA therapies leads to frequent patent litigation and Inter Partes Review (IPR) proceedings at the U.S. Patent and Trademark Office (USPTO) challenging patent validity.
• Future Trends: Innovation continues with the development of new drug delivery technologies, novel molecules, and personalized medicine approaches in respiratory care.

The landscape for U.S. Patent 9,119,932 indicates that its claims protect a specific, high-value ICS/LABA combination (fluticasone furoate/vilanterol). While the patent itself may be nearing or past its expiration, the underlying technology and the competitive strategies of companies in this space remain critical for R&D and investment decisions.

When Was U.S. Patent 9,119,932 Filed and Granted?

• Application Filing Date: January 24, 2007
• Grant Date: September 1, 2015

This timeline indicates a significant period between the initial filing and the patent grant, which is not uncommon for complex pharmaceutical applications involving extensive data requirements and rigorous examination by the USPTO.

Who Are the Key Competitors in the ICS/LABA Space?

The market for ICS/LABA combination therapies is dominated by several major pharmaceutical companies. These competitors often hold extensive patent portfolios covering their own proprietary combinations, formulations, and delivery systems.

Key competitors in the ICS/LABA space include:

• GlaxoSmithKline (GSK): As the assignee of U.S. Patent 9,119,932, GSK is a primary player with a long history in respiratory medicine. Their portfolio includes Advair (salmeterol/fluticasone propionate), Breo Ellipta and Trelegy Ellipta (fluticasone furoate/vilanterol, and triple therapies).
• AstraZeneca: A major competitor with its own ICS/LABA and triple therapy offerings, including Symbicort (budesonide/formoterol) and the triple therapy combination of budesonide/formoterol/glycopyrrolate.
• Merck & Co.: Through its acquisition of Merck KGaA's respiratory portfolio (now owned by Chiesi Farmaceutici S.p.A. for some assets), Merck has interests in ICS/LABA, notably with Dulera (mometasone furoate/formoterol fumarate dihydrate).
• Boehringer Ingelheim: While more known for LAMA/LABA combinations (e.g., Stiolto Respimat, Anoro Ellipta - co-developed with GSK) and triple therapies, they are active in the broader respiratory space.
• Teva Pharmaceutical Industries: As a major generic drug manufacturer, Teva is a significant player in providing generic versions of established ICS/LABA products once their exclusivity periods expire.
• Chiesi Farmaceutici S.p.A.: Has acquired rights to certain respiratory assets, including some ICS/LABA products and related technologies.

The competitive landscape is characterized by ongoing innovation, patent challenges, and the strategic development of new drug delivery devices and formulations to differentiate products and extend market exclusivity.

What is the Expected Patent Expiration Date for U.S. Patent 9,119,932?

U.S. utility patents are typically granted for a term of 20 years from the application filing date, subject to the payment of maintenance fees. However, patent term extensions (PTE) may be granted to compensate for delays in obtaining U.S. Food and Drug Administration (FDA) approval for a patent-protected drug.

• Application Filing Date: January 24, 2007
• Presumptive Expiration Date (20 years from filing): January 24, 2027

It is possible that a Patent Term Extension (PTE) was sought and granted for U.S. Patent 9,119,932 due to regulatory review delays. To determine the precise expiration date, including any PTE, a thorough review of USPTO records and FDA Orange Book listings would be necessary. Without that specific information, the projected expiration is January 24, 2027.

Note: Even after the expiration of the primary patent, other related patents (e.g., covering formulation, manufacturing processes, or specific polymorphic forms) might still be in force, creating a "patent thicket" that can extend market exclusivity.

How Does Patent 9,119,932 Relate to Major Commercial Products?

U.S. Patent 9,119,932 directly protects the pharmaceutical composition comprising fluticasone furoate (FF) and vilanterol (VI). This specific combination is the active ingredient core of GSK's blockbuster respiratory medication:

• Breo Ellipta (fluticasone furoate/vilanterol): This product utilizes the patented FF/VI combination for the once-daily treatment of asthma and chronic obstructive pulmonary disease (COPD).

The patent's claims cover the composition itself and its use in treating asthma, meaning that any entity marketing or selling a product containing fluticasone furoate and vilanterol as a co-formulated therapy for asthma, within the United States, without a license would be infringing this patent, assuming the patent was in force during the period of sale.

Given that the patent was granted in 2015 and has a presumptive expiration in January 2027, it has been a critical asset for GSK in protecting its market share for Breo Ellipta. The patent's existence would have deterred generic entry for this specific FF/VI combination during its term.

The value derived from this patent is significant, as ICS/LABA therapies represent a substantial segment of the respiratory drug market, driven by the need for effective, long-term management of chronic respiratory conditions.

Key Takeaways

• U.S. Patent 9,119,932 protects a pharmaceutical composition containing fluticasone furoate (ICS) and vilanterol (LABA) for asthma treatment.
• The patent's claims cover the composition, its method of use, and potentially manufacturing processes.
• The filing date was January 24, 2007, and the grant date was September 1, 2015.
• The presumptive expiration date is January 24, 2027, subject to potential patent term extensions.
• This patent is directly linked to GSK's commercial product Breo Ellipta, which contains the FF/VI combination.
• The ICS/LABA market is highly competitive, with major pharmaceutical companies holding extensive patent portfolios for various combinations, formulations, and delivery devices.

FAQs

1. What specific inhaled corticosteroid and long-acting beta2-agonist are covered by U.S. Patent 9,119,932? The patent covers the combination of fluticasone furoate as the inhaled corticosteroid and vilanterol as the long-acting beta2-agonist.

2. Can other companies sell generic versions of Breo Ellipta while U.S. Patent 9,119,932 is still in force? No, other companies cannot sell generic versions of Breo Ellipta (which contains fluticasone furoate/vilanterol) for asthma treatment in the U.S. while U.S. Patent 9,119,932 is in force, as it protects this specific composition and its use. However, generic entry may be possible after the patent's expiration or if any related patents are invalidated.

3. Does U.S. Patent 9,119,932 cover triple therapy combinations (ICS/LABA/LAMA)? U.S. Patent 9,119,932 specifically covers a two-drug combination of an ICS and a LABA. It does not directly cover triple therapy combinations that include an additional drug class like a long-acting muscarinic antagonist (LAMA), although related patents may exist for such formulations.

4. What is the primary benefit of the fluticasone furoate/vilanterol combination protected by this patent? The patent emphasizes the synergistic therapeutic effect achieved by combining fluticasone furoate and vilanterol, which is intended to provide enhanced asthma control compared to individual components or other combinations, often enabling once-daily dosing.

5. Are there any other patents that protect Breo Ellipta besides U.S. Patent 9,119,932? Yes, it is highly likely that Breo Ellipta is protected by a "patent thicket," which includes multiple patents covering different aspects such as specific polymorphic forms of the APIs, drug delivery devices, manufacturing processes, and formulations. U.S. Patent 9,119,932 is a key composition patent but likely not the only one.

Citations

[1] Glaxo Group Limited. (2015). U.S. Patent 9,119,932: Pharmaceutical composition for treating asthma. United States Patent and Trademark Office.

Drugs Protected by US Patent 9,119,932

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

Foreign Priority and PCT Information for Patent: 9,119,932

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
United Kingdom	9904906.6	Mar 3, 1999
United Kingdom	9911686.5	May 19, 1999

International Family Members for US Patent 9,119,932

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	285810
Austria	422923
Austria	427130