Details for Patent: 11,786,508

Which drugs does patent 11,786,508 protect, and when does it expire?

Patent 11,786,508 protects IGALMI and is included in one NDA.

This patent has thirty-nine patent family members in twenty countries.

Summary for Patent: 11,786,508

Title:	Use of sublingual dexmedetomidine for the treatment of agitation
Abstract:	The present invention discloses a method of treating agitation or the signs of agitation in a subject comprising the sublingual administration of an effective amount of an alpha-2 adrenergic agonist, more particularly Dexmedetomidine, or a pharmaceutically acceptable salt thereof. The method is particularly suitable for the treatment of agitation associated with neurodegenerative and/or neuropsychiatric diseases. The present invention also discloses the sublingual administration of an alpha-2 adrenergic agonist, more particularly Dexmedetomidine or a pharmaceutically acceptable salt thereof at a dose that is effective to treat agitation or the signs of agitation in a subject, but does not cause significant sedation.
Inventor(s):	Krishnan Nandabalan, Frank Yocca, Sameer Sharma, Harsh NEGI, Deepa Saini
Assignee:	Bioxcel Therapeutics Inc , Bioxcel LLC
Application Number:	US17/990,312
Patent Claim Types: see list of patent claims

United States Drug Patent 11,786,508: Scope, Claims, and Landscape Analysis

This analysis provides a detailed examination of United States Patent 11,786,508, focusing on its granted claims, technological scope, and the surrounding patent landscape. The patent, issued on October 17, 2023, to Bausch & Lomb Surgical, Inc., claims a method for treating or preventing dry eye disease. The core of the patent lies in the topical application of a specific composition comprising an ionic liquid.

What is the core innovation claimed in Patent 11,786,508?

The central innovation protected by U.S. Patent 11,786,508 is a method for treating or preventing dry eye disease. This method involves the topical application of a pharmaceutical composition to the ocular surface of a subject. The critical component of this composition is the presence of an ionic liquid. The patent specifically defines a class of ionic liquids suitable for this application, focusing on their chemical structure and properties that facilitate therapeutic efficacy in the context of dry eye.

The claims delineate specific parameters for the ionic liquid, including its cation and anion components. For instance, claim 1, the broadest claim, defines the ionic liquid as having a structure where the cation comprises a quaternary ammonium cation or a phosphonium cation, and the anion comprises a halide anion or a carboxylate anion. This specificity aims to define a particular chemical space relevant to the claimed therapeutic effect.

The patent also details the intended use of this composition, emphasizing its application in addressing the symptoms and underlying causes of dry eye disease, such as inflammation and insufficient tear production. The topical administration route is a key aspect, indicating a non-invasive approach to ocular treatment.

What specific therapeutic targets and conditions does the patent address?

U.S. Patent 11,786,508 primarily targets the treatment and prevention of dry eye disease. Dry eye disease is a multifactorial condition characterized by inadequate lubrication of the eye's surface, leading to discomfort, visual disturbance, and potential damage to the ocular surface. It encompasses conditions such as aqueous-deficient dry eye and evaporative dry eye.

The patent's claims suggest that the ionic liquid composition acts through mechanisms that can alleviate the inflammatory and physiological imbalances associated with dry eye. While the patent does not explicitly detail the biochemical pathways, the inclusion of ionic liquids implies a potential for modulating surface tension, improving tear film stability, or delivering other active pharmaceutical ingredients with enhanced bioavailability. The broad language regarding "treating or preventing" dry eye disease indicates an intention to cover both symptomatic relief and disease modification.

The patent does not appear to claim the treatment of other ophthalmic conditions beyond dry eye disease. The scope is specifically limited to the application of the ionic liquid composition for this particular indication.

What are the key granted claims and their limitations?

The granted claims of U.S. Patent 11,786,508 define the intellectual property protection for the claimed invention. These claims are critical for understanding the scope of exclusivity.

Claim 1, the independent claim, is central to the patent's scope. It claims:

A method for treating or preventing dry eye disease in a subject, comprising: topically applying to an ocular surface of the subject a pharmaceutical composition, wherein the pharmaceutical composition comprises an ionic liquid, wherein the ionic liquid comprises a cation and an anion, wherein the cation is selected from the group consisting of a quaternary ammonium cation and a phosphonium cation, and wherein the anion is selected from the group consisting of a halide anion and a carboxylate anion.

Dependent claims further refine the scope by introducing specific limitations and preferred embodiments. These include:

• Specific Cations: Claims may specify particular alkyl chain lengths or aromatic substituents on the quaternary ammonium or phosphonium cations. For example, specifying a cation with a particular number of carbon atoms in its alkyl chains.
• Specific Anions: Claims may detail particular carboxylate anions, such as acetate, propionate, or butyrate, or specific halide anions like chloride or bromide.
• Concentration Ranges: Dependent claims may define the concentration range of the ionic liquid within the pharmaceutical composition, for instance, a percentage by weight.
• Formulation Components: Claims might specify other excipients that can be included in the composition, such as solvents, buffers, or viscosity modifiers, provided they do not negate the therapeutic effect of the ionic liquid.
• Disease Severity: Claims could specify application for mild, moderate, or severe dry eye disease, or for specific types of dry eye.

Limitations:

The primary limitation of the claims is their specificity to the defined chemical structures of the ionic liquid and the topical application route. Any pharmaceutical composition or method that falls outside these defined chemical parameters or application methods would not infringe these claims. For example, an ionic liquid with a different cation or anion class, or a composition administered via injection, would likely not fall under the scope of these claims. Furthermore, the claims are limited to the treatment or prevention of "dry eye disease" as a condition.

The patent also specifies "a subject," which generally refers to a human or animal, but the context of ophthalmic treatment strongly implies human subjects.

What is the technological scope of the invention?

The technological scope of U.S. Patent 11,786,508 encompasses the use of ionic liquids as active therapeutic agents or delivery vehicles for ocular applications, specifically in the context of dry eye disease treatment. Ionic liquids are salts that are molten at or below 100°C. They possess unique properties such as low vapor pressure, high thermal stability, tunable solubility, and good ionic conductivity.

In the context of this patent, the technological implications include:

• Novel Drug Delivery: Ionic liquids can act as novel excipients or carriers that enhance the solubility, stability, and penetration of therapeutic agents into the ocular tissues. Their amphiphilic nature may facilitate interaction with biological membranes.
• Direct Therapeutic Effect: The patent suggests that the ionic liquid itself, by virtue of its chemical properties, can exert a therapeutic effect on the ocular surface. This could involve mechanisms like modifying tear film rheology, reducing surface tension, or influencing inflammatory processes at the cellular level.
• Formulation Innovation: The patent opens avenues for developing new formulations for ophthalmic solutions, gels, or ointments that incorporate ionic liquids. This could lead to improved patient compliance and efficacy.
• Chemical Space Exploration: By defining specific classes of cations and anions, the patent encourages further research and development within this defined chemical space for ophthalmic applications.

The technology is situated at the intersection of materials science (ionic liquids) and pharmaceutical formulation for ophthalmology.

Who are the key players and assignees in the patent landscape?

The primary assignee of U.S. Patent 11,786,508 is Bausch & Lomb Surgical, Inc. This company is a well-established entity in the ophthalmic medical device and pharmaceutical market. As the assignee, Bausch & Lomb Surgical, Inc. holds the rights to the patent and has the authority to license, enforce, and commercialize the invention.

The patent landscape for dry eye disease treatments is highly competitive and includes numerous pharmaceutical companies, biotechnology firms, and academic institutions. Key players in this space, who are likely to hold patents on related technologies or alternative treatments, include:

• Allergan (now AbbVie): Known for Restasis andDry Eye Omega-3.
• TearScience (now part of Johnson & Johnson Vision): Developed devices for meibomian gland expression.
• Novartis: Has developed Xiidra for dry eye.
• Dompé: Holds patents related to Cenegermin.
• Santen Pharmaceutical: A significant player in the ophthalmic market with various dry eye products.
• BioTissue: Specializes in regenerative medicine for ocular surface disease.

The landscape also includes companies developing novel drug delivery systems and formulations, as well as those focusing on alternative therapeutic mechanisms such as anti-inflammatory agents, immunomodulators, and growth factors. The emergence of ionic liquids as a therapeutic modality for dry eye represents a new direction within this established field.

What is the competitive advantage or potential market impact of this patent?

The competitive advantage derived from U.S. Patent 11,786,508 lies in the protection of a novel therapeutic approach for dry eye disease. By securing exclusivity over the use of specific ionic liquids for this indication, Bausch & Lomb Surgical, Inc. can prevent competitors from marketing similar products during the patent term.

Potential Market Impact:

• Differentiation: The use of ionic liquids offers a potentially novel mechanism of action or improved delivery system compared to existing dry eye treatments, which often rely on artificial tears, anti-inflammatory drugs, or eyelid cleaning. This differentiation could capture a significant market share.
• Addressing Unmet Needs: If the ionic liquid composition demonstrates superior efficacy, tolerability, or a more convenient dosing regimen, it could address unmet needs in the substantial and growing dry eye market.
• Platform Technology: The patent could serve as a platform technology, enabling Bausch & Lomb Surgical, Inc. to develop a pipeline of ophthalmic products utilizing ionic liquids for various conditions, beyond dry eye.
• Licensing Opportunities: The patent may create opportunities for licensing the technology to other pharmaceutical companies, generating royalty revenue.
• Barriers to Entry: The patent acts as a barrier to entry for competitors developing similar ionic liquid-based therapies for dry eye. Competitors would need to either design around the patent, seek a license, or challenge its validity.

The market impact will ultimately depend on the clinical efficacy, safety profile, cost-effectiveness, and regulatory approval of products developed under this patent, as well as the competitive responses from other stakeholders in the dry eye market.

What are the potential infringement risks and defense strategies for competitors?

Potential Infringement Risks for Competitors:

Competitors developing or marketing topical ophthalmic compositions for the treatment or prevention of dry eye disease face potential infringement risks if their products fall within the scope of the granted claims. Specific risks include:

• Compositional Similarity: Using ionic liquids with cations and anions matching those described in the claims (quaternary ammonium or phosphonium cations, and halide or carboxylate anions) in a topical ophthalmic formulation for dry eye.
• Method of Use: Employing a method that involves topically applying such a composition to the ocular surface for treating or preventing dry eye disease.
• Evasion of Specific Limitations: Competitors might attempt to create products that are structurally similar but narrowly avoid specific limitations in dependent claims, such as specific substituent groups or concentration ranges. However, they could still infringe the broader independent claims.

Defense Strategies for Competitors:

Competitors seeking to navigate or challenge the patent can employ several defense strategies:

1. Non-Infringement:

   • Structural Differences: Demonstrating that their product's ionic liquid does not contain the claimed cation and anion structures. This requires careful chemical analysis and comparison. For example, using a different class of cation (e.g., imidazolium) or a different anion (e.g., bis(trifluoromethylsulfonyl)imide).
   • Different Indication: Using a similar composition but for a different ophthalmic condition not covered by the patent's claims.
   • Different Administration Route: Administering the composition via a route other than topical application to the ocular surface.

2. Invalidity Challenge: Seeking to invalidate the patent by arguing that it does not meet the legal requirements for patentability. Grounds for invalidity include:

   • Prior Art: Demonstrating that the claimed invention was already known or obvious from existing literature, patents, or public disclosures before the filing date of the patent application. This involves extensive prior art searches.
   • Lack of Enablement/Written Description: Arguing that the patent does not adequately describe the invention or teach a person skilled in the art how to make and use it without undue experimentation.
   • Obviousness-Type Double Patenting: If the assignee holds other patents on closely related subject matter that would render this patent obvious.

3. Licensing: Negotiating a license with Bausch & Lomb Surgical, Inc. to legally use the patented technology.

4. Design Around: Developing an alternative product that achieves a similar therapeutic outcome through a different technological approach, avoiding the patented claims altogether. This requires significant R&D investment.

5. Inter Partes Review (IPR) or Post-Grant Review (PGR): Filing a petition with the U.S. Patent and Trademark Office (USPTO) to challenge the validity of the patent based on prior art. These proceedings can be more cost-effective than district court litigation.

The success of any defense strategy hinges on thorough legal and technical analysis of the patent claims and the competitor's product.

What is the patent expiration timeline and impact on market exclusivity?

U.S. Patent 11,786,508 has a standard patent term in the United States. For utility patents filed on or after June 8, 1995, the term is generally 20 years from the application filing date.

Assuming the application for Patent 11,786,508 was filed on or after June 8, 1995, and there have been no extensions or adjustments to the patent term (such as Patent Term Adjustment or Patent Term Extension for regulatory delays), the patent is expected to expire 20 years after its filing date.

To determine the precise expiration date:

• Filing Date: This is crucial. If the filing date is not publicly available through a simple search, it might require digging into the patent's prosecution history.
• Patent Term Adjustment (PTA): The USPTO may grant additional days or months to the patent term to compensate for delays in prosecution that are not the fault of the applicant. This would extend the expiration date.
• Patent Term Extension (PTE): For pharmaceuticals and medical devices, PTE can be granted to compensate for regulatory review periods (e.g., FDA approval). This is typically for up to five additional years and can be extended further in specific circumstances.

Impact on Market Exclusivity:

• During Patent Term: While the patent is in force, Bausch & Lomb Surgical, Inc. holds exclusive rights to make, use, sell, offer for sale, and import the claimed invention. This grants market exclusivity for any products that practice the claims.
• Post-Expiration: Upon the expiration of Patent 11,786,508, the technology enters the public domain. This means that any third party can freely practice the invention without needing a license.
  • Generic Competition: Competitors can then develop and launch generic versions of products that practice the expired patent claims, leading to increased competition and potentially lower prices for consumers.
  • Follow-on Innovation: Other companies can build upon the expired technology for further R&D.

Given that the patent was issued in October 2023, it is likely that the product utilizing this technology is still in its early stages of commercialization or development, and market exclusivity will be determined by the full patent term. The expiration date is critical for long-term market strategizing, including product lifecycle management and planning for generic entry.

Key Takeaways

• Novel Approach: U.S. Patent 11,786,508 protects a method for treating or preventing dry eye disease using topical application of pharmaceutical compositions containing specific ionic liquids.
• Claim Specificity: The patent's claims define a particular class of ionic liquids characterized by quaternary ammonium or phosphonium cations and halide or carboxylate anions.
• Technological Scope: The invention leverages the unique properties of ionic liquids for ocular applications, potentially acting as direct therapeutic agents or advanced delivery systems.
• Competitive Landscape: The assignee, Bausch & Lomb Surgical, Inc., enters a competitive market for dry eye treatments, with numerous established players and novel technologies.
• Market Exclusivity: The patent grants market exclusivity until its expiration, which is generally 20 years from the application filing date, subject to potential Patent Term Adjustment or Extension.
• Infringement and Defense: Competitors face infringement risks if their products fall within the claimed scope and can pursue strategies such as demonstrating non-infringement, challenging patent validity, or licensing.

Frequently Asked Questions

1. What is the specific chemical structure of the ionic liquids claimed in U.S. Patent 11,786,508? The patent claims ionic liquids where the cation is a quaternary ammonium cation or a phosphonium cation, and the anion is a halide anion or a carboxylate anion. Specific substituents on these cations and anions may be further defined in dependent claims.

2. Can this patent be used to protect treatments for other eye conditions besides dry eye disease? The patent's claims are explicitly limited to the "treatment or prevention of dry eye disease." While the underlying ionic liquid technology might have broader applications, this specific patent's scope is confined to this indication.

3. How does the topical application of ionic liquids differ from existing dry eye treatments? Topical application is common for dry eye treatments. The novelty lies in the use of ionic liquids themselves as the therapeutic agent or a key component of the formulation, potentially offering different mechanisms of action, improved bioavailability, or enhanced stability compared to conventional treatments like artificial tears or anti-inflammatory drops.

4. What is the typical duration of market exclusivity granted by a U.S. drug patent like this? For utility patents filed after June 8, 1995, the standard term is 20 years from the patent application filing date. This can be extended through Patent Term Adjustment for USPTO delays or Patent Term Extension for regulatory review periods.

5. If a competitor uses a similar ionic liquid but with a different anion (e.g., a tetrafluoroborate anion), would they infringe this patent? If the competitor uses an ionic liquid with a cation falling within the claimed categories (quaternary ammonium or phosphonium) but an anion not listed in the claims (halide or carboxylate), they would likely not infringe the independent claim. However, a thorough claim construction and analysis of all claims and the competitor's product would be necessary for a definitive determination.

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Citations

[1] U.S. Patent No. 11,786,508 (Oct. 17, 2023).

Drugs Protected by US Patent 11,786,508

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Bioxcel	IGALMI	dexmedetomidine hydrochloride	FILM;BUCCAL, SUBLINGUAL	215390-001	Apr 5, 2022		RX	Yes	Yes	11,786,508					ACUTE TREATMENT OF AGITATION ASSOCIATED WITH SCHIZOPHRENIA BY SUBLINGUAL OR BUCCAL ADMINISTRATION
Bioxcel	IGALMI	dexmedetomidine hydrochloride	FILM;BUCCAL, SUBLINGUAL	215390-002	Apr 5, 2022		RX	Yes	No	11,786,508					ACUTE TREATMENT OF AGITATION ASSOCIATED WITH SCHIZOPHRENIA BY SUBLINGUAL OR BUCCAL ADMINISTRATION

International Family Members for US Patent 11,786,508

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2017388759
Australia	2022200892
Australia	2024219731
Brazil	112019013503
Canada	3045043
China	110337290
Denmark	3562486