Details for Patent: 9,642,913

Summary for Patent: 9,642,913

Title:	Pharmaceutical composition including alkyl glycoside and an anti-seizure agent
Abstract:	A composition including a surfactant and at least one alkyl glycoside and/or saccharide alkyl ester and a drug. The surfactant composition(s) when admixed with a drug is non-toxic and non-irritating, while stabilizing and increasing the bioavailability of the drug. The invention also provides compositions that enhance absorption of drugs via the oral, ocular, nasal, nasolacrimal, inhalation or pulmonary, oral cavity (sublingual or Buccal cell) or CSF delivery route of a patient, including but not limited to insulin, glucagon and exendin-4.
Inventor(s):	Edward T. Maggio
Assignee:	Aegis Therapeutics LLC
Application Number:	US14/152,686
Patent Claim Types: see list of patent claims	Composition; Delivery;

US Patent 9,642,913: Claim Scope, Expiration, Orange Book Status, and Intranasal Antiseizure Patent Landscape

US Patent 9,642,913 protects intranasal compositions that combine an antiseizure agent with dodecyl-beta-D-maltoside, also called dodecyl maltoside or DDM. The independent claims require an intranasal route, an anti-seizure central nervous system compound, DDM, and increased absorption or bioavailability in cerebrospinal fluid. Claims 1 and 5 impose a DDM concentration range of approximately 0.01% to 1.0%; claim 4 separately requires a hydrophile-lipophile balance, or HLB, range of approximately 10 to 20.

The patent is technically focused and narrower than a general patent covering all intranasal antiseizure products. A competing product that does not contain DDM should not fall within the literal scope of these claims, although separate patents may create independent infringement risk.

What does US Patent 9,642,913 claim?

The patent has two independent composition claims and five dependent claims in the claim set provided.

Claim	Core subject matter	Additional limitation
1	Intranasal composition containing DDM and an anti-seizure agent	DDM at about 0.01% to 1.0%; increased CSF absorption and bioavailability
2	Composition of claim 1	Drop, spray, aerosol, or sustained-release format
3	Composition of claim 1	Specified mucosal delivery-enhancing agents
4	Intranasal composition containing DDM and an anti-seizure agent	DDM has HLB of about 10 to 20; increased CSF absorption and bioavailability
5	Composition of claim 4	DDM at about 0.01% to 1.0%
6	Composition of claim 4	Drop, spray, aerosol, or sustained-release format
7	Composition of claim 4	Specified mucosal delivery-enhancing agents

The claims are composition claims. They do not expressly require a particular dose, administration frequency, disease indication, patient age, seizure type, or named antiseizure molecule.

What technical elements must be present for literal infringement?

A product would generally need to satisfy every limitation of at least one asserted claim. The central elements are:

1. An intranasal pharmaceutical composition.
2. A compound that affects the central nervous system.
3. The compound must be an anti-seizure agent.
4. Dodecyl-beta-D-maltoside must be present as the alkyl glycoside.
5. For claim 1, DDM must be present at approximately 0.01% to 1.0%.
6. For claim 4, DDM must have an HLB value of approximately 10 to 20.
7. The DDM must increase absorption and bioavailability of the antiseizure agent in CSF.

Claims 2 and 6 add a delivery format. A spray is not required for the independent claims. A drop, aerosol, or sustained-release system may also qualify if all independent-claim limitations are met.

Claims 3 and 7 add a defined list of mucosal delivery-enhancing agents:

• Citric acid
• Sodium citrate
• Propylene glycol
• Glycerin
• Ascorbic acid
• Sodium metabisulfite
• Disodium EDTA
• Benzalkonium chloride
• Sodium hydroxide
• Combinations of those agents

The list is closed as drafted. An excipient not included in the list would not satisfy the express limitation of claims 3 or 7, although it could still be relevant to claims 1 or 4.

How broad is the anti-seizure-agent limitation?

The claims do not identify a single active ingredient. “Anti-seizure agent” can potentially cover multiple small-molecule antiseizure drugs, subject to the patent’s specification, prosecution history, and applicable claim-construction principles.

Potentially relevant drug classes include:

• Benzodiazepines, such as midazolam and diazepam
• Barbiturates, such as phenobarbital
• Sodium-channel agents, such as carbamazepine and lacosamide
• GABA-related agents, such as vigabatrin
• Broad-spectrum antiseizure drugs, such as levetiracetam and valproate

The breadth creates an enablement and written-description issue if the specification does not demonstrate or adequately teach the full range of claimed antiseizure compounds. A challenger could argue that the patent supports only a narrower group of compounds or particular formulations.

The functional requirement that DDM “increases absorption and bioavailability” also matters. The claim does not merely require DDM to be present. It requires a pharmacokinetic effect in CSF. Product testing, formulation composition, pharmacokinetic data, and the meaning of “increases” compared with an appropriate control would become important in an infringement dispute.

What formulation technologies are protected?

The patent covers DDM-based intranasal delivery systems rather than a particular device platform.

DDM concentration

Claims 1 and 5 specify a range of about 0.01% to 1.0%. The range is broad enough to cover a 100-fold concentration span. “About” may create a limited tolerance around the endpoints, but the permissible range would depend on intrinsic claim construction and prosecution history.

A formulation with DDM below 0.01% or above 1.0% could avoid the literal concentration limitation of claims 1 and 5. It could still face risk under claim 4 if the product satisfies the HLB and functional limitations.

HLB requirement

Claim 4 requires an HLB value of approximately 10 to 20 and identifies DDM as the alkyl glycoside. HLB values can vary based on the calculation method, experimental assumptions, and product specifications. That creates a potential claim-construction and testing issue.

Claim 4 does not expressly include the 0.01% to 1.0% concentration range. That limitation enters only through claim 5. A DDM concentration outside the stated range may therefore remain within the potential literal scope of claim 4 if the other limitations are met.

Delivery format

Claims 2 and 6 cover:

• Drops
• Sprays
• Aerosols
• Sustained-release formats

The independent claims are not limited to commercially conventional metered nasal sprays. A single-dose device, pump spray, aerosolized system, or sustained-release intranasal format could be relevant.

When does US Patent 9,642,913 lose exclusivity?

US Patent 9,642,913 issued on May 9, 2017. The patent’s ordinary expiration date cannot be calculated reliably from the patent number or claim text alone because US patent term depends on the earliest effective nonprovisional filing date, patent-term adjustment, terminal disclaimers, and any applicable patent-term extension. The governing framework generally provides a term of 20 years from the earliest effective nonprovisional filing date, subject to statutory adjustments. (35 U.S.C. § 154.)

The patent’s practical exclusionary period is therefore controlled by the patent record, not by the 2017 issue date. Patent expiration also does not necessarily determine market entry. Regulatory exclusivity, later continuation patents, formulation patents, device patents, and drug-specific method-of-use patents can create separate barriers.

Is US Patent 9,642,913 listed in the Orange Book?

An Orange Book listing is product-specific. FDA lists patents submitted for approved drug products, not every patent that may theoretically cover a formulation or delivery technology. A patent covering DDM-enabled intranasal delivery would generally require linkage to an approved product containing the claimed active ingredient and formulation.

The major US rescue products provide useful comparisons:

Product	Active ingredient	Sponsor	Intranasal formulation relevance
Nayzilam	Midazolam	UCB	Intranasal benzodiazepine product
Valtoco	Diazepam	Neurelis	Intranasal benzodiazepine product
BAQSIMI	Glucagon	Lilly	Intranasal powder, not an antiseizure product

Nayzilam and Valtoco are small-molecule products, not biologics. Their Orange Book patent positions depend on the patents submitted for their approved formulations, methods of use, devices, and manufacturing processes. A DDM patent is not automatically an Orange Book-listed patent for either product. The approved labels and inactive-ingredient disclosures should be compared with the DDM limitation before assuming coverage. (FDA, 2024a, 2024b.)

What generic entry risks exist?

The patent creates the greatest risk for a generic or 505(b)(2) applicant that proposes all of the following:

• The same or a therapeutically equivalent antiseizure active ingredient
• Intranasal administration
• DDM as a permeability or absorption enhancer
• DDM concentration within approximately 0.01% to 1.0%
• A demonstrated increase in CSF absorption or bioavailability

A Paragraph IV certification would be relevant only if the patent is listed in the Orange Book for the reference product. If it is not listed, the applicant may still face a patent infringement action based on a product-specific statutory notice or other patent theory, but the Orange Book automatic stay mechanism would not operate in the same manner. (21 U.S.C. § 355(j).)

A design-around strategy could involve:

• Removing DDM
• Using a different absorption enhancer
• Selecting a DDM concentration outside the claimed range
• Using a formulation that does not produce the claimed CSF effect
• Developing a non-intranasal dosage form
• Challenging whether the active ingredient qualifies as an anti-seizure agent

Each approach introduces separate technical, regulatory, or patent risks. Substituting another surfactant may implicate unrelated patents covering alkyl glycosides, surfactant systems, permeation enhancers, or device combinations.

Which companies are most exposed to this patent?

Exposure is highest for companies developing intranasal rescue medicines that use DDM or a closely related alkyl glycoside. Potentially relevant commercial groups include:

• Sponsors of intranasal benzodiazepines
• Developers of intranasal levetiracetam or other antiseizure agents
• Companies licensing Intravail or comparable intranasal absorption technology
• 505(b)(2) developers pursuing rapid-onset seizure rescue products
• Device companies supplying nasal sprays for CNS drugs

The patent is less relevant to products that use conventional aqueous nasal formulations without DDM. It is also less relevant to oral, buccal, injectable, rectal, or transdermal antiseizure products unless a separate claim or patent family covers those routes.

How strong is the patent estate?

The supplied claims have meaningful technical specificity but several potential pressure points.

Strengths

• DDM is expressly identified rather than claimed only by a broad genus.
• The claims target a specific intranasal use case.
• Claims 1 and 5 establish a defined concentration range.
• Claims 2, 3, 6, and 7 create narrower fallback positions.
• The CSF absorption limitation ties the formulation to a pharmacokinetic result.

Vulnerabilities

• “Suitable nontoxic” may invite indefiniteness arguments if the specification does not provide objective boundaries.
• “About” creates endpoint uncertainty.
• HLB measurement may vary depending on methodology.
• “Increases absorption and bioavailability” requires a baseline and a reliable test method.
• The anti-seizure-agent genus may be challenged for written description or enablement breadth.
• The claims are composition claims, so a product that uses a different enhancer may avoid literal infringement.

Patent strength cannot be measured from the claims alone. Prosecution amendments, cited prior art, examiner interviews, continuity data, terminal disclaimers, and post-grant proceedings materially affect enforceability.

What prior-art and competitive patents are most relevant?

The closest technical prior art is likely to include:

• Intranasal delivery of CNS-active compounds
• Alkyl glycoside absorption enhancers
• Dodecyl maltoside and related maltoside surfactants
• Intranasal benzodiazepine formulations
• Nasal delivery systems designed to improve CSF exposure
• Mucosal formulations containing citrate, glycerin, propylene glycol, EDTA, or benzalkonium chloride

The principal competitive patent categories are:

Patent category	Typical commercial function
Active-ingredient patents	Protect the antiseizure molecule
Intranasal formulation patents	Protect concentration, pH, excipients, and stability
Absorption-enhancer patents	Protect DDM or alternative permeation enhancers
Device patents	Protect pumps, actuators, dose counters, and delivery geometry
Method-of-use patents	Protect seizure rescue, seizure clusters, or status epilepticus
Manufacturing patents	Protect sterile filling, particle engineering, or spray production
Combination patents	Protect active ingredient plus enhancer or device

A freedom-to-operate review must assess the entire family and relevant continuation applications. A single issued patent may be only one layer of the estate.

What litigation and settlement issues should be reviewed?

The key litigation questions are:

1. Has the patent been asserted against an intranasal antiseizure product?
2. Has any party filed an inter partes review or post-grant challenge?
3. Were claims amended during prosecution to overcome prior art?
4. Is there a terminal disclaimer tying the patent to another patent?
5. Are there continuation or divisional patents with broader claims?
6. Has the patent been licensed to a nasal-delivery technology company?
7. Does any settlement restrict a generic or 505(b)(2) launch date?

The claim text alone does not establish an infringement action, Paragraph IV dispute, settlement agreement, or license. Those issues must be distinguished from the technical scope of US 9,642,913.

How does this patent compare with Nayzilam and Valtoco?

US 9,642,913 is enhancer-centered. Nayzilam and Valtoco are product-centered commercial benchmarks.

Issue	US 9,642,913	Nayzilam	Valtoco
Protected concept	DDM-enabled intranasal antiseizure composition	Approved intranasal midazolam product	Approved intranasal diazepam product
Required active	Any qualifying anti-seizure agent	Midazolam	Diazepam
DDM required	Yes, under supplied claims	Must be confirmed against the approved formulation	Must be confirmed against the approved formulation
Patent risk type	Formulation and delivery technology	Drug, formulation, method, and device patents	Drug, formulation, method, and device patents
Biosimilar pathway	Not applicable	Not applicable	Not applicable
Generic pathway	Potential 505(b)(2) or ANDA issue depending on listing and product	ANDA or 505(b)(2), subject to listed patents and exclusivity	ANDA or 505(b)(2), subject to listed patents and exclusivity

Neither Nayzilam nor Valtoco establishes infringement merely because each is an intranasal antiseizure product. DDM, concentration, pharmacokinetic effect, and the full claim limitations remain decisive.

Key Takeaways

• US 9,642,913 is directed to intranasal antiseizure compositions containing dodecyl-beta-D-maltoside.
• Claims 1 and 5 require approximately 0.01% to 1.0% DDM.
• Claim 4 requires DDM with an HLB of approximately 10 to 20 but does not independently recite the concentration range.
• The claims require increased absorption and bioavailability in CSF, creating a pharmacokinetic proof issue.
• Drops, sprays, aerosols, and sustained-release formats are covered only by dependent claims.
• The patent is not automatically an Orange Book patent for Nayzilam, Valtoco, or another product.
• No biosimilar pathway applies because antiseizure agents covered by these claims are generally small molecules.
• Generic and 505(b)(2) exposure is highest for products that deliberately use DDM in an intranasal antiseizure formulation.
• The patent’s exact expiration date requires review of the patent-term calculation, PTA, terminal disclaimers, and continuity data.
• Continuation patents, licenses, formulation patents, device patents, and method-of-use patents may materially expand the commercial risk beyond this claim set.

FAQs About US Patent 9,642,913

Does US Patent 9,642,913 cover intranasal midazolam?

It may cover an intranasal midazolam composition only if the product also satisfies the DDM, concentration or HLB, antiseizure-agent, and CSF bioavailability limitations.

Can a formulation avoid the patent by using a different nasal absorption enhancer?

A formulation that omits DDM should avoid the literal DDM limitation in the supplied claims. Separate patents covering the substitute enhancer, active ingredient, formulation, or device may still apply.

Does the patent cover intranasal diazepam?

The claims can potentially encompass diazepam as an anti-seizure agent, but only when the intranasal composition contains DDM and satisfies the remaining limitations.

Is DDM the same as dodecyl maltoside?

DDM commonly refers to dodecyl-beta-D-maltoside, a nonionic alkyl glycoside surfactant. Product specifications should be checked because chemical identity, isomeric form, purity, and concentration can affect claim analysis.

Can an expired active-ingredient patent still leave risk under this patent?

Yes. A product can face a separate formulation or delivery patent after the active ingredient’s basic compound patent expires. Patent expiry must be assessed patent by patent.

References

1. Food and Drug Administration. (2024a). Nayzilam (midazolam) nasal spray prescribing information. U.S. Department of Health and Human Services.

2. Food and Drug Administration. (2024b). Valtoco (diazepam) nasal spray prescribing information. U.S. Department of Health and Human Services.

3. Food and Drug Administration. (2024c). Approved drug products with therapeutic equivalence evaluations. U.S. Department of Health and Human Services.

4. United States Code. (2024). 21 U.S.C. § 355: New drugs.

5. United States Code. (2024). 35 U.S.C. § 154: Contents and term of patent; provisional rights.

6. United States Patent and Trademark Office. (2017). US Patent No. 9,642,913. Government of the United States.

Drugs Protected by US Patent 9,642,913

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

International Family Members for US Patent 9,642,913

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	3678649		301317	Netherlands
European Patent Office	3678649		CA 2025 00007	Denmark
European Patent Office	3678649		PA2025507	Lithuania
European Patent Office	3678649		C20250011	Finland
European Patent Office	3678649		122025000010	Germany