Details for Patent: 9,757,384

Which drugs does patent 9,757,384 protect, and when does it expire?

Patent 9,757,384 protects VYKAT XR and is included in one NDA.

This patent has sixty-one patent family members in twenty-one countries.

Summary for Patent: 9,757,384

Title:	Methods for treating subjects with Prader-Willi syndrome or Smith-Magenis syndrome
Abstract:	Provided are immediate or prolonged administration of certain potassium ATP (KATP) channel openers, optionally in combination with growth hormone, to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of KATP channel openers that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are methods of co-administering KATP channel openers with other drugs (e.g., in combination with growth hormone) to treat diseases of humans and animals (e.g., Prader-Willi Syndrome (PWS), Smith-Magenis syndrome (SMS), and the like.
Inventor(s):	Neil M. Cowen
Assignee:	Essentialis Inc
Application Number:	US14/940,018
Patent Claim Types: see list of patent claims	Use; Composition; Formulation; Delivery;

United States Drug Patent 9,757,384: Claim Scope, Patent Strength, and Diazoxide Patent Landscape

US Patent No. 9,757,384 protects a treatment method using diazoxide, including diazoxide choline, to reduce aggressive behavior in patients with Prader-Willi syndrome (PWS) or Smith-Magenis syndrome (SMS). The core commercial limitation is a treatment duration of at least 10 weeks. The patent does not broadly claim diazoxide as a compound, nor does it independently claim every diazoxide formulation. Its principal value is a disease-specific, behavior-specific method-of-use right.

The claims cover oral and modified-release formulations, once-daily and twice-daily dosing, treatment lasting one or more years, combination therapy, concomitant human growth hormone, and treatment in which circulating IGF-1 does not increase. Claim 14 creates a narrower alternative directed to a formulation consisting essentially of diazoxide or a pharmaceutically acceptable salt.

What does US Patent 9,757,384 protect?

The patent protects administering diazoxide to a subject with PWS or SMS when the administration reduces one or more aggressive behaviors and continues for at least 10 weeks.[1]

Claim group	Subject matter	Commercial significance
Claim 1	Diazoxide treatment for aggressive behavior in PWS or SMS for at least 10 weeks	Broadest independent method claim
Claim 2	Diazoxide choline salt	Targets the active ingredient used in modified-release DCCR products
Claim 3	Oral administration	Covers the commercially practical route
Claims 4-5	Release-rate excipients and delayed release	Reaches controlled-release formulations
Claim 6	At least one additional active ingredient	Covers combination products
Claims 7-8	Concomitant human growth hormone, including injection	Addresses common PWS treatment combinations
Claim 9	Treatment for one or more years	Supports chronic-treatment use
Claim 10	No increase in circulating IGF-1	Narrows the method through a physiological outcome
Claim 11	A second product intended to further reduce aggression	Covers adjunctive behavioral or pharmacological therapy
Claims 12-13	Twice-daily or once-daily administration	Covers both principal dosing schedules
Claim 14	Formulation consisting essentially of diazoxide or a salt	Narrower composition and method combination

The patent is a method-of-treatment patent. It does not, based on the supplied claims, claim:

• Diazoxide as a chemical compound;
• Diazoxide choline as a standalone composition without a treatment step;
• Treatment of hyperphagia generally;
• Treatment of obesity, insulin resistance, or endocrine abnormalities absent the claimed behavioral result;
• All uses of diazoxide in PWS or SMS;
• Treatment of aggressive behavior in unrelated neurodevelopmental disorders.

How broad is independent claim 1?

Claim 1 has four central limitations:

1. The subject has PWS or SMS.
2. The formulation contains an effective amount of diazoxide or a pharmaceutically acceptable salt.
3. The formulation is administered for at least 10 weeks.
4. Administration reduces one or more aggressive behaviors.

The claim does not specify:

• A particular dose;
• A particular diazoxide concentration;
• A particular release profile;
• A particular tablet, capsule, liquid, or suspension;
• A particular behavioral rating scale;
• A minimum percentage reduction;
• A specific definition of aggressive behavior;
• Once-daily or twice-daily dosing;
• A requirement that the patient be an adult or child.

That structure gives claim 1 substantial formulation flexibility. A product could potentially fall within the claim even if its release technology, dose, and dosage form differ from the commercial product, provided the product is administered to the specified patient population for the required duration and achieves the claimed behavioral reduction.

The principal limitation is the behavioral outcome. A party seeking to enforce the claim would need to establish that the treatment reduced one or more aggressive behaviors. A product used only to reduce hyperphagia, improve metabolic parameters, or alter endocrine function would not necessarily satisfy the claim.

What does “aggressive behaviors” mean under the patent?

The claims do not define aggressive behavior by a numerical threshold or named assessment instrument. That creates both breadth and litigation risk.

Potentially relevant behavior may include physical aggression, verbal aggression, tantrums, outbursts, impulsive conduct, property destruction, or other clinically recorded aggressive conduct. The scope would depend on the patent specification, prosecution history, expert testimony, and the factual record concerning how the term was used at the relevant time.

The lack of a quantitative threshold may assist enforcement against clear clinical use of diazoxide for aggression. It may also create validity and infringement disputes over:

• Whether a reported behavior qualifies as “aggressive”;
• Whether the reduction was caused by diazoxide;
• Whether a reduction occurred during the required 10-week period;
• Whether the patient had PWS or SMS;
• Whether the claimed result was merely incidental to treatment for another condition.

The claim uses a functional result limitation: “wherein administration reduces one or more aggressive behaviors.” The limitation is not eliminated because the product label does not expressly promise that result. Actual use, prescribing intent, clinical protocols, promotional materials, or patient records could become relevant in a method-of-use dispute.

What additional protection is provided by claims 2 through 14?

How does claim 2 protect diazoxide choline?

Claim 2 expressly identifies diazoxide choline as the pharmaceutically acceptable salt. This is commercially important because diazoxide choline is associated with modified-release diazoxide products developed for PWS.

Claim 2 remains dependent on all limitations of claim 1. It therefore requires:

• PWS or SMS;
• treatment of aggressive behavior;
• diazoxide choline;
• at least 10 weeks of administration; and
• a reduction in aggressive behavior.

The claim does not independently cover diazoxide choline for hyperphagia or other PWS symptoms.

What do claims 4 and 5 cover?

Claims 4 and 5 reach formulations containing excipients that affect the release rate of diazoxide. Claim 5 narrows the scope to an excipient that delays release.

These claims are directed to formulation architecture rather than merely the active ingredient. They may cover:

• Matrix-forming excipients;
• Polymer-based release retardants;
• Coatings;
• Granulation systems;
• Other excipient systems that delay diazoxide release.

The claims do not require a particular excipient by name. That increases potential breadth but also creates an interpretation issue: the formulation must include an excipient that actually affects or delays release, not merely an inert tablet ingredient.

What is the significance of claim 6?

Claim 6 permits at least one additional active ingredient. It can cover diazoxide used with another active pharmaceutical ingredient, subject to the limitations inherited from claim 1.

The claim is potentially relevant to combination therapy involving treatments for:

• PWS-related endocrine conditions;
• Behavioral symptoms;
• Sleep or psychiatric comorbidities;
• Metabolic complications.

The additional active ingredient does not eliminate the requirement that diazoxide administration reduce aggressive behavior.

How does claim 7 address human growth hormone?

Claim 7 covers diazoxide treatment administered together with human growth hormone. Claim 8 narrows that combination by specifying injection of human growth hormone.

This combination is commercially relevant because growth hormone is an established treatment consideration in PWS. The claim does not require that human growth hormone itself reduce aggression. Diazoxide remains the treatment component tied to the claimed behavioral result.

What do claims 12 and 13 protect?

Claims 12 and 13 separately cover twice-daily and once-daily administration. They provide dosing-specific fallback positions if broader claim 1 is challenged.

A once-daily product and a twice-daily product could therefore face different infringement analyses. A regimen administered at an interval that is neither once daily nor twice daily may avoid these dependent claims while still potentially implicating claim 1.

Why is claim 14 important?

Claim 14 covers a method using a formulation that “consists essentially of” diazoxide or a pharmaceutically acceptable salt.

“Consists essentially of” generally permits components that do not materially affect the basic and novel characteristics of the claimed formulation. Excipients may remain permissible, but additional active ingredients are more difficult to reconcile with this language.

Claim 14 is narrower than claim 1 because it imposes a formulation-composition limitation. It may be useful against a product whose formulation contains diazoxide or diazoxide choline as the principal active ingredient but does not include another material that changes the formulation’s basic and novel characteristics.

When does US Patent 9,757,384 lose exclusivity?

US Patent 9,757,384 issued on September 12, 2017.[1] Its expiration date depends on the earliest effective nonprovisional filing date, applicable patent-term adjustment, terminal disclaimers, and any patent-term extension.

For a US utility patent, the ordinary term is generally 20 years from the earliest effective nonprovisional filing date, subject to statutory adjustments under 35 U.S.C. §§ 154 and 156.[2] The patent’s issue date is not the ordinary term endpoint.

Exclusivity component	Relevance to US 9,757,384
Patent term	Based principally on the effective nonprovisional filing date
Patent-term adjustment	May extend the ordinary term for USPTO examination delays
Patent-term extension	May be available for qualifying regulatory review, subject to statutory limits
Patent-term disclaimer	Could shorten the term if present in the file history
Regulatory exclusivity	Separate from the patent and tied to FDA approval and product status
Foreign rights	Controlled by corresponding national patents, not by the US patent

The supplied claims do not establish the exact terminal expiration date. The controlling date must be taken from the USPTO patent record and term calculation.

What is the Orange Book status of US 9,757,384?

An Orange Book listing is not automatic merely because a patent covers a drug-related method. FDA regulations generally permit NDA holders to submit patents that claim the approved drug substance, drug product, or an approved method of use.[3]

US 9,757,384 is directed to reducing aggressive behavior in PWS or SMS. A listing question therefore turns on whether the approved product labeling includes that method of use. A patent directed to aggressive behavior would face a listing issue if the approved label covers only a different PWS symptom, such as hyperphagia, without identifying aggression as an approved use.

The distinction is material:

Patent subject	Typical Orange Book relevance
Active ingredient composition	Potential drug-substance patent
Tablet or controlled-release formulation	Potential drug-product patent
FDA-approved method of use	Potential method-of-use listing
Unapproved behavioral use	Generally weaker basis for Orange Book listing
General research or off-label use	Not equivalent to an approved method of use

A patent may remain enforceable even if it is not listed in the Orange Book. The principal difference is procedural. An Orange Book-listed patent can trigger a statutory Paragraph IV notice and a potential 30-month stay under the Hatch-Waxman framework.[4] A nonlisted method-of-use patent does not create the same automatic ANDA litigation mechanism.

What Paragraph IV challenges could affect this patent?

If the patent is listed against an approved diazoxide product, an ANDA applicant could certify under Paragraph IV that the patent is invalid, unenforceable, or not infringed.[4]

Potential Paragraph IV theories would likely focus on:

• Lack of written description for the full range of aggressive behaviors;
• Enablement across both PWS and SMS;
• Obviousness based on prior diazoxide use, PWS behavioral literature, or clinical evidence;
• Insufficient evidence that diazoxide produces the claimed behavioral reduction;
• Indefiniteness of “aggressive behaviors”;
• Failure to meet the at-least-10-week limitation;
• Noninfringement based on a different patient population or treatment purpose;
• Noninfringement based on a label carve-out.

The result limitation may make a facial ANDA challenge difficult if the generic label omits the aggressive-behavior use. The analysis would then depend on actual prescribing, physician instructions, promotional conduct, and whether the proposed label encourages the patented method.

What generic launch risks exist for diazoxide products?

Diazoxide is an established active ingredient, but a modified-release diazoxide choline product can face different competition from immediate-release diazoxide products.

Immediate-release diazoxide

Generic immediate-release diazoxide may avoid this patent if it is not promoted or used for reducing aggression in PWS or SMS. It may also avoid claims requiring a delayed-release excipient or a specific dosing frequency.

Modified-release diazoxide choline

A modified-release diazoxide choline product is closer to the commercial and technical center of the patent. It may face greater risk if:

• The label identifies PWS or SMS;
• The product is administered for chronic treatment;
• The label or promotional materials refer to aggression;
• Clinical evidence establishes reduced aggressive behavior;
• The formulation uses release-delaying excipients.

Label carve-outs

A generic applicant may seek to omit a patented method from its label while retaining approval for noninfringing uses. This strategy is more effective when the patented behavioral use is separable from the approved indication and the remaining label does not encourage the patented method.

Does this patent create biosimilar risk?

No. Diazoxide is a small molecule, and an abbreviated generic application under Section 505(j) is the relevant pathway. The Biologics Price Competition and Innovation Act biosimilar pathway under Section 351(k) does not apply to diazoxide or diazoxide choline.[5]

The relevant competitive risks are:

• ANDA approval;
• Paragraph IV litigation;
• Label-skinny generic entry;
• Formulation design-around;
• Off-label prescribing;
• Competing PWS therapies.

How strong is the patent estate around diazoxide and PWS?

US 9,757,384 has meaningful method-of-use value but limited standalone control over the entire diazoxide market.

Strength factor	Assessment
Disease specificity	Strong: limited to PWS or SMS
Behavioral-use specificity	Strong: directed to reduction of aggressive behavior
Formulation flexibility	Broad in claim 1; narrower in claims 4, 5, and 14
Dose specificity	Broad claim 1 has no fixed dose
Duration	Clear 10-week threshold strengthens claim construction
Active ingredient scope	Covers diazoxide and pharmaceutically acceptable salts
Composition exclusivity	Limited; the patent is not a broad compound patent
Orange Book leverage	Depends on alignment with approved labeling and listing
Design-around potential	Moderate to high for nonbehavioral uses, different populations, or omitted indications
Litigation leverage	Strongest where clinical use and promotional conduct clearly target aggression

A broader commercial estate may include separate patents covering diazoxide choline, controlled-release formulations, manufacturing processes, dosage forms, and approved PWS indications. Those rights must be analyzed separately from US 9,757,384. The claims supplied here do not establish the scope or expiration of any other family member.

What patent litigation and settlement risks should companies monitor?

The most important litigation questions are factual rather than chemical:

1. Does the defendant’s label identify aggression as a treatment target?
2. Does the prescribing information encourage use in PWS or SMS?
3. Is the accused formulation administered for at least 10 weeks?
4. Does the clinical protocol record a reduction in aggressive behavior?
5. Does the product contain diazoxide choline or another covered salt?
6. Does the formulation use release-delaying excipients?
7. Is human growth hormone administered concurrently?
8. Does the defendant rely on a label carve-out?

Potential settlement structures include:

• Delayed generic entry;
• A license limited to nonbehavioral indications;
• A covenant not to sue for a specified dosage form;
• A license covering only PWS or only SMS;
• A settlement conditioned on label restrictions;
• A manufacturing or supply agreement.

No settlement terms can be inferred from the claims alone. A current litigation and settlement assessment requires the USPTO file, PACER records, FDA listing data, and the relevant commercial product labels.

What manufacturing and geographic barriers exist?

The patent’s manufacturing relevance is indirect. Claims 4 and 5 may affect controlled-release formulation design, but they do not claim a specific manufacturing process. A competitor could potentially design around the formulation claims by using:

• A different release mechanism;
• A different excipient system;
• An immediate-release formulation;
• A different diazoxide salt;
• A different dosage form.

The geographic scope of US 9,757,384 is limited to the United States. Corresponding foreign applications or granted patents may create separate rights in Europe, Japan, China, Canada, Australia, and other markets. Patent family members must be reviewed individually because claim scope, prosecution amendments, expiration dates, and enforceability may differ by country.

What are the likely generic launch scenarios?

Scenario 1: Nonbehavioral label

A generic applicant obtains approval for a use that does not identify aggression. Risk to US 9,757,384 is lower, although induced-infringement questions may remain if the product is marketed for the patented use.

Scenario 2: Label carve-out

The applicant excludes the aggressive-behavior use while retaining other approved uses. This is the most direct Hatch-Waxman design-around if FDA labeling permits the separation.

Scenario 3: Full label with Paragraph IV

The applicant challenges the patent and seeks approval for the full relevant use. Litigation risk is highest, but an invalidity or noninfringement judgment could remove the principal barrier.

Scenario 4: Formulation design-around

The competitor uses a release system outside claims 4 and 5. Claim 1 may still matter if the product is used for the claimed population, duration, and behavioral outcome.

Scenario 5: Off-label erosion

Generic diazoxide enters for other uses and is prescribed off-label to PWS patients. This can reduce commercial exclusivity without necessarily producing a clean patent-infringement case.

Key Takeaways

• US 9,757,384 is primarily a disease-specific method-of-use patent.
• The core invention is diazoxide treatment for aggressive behavior in PWS or SMS for at least 10 weeks.
• Diazoxide choline is expressly covered by dependent claim 2.
• Claims 4 and 5 address release-modifying and delayed-release excipients.
• Claims 7 and 8 cover combination use with injectable human growth hormone.
• Claim 14 is narrower because it requires a formulation consisting essentially of diazoxide or a pharmaceutically acceptable salt.
• The patent does not broadly monopolize diazoxide, diazoxide choline, PWS treatment, or hyperphagia treatment.
• Generic risk is highest when a product targets PWS or SMS aggression, uses diazoxide choline, employs modified release, and is administered chronically.
• The patent’s Orange Book leverage depends on whether the approved labeling covers the claimed aggressive-behavior method.
• Diazoxide is subject to generic, not biosimilar, competition.
• Exact expiration, Orange Book listing, family coverage, and litigation status require review of the current USPTO, FDA, and court records.

Frequently Asked Questions

Is US 9,757,384 a patent on diazoxide choline itself?

No. The claims supplied are treatment-method claims. Claim 2 specifically covers use of diazoxide choline in the claimed PWS or SMS behavioral treatment.

Can a generic sell diazoxide for non-PWS indications?

Potentially. The patent claims require a subject with PWS or SMS and a reduction in aggressive behavior. A non-PWS indication may avoid the literal scope of these claims, subject to other patents and infringement theories.

Does once-daily dosing fall within the patent?

Yes. Claim 13 expressly covers once-daily administration, while claim 1 does not require a particular dosing frequency.

Does the patent cover treatment lasting less than 10 weeks?

The supplied independent claims require administration for at least 10 weeks. A regimen shorter than that may avoid literal infringement of claims 1 and 14, subject to claim construction and other patent rights.

Does FDA approval for PWS automatically make this patent enforceable?

No. FDA approval and patent enforceability are separate issues. Approval may affect Orange Book listing and Hatch-Waxman procedures, but validity, infringement, written description, enablement, and enforceability remain legal questions under patent law.

References

1. United States Patent and Trademark Office. (2017). U.S. Patent No. 9,757,384.
2. 35 U.S.C. §§ 154, 156 (2018).
3. U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations: Orange Book.
4. 21 U.S.C. § 355(j) (2018).
5. 42 U.S.C. § 262(k) (2018).

Drugs Protected by US Patent 9,757,384

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Soleno Therap	VYKAT XR	diazoxide choline	TABLET, EXTENDED RELEASE;ORAL	216665-001	Mar 26, 2025		RX	Yes	No	9,757,384					REDUCING HYPERPHAGIC AGGRESSIVE BEHAVIORS IN PRADER-WILLI SYNDROME PATIENTS
Soleno Therap	VYKAT XR	diazoxide choline	TABLET, EXTENDED RELEASE;ORAL	216665-002	Mar 26, 2025		RX	Yes	No	9,757,384					REDUCING HYPERPHAGIC AGGRESSIVE BEHAVIORS IN PRADER-WILLI SYNDROME PATIENTS
Soleno Therap	VYKAT XR	diazoxide choline	TABLET, EXTENDED RELEASE;ORAL	216665-003	Mar 26, 2025		RX	Yes	Yes	9,757,384					REDUCING HYPERPHAGIC AGGRESSIVE BEHAVIORS IN PRADER-WILLI SYNDROME PATIENTS

International Family Members for US Patent 9,757,384

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	E463249
Australia	2005280058
Australia	2010246520
Australia	2015346196
Australia	2019202906
Brazil	112017009986
Canada	2578224