Details for Patent: 12,329,749

Which drugs does patent 12,329,749 protect, and when does it expire?

Patent 12,329,749 protects BREKIYA (AUTOINJECTOR) and is included in one NDA.

Summary for Patent: 12,329,749

Title:	Low concentration delivery of an ergoline derivative for treatment of a headache
Abstract:	Provided are ergoline derivative containing medicaments disposed within a preassembled, prefilled, single-use delivery device, methods for administering a medicament using a preassembled, prefilled, single-use delivery device, and systems or kits that contain one or more preassembled, prefilled, single-use devices and user instructions, such as for treatment of a migraine or other headache.
Inventor(s):	Ralph Solarski, Robert Edward Malone
Assignee:	Relevale Inc
Application Number:	US17/365,750
Patent Claim Types: see list of patent claims	Use; Delivery; Device; Dosage form;

Scope and claims of US Patent 12,329,749: ergoline (dihydroergotamine) auto-injector, pH 3–8, and 0.3–1.5 mg/mL concentration

Executive summary: US 12,329,749 is a US-focused patent estate centered on a prefilled, single-use auto-injector containing an ergoline derivative medicament, with two claim pillars. First, device architecture and actuation are claimed as a syringe-injector system with a dosing mechanism and a trigger that advances both syringe and needle to discharge through a hollow injection needle. Second, the medicament is constrained by composition and physicochemical windows: pH between about 3 and about 8 and ergoline derivative concentration between about 0.3 mg/mL and about 1.5 mg/mL, with dependent claims tightening to specific concentration ranges and to dihydroergotamine mesylate. Method-of-use claims track treatment of headache by administering the same constrained medicament using the preassembled, prefilled single-use delivery device. The independent claim set is drafted to deter “design-around” substitution that changes either (i) the injection format or actuation architecture or (ii) the pH and concentration ranges.

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What does US 12,329,749 claim in the US for ergoline auto-injectors?

Direct answer: The patent claims (1) an ergoline-derivative medicament placed in a specific auto-injector device architecture with trigger-activated dosing that drives a hollow injection needle, constrained to medicament pH 3–8 and ergoline concentration 0.3–1.5 mg/mL; and (2) a method of treating headache by administering that medicament using that device, with the same pH and concentration constraints.

Claim 1 (independent) scope: device + medicament constraints

Claim 1 combines three legal and technical constraints:

1. Active substance scope

   • “ergoline derivative containing medicament comprising dihydroergotamine or a pharmaceutically acceptable salt thereof.”
   • Dependent claim 2 narrows to dihydroergotamine mesylate.

2. Auto-injector device architecture

   • syringe containing the medicament
   • hollow injection needle operably coupled to a distal end of the syringe
   • dosing mechanism operably adjacent to the proximal end of the syringe
   • trigger mechanism operably coupled to the dosing mechanism
   • trigger actuation “causes the dosing mechanism to advance the syringe and the injection needle” and discharges medicament “though the injection needle.”

3. Formulation/physicochemical windows

   • medicament pH between about 3 and about 8
   • ergoline derivative concentration about 0.3 mg/mL to about 1.5 mg/mL

This is not a pure device claim and not a pure formulation claim. It is an integrated “device containing medicament” claim, which narrows infringement to products that meet both the device structure and the medicament constraints.

Claim 8 (independent) scope: method-of-use tied to the same device and formulation windows

Claim 8 recites:

• treating a headache person by administering an ergoline derivative medicament using preassembled, prefilled, single use delivery device
• steps:
  • placing against injection site
  • actuating trigger mechanism, advancing syringe and needle, discharging through needle
  • maintaining device while needle penetrates and medicament is injected into the site
• the medicament constraints match claim 1:
  • pH 3–8
  • ergoline concentration 0.5–1.5 mg/mL (note the narrower lower bound in claim 8 vs claim 1)

Dependent claims 9–15 tighten specific actives, ranges, and dose size.

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How do the dependent claims narrow the medicament composition and dosing windows?

Direct answer: Dependent claims narrow active ingredient identity (dihydroergotamine mesylate), impose narrower concentration sub-ranges, and in one claim specify a representative composition including ethanol, glycerin, water for injection, and an explicit pH-adjusting buffer system.

Concentration windows (formulation claim narrowing)

• Claim 3: concentration 0.5–1.4 mg/mL
• Claim 4: concentration 0.8–1.2 mg/mL
• Claim 6: fixed example target: “about 1.0 mg dihydroergotamine mesylate” with stated excipients and pH-adjustment to 3.4–4.9
• Claim 13: concentration “about 1.5 mg/mL” (upper bound pin)

pH window scope

• Claim 1: pH between about 3 and about 8
• Claim 6: pH between about 3.4 and about 4.9 (tight example for dihydroergotamine mesylate formulation)

Excipients and buffer system

• Claim 5 (functional): tonicity adjusting agents, buffers, antioxidants, stabilizers, nonionic wetting/clarifying agents, viscosity modifiers

• Claim 6 (specific composition):

  • about 1.0 mg dihydroergotamine mesylate
  • about 49.0 mg ethanol
  • about 150 mg glycerin
  • about 800 mg water for injection
  • buffer comprising sodium hydroxide and/or methane sulfonic acid to adjust pH to 3.4–4.9

• Claim 7 (functional, excipients): alcohol, glycerin, water for injection

Dose recitations (method claims)

• Claim 14: 0.1 mg to 10 mg per injection
• Claim 15: 1 to 2 mg per injection

These dose recitations are broad enough to cover many dosing schemes; the key discrimination remains the combination of device + medicament concentration/pH constraints.

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What is the device claim structure, and what design-arounds are blocked by US 12,329,749?

Direct answer: The patent requires a prefilled syringe/needle architecture with a trigger coupled to a dosing mechanism that advances the syringe and needle to discharge medicament. Products with materially different delivery mechanics may avoid infringement even if they use the same pH and concentration ranges.

Device elements that must be present (as written in Claim 1)

A would-be infringing auto-injector must have:

1. prefilled syringe containing the constrained medicament
2. hollow injection needle attached to the distal end of the syringe
3. dosing mechanism adjacent to proximal end
4. trigger mechanism coupled to the dosing mechanism
5. trigger actuation drives relative advancement of syringe and needle such that medicament is discharged through needle

Likely “blocked” variants (conceptual)

• Non-needle delivery formats (needle-free jets, transdermal patches) are outside claim language.
• Delivery formats where the syringe is not advanced by a dosing mechanism triggered in the claimed manner may be non-infringing.
• Metered-flow systems where injection occurs without syringe-and-needle advancement driven by a trigger/dosing mechanism as claimed.

How the formulation windows create an additional barrier

Even if a competitor matches the device mechanics, the product must also land inside:

• pH 3–8 (or pH in tight example only if that dependent claim is asserted)
• concentration about 0.3–1.5 mg/mL (and for method claim 8, about 0.5–1.5 mg/mL)

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How does US 12,329,749 compare with typical ergoline formulation patents and delivery-device patents?

Direct answer: The claim strategy is “stacked constraints”: it pairs an auto-injector mechanical architecture with narrow formulation/physicochemical ranges. Many formulation-only patents can be avoided by changing pH/excipients. Many device-only patents can be avoided by changing device mechanics. This patent claims both simultaneously for the same drug class and delivery format.

Comparison in claim drafting philosophy

• Formulation-heavy patents often cover “a composition comprising dihydroergotamine mesylate with excipients and pH.” Those are vulnerable to substitution outside the disclosed pH and concentration ranges.
• Device-heavy patents often claim “an auto-injector” with trigger/dosing/needle actuation, sometimes without prescribing the exact medicament pH and concentration.
• US 12,329,749 covers products that meet both. That reduces infringement pathways for competitors planning a clean-room change on only one axis.

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What patents likely sit next to US 12,329,749 in the ergoline auto-injector landscape?

Direct answer: US 12,329,749 is best treated as a composite “device + constrained medicament” patent. In practice, it typically coexists (in a brand or license package) with adjacent portfolios in four buckets:

1. Drug substance or salt form (dihydroergotamine and/or mesylate)
2. Liquid/Injectable formulation (pH, solvent system such as ethanol/glycerin, tonicity agents, buffers, antioxidants)
3. Delivery system (prefilled single-use auto-injector mechanics, syringe/needle coupling, trigger and dosing mechanisms)
4. Method-of-use (headache treatment using a device-administered injectable)

However, without the actual patent bibliographic data (publication number, assignee, prosecution history, cited art, or family identifiers), a complete, accurate map of co-pending or related US patents cannot be produced solely from the claim text provided.

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What is the Orange Book status of US 12,329,749?

Direct answer: Orange Book status is tied to an approved drug product and listed patent codes, not to a standalone US patent number alone. No Orange Book listing can be determined from the claim text alone.

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When does US 12,329,749 lose exclusivity, and how would expiration affect generic entry?

Direct answer: Exclusivity and patent expiration timing depend on the patent’s grant date, filing date, maintenance status, terminal disclaimer terms, and any patent-term adjustment or extension. Those facts are not present in the claim text provided, so a definitive expiration timeline cannot be computed.

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What litigation risks does the claim scope create for generic or biosimilar entrants?

Direct answer: The integrated claim drafting increases risk for any entrant attempting to market an auto-injector containing dihydroergotamine with:

• pH 3–8 and concentration 0.3–1.5 mg/mL, while using
• a delivery device with the trigger/dosing mechanism advancing syringe and needle to discharge through a hollow needle.

Even small modifications that remain within the specified windows can preserve infringement exposure. Conversely, a full design-around usually requires changing either (i) the delivery mechanics so that the dosing/advancement sequence is materially different from the claim language, or (ii) the formulation pH/concentration so the medicament falls outside the claimed windows.

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What formulations are explicitly covered by US 12,329,749, and what is the “core” composition?

Direct answer: The patent’s “core” formulation is defined by:

• dihydroergotamine (or salt; mesylate specified in dependent claim 2)
• pH 3–8 (example pH 3.4–4.9)
• concentration 0.3–1.5 mg/mL (example points around 1.0 mg and about 0.8–1.2 mg/mL)
• a solvent/excipient framework including ethanol and glycerin and water for injection

The most explicit, litigation-relevant embodiment is Claim 6’s example: dihydroergotamine mesylate in a system with ethanol, glycerin, water, and a NaOH and/or methanesulfonic acid buffer to hit pH 3.4–4.9.

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Where are the practical infringement “touchpoints” for an auto-injector product?

Direct answer: Infringement will turn on whether the commercial product meets three observable/legal elements simultaneously.

Touchpoint map

1. Does the product use a prefilled syringe and hollow needle auto-injector?
2. Does actuation advance syringe and needle via a dosing mechanism coupled to a trigger?
3. Does the released medicament have pH 3–8 and dihydroergotamine concentration within 0.3–1.5 mg/mL (or 0.5–1.5 mg/mL for the method claim)?

These are testable by product inspection, device schematics, and formulation analysis.

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Key Takeaways

• US 12,329,749 claims an integrated system: auto-injector mechanical architecture + dihydroergotamine-containing medicament with pH 3–8 and concentration 0.3–1.5 mg/mL.
• Dependent claims narrow to dihydroergotamine mesylate and specific concentration sub-ranges, and include an explicit example formulation with ethanol, glycerin, water for injection, and NaOH and/or methanesulfonic acid buffer targeting pH 3.4–4.9.
• The method-of-use claims tie headache treatment to administration using the claimed prefilled single-use delivery device and constrained medicament parameters.
• The dual constraint approach reduces design-around options: a competitor typically must change either delivery mechanics (beyond the claim language) or formulation pH/concentration (outside the claimed windows).

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FAQs

1) Can a competitor avoid US 12,329,749 by switching from dihydroergotamine to another ergoline?
Not if the alternative is still an “ergoline derivative” but Claim 1 as provided requires dihydroergotamine or a pharmaceutically acceptable salt.

2) Does the patent cover only dihydroergotamine mesylate, or also other salts?
Claim 1 covers dihydroergotamine or any pharmaceutically acceptable salt; Claim 2 specifically calls out dihydroergotamine mesylate.

3) What is the most specific formulation embodiment in the claim set?
Claim 6 is the most explicit: it recites a representative formulation with ethanol, glycerin, water for injection, and a NaOH and/or methanesulfonic acid buffer to reach pH 3.4–4.9.

4) Are concentration ranges identical in the device claim and the method claim?
No. Claim 1 uses about 0.3–1.5 mg/mL, while Claim 8 uses about 0.5–1.5 mg/mL.

5) What device changes would most directly reduce infringement exposure?
Changes that eliminate the claimed trigger/dosing mechanism sequence that advances the syringe and hollow needle to discharge medicament through the needle.

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References

1. Provided claim text for US Patent 12,329,749 (as supplied in the prompt).

Drugs Protected by US Patent 12,329,749

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Amneal	BREKIYA (AUTOINJECTOR)	dihydroergotamine mesylate	SOLUTION;SUBCUTANEOUS	215400-001	May 14, 2025		RX	Yes	Yes			Y			ACUTE TREATMENT OF MIGRAINE WITH OR WITHOUT AURA IN ADULTS
Amneal	BREKIYA (AUTOINJECTOR)	dihydroergotamine mesylate	SOLUTION;SUBCUTANEOUS	215400-001	May 14, 2025		RX	Yes	Yes			Y			ACUTE TREATMENT OF CLUSTER HEADACHES IN ADULTS