Details for Patent: 12,186,360

Which drugs does patent 12,186,360 protect, and when does it expire?

Patent 12,186,360 protects QBRELIS and is included in one NDA.

This patent has ten patent family members in eight countries.

Summary for Patent: 12,186,360

Title:	Lisinopril formulations
Abstract:	Provided herein are stable lisinopril oral liquid formulations. Also provided herein are methods of using lisinopril oral liquid formulations for the treatment of certain diseases including hypertension, heart failure and acute myocardial infarction.
Inventor(s):	Gerold L. Mosher, David W. Miles
Assignee:	Azurity Pharmaceuticals Inc
Application Number:	US18/663,349
Patent Claim Types: see list of patent claims	Formulation; Compound;

US Patent 12,186,360 (lisinopril oral liquid) claims scope, construction, and US patent estate analysis

Executive summary: US 12,186,360 covers aqueous lisinopril oral liquid formulations defined by a preservative/preservative system, sweet-taste components, a pH window (about 4 to about 8), and stability at 25±5°C for specified minimum durations. Claim 1 is broad on sweet-taste “means” but specific on preservative selection and stability. Claim 10 narrows to a defined anti-microbial activity component plus a defined sweetener set. Dependent claims further pin down lisinopril dihydrate, ~1 mg/mL, and tighter pH bands (4–5.2; 5–8) plus extended stability. The patent’s practical enforcement scope in the US is strongest against commercial oral liquids that combine aqueous lisinopril with one of the enumerated preservatives, sweeteners from the listed group, and formulation stability claims in the claimed temperature regime.

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What does US Patent 12,186,360 claim protect for lisinopril oral liquid formulations?

Direct scope (independent claim 1): An oral liquid containing:

1. Active: lisinopril or pharmaceutically acceptable salt
2. Preservative system: selected from the enumerated list
   • ascorbic acid, BHA, BHT, citric acid, erythorbic acid, sodium ascorbate
   • methylparaben, ethylparaben, propylparaben, butylparaben
   • benzoic acid, sodium benzoate
   • potassium sorbate
3. Vehicle: water-containing liquid vehicle
4. Sweet taste: “means for providing a sweet taste”
5. Physicochemical limits: pH between about 4 and about 8
6. Performance/stability: stable at about 25±5°C for at least 6 months

Built-in limitations that matter for claim coverage:

• Water-based oral liquid: “liquid vehicle comprises water.” Non-aqueous or predominantly non-aqueous systems fall outside literal scope.
• Enumerated preservative list is limiting: Claim 1 requires the preservative to be from the specified set. If the formulation uses a different preservative (eg, sorbic acid vs “potassium sorbate” only, or phenoxyethanol, chlorobutanol, benzyl alcohol, etc.), literal claim 1 coverage depends on whether that preservative is within the claim’s enumerated categories (including salts, as allowed).
• pH window controls: “about 4 to about 8” caps extremes. A product at pH 3.8 or 8.3 may still be argued “about,” but literal risk increases as you move away from the window.
• Stability is part of the claim: Coverage is not just compositional. The accused formulation must meet the claimed stability threshold at 25±5°C for at least the stated duration. If the market product is reformulated to reduce stability claims or fails stability testing, infringement risk changes materially.

Claim 1 sweet-taste “means” breadth

Claim 1 does not list sweeteners; it uses “means for providing a sweet taste.” That expands the range of sweetener chemistries potentially captured, while still tethering sweetness to oral-liquid formulations in the pH/preservative/stability envelope.

Claim 1 preservative examples that are explicitly in-scope

The preservative list includes antioxidant-type ingredients (ascorbic acid, erythorbic acid, sodium ascorbate) and classic preservative agents (parabens, benzoates, potassium sorbate), plus citric acid and BHA/BHT/citric systems. This matters because many oral-liquid palatability and shelf-life systems use one of these preservatives.

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How does dependent claim 2 narrow US 12,186,360 scope (lisinopril dihydrate)?

Claim 2: Claim 1 formulation where the lisinopril is lisinopril dihydrate.

Enforcement implication: If an accused product uses lisinopril in a different solid form (eg, anhydrous lisinopril) the claim 2 dependent coverage may not apply, but claim 1 may still apply because claim 1 only requires “lisinopril or a pharmaceutically acceptable salt thereof.”

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What concentration and pH ranges are captured in dependent claims 3–4?

• Claim 3: lisinopril at about 1 mg/mL (or salt)
• Claim 4: pH about 4 to about 5.2 (tighter than claim 1)

Enforcement implication: If a competitor’s oral liquid is at a different nominal concentration (eg, 0.5 mg/mL or 2 mg/mL), claim 3 may not be asserted cleanly, but claim 1 still can be (concentration is not in claim 1). pH tightening in claim 4 gives a narrower hook for products formulated near the lower end of the claim 1 range.

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How do claims 5–7 add mechanism and stability duration limits?

Claim 5: lisinopril functions as buffer

This is a functional limitation: “lisinopril or a pharmaceutically acceptable salt thereof functions as a buffer.”

Enforcement implication: Many formulations use citrate/acetate or added buffering agents. If lisinopril salt identity and system behavior is used as the buffering element, claim 5 can strengthen the formulation-specific argument. If the buffer is dominated by other buffering agents, claim 5 may be harder to prove, while claim 1 remains independent of this function.

Claim 6–7: extended stability

• Claim 6: stable at 25±5°C for at least 12 months
• Claim 7: stable at 25±5°C for at least 18 months

Enforcement implication: These provide escalating “performance claims.” A competitor product could be stable for 6 months but not 12 months, narrowing viable asserted claims to claim 1 only.

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How broad is Claim 8–9’s sweet-taste limitation?

• Claim 8: sweet taste means is a natural or synthetic sugar, sweetener, or combination
• Claim 9: sweetener selected from a list including xylitol, mannitol, sorbitol, glycerin, maltitol, sucrose, aspartame, sucralose, saccharin, acesulfame, salts, and combinations.

Enforcement implication: Claims 8–9 are narrower than claim 1’s “means.” They provide a cleaner infringement theory where a product uses one of the enumerated sweeteners.

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What does independent claim 10 add that differs from claim 1?

Claim 10 recasts the formulation with a different architecture:

1. lisinopril (or salt)
2. means for providing anti-microbial activity in the oral liquid
3. water-containing liquid vehicle
4. sweetener wherein sweetener comprises enumerated agents
5. pH between about 4 and about 8
6. stability at 25±5°C for at least 6 months

Key differences vs claim 1:

• Sweetness is constrained to enumerated sweeteners in claim 10 (unlike claim 1’s open “means”).
• The “anti-microbial activity” is “means for providing,” which is then tied to a preservative set in dependent claim 19.
• Claim 10 requires both anti-microbial means and defined sweetener list composition.

Claim 10 sweetener constraint

Claim 10 captures oral liquids where the sweetener comprises one of: xylitol, mannitol, sorbitol, glycerin, maltitol, sucrose, aspartame, sucralose, saccharin, acesulfame, or salts.

If a product uses a non-enumerated sweetener or a sweetener blend where the enumerated set is not used, claim 10 coverage is constrained.

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Which additional product attributes are pinned down in dependent claims 11–19?

• Claim 11: lisinopril is lisinopril dihydrate
• Claim 12: lisinopril at about 1 mg/mL
• Claim 13: sweetener is xylitol or sucralose
• Claim 14: lisinopril functions as a buffer
• Claim 15: pH between about 5 and about 8
• Claim 16: pH between about 4 and about 5.2
• Claim 17: stability at 25±5°C for at least 12 months
• Claim 18: stability at 25±5°C for at least 18 months
• Claim 19: anti-microbial means is a preservative selected from:
  sodium benzoate, benzoic acid, ascorbic acid, methylparaben, ethylparaben, propylparaben, butylparaben, salts, and combinations

Enforcement implication: Claim 19 is the narrowest preservative hook in the claim 10 lineage. It excludes preservative options included in claim 1 (eg, potassium sorbate, citric acid, BHA/BHT, erythorbic acid) unless those fall under “anti-microbial activity” as a “means” not limited to the claim 19 preservatives. In litigation practice, claim 19 gives a clean literal prescriptive set if a competitor uses benzoate/paraben/ascorbic preservative systems.

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Claim construction and likely infringement tests for US 12,186,360

1) “Oral liquid formulation”

A competitor’s dosage form must be an oral liquid. That includes syrups, oral solutions, and similar aqueous liquids with oral administration.

2) “Liquid vehicle comprises water”

If a competitor uses co-solvents where water is a minor component, they risk failing this limitation. If water is present as a main vehicle component, literal satisfaction is likely.

3) Preservative/anti-microbial means limitations

• Claim 1’s preservative is an enumerated list, which is a typical direct compositional limitation.
• Claim 10 uses “means for anti-microbial activity,” which can be argued broadly but is likely to be constrained by dependent claim 19 in enforcement strategies.

4) pH “about 4 to about 8”

“About” introduces tolerance. In infringement analysis, the product’s measured pH in relevant samples and stability studies becomes central.

5) Stability at 25±5°C for at least 6 months

This is a functional/performance limitation. Practically, claim validity and enforcement will turn on stability data at the claimed temperature range and the time threshold.

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What does this patent’s claim set imply about “design-around” levers?

Based on the claim elements, the biggest literal design-around pathways are:

1. Preservative switch outside the enumerated list (claim 1) or outside the claim 19 list (claim 10 lineage)
2. Sweetener substitution not captured by claim 9/10 enumerations (harder if only claim 1 is asserted)
3. pH outside the 4–8 window (or at the edges in a way that avoids “about”)
4. Stability strategy that fails the at-least-6-month (or 12/18-month) performance requirement
5. Non-aqueous or materially non-water vehicle

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US patent landscape for US 12,186,360: what this claim profile signals for surrounding claims in the same estate

Given only the claims excerpt, the landscape can be analyzed only at the level of intra-claim coverage density and typical related patent categories (not confirmed other patent numbers).

High-probability neighboring claim themes (within the same family or related families)

1. Other dosage strengths of lisinopril oral liquids (since dependent claim 3 is at ~1 mg/mL)
2. Other pH windows or buffering systems (claims 4, 14)
3. Other sweetener combinations (claim 8–9)
4. Alternative preservative systems including those excluded by claim 10/19 narrower list
5. Manufacturing method claims for stabilizing lisinopril in aqueous oral solutions (commonly present in formulation patents)
6. Packaging or storage conditions (often used to reinforce stability)

Those themes matter because they influence whether competitors face multiple overlapping hooks for different strengths and parameter sets.

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How does this claim set map to generic or biosimilar risk in the US?

Small molecule generics (lisinopril oral liquid)

This is a small-molecule formulation patent. Generic risk in the US typically comes from:

• ANDA formulations that use the same API but may change excipients and process.
• Whether the ANDA product’s excipient system and stability metrics land within the claim boundaries.

Potential “Paragraph IV style” exposure

Where a competitor’s proposed product:

• uses one of the enumerated preservatives in claim 1, and
• uses an oral aqueous vehicle with pH 4–8, and
• uses sweeteners that satisfy claim 9 or fits claim 1’s broad sweet-taste “means,” and
• can meet 25±5°C stability duration, the patent becomes a straightforward infringement target.

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Commercial infringement targets: what product configurations are most exposed?

Highest exposure combinations by claim coverage:

1. Lisinopril oral liquid using benzoates/parabens/ascorbic acid preservatives, in an aqueous system, pH 4–8, with sweeteners such as xylitol or sucralose or other claim 9 enumerated sweeteners, and stability at least 6 months (and potentially 12 or 18 months).
2. Lisinopril dihydrate oral solutions at around 1 mg/mL, pH 4–5.2, stability at 12/18 months.

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Key takeaways on scope and claim strength for US 12,186,360

• The patent is formulation-scoped: aqueous lisinopril oral liquids with enumerated preservatives (claim 1) and defined pH and stability performance.
• Claim 10/19 provide a second infringement pathway that is more excipient-specific for sweetness and anti-microbial systems.
• Design-around effort should focus on preservative selection and anti-microbial system choice, then on sweetener set and pH/stability.
• The stability limitation is not cosmetic; it is a litigation-driving performance element.

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FAQs

1) Does US 12,186,360 cover lisinopril oral liquids without sweeteners if they taste “neutral”?

Claim 1 requires a “means for providing a sweet taste.” If no sweet-taste providing component is used, literal coverage is unlikely. Claim 10 also requires a sweetener comprising the enumerated set.

2) If a product uses citric acid plus benzoate, does it fall under claim 1?

Yes if the preservative component used matches the enumerated preservative selection in claim 1. The claim language requires the preservative is selected from the listed group; systems using listed preservatives can still qualify depending on how the product defines/allocates preservative roles.

3) Can an “anhydrous lisinopril” product avoid claim 2?

Claim 2 is limited to lisinopril dihydrate, so it can be avoided for that dependent claim. Independent claim 1 remains potentially applicable if lisinopril (in any form) is used.

4) How do pH adjustments impact infringement risk under claims 4 and 16?

Claims 4 and 16 are tighter subranges (4–5.2). Products formulated with pH outside those tighter windows shift risk to independent claim 1/10 ranges, which still require pH 4–8.

5) Is the stability requirement a gating issue even when composition matches?

Yes. The claims require stability at 25±5°C for at least the stated duration. Composition that matches but fails stability thresholds weakens literal infringement positions for the stability-dependent claims.

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Key Takeaways

• US 12,186,360 is anchored to aqueous lisinopril oral liquids with pH 4–8 and specified shelf-life stability at 25±5°C.
• Claim 1: enumerated preservatives + broad sweet-taste “means” + stability ≥6 months.
• Claim 10: enumerated sweeteners + anti-microbial means + stability ≥6 months, with claim 19 narrowing preservative types.
• Best infringement targets are products using benzoates/parabens/ascorbic preservatives, sweeteners such as xylitol/sucralose, and meeting stability requirements.
• Best design-arounds are preservative substitution outside the enumerated list and pH/stability moves outside the claimed performance envelope.

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References (APA)

No references can be provided from the prompt alone because no source documents (patent publication number, assignee, prosecution history, specification text, or FDA/Orange Book listings) were included to support citation.

Drugs Protected by US Patent 12,186,360

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Azurity	QBRELIS	lisinopril	SOLUTION;ORAL	208401-001	Jul 29, 2016		RX	Yes	Yes	12,186,360		Y

International Family Members for US Patent 12,186,360

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Canada	3003274
China	108472252
China	112972370