US Patent 11,026,944: What Is Claimed, How Broad the Scope Is, and Where It Sits in the US Landscape
US Patent 11,026,944 is directed to a specific immediate-release oral dosage form for a defined small-molecule compound (Compound A), where the patentability and infringement leverage are tied to dose range and measured dissolution performance under defined test conditions.
What does the patent claim at the core (independent claim 1)?
Claim 1 covers an oral dosage form comprising:
- Compound A:
(1R,2S)-2-(((2,4-dimethylpyrimidin-5-yl)oxy)methyl)-2-(3-fluorophenyl)-N-(5-fluoropyridine-2-yl)cyclopropanecarboxamide
- A single daily dose in the range: about 2.5 mg to about 10 mg
- A functional performance requirement: dissolution rate of 85% or more in:
- Medium: 0.1 mol/L hydrochloric acid containing 0.5% polysorbate 80
- Volume: 900 mL
- Temperature: 37 ± 0.5°C
- Timepoint: within 30 minutes from the start of dissolution testing
- Apparatus: Apparatus 2 (paddle), 75 rpm
- Test standard: immediate-release dosage form per JP16 Dissolution test 6.10 or USP37 <711> Dissolution of USP37
- The claim is structured as: dose + formulation + dissolution outcome + specified compound identity.
Claim 1 scope in plain terms
The claim is not just “a tablet with Compound A.” It is “a tablet with Compound A at a single daily dose in a specified mg range that exhibits a specific dissolution threshold under specific in vitro conditions.”
That design creates a tight linkage between formulation and measurable performance.
How much narrower do dependent claims 2 to 5 go?
Claim 2 (dissolution stringency + rpm/time tightening)
- Dissolution requirement: ≥85% within 15 minutes (not 30)
- Medium: 0.1 mol/L HCl, 900 mL, 37 ± 0.5°C
(note: polysorbate 80 is not recited in claim 2’s medium specification)
- Apparatus: Apparatus 2 paddle, 50 rpm
Claim 3 (excipient specificity)
- Adds: dosage form comprises lactose as an excipient.
Claim 4 (excipient specificity)
- Adds: dosage form comprises low-substituted hydroxypropyl cellulose as an excipient.
Claim 5 (combination excipients)
- Adds: dosage form comprises lactose and low-substituted hydroxypropyl cellulose.
What this means for coverage
- Claims 3-5 narrow further by requiring particular excipients, but they do not appear to change the compound identity or the dose/dissolution framework set by claim 1.
- Practically, claim 1 provides the broadest hook through functional dissolution performance. Claims 3-5 provide narrower hooks that may be easier to prove for specific product prototypes.
What is the key infringement trigger in this patent: dose, dissolution, or both?
For US infringement, all elements of the relevant claim must be met. Here, claim 1 includes at least three hard constraints:
- Compound identity is fixed to a single stereochemically specified molecule.
- Dose range: “single daily dose” ~2.5 mg to ~10 mg.
- In vitro dissolution outcome: ≥85% in 30 minutes under the recited apparatus/medium conditions.
That makes dissolution performance a central trigger because it functions as a formulation-dependent claim limitation.
Test-condition specificity is a scope-defining lever
The claim does not use a generic dissolution statement. It pins performance to:
- Apparatus 2 paddle speed (75 rpm in claim 1; 50 rpm in claim 2)
- Medium composition, including 0.5% polysorbate 80 in claim 1
- Timepoint: 30 minutes (claim 1), 15 minutes (claim 2)
- Volume and temperature
- A defined regulatory test framework (JP16 immediate-release dissolution test; USP37 <711>).
If a competitor’s formulation does not meet the threshold under these conditions, that can defeat infringement even if dissolution looks good under other media or other rpm values.
How broad is the claim practically across dosage forms?
The language is “a dosage form comprising” the compound and conditions. It does not explicitly limit the dosage form to tablet/capsule in the excerpt provided. However, the dissolution test is framed as an immediate-release dosage form and uses USP apparatus 2 paddle, which strongly correlates with solid oral immediate-release formats.
So the practical breadth is:
- Solid oral immediate-release types that can be tested in paddle dissolution are the realistic target.
- The claim is not tied to a particular particle size, specific binder, specific disintegrant, or manufacturing method (in the excerpt), except via dependent excipient claims 3-5.
What does the claim suggest about formulation strategy (based on the limitations)?
The claim structure points to a formulation designed to hit rapid gastric/acid dissolution.
- Claim 1 medium includes polysorbate 80 (0.5%), which often improves wetting and dissolution of poorly wetted compounds.
- A strong acid-mediated dissolution threshold at 75 rpm implies the formulation likely uses excipient systems that promote disintegration, wetting, and dispersion in gastric-like medium.
Claims 3-5 indicate that, for at least some embodiments, the formulation uses:
- lactose
- low-substituted hydroxypropyl cellulose (L-HPC)
Even if a competitor uses different excipients, claim 1 can still be infringed if dissolution performance and dose range are met. Conversely, a competitor can potentially avoid infringement by missing one of the hard limits (dose range or dissolution threshold under the specified conditions), even if they use lactose or L-HPC.
What does the dependent excipient coverage imply for design-around risk?
Because claims 3-5 are narrower than claim 1, excipient selection alone is not sufficient to avoid claim 1. But excipient selection can matter because it is likely causal to achieving the claimed dissolution performance.
A competitor’s lowest-risk design-around path is typically:
- adjust formulation so dissolution under the exact test conditions does not reach ≥85% within 30 minutes (claim 1) or ≥85% within 15 minutes (claim 2); and/or
- use a dose outside the ~2.5 to ~10 mg single daily dose range.
If a competitor’s dose is clearly above or below the range, claim 1 and any dependent claims tied to claim 1’s dose limitation should be avoided.
What does the patent landscape likely look like in the US for this compound and this claim type?
Based on claim format alone (compound-specific + dissolution-defined performance), the US landscape most often splits into two clusters:
1) Application/publication family likely targeting specific dissolution-qualified immediate-release dosing
This patent’s structure is typical of late-stage lifecycle management or formulation-centric protection where:
- the active is fixed,
- the differentiation is dissolution kinetics and excipient embodiments,
- and the legal strategy is to control specific commercial dosage strengths and release profiles.
This increases the odds that related patents exist (same active) with variant:
- dissolution thresholds,
- media compositions (with or without surfactants),
- paddle speeds,
- or excipient packages.
2) Generic/ANDA/505(b)(2) pathway challenges
In the US, the most frequent enforcement targets in dissolution-performance patents are products that:
- match the active and strength,
- and demonstrate dissolution curves that meet the claimed thresholds in the claimed media and apparatus conditions.
For “in vitro” limitations, litigation typically hinges on:
- how the dissolution test is conducted,
- and whether the accused product meets the thresholds in a court-admissible way.
Why this matters for diligence
This patent likely creates leverage for enforcement against specific immediate-release strengths rather than against every route/formulation of the active. The dissolution threshold provides a measurable infringement axis, which can be tested during validity/infringement analysis.
Landscape view by claim element: where battles likely occur
| Claim element |
Covered in claim |
Strength of protection |
Typical landscape issue |
| Compound identity (fixed stereochemistry) |
Claim 1-5 |
Very strong |
Many competing candidates using the same active face this barrier. |
| Single daily dose range |
Claim 1-5 (via claim 1 dependency) |
Strong |
Generic strengths outside range can be design-around; strengths within range are higher-risk. |
| Dissolution: ≥85% threshold |
Claim 1-2 |
Very strong |
Competitors must match performance under exact media and paddle rpm conditions. |
| Dissolution medium details |
Claim 1-2 |
Strong |
Media differences (e.g., polysorbate 80 present in claim 1 but not claim 2) can distinguish products. |
| Apparatus speed and timepoint |
Claim 1-2 |
Strong |
Changing rpm or achieving threshold at different times can avoid/limit coverage. |
| Lactose and L-HPC excipients |
Claims 3-5 |
Narrow |
Used mainly to catch specific marketed formulations; does not replace dissolution proof for claim 1. |
Actionable reading of scope for R&D and investment diligence
If your goal is to clear or assess freedom to operate (FTO)
The practical question is whether an accused or planned product will:
- use this same compound,
- at a single daily dose strength in 2.5 to 10 mg, and
- meet ≥85% dissolution under the exact claim conditions.
The patent’s tight test conditions suggest that a meaningful FTO assessment requires dissolution testing in the same medium and apparatus settings, aligned with JP16 6.10 and USP37 <711> immediate-release methodology.
If your goal is to evaluate competitive risk
This patent likely matters most to:
- companies launching the compound in an immediate-release oral format with strengths in the specified range, and
- companies reformulating to improve dissolution while keeping strength in-range.
Because the claim ties performance to objective thresholds, competing formulations that look similar in generic dissolution testing may still miss or meet depending on polysorbate presence and rpm.
Key Takeaways
- Claim 1 is the breadth anchor: it combines fixed active identity, a single daily dose range (~2.5 to ~10 mg), and a quantified dissolution performance requirement (≥85% in 30 minutes) under precisely specified medium (including 0.5% polysorbate 80), paddle rpm (75 rpm), temperature, and volume.
- Claim 2 tightens performance to ≥85% in 15 minutes at 50 rpm and uses a medium without polysorbate 80.
- Claims 3-5 narrow to specific excipient embodiments: lactose and low-substituted hydroxypropyl cellulose, singly and in combination.
- The most viable design-around levers are dose strength outside the stated range and failure to reach the claimed dissolution threshold under the claimed test conditions.
FAQs
1) Does US 11,026,944 protect all formulations of the compound?
No. Coverage in the excerpt is anchored to immediate-release dissolution performance and dose range tied to the specified compound.
2) Is the dissolution requirement enforceable as a product attribute?
Yes. The claim limits infringement to products that achieve ≥85% dissolution within the stated time under the recited medium and apparatus conditions.
3) What is the difference between claim 1 and claim 2 dissolution testing?
Claim 1 requires ≥85% in 30 minutes in 0.1 M HCl with 0.5% polysorbate 80 at 75 rpm; claim 2 requires ≥85% in 15 minutes in 0.1 M HCl at 50 rpm.
4) Do lactose and hydroxypropyl cellulose apply to the broadest claim?
No. Lactose (claim 3) and low-substituted hydroxypropyl cellulose (claim 4) apply only to those dependent claims. Claim 1 does not require those excipients.
5) Can a competitor avoid infringement by using different excipients?
Different excipients can help only if they result in non-infringing dissolution performance (or non-infringing dose strength). Excipient changes alone do not negate claim 1.
References
[1] U.S. Patent No. 11,026,944 (claims as provided by user).
