United States Patent 11,260,047: What the Claims Cover, Where They Stop, and How to Map the Patent Landscape
What does US Drug Patent 11,260,047 claim in plain claim-scope terms?
US 11,260,047 is directed to a tablet formulation built around AG10 (or a pharmaceutically acceptable salt) at high drug load and a specific microcrystalline cellulose (MCC) filler morphology/particle-structure definition, plus optional formulation add-ons (disintegrants, lubricants, coating, inorganic salts) and dissolution-performance limitations.
Core claim concept: high AG10 load + specific MCC morphology
The claims repeatedly require:
- A tablet formulation comprising AG10 or a pharmaceutically acceptable salt
- The formulation contains at least 40% by weight AG10 (or salt) (independent claim)
- One or more fillers comprise high-grade microcrystalline cellulose defined by cellulose polymer particle characteristics:
- (i) spherical morphology and porous structure, or
- (ii) needle-like particle shape
This means the protected composition space is not “any MCC-containing tablet with AG10.” It is MCC with a specific morphology/porosity/shape characterization plus a high AG10 weight fraction.
Claim 1 scope: independent claim and its boundary conditions
Claim 1 defines the baseline protected formulation:
- Tablet formulation comprising:
- AG10 or pharmaceutically acceptable salt
- one or more fillers
- Quantitative limits:
- at least 40% by weight AG10 (or salt)
- Filler definition:
- fillers include high-grade MCC characterized by cellulose polymers with either:
- spherical morphology and porous structure, or
- needle-like particle shape
Practical boundary implications for design-arounds
To avoid literal infringement of claim 1, a competitor generally needs to break at least one required element:
- Drop AG10 below 40 wt%, or
- Use MCC that fails the spherical porous or needle-like morphological/structural definition, or
- Avoid MCC as the required “high-grade” type as defined.
Because the claim is structural/functional at the filler-definition level, design-around is often less about generic “MCC grade” labeling and more about particle morphology/porosity/shape characterization and the ability to show the filler does not match the defined MCC characterization.
How dependent claims tighten the protected composition space
Drug load ranges (claims 2-6)
Dependent claims narrow AG10 wt% compositions:
- Claim 2: about 40-85% AG10
- Claim 3: about 50-75%
- Claim 4: about 50%
- Claim 5: about 66.7%
- Claim 6: about 75%
These dependent claims do not replace claim 1; they sit “inside” the claim 1 requirement set. They make it harder for competitors to target “near 40%” or “midrange” without still falling into an explicitly claimed sub-range.
Filler amount ranges (claims 7-10)
These claims constrain how much of the tablet is filler (the MCC is part of the “fillers”):
- Claim 7: fillers comprise about 1-60 wt%
- Claim 8: about 5-55 wt%
- Claim 9: about 10-50 wt%
- Claim 10: about 15-45 wt%
Again, these are dependent ranges on the claim 1 formulation concept.
Other filler components (claims 11-12)
- Claim 11: fillers further comprise a cellulose derivative or an inorganic salt
- Claim 12: fillers further comprise silicon dioxide (SiO2)
These enlarge the “allowed” formulation options without changing the core requirement that MCC with the defined morphology must be present as part of the filler system.
Disintegrants (claims 13-16)
- Claim 13: disintegrant(s) 1-15 wt%
- Claim 14: 3-8 wt%
- Claim 15: about 6 wt%
- Claim 16: disintegrant comprises croscarmellose sodium
This creates a second axis of protection: even with the same MCC morphology and high AG10, the claims also cover commonly used disintegrant levels and an explicitly named disintegrant.
Lubricants (claims 17-19)
- Claim 17: lubricant(s) 0.1-8 wt%
- Claim 18: about 1.5 wt%
- Claim 19: lubricant comprises magnesium stearate
This is common tablet excipient territory, but it is still claim-covered when paired with the MCC definition and the high AG10 content.
Dissolution performance (claims 20-23)
- Claim 20: tablet is at least 75% dissolved in 0.1N HCl, 37 ± 0.5°C, Apparatus II (paddles), 50 rpm, 10 minutes
- Claim 21: at least 85% dissolved
- Claim 22: at least 95% dissolved
- Claim 23: dissolution test is performed at least three months after preparation
This is an important evidentiary/functional limitation: it is not only a composition claim; it also captures performance and stability over time (test timing at ≥3 months).
Coating (claim 24)
- Claim 24: further comprising a coating agent
Claim 25: specific identity relationship
- Claim 25: AG10 is the pharmaceutically acceptable salt form of Formula Ia
This ties AG10 to a particular chemical identity (Formula Ia salt form). If a product uses a different salt form or a non-AG10 form, claim coverage is affected unless the accused product is still “AG10” (or a pharmaceutically acceptable salt as characterized in the patent).
Claim 26: how it broadens into a “particular excipient set”
Claim 26 recasts protection as a tablet formulation containing a defined excipient package plus the morphology-defined MCC and a set of typical tablet formulation components:
- At least 40 wt% AG10 (or salt)
- A filler set including:
- high-grade MCC filler
- inorganic salt filler
- disintegrant
- lubricant
- MCC morphology must still be:
- spherical morphology and porous structure, or
- needle-like particle shape
This claim is effectively a “composition checklist” version. It can be particularly useful in enforcement because it reduces ambiguity about which excipients are required beyond the MCC morphological definition.
What is the actionable infringement trigger?
A tablet infringes if it meets:
- AG10 (or its pharmaceutically acceptable salt) at ≥40 wt%, and
- includes MCC characterized by either (i) spherical porous or (ii) needle-like cellulose polymer morphology/structure, and
- falls within the optional dependent elements if those dependent claims are asserted (drug load sub-ranges, filler wt%, disintegrant identity/level, lubricant identity/level), and/or
- satisfies dissolution-performance parameters if the asserted claims include claims 20-23.
Why the MCC morphology definition is the key claim lever
Most generic tablet compositions can be modified to include disintegrants or lubricants, and drug load can be tuned. The hardest constraint to replicate or invalidate is:
- “high-grade microcrystalline cellulose characterized by cellulose polymers with (i) spherical morphology and porous structure or (ii) needle-like particle shape.”
This turns excipient selection into a material-structure matching problem. Enforcement and validity challenges can hinge on:
- what exact MCC grade(s) meet the described morphological characterization, and
- what analytical method supports that characterization in practice.
Scope map: where the patent is strong vs. where it thins
Strongest coverage zones
Zone A: High AG10 wt% + defined MCC morphology
- Claim 1 plus dependent ranges 2-6 set a dense protected composition lattice around mid-to-high drug loading (40-85 wt% and specific points at 50, 66.7, 75).
Zone B: Performance-anchored claims
- Claims 20-23 add a dissolution benchmark (≥75% up to ≥95%) in 0.1N HCl using Apparatus II conditions and a 3-month post-prep test requirement.
Zone C: “Checklist” excipient package
- Claim 26 requires a set of excipients (inorganic salt filler, disintegrant, lubricant) together with the MCC morphology and high drug load.
Potentially thinner coverage areas
1) Products with AG10 below 40 wt%
- This is the most direct quantitative escape from claim 1.
2) MCC that does not match the defined morphology
- If the accused formulation uses MCC sourced/manufactured/characterized such that it is not “spherical porous” or “needle-like” by the patent’s defined characterization, literal infringement is at risk.
3) Dissolution-target differences
- If an accused product does not meet the claimed dissolution profile in the specified method or does not sustain the performance after ≥3 months, dependent claims 20-23 may not read on it.
4) Non-AG10 salt forms
- Claim 25 anchors AG10 to a salt form of Formula Ia. If the active is not “AG10” and not that specified salt characterization, claim scope may not apply.
How to interpret the “filler” architecture across claims
The claims use “fillers” in a way that can include:
- MCC with the morphology definition (required)
- silicon dioxide (optional in dependent claim 12)
- cellulose derivative or inorganic salt (optional in claim 11)
- inorganic salt filler appears as required element in claim 26
So the protected excipient system can be “MCC plus additional excipients,” not “MCC only.”
What does this mean for the US patent landscape assessment?
Without the underlying application history, family members, expiry dates, or the patent’s full bibliographic record (assignee, filing date, and whether it is part of an ANANDA/ANDA or salt/formulation series), the landscape can only be mapped at the claim-coverage level based on the claim text provided.
That said, the enforceable claim architecture strongly suggests a formulation-specific protection strategy where competitors are likely to face risk if they:
- use AG10 at high loading and
- use MCC with morphology matching and
- meet dissolution performance benchmarks.
In practice, the landscape risk is less about alternative excipient choices and more about:
- whether the competitor’s MCC matches the morphology characterization, and
- whether the competitor’s formulation meets the dissolution profile claimed.
Key Takeaways
- US 11,260,047 protects a tablet formulation with AG10 (or its specified pharmaceutically acceptable salt) at ≥40 wt% and high-grade MCC defined by specific cellulose morphology/structure: spherical porous or needle-like.
- Dependent claims carve out drug-load ranges (40-85 wt%, 50-75 wt%, and discrete 50/66.7/75 wt% targets) and filler wt% ranges (1-60 down to 15-45).
- Optional dependent elements (disintegrants, lubricants, SiO2, cellulose derivatives, coating) become enforceable when paired with the core AG10 + morphology-defined MCC.
- Performance limitations (0.1N HCl, 37°C, App II paddles 50 rpm, 10 minutes, with ≥75% to ≥95% dissolution) plus a ≥3-month stability timing requirement are part of the protected claim set.
- The main design-around lever is breaking either the AG10 wt% threshold (<40) or using MCC that fails the patent’s morphology/structure characterization; a secondary lever is dissolution performance and salt identity (AG10 as Formula Ia salt form).
FAQs
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Is the patent claiming “AG10 tablets” broadly?
No. It requires AG10 (or its pharmaceutically acceptable salt) at ≥40 wt% plus MCC with specific morphology/structure (spherical porous or needle-like cellulose polymer shape).
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Can a different disintegrant avoid the patent?
Not by itself. Disintegrants are part of dependent coverage. Avoiding the patent generally requires breaking the core requirements (AG10 wt% and MCC morphology definition), then also addressing any dependent claim asserted (for example, croscarmellose sodium at claimed levels).
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Does dissolution testing matter for scope?
Yes for claims that include performance limits. Claims 20-23 add specific dissolution method conditions, thresholds, and a post-preparation timing of at least three months.
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Is silicon dioxide covered?
Silicon dioxide is included in dependent claim 12 as part of fillers. It does not define the core claim by itself, but it becomes relevant if the asserted dependent claim includes it.
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What is the most likely formulation-risk point for competitors?
The MCC morphology/porosity/particle shape definition tied to “high-grade microcrystalline cellulose,” combined with high AG10 loading.
References
[1] US Patent 11,260,047 (claims as provided by user).
