Scope, Claim Structure, and US Patent Landscape for US Drug Patent 9,056,057
What does US 9,056,057 claim, in core terms?
US 9,056,057 claims particulate formulations intended for improved performance in mucus using a specific “core + triblock copolymer surface-altering agent” architecture. The dominant scope is defined by three technical pillars that are all required in claim 1 (and therefore in claim 2):
1) Core particle composition and drug solubility constraint
- Core particle contains a solid pharmaceutical agent (or salt).
- The agent or salt has aqueous solubility ≤ 1 mg/mL at 25°C at any point throughout the pH range (claim 1).
- Drug constitutes ≥ 80 wt% of the core particle.
- Polymer constitutes < 20 wt% of each core particle.
2) Surface-altering agent chemistry and brush-like hydrophilicity
- Coating surrounds the core particle.
- Surface-altering agent comprises a triblock copolymer with hydrophilic-hydrophobic-hydrophilic configuration.
- Hydrophobic block MW ≥ 2 kDa.
- Hydrophilic blocks constitute ≥ 15 wt% of the triblock copolymer.
- Hydrophobic block associates with the core particle surface.
- Hydrophilic block is present at the coated particle surface and renders the coated particle hydrophilic.
- Surface density constraint: coating is present at ≥ 0.001 molecules/nm² (claim 1).
3) Mucus transport / motion performance requirement
- Coated particles have relative velocity > 0.5 in mucus (claim 1).
Claims 4 to 28 then narrow or specify these pillars (attachment mode, surface density, copolymer composition, drug form, and delivery routes/carriers).
How broad is claim 1 and what are its hard boundaries?
Claim 1 required elements (all must be present)
A. Core + drug constraint
- Solid pharmaceutical agent or salt inside a core.
- Solubility ≤ 1 mg/mL at 25°C across the pH range.
- ≥ 80 wt% drug in the core.
- < 20 wt% polymer in the core.
B. Coating composition and structural constraints
- Triblock copolymer with hydrophilic block – hydrophobic block – hydrophilic block.
- Hydrophobic block MW ≥ 2 kDa.
- Hydrophilic blocks ≥ 15 wt% of triblock.
- Hydrophobic block associates with core surface.
- Hydrophilic block is at the coated particle surface and makes it hydrophilic.
- Surface density ≥ 0.001 molecules/nm².
C. Mucus performance
- Relative velocity > 0.5 in mucus.
Key “scope levers” that set infringement lines
These are the elements that most directly convert a “similar concept” into claim coverage:
| Lever |
Threshold in claim 1 |
Practical meaning for design-around |
| Drug aqueous solubility |
≤ 1 mg/mL at 25°C across pH range |
Changing to a more soluble drug or salt outside that constraint can exit scope |
| Core drug fraction |
≥ 80 wt% drug; polymer < 20 wt% |
Higher excipient/polymer loading can exit |
| Triblock composition |
Hydrophobic MW ≥ 2 kDa; hydrophilic wt% ≥ 15% |
Using different block MWs or lower hydrophilic fraction can exit |
| Surface density |
≥ 0.001 molecules/nm² |
Lower grafting/coverage can exit |
| Transport performance |
Relative velocity > 0.5 in mucus |
If measured relative velocity does not exceed the threshold, scope may not read |
How do claim 2, claim 3, and independent protection differ?
Claim 2 (method of delivery to mucus)
Claim 2 is the “same formulation” as claim 1, but reframed as delivery:
- “Delivering to a mucus membrane” a composition meeting the full claim 1 composition constraints.
- The mucus setting ties scope to use in mucus, not just a passive material.
Claim 3 (method of forming coated particles)
Claim 3 targets manufacturing steps:
- Combine core particles with a solution comprising the surface-altering agent that satisfies the same solubility and loading constraints.
- Coat the core particles with the triblock copolymer to form coated particles meeting the mucus velocity constraint.
In practice, claim 3 offers a separate infringement pathway even when end-user administration is handled differently, so long as the method steps produce the defined coated particles.
What do the dependent claims add? (Claims 4 to 28)
Dependent claims narrow claim 1 using attachment mode, density, copolymer specs, drug forms, particle sizes, diffusion/transport metrics, and administration routes.
Surface attachment and coverage
- Claim 4: surface-altering agent covalently attached to the core.
- Claim 5: surface-altering agent non-covalently adsorbed to the core.
- Claim 6: surface density ≥ 0.01 molecules/nm² (note the step-up from claim 1’s ≥ 0.001).
Copolymer fraction and identity
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Claim 7: hydrophilic blocks ≥ 30 wt% of the triblock.
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Claim 8: hydrophobic block MW ≥ 3 kDa (step-up from claim 1’s ≥ 2 kDa).
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Claim 9: specific exemplars: poly(ethylene oxide)-poly(propylene oxide)-poly(ethylene oxide) or poly(ethylene glycol)-poly(propylene oxide)-poly(ethylene glycol).
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Claims 10-13: more specific definitions:
- hydrophilic block is PEG/PEO or derivative (claim 10),
- hydrophilic block MW ≥ 2 kDa (claim 11),
- hydrophobic block is poly(propylene oxide) (claim 12),
- hydrophobic block MW ≥ 3 kDa (claim 13).
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Claim 14: coating solution concentration ≥ 0.1% (w/v).
Drug solid form
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Claims 15-17: drug is crystalline, amorphous, or salt form (as applicable to claim 1’s “solid pharmaceutical agent or salt” universe).
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Claims 18-20: drug can be therapeutic or diagnostic; can be small molecule, peptide, peptidomimetic, protein, nucleic acid, or lipid.
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Claim 20: tighter solubility option: ≤ 0.1 mg/mL at 25°C.
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Claim 21: tighter drug wt% option: ≥ 85 wt% drug.
Particle size and transport/diffusion metrics
- Claim 22: core particle size 20 nm to 1 μm.
- Claim 23: coated particle size 20 nm to 1 μm.
- Claim 24: diffusion in human cervicovaginal mucus has diffusivity > 1/500 of diffusivity through water over 1 second (a specific relative diffusivity metric).
- Claim 25: coated particles relative velocity > 0.8 in mucus (step-up from claim 1’s > 0.5).
- Claim 26: mucus is human cervicovaginal mucus.
Formulations and administration
- Claim 27: pharmaceutical composition includes claim 1 composition plus one or more pharmaceutically acceptable carriers.
- Claim 28: pharmaceutical preparation suitable for inhalation, injection, or topical administration to a mucus membrane.
Where is the “center of gravity” in the claim set?
The broadest independent protection sits in claim 1, anchored by the combination of:
- low-solubility solid drug core (≤ 1 mg/mL across pH),
- high drug loading in the core (≥ 80 wt%),
- specific triblock copolymer surface chemistry (PEO/PEG-PO-PEO/PEG-like with MW and wt% constraints plus a surface density minimum),
- a measured transport threshold in mucus (relative velocity > 0.5).
Dependent claims then create “fallback positions” by tightening thresholds (surface density, hydrophilic wt%, MWs, solubility, drug wt%, particle size, relative velocity, cervicovaginal mucus, diffusion metric) and by defining variants (attachment covalent vs noncovalent, drug solid form, routes, carrier-containing formulation).
How does this claim architecture shape the infringement profile?
Likely broad infringement triggers
An accused product/process is most likely to fall within the claim set if it satisfies all of:
- coated particulate delivery to mucus with measurable relative velocity > 0.5; and
- the coated particles have a tributyl/hydrophilic-hydrophobic-hydrophilic block surface architecture meeting MW and wt% thresholds; and
- the core is a low-solubility solid drug formulation with ≥ 80 wt% drug and < 20 wt% polymer; and
- coating achieves ≥ 0.001 molecules/nm² surface coverage.
Likely non-infringement levers (design-around categories)
Competitors can avoid literal claim reading by changing one required component or threshold:
- improve drug solubility so it no longer fits ≤ 1 mg/mL across pH;
- reformulate the core so the drug no longer stays ≥ 80 wt% (or polymer exceeds <20 wt%);
- use a non-matching copolymer architecture (different block layout or insufficient hydrophilic wt%);
- use copolymer blocks below required MWs;
- reduce effective coating surface density below 0.001 molecules/nm²;
- fail the measured mucus motion metric (relative velocity or diffusion constraint).
US patent landscape analysis for 9,056,057 (scope-to-family mapping approach)
You provided the claim text, but not bibliographic metadata (publication numbers, priority dates, inventors/assignees, related family members), and you did not provide the actual patent document content beyond claim statements. Without those bibliographic anchors, a complete, accurate US landscape map (continuations, divisionals, related filings by competitors, prosecution history, and citing/cited art networks) cannot be produced without risking factual errors.
Given that constraint, the landscape analysis below is limited to a claim-driven landscape typology: the categories of prior art and follow-on patents that typically litigate around these exact technical constraints (polymer-coated mucus-transport particles, low-solubility drug cores, block-copolymer surface layers, and measured mucus relative mobility). This typology is actionable for freedom-to-operate work, but it is not an allegation about specific named patents.
Claim-driven prior art clusters likely relevant to validity/obviousness
1) Mucus-penetrating particles via hydrophilic polymer coatings
- Prior art often includes PEG/PEO-like hydrophilic coatings, zwitterionic layers, and block copolymer brushes designed to reduce mucoadhesion and increase penetration.
- Validity attack points are usually the novelty of the triblock specific architecture, density threshold, and the quantified mucus motion metric.
2) Low-solubility drug particulate cores and amorphous/crystalline/salt forms
- Prior art covers solid dispersion, high drug loading matrices, salts, and particle engineering to manage dissolution.
- In this claim set, the novelty defense often depends on the coupling of a specific triblock coating with a particular low-solubility and high drug wt% core.
3) Measured mucus transport and experimental comparators
- Many patents describe “improved penetration” without hard thresholds that are reproducible across assays.
- Here the patent uses explicit metrics: relative velocity > 0.5 and alternative diffusion relation in cervicovaginal mucus.
- That makes prior art with direct quantitative mobility outcomes particularly relevant.
Claim-driven follow-on filings likely to appear around this disclosure
1) Copolymer parameter sweeps
- Expect families that keep the triblock concept but vary:
- hydrophilic block wt% (claim 7),
- hydrophobic MW (claims 8, 13),
- surface density targets (claim 6),
- attachment modes (claims 4 and 5).
2) Mucus-specific embodiments
- Expect continuation/divisional claims narrowing mucus type (claim 26) and strengthening the mucus metric (claim 25, claim 24).
3) Route and formulation packaging
- Expect follow-on patents that map the same particles into inhalation/injection/topical mucus membrane contexts (claim 28) with carrier systems (claim 27).
What are the strongest claim features for enforcement leverage?
1) Quantified mucus transport requirement (relative velocity threshold)
- Mobility metrics tend to narrow the claim reading and can help distinguish from generic hydrophilic coating art.
2) Triblock copolymer specificity (MW and hydrophilic wt%) plus adsorption behavior
- The requirement that the hydrophobic block associates with the core and that the hydrophilic block is present at the coated surface operationalizes the polymer’s role.
3) Surface density in molecules/nm²
- Coverage density constraints are often the most litigated detail because they require either direct measurement or defensible estimation tied to a protocol.
4) Core drug wt% and low solubility across pH
- These two constraints convert the formulation from a general platform into a narrow product class targeting low-solubility actives in highly drug-loaded cores.
What is the likely scope of “equivalents” around the numerical thresholds?
The claim language uses numerical cutoffs (≤, ≥, and >). In practice:
- If an accused product lands near but just outside a threshold (for example, relative velocity 0.48 vs 0.51), the fight moves to measurement method comparability and whether the numerical boundary is treated as a hard limitation.
- Surface density and mucus velocity are particularly assay-dependent. That increases the importance of choosing an infringement testing method consistent with the patent’s described measurement framework, even when not stated in your excerpt.
Key Takeaways
- Claim 1 defines a tightly coupled formulation: a high drug wt% low-solubility solid core (≤ 1 mg/mL across pH) plus a PEO/PEG-like triblock coating with hydrophobic block MW ≥ 2 kDa, hydrophilic blocks ≥ 15 wt%, and surface density ≥ 0.001 molecules/nm², achieving mucus relative velocity > 0.5.
- Claims 2 and 3 add use and manufacture pathways, respectively, but they keep the same hard composition and mucus performance requirements.
- Dependent claims create enforceable fallbacks by tightening the triblock parameters, increasing surface density and hydrophilic fraction, narrowing solubility (≤ 0.1 mg/mL), adding specific mucus type (cervicovaginal), specifying diffusion behavior, and defining particle size ranges.
- A claim-driven landscape map centers on (i) mucus-penetrating hydrophilic polymer coatings, (ii) low-solubility solid formulations, and (iii) quantitative mucus mobility assays with reproducible thresholds.
FAQs
1) Is US 9,056,057 a platform patent for any drug?
No. Claim 1 is limited to solid drugs/salts with aqueous solubility ≤ 1 mg/mL at 25°C across the pH range, plus a core composition where drug is ≥ 80 wt% and polymer is < 20 wt%.
2) What polymer architecture must the coating use?
A triblock copolymer with hydrophilic-hydrophobic-hydrophilic configuration, with hydrophobic block MW ≥ 2 kDa and hydrophilic blocks ≥ 15 wt%, and with the hydrophobic block associating with the core surface.
3) How can someone design around this patent?
By failing at least one required element: drug solubility constraint, core drug wt% fraction, triblock MW/wt% thresholds, coating surface density, or the mucus relative velocity > 0.5 requirement.
4) Does the patent cover both covalent and noncovalent attachment?
Yes. Claims 4 and 5 explicitly cover covalent attachment and noncovalent adsorption embodiments.
5) Does the patent specify mucus type and transport measurements?
Yes. Claim 26 specifies human cervicovaginal mucus, and claim 24 includes a specific relative diffusion relationship. Claim 1 and claim 25 set relative velocity thresholds in mucus.
References
[No sources were provided or cited in the supplied materials.]
