United States Patent 11,564,916: Scope of Claims, Claim-Chartable Elements, and Competitive Patent Landscape
What is US 11,564,916 claim scope for cystic fibrosis (CF) treatment?
US 11,564,916 is directed to methods of treating or lessening the severity of cystic fibrosis by administering an oral pharmaceutical solid dosage where the active is N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) formulated as a solid dispersion with specific excipient chemistry and crystallinity constraints. The independent claim set is structured around:
1) A solid dispersion defined by exact composition and amorphous/crystalline limits (claims 1, 24, 35).
2) A tablet formulation layer that allocates wt% ranges for dispersion, filler, disintegrant, surfactant, binder, glidant, lubricant (claim 24).
3) Use conditions that expand the practical commercial method through food and co-therapy timing and dosing frequency (claims 15-23, 26-34, 37-40).
The claims are tightly tethered to:
- Composition of the solid dispersion:
- Compound 1: 80 wt% of the dispersion, where substantially amorphous Compound 1 contains <15% crystalline Compound 1 (independent baseline).
- HPMCAS: 19.5 wt% of dispersion
- SLS: 0.5 wt% of dispersion
- Optional crystallinity tightenings:
- “Substantially amorphous Compound 1 comprises <5% crystalline Compound 1” (claims 9, 25, 36)
- Tablet-level composition constraints (independent claim 35 is exact at the composition level; claim 24 uses ranges).
- Hardness, dose amount, and administration schedule (claim 12, 13-20, 26-30).
What are the protected method elements in Claim 1 (core functional coverage)?
Claim 1:
A method of treating or lessening CF severity in a patient comprising administering a pharmaceutical composition having a solid dispersion with:
- 80 wt% of amorphous or substantially amorphous Compound 1
- <15% crystalline Compound 1 in the “substantially amorphous” portion
- 19.5 wt% HPMCAS
- 0.5 wt% SLS
Further claim scope expansions within Claim 1 dependent set:
- Tablet/compression performance:
- Hardness: 98 N or 10 kp ±20% (claim 12)
- Dose amount anchors:
- Contains 150 mg Compound 1 (claim 13)
- Contains 100 mg Compound 1 (claim 14)
- Oral dosing frequency:
- Twice per day (claim 15)
- Every 12 hours (claim 16)
- Once per day (claim 17)
- Food-timing window:
- Concurrent with “high fat, high calorie CF meal or snack” (claim 18)
- 30 minutes after such meal/snack (claim 19)
- Co-therapy timing:
- Concurrent/prior/subsequent to an “additional therapeutic agent” (claim 20)
- Additional agent types include mucolytic, bronchodilator, antibiotic/anti-infective, anti-inflammatory, CFTR modulator other than Compound 1, nutritional agent (claim 21)
CFTR modulator specificity:
- Additional therapeutic agent is a CFTR modulator other than Compound 1 (claim 22)
- The named modulator is:
(3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid) (claim 23)
How does dependent claim 2-8 broaden formulation freedom while staying within the same dispersion?
These do not replace the dispersion requirements; they add typical solid dosage scaffolding:
- Add microcrystalline cellulose: 30.5 wt% (claim 2)
- Add lactose: 30.4 wt% (claim 3)
- Add sodium croscarmellose: 3 wt% (claim 4)
- Add SLS: 0.5 wt% (claim 5) (note: this is tablet/composition-level SLS, distinct from the SLS inside the dispersion which is locked at 0.5 wt% of dispersion in claim 1)
- Add colloidal silicon dioxide: 0.5 wt% (claim 6)
- Add magnesium stearate: 1.0 wt% (claim 7)
- Require solid dispersion: 34.1 wt% of composition (claim 8)
What is the “tablet composition range” coverage in Claim 24?
Claim 24 is the most commercially scalable “formulation envelope.” It locks:
- The presence of a tablet and a solid dispersion constituting 30% to 50% by weight of the tablet.
- The dispersion composition is fixed to the same internal recipe (80% Compound 1, 19.5% HPMCAS, 0.5% SLS; amorphous constraint <15% crystalline).
Then it imposes general tablet excipient classes and ranges:
| Component |
Claim 24 amount (wt% of tablet) |
| Solid dispersion |
30% to 50% |
| Filler |
25% to 50% |
| Disintegrant |
1% to 10% |
| Surfactant |
0.3% to 2% |
| Binder |
20% to 45% |
| Glidant |
0.09% to 1.0% |
| Lubricant |
0.1% to 2% |
Food, dose, and schedule variants are then layered onto the tablet method:
- Dispensed as tablet and administered:
- Twice/day or q12h or once/day (claims 26-28)
- Concurrent with or 30 minutes after high-fat/high-calorie CF meal/snack (claims 29-30)
- Concurrent/prior/subsequent to additional therapeutic agent (claims 31-34)
Crystallinity tighten option:
- <5% crystalline Compound 1 (claim 25)
CFTR modulator specificity:
- Additional therapeutic agent being the named CFTR modulator (claims 33-34)
What is the “exact composition” coverage in Claim 35?
Claim 35 expands coverage from ranges to an exact tablet composition.
Exact wt% allocation (Claim 35):
| Component |
wt% of pharmaceutical composition |
| Solid dispersion |
34.1% |
| - within dispersion: Compound 1 |
80% of dispersion |
| - within dispersion: HPMCAS |
19.5% of dispersion |
| - within dispersion: SLS |
0.5% of dispersion |
| Microcrystalline cellulose |
30.5% |
| Lactose |
30.4% |
| Sodium croscarmellose |
3% |
| SLS (tablet-level) |
0.5% |
| Colloidal silicon dioxide |
0.5% |
| Magnesium stearate |
1.0% |
Claim 35 dependent expansions:
- <5% crystalline Compound 1 (claim 36)
- Administration with additional therapeutic agent (claim 37)
- Additional agent types including CFTR modulator other than Compound 1 (claim 38)
- Additional agent is CFTR modulator other than Compound 1 (claim 39)
- Named CFTR modulator identity (claim 40)
This claim is the clearest infringement target because it specifies a complete quantitative recipe for the tablet.
How the claims map to enforceable “infringement hooks”
US 11,564,916 is strongest where a product meets all of the following:
1) Active identity: Compound 1 as named in the claims.
2) Dispersion identity: solid dispersion with HPMCAS and SLS at the stated proportions.
3) Crystallinity:
- Substantially amorphous Compound 1 must be <15% crystalline (baseline), and optionally <5% in narrower dependents.
4) Solid dosage form: tablet-level embodiment is explicit (claim 24 and claim 35).
5) Administration practice: twice/day or q12h or once/day, and food timing (concurrent or 30 minutes post high-fat/high-calorie CF meal/snack).
6) Co-therapy: the claims include a method extension for dosing in conjunction with other therapeutics, including a specific CFTR modulator.
From a freedom-to-operate perspective, the enforcement surface increases because the patent includes:
- Exact formulation (claim 35)
- Range-based formulation (claim 24)
- Operational dosing conditions (claims 15-23 and 26-34)
What does the patent landscape look like for this claim theme?
With only the claim text provided, a full patent landscape requires external source confirmation (US publication numbers, family members, assignee, priority, prosecution history, and cited art). No reliable landscape can be produced from claim text alone without generating inaccurate or fabricated citations.
Given the operating constraints, no complete patent-landscape mapping (competing US filings, blocking patents, design-around candidates, or family continuations) is provided here.
Practical “design-around” pressure points implied by the claim language
Even without a competitor-specific landscape, the claim structure highlights the main levers that can determine whether a product lands inside or outside the protected scope:
1) Dispersion formulation lock
- The dispersion composition (80% Compound 1, 19.5% HPMCAS, 0.5% SLS) is fixed in claims 1 and 24 and embedded within claim 35.
- A design-around must change at least one of these dispersion-defining features, not merely tablet excipients.
2) Amorphous/crystalline definition
- The claims use quantitative crystallinity thresholds (<15% and dependent <5%).
- Any alternative process or stabilization strategy risks crossing into the same crystallinity definition unless analytical methods show the threshold is avoided.
3) Tablet excipient allocations
- Claim 35 is exact at the composition level; claim 24 is a constrained range.
- If the product targets the same dispersion but changes tablet excipient identity or quantity, it may still fall within claim 24’s range envelope.
4) Food-timing and dosing schedule
- The method claims broaden to how the patient takes the tablet relative to a high-fat/high-calorie meal/snack.
- If commercial labeling avoids those timings, it can reduce direct match to those dependent claims (but may still meet the base claim if the independent claim does not recite timing).
5) Co-therapy and CFTR modulator inclusion
- The inclusion of a named CFTR modulator in dependent claims increases the likelihood that certain real-world regimens are captured.
- Avoiding that specific co-therapy timing or inclusion can matter for dependent claim coverage.
Key Takeaways
- US 11,564,916 protects methods of treating CF severity using oral tablet formulations where the active is Compound 1 in a solid dispersion with HPMCAS and SLS and an explicit crystallinity ceiling (<15% crystalline; narrower option <5%).
- The claim set includes:
- Exact dispersion recipe (claims 1, 24, 35 embedded),
- Exact tablet recipe (claim 35),
- Range-based tablet envelope (claim 24),
- Operational use conditions covering dose frequency, meal timing, and co-therapy, including a specific named CFTR modulator (claims 23, 34, 40).
- Landscape-wide competitive mapping cannot be stated from claim text alone under the requirement for complete accuracy; enforceability risk must be evaluated using the full patent record and family/citations.
FAQs
1) Does the patent protect the compound itself or only the method of treatment?
It protects methods of treating or lessening the severity of cystic fibrosis by administering the claimed pharmaceutical composition/tablet.
2) What is the single most defining technical requirement in the claims?
The solid dispersion composition and crystallinity constraint: Compound 1 at 80 wt% of dispersion with <15% crystalline and dispersion excipients HPMCAS (19.5 wt%) and SLS (0.5 wt%).
3) Which claim is best aligned with an exact product recipe?
Claim 35, which gives a full tablet-level exact wt% composition including microcrystalline cellulose, lactose, sodium croscarmellose, tablet-level SLS, colloidal silicon dioxide, and magnesium stearate.
4) Which claim provides the widest formulation freedom while still capturing infringement?
Claim 24, which allows a solid dispersion at 30% to 50% of the tablet and ranges for filler, disintegrant, surfactant, binder, glidant, and lubricant.
5) Do the claims require administration with a CFTR modulator?
No. They extend method coverage to cases where an additional therapeutic agent is administered, including CFTR modulators other than Compound 1, and include a dependent claim with a named CFTR modulator.
References
- (No external sources cited; response limited to claim text provided.)
