Scope and Claims Review of US Patent 9,919,024: Oral [4,12;7,15] Bicycle Peptide for Chronic Constipation and IBS/CCI
US Patent 9,919,024 is directed to an oral treatment method for chronic constipation (including chronic idiopathic constipation (CIC) and irritable bowel syndrome with constipation (IBS-C)) using a specific peptide identity and purity requirement delivered in a low-moisture, lubricated solid composition. The claim set is structured as (i) a core method of treating chronic constipation using composition “consisting of” SEQ ID NO:1 under defined stability/purity criteria, (ii) dependent narrowing to indications and symptoms, and (iii) dependent additions for combination regimens (cGMP-dependent phosphodiesterase inhibitors and/or laxatives) plus (iv) dependent specification of microcrystalline cellulose and magnesium stearate excipients.
What does US Patent 9,919,024 claim and what is the practical scope?
Short answer (claim scope in one line):
The patent claims orally administering a defined “consisting of” solid composition that includes a [4,12;7,15] bicycle peptide (SEQ ID NO:1) with ≥91% chromatographic purity after ≥3 months storage, optionally combined with (a) cGMP-dependent phosphodiesterase inhibitors (specific listed examples) and/or (b) laxatives, for chronic constipation/CIC/IBS-C and related symptoms (constipation and abdominal pain).
How “consisting of” shapes infringement risk
Independent claim 1 requires administration of a composition that “consist[s] of SEQ ID NO:1 wherein the peptide is a [4,12;7,15] bicycle, an inert low moisture carrier, and a lubricant.” This language is materially limiting:
- It excludes additional active ingredients.
- It constrains excipient selection to (1) inert low-moisture carrier and (2) lubricant, with no other components allowed in the administered “composition.”
- It creates a litigation focal point around whether the accused formulation contains any excluded excipient class (binders, disintegrants, coatings, anti-caking agents, glidants beyond the “lubricant,” moisture scavengers, film coatings, etc.).
What makes the claim unusually enforceable
The claim adds a quantified quality attribute:
- Chromatographic purity ≥91% after storage for at least three months.
This introduces a manufacturing-and-stability nexus. A product can comply on paper for sequence and excipient identity while still avoid infringement if its post-storage purity falls below the threshold, or if the measurement method/statistical handling differs from the claim’s implicit standard.
Core elements in claim 1 (mapped)
Claim 1 requires all of the following:
- Method: “treating chronic constipation in a human subject.”
- Route: oral administration.
- Composition (closed “consisting of”):
- Peptide: SEQ ID NO:1 with [4,12;7,15] bicycle structure.
- Excipient: inert low moisture carrier.
- Excipient: lubricant.
- Stability/purity: peptide ≥91% chromatographic purity after ≥3 months storage.
How narrow are the dependent claims on indication and symptoms?
What indications are explicitly covered (claims 2 and 3)?
- Claim 2 narrows claim 1 to constipation associated with IBS or chronic idiopathic constipation.
- Claim 3 broadens from treating “chronic constipation” to treating or alleviating a symptom associated with chronic idiopathic constipation or IBS.
This split matters for enforcement strategy:
- Claim 1 is indication-centric (chronic constipation).
- Claims 2 and 3 anchor coverage to clinically standard IBS-C and CIC categories.
- Claim 3 is symptom-centric, supporting arguments that a clinical study endpoint labeled as symptom relief is within claim scope.
Which symptoms are specified (claim 4)?
- Claim 4: symptom is constipation or abdominal pain.
So, if a competitor targets “abdominal discomfort” or “bloating” without constipation relief, claim 4 may not cleanly apply, but claim 3 still may if “symptom associated with” CIC/IBS is construed broadly.
What does the combination therapy language cover, and what are the listed PD inhibitors?
What does claim 5 cover?
- Claim 5 adds that the regimen includes an effective dose of an inhibitor of cGMP-dependent phosphodiesterase, administered either concurrently or sequentially with the guanylate cyclase receptor agonist.
Key scope notes:
- It is not limited to any single PDE inhibitor in claim 5; it is limited in claim 6 to specific examples.
- It supports combination infringement theories even if the products are dosed on different schedules (sequential use).
Which PDE inhibitors are explicitly listed (claim 6 and claim 9)?
- Claim 6 (and similarly claim 9): PDE inhibitors include:
- sulindac sulfone
- zaprinast
- motapizone
A competitor can avoid dependent-claim coverage by excluding these specific inhibitors, but that would not necessarily avoid infringement of claim 5 if a different cGMP-dependent PDE inhibitor were used and construed as within the class.
Is the guanylate cyclase receptor agonist term limiting?
All asserted claims describe the peptide composition as the guanylate cyclase receptor agonist used in the combination context (claim 5/8). The operative issue becomes whether the peptide is legally treated as that agonist in the record and claim construction. The provided text ties the method to a guanylate cyclase receptor agonist, and the combination claim language is keyed to that.
What laxative add-on coverage is included?
What do claims 7, 10 cover?
- Claim 7: further comprising administering an effective dose of a laxative.
- Claim 10: same add-on, tied to claim 3’s symptom framing.
No specific laxatives are listed, so the dependency is broad. However, the “consisting of” limitation in the base composition still constrains the peptide solid composition. The laxative is a separate co-administered agent.
What is the excipient-specific scope (microcrystalline cellulose and magnesium stearate)?
What carrier and lubricant embodiments are explicitly claimed?
The patent includes multiple dependent claims that specify particular excipient identities:
- Claim 11: inert low moisture carrier = microcrystalline cellulose (MCC)
- Claim 12: lubricant = magnesium stearate
- Claims 13–16: combinations of MCC and magnesium stearate, each with indication anchoring to claim 1 or claim 3.
Practical meaning:
- A product using MCC + magnesium stearate inside a closed “consisting of” solid composition has heightened alignment to dependent claim coverage.
- A product using different low-moisture carriers (e.g., low-moisture starches, mannitol grades, other diluents) could escape these dependent claims while still potentially falling within claim 1’s broader “inert low moisture carrier” language depending on how “inert” and “low moisture” are construed.
How does the purity after storage requirement interact with formulation design?
The key phrase is: “chromatographic purity of no less than 91% after storage for at least three months.”
Potential design-around hooks
Even without altering the peptide identity or “consisting of” excipient set, competitors can attempt to avoid infringement by:
- Ensuring the product’s peptide purity after 3 months is <91%, or by selecting a storage test design that yields a different measured impurity profile under the claim’s required assay conditions.
- Using formulation/processing controls to shift impurities below the measured chromatographic threshold, or conversely to ensure compliance only if the claim’s purity methodology is not met.
Enforcement focus
In litigation, this type of claim typically drives:
- Discovery into stability studies, intermediate testing, and release spec rationales.
- Expert debate on chromatographic method equivalence and the definition of “chromatographic purity” used in the patent.
Which method-of-use layers exist within this single US patent?
This patent blends multiple claim theories:
- Treatment of a disease state: chronic constipation (claim 1).
- Treatment linked to IBS/CIC association: claim 2 and claim 3 (symptom-based).
- Symptom alleviation: constipation or abdominal pain (claim 4).
- Combination regimen:
- PDE inhibitor + guanylate cyclase receptor agonist (claims 5–6 and 8–9).
- Laxative add-on (claims 7 and 10).
From an infringement standpoint, the independent claim 1 captures the core delivery + stability + peptide structure requirements, while dependent claims create layered coverage for specific add-ons.
Patent landscape beyond this US patent: how to assess breadth and likely coverage density
No additional information was provided for:
- patent family members (continuations/divisionals, counterpart PCT/EP/CN filings),
- related US patents in the same family,
- assignee name,
- FDA product(s) linked to the peptide/sequence,
- Orange Book listings,
- PTAB or district court litigation records,
- prosecution history that could limit claim interpretation.
Because the prompt is limited to the claims text for US Patent 9,919,024, a complete “landscape” across patents, jurisdictions, or FDA status cannot be produced accurately.
What can be stated from the claim set alone is that the patent’s scope strategy is formulation-anchored plus method-of-use anchored:
- Formulation: peptide structural constraint + excipient categories + closed composition.
- Quality: quantitative purity after storage.
- Use: constipation/IBS-C/CIC symptom targets.
- Combinations: cGMP-PDE inhibitors and laxatives.
This combination suggests the estate is likely built to defend against:
- obvious peptide sequence knockoffs (structural definition),
- formulation substitutions that keep the peptide but swap excipients (closed “consisting of”),
- instability-driven impurity changes (purity threshold),
- monotherapy-only products by capturing common combination strategies.
How strong is the enforceable core of US 9,919,024?
Strengths (based on claim language)
- Closed composition: “consisting of” restricts excipient additions, raising infringement leverage against non-identical formulations.
- Defined peptide architecture: “[4,12;7,15] bicycle” plus SEQ ID NO:1 is a strong identity anchor.
- Quantified stability/purity: purity after storage creates measurable, product-specific infringement triggers.
- Route-limited: “orally administering” limits scope to oral products.
Likely friction points (based on claim structure)
- If an accused product uses an oral dosage form that includes additional components inside the “composition” beyond the allowed three categories, infringement of claim 1 becomes harder.
- If an accused product’s measured chromatographic purity after 3 months is below 91%, it can be a direct non-infringement path.
- If the competitor’s peptide is outside the “[4,12;7,15] bicycle” definition (even if it retains similar pharmacology), the claim is avoided.
Key Takeaways
- US 9,919,024 is a method-of-use patent for oral treatment of chronic constipation, including IBS-C and chronic idiopathic constipation, using a SEQ ID NO:1 peptide that is a [4,12;7,15] bicycle.
- The invention is tightly tied to a closed composition: the peptide plus an inert low-moisture carrier and a lubricant, with no other components allowed within that “composition.”
- The claim includes a measurable formulation quality requirement: ≥91% chromatographic purity after ≥3 months storage.
- Dependent claims layer in:
- symptom-based coverage (constipation or abdominal pain),
- combination therapy with cGMP-dependent phosphodiesterase inhibitors (sulindac sulfone, zaprinast, motapizone) and/or laxatives,
- excipient embodiments: microcrystalline cellulose and magnesium stearate.
FAQs
1) Does the “consisting of” limit the presence of coatings or additional excipients in the oral dosage form?
The claim language limits the “composition” administered to include only the peptide, the inert low moisture carrier, and the lubricant; additional components can be a key non-infringement issue.
2) Can a competitor avoid the patent by using a different cGMP-dependent phosphodiesterase inhibitor than those named?
Claim 5 covers a cGMP-dependent phosphodiesterase inhibitor class; claim 6 narrows to named examples. Using a different inhibitor may avoid dependent-claim coverage but may still risk claim 5.
3) Is the purity requirement part of claim 1’s infringement analysis?
Yes. Claim 1 requires peptide chromatographic purity ≥91% after 3 months storage, making formulation stability and assay results central.
4) Does the patent cover only constipation, or also abdominal pain?
It covers both: constipation is explicit and abdominal pain is explicitly included in claim 4 as a symptom.
5) Are MCC and magnesium stearate mandatory for infringement?
No. They appear in dependent claims (11–16). Claim 1 uses broader excipient categories, though the excipient selection affects infringement arguments.
References
- United States Patent 9,919,024 (claim set provided in prompt).
