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Patent landscape, scope, and claims: |
US Patent 10,961,250: Scope of Claims, Coverage Limits, and US Patent Landscape for a Besylate Salt Composition (Dextrose/Saline) and Sedation Methods
US Drug Patent 10,961,250 claims a pharmaceutical composition and sedation method built around a specific chemical form: a besylate salt of a “compound of formula (I),” formulated as aqueous solutions with dextrose or saline, including lyophilized-to-aqueous embodiments. The patent’s practical scope is narrow on formulation identity (besylate salt + aqueous dextrose/saline + optionally lyophilized precursor) and broad on intended use (sedation).
Claim-set in brief (what is actually protected)
- Composition claims (claims 1–7) cover:
- Aqueous solution containing a besylate salt of formula (I) + carriers/excipients and dextrose or saline.
- Specific sub-embodiments where the aqueous solution is saline (claim 2) or dextrose (claim 3).
- Lyophilized composition containing the besylate salt + dextrose or saline (claim 4).
- Reconstituted aqueous composition made from the lyophilized composition (claims 5–7), again split into saline (6) or dextrose (7).
- Method claim (claims 8–10) covers:
- Sedation by administering an effective amount of the same besylate salt aqueous dextrose/saline compositions.
- Again split into saline vs dextrose aqueous solutions (9–10).
This claim structure indicates the inventor positions the patent around salt form + delivery vehicle rather than around the active molecule alone or around a single dosing regimen.
What patents protect a besylate salt pharmaceutical composition in dextrose or saline aqueous solution (and lyophilized forms)?
US 10,961,250 is directly targeted at:
- Salt identity: “besylate salt of the compound of formula (I).”
- Formulation medium: aqueous solution comprising dextrose or saline.
- Solid-to-liquid platform: lyophilized composition with dextrose or saline, then aqueous composition from that lyophilized product.
How the claim language constrains design-around
The protective hook is not merely “aqueous solution.” It is aqueous solution comprising dextrose or saline with the active present as a besylate salt.
Key constraints implied by the text:
- If a competitor uses a different counterion (e.g., hydrochloride, maleate, acetate), the claim language as written does not read onto it.
- If a competitor uses an aqueous solution but neither dextrose nor saline is present (e.g., phosphate buffer, mannitol-based vehicles, lactated Ringer’s only, etc.), the claim text may avoid literal coverage.
- If a competitor uses a lyophilized product but the lyophilization formulation does not include dextrose or saline as recited in the claim, that can also create a non-infringing route.
Claim coverage summary table
| Claim |
Coverage type |
Required elements (from claim text) |
Vehicle constraints |
Key vulnerability for generics/competitors |
| 1 |
Composition |
Besylate salt of formula (I) + pharmaceutically acceptable carrier + aqueous solution |
Must be dextrose or saline |
Counterion or vehicle swap avoids |
| 2 |
Composition |
Same as claim 1 |
Must be saline |
Uses dextrose-only avoids |
| 3 |
Composition |
Same as claim 1 |
Must be dextrose |
Uses saline-only avoids |
| 4 |
Lyophilized composition |
Besylate salt of formula (I) + carriers + dextrose or saline |
Lyophilized includes recited vehicle |
Vehicle formulation change avoids |
| 5 |
Reconstituted aqueous composition |
Aqueous composition comprising lyophilized composition of claim 4 |
Inherits dextrose/saline requirement |
Changing lyophilized composition avoids |
| 6 |
Reconstituted saline sub-case |
Same as claim 5 |
Must be saline |
Dextrose-only avoids |
| 7 |
Reconstituted dextrose sub-case |
Same as claim 5 |
Must be dextrose |
Saline-only avoids |
| 8 |
Method of use |
Administer effective amount of composition from claim 1 |
Aqueous solution must be dextrose or saline |
Use different vehicle or avoid “sedation” indication |
| 9 |
Method sub-case |
Same as claim 8 |
saline |
Dextrose route avoids |
| 10 |
Method sub-case |
Same as claim 8 |
dextrose |
Saline route avoids |
Does US 10,961,250 cover lyophilized-to-injection products, and what are the practical “form” boundaries?
Yes. Claims 4–7 build a two-stage coverage chain:
- Stage 1: a lyophilized formulation that includes the besylate salt plus dextrose or saline.
- Stage 2: an aqueous pharmaceutical composition comprising that lyophilized composition.
How boundary conditions typically matter for enforcement
The claims appear to treat the lyophilized product as the defined source, then require the aqueous composition to comprise the lyophilized composition. In disputes, enforcement usually targets:
- Whether the marketed product is truly lyophilized (vs spray-dried, freeze-dried with different handling, etc.).
- Whether the lyophilized cake contains dextrose or saline in the sense recited.
- Whether reconstitution yields an aqueous solution meeting claims 5–7.
Likely claim interpretation themes
- The formulation is defined by vehicle class (dextrose or saline), not by specific concentrations in your excerpt.
- The salt form is defined by “besylate salt.” That typically pushes analysis toward solid form chemistry (counterion identity, salt stability) rather than excipient selection alone.
What is the scope of the “sedation” method claim, and does route or indication matter?
Claims 8–10 cover a method of producing sedation by administering an effective amount of the claimed composition.
What the text does not specify (in your excerpt):
- No explicit route (IV, IM, SC, oral).
- No dosage schedule or titration scheme.
- No patient population or setting.
This means the claim is likely to be interpreted based on the composition (aqueous dextrose/saline, besylate salt) plus the intended physiological effect (“sedation”).
Practical implications for design-around
- A competitor changing the composition may avoid literal coverage, even if they still achieve sedation using a different formulation medium or a non-besylate salt.
- A competitor keeping the exact composition but changing the claimed effect may raise factual and claim construction issues. Still, for method-of-use claims tied to sedation, the marketed or labeled use is often the enforcement trigger.
Which compound is “compound of formula (I)” in US 10,961,250, and how does that affect claim scope?
Your excerpt includes formula (I) but does not identify the compound name. Without the formula definition or the specification’s identification of formula (I), it is not possible to map the “besylate salt of compound of formula (I)” to a concrete active pharmaceutical ingredient.
Because the scope is defined by “besylate salt of the compound of formula (I),” the entire claim set is chemically tethered. Without identifying the compound, it is not possible to:
- enumerate other patents in the same chemical family,
- assess whether overlapping estates exist (e.g., polymorphs, other salts, prodrugs),
- evaluate likely competitor products or generic candidates.
Per the constraints, this analysis therefore focuses on claim architecture and landscape logic driven by your claim text, not on drug-specific competitor mapping.
How many other US patents likely overlap US 10,961,250 for besylate-salt aqueous dextrose/saline formulations?
A composition anchored on:
- a specific salt form (besylate),
- a specific vehicle class (dextrose/saline),
- and a solid-state platform (lyophilized-to-aqueous),
typically coexists with satellite patent families in one or more of these buckets:
- other salt forms of the same API,
- lyophilization process and cake composition,
- reconstitution and storage stability,
- use claims tied to sedation or anesthesia.
However, without the patent’s bibliographic data (title, assignee, priority, specification disclosures) and without an external patent database lookup, the number and identity of overlapping US patents cannot be asserted accurately.
When does US 10,961,250 lose exclusivity, and how does that interact with Paragraph IV and Hatch-Waxman?
Timing and exclusivity cannot be determined from claim text alone. Patent expiration depends on:
- earliest priority date,
- filing and patent term adjustments,
- PTA/PTE,
- terminal disclaimers,
- and any regulatory exclusivities impacting Orange Book listing (if present).
No Orange Book listing or FDA exclusivity information is provided in your prompt, so expiration and exclusivity interaction cannot be stated.
What is the Orange Book status of US 10,961,250, and which generic routes face the highest risk?
Orange Book status is not derivable from claims alone. The Orange Book listing typically requires:
- linkage of the patent to a specific NDA/ANDA,
- assignment of patent type (drug substance vs drug product vs method of use),
- and the listed dosage forms.
Because your excerpt does not include the NDA/ANDA number, product name, or listing details, the Orange Book status cannot be provided.
What patent litigation could be triggered by formulation substitutions (dextrose vs saline; lyophilized vs aqueous)?
Given the claim’s explicit vehicle discrimination, litigation risk concentrates on:
- whether a competitor’s product uses the besylate salt (counterion swap is a primary design-around),
- whether the aqueous vehicle includes dextrose or saline (vehicle class swap is another primary design-around),
- whether a competitor’s product is properly characterized as lyophilized with the claimed vehicle inclusion (for claims 4–7),
- and whether a method claim aligns with actual administration to produce sedation.
In disputes, claim charts usually pivot on analytical testing:
- salt identity (counterion confirmation),
- formulation composition (presence of dextrose vs saline),
- physical form classification (lyophilized process evidence),
- and use context (clinical protocol, labeling, or actual administration).
How does US 10,961,250 compare with typical besylate-salt formulation patents for injectable sedatives?
From the claim set structure alone, US 10,961,250 follows a common formulation IP pattern:
- Drug substance form: specific salt (besylate).
- Drug product vehicle: dextrose or saline aqueous solution.
- Solid-state extension: lyophilized composition.
- Use: sedation.
Compared with broader formulation patents, this one is:
- more constrained on vehicle (dextrose/saline only, per the literal text),
- and more constrained on solid-state (lyophilized is explicitly claimed).
Compared with patents that only claim the API salt itself, it adds:
- formulation constraints and a reconstitution pathway,
- and a medical method.
That combination raises the likelihood that generic challengers must change at least one of salt identity or vehicle medium or both.
Which geographic jurisdictions does US 10,961,250 cover, and what does that mean for cross-border licensing?
US 10,961,250 covers patent rights within the United States (subject to the usual enforcement reach for US patents). Cross-border protection depends on corresponding family members filed in other jurisdictions. Your prompt does not provide the family or country filings, so international coverage cannot be enumerated.
What generic entry risks exist for a besylate salt sedation product with dextrose/saline aqueous formulation?
The risk profile for a generic or follow-on formulation is driven by the claim elements:
- If a generic uses the same besylate salt and matches the aqueous dextrose/saline formulation, it risks direct infringement of claims 1–3 and 8–10.
- If it changes to saline vs dextrose, it may still fall within claim 1 or the method claim 8 unless it eliminates both dextrose and saline.
- If it sells a lyophilized product that includes dextrose or saline in the lyophilized composition and is used to produce an aqueous solution matching claims 5–7, it risks coverage across the lyophilized and reconstituted claims.
The most direct route to reduce risk is to change at least one required element:
- counterion (not besylate),
- aqueous vehicle class (not dextrose or saline),
- or solid-state/vehicle composition so that claims 4–7 are not met.
Key Takeaways
- US 10,961,250 claims besylate-salt-based pharmaceutical compositions of a “compound of formula (I)” in aqueous dextrose or saline, with an explicit lyophilized-to-aqueous chain.
- The strongest practical coverage is in products that are chemically besylate and formulated as dextrose or saline solutions, including reconstituted formats from a lyophilized drug product.
- The method claims cover sedation via administration of the same formulation types; the claim text does not limit route, dose, or patient group in your excerpt.
- Design-around leverage is highest through counterion change and/or vehicle change away from dextrose/saline; avoiding lyophilized claimed compositions can also reduce exposure for claims 4–7.
FAQs
-
Can a different counterion than besylate avoid infringement of US 10,961,250?
Changing from a besylate salt to a different counterion typically avoids claims requiring “besylate salt,” including method claims tied to the besylate composition.
-
If a product swaps from saline to dextrose, does it still infringe?
If it still contains a besylate salt of formula (I) in an aqueous solution with dextrose or saline, claim 1 and the corresponding method claim 8 can still read onto it.
-
Does US 10,961,250 cover only aqueous solutions, or also lyophilized products?
It covers both: a lyophilized composition (claim 4) and an aqueous composition comprising that lyophilized composition (claims 5–7).
-
Is the sedation method claim limited to a specific route of administration?
Your excerpt does not specify route, so coverage depends on claim construction and the composition being administered; route is not facially constrained by the claim language provided.
-
What formulation changes create the lowest infringement risk under these claims?
The lowest risk comes from changing at least one required element: using a non-besylate salt and/or using an aqueous vehicle that is not dextrose and not saline, and avoiding the claimed lyophilized composition pathway where relevant.
References
- US Patent 10,961,250 (claims provided in prompt).
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