United States Patent 8,501,760: What Do the Claims Cover and How Broad Is the Patent Landscape?
US 8,501,760 claims a specific oral solid capsule composition for a single defined API: the monohydrochloride monohydrate of 4-Methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-N-[5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl]benzamide (the “therapeutic compound”). The claim set narrows scope primarily through (i) API identity and salt form, (ii) granule-in-capsule dosage form, (iii) surfactant and lubricant concentration caps, and (iv) in claim 6, a tight weight-ratio formulation with a wet granulation external phase containing water.
What is protected at claim level?
- Core product-by-formulation protection (claim 1): capsule containing granules with the defined API monohydrochloride monohydrate mixed with excipients plus specified performance excipient classes under strict concentration ceilings.
- Formulation narrowing (claims 2-4): fixes lubricant to magnesium stearate; surfactant to poloxamer and then to poloxamer 188.
- Process limitation (claim 5): adds granulation drying to yield a powder blend of granules.
- Hard “numerical” formulation capture (claim 6): fixes exact percentages for API, surfactant, diluents, disintegrant, glidant, lubricant, and water in an external phase.
This structure is typical of patents used to protect generic entry into immediate-release oral solids when the active and salt form are known: the patentee aims to block “workalike” formulations that change excipients or their levels while remaining in the same dosage form.
Claim 1: Capsule/Granule Composition Scope and Numeric Boundaries
Claim 1 recites an oral solid in capsule form comprising:
- Granule that contains:
- Therapeutic compound as the monohydrochloride salt of the named benzamide heteroaryl compound
- Specifically as a monohydrate
- In an intimate mixture with at least one pharmaceutically acceptable excipient
- The granule further contains:
- Surfactant at 0 to 1% by weight of the pharmaceutical composition
- Lubricant at a concentration that does not exceed 1% by weight of the pharmaceutical composition
What claim 1 definitively covers
- Dosage form: capsule.
- Granule architecture: granule is the internal unit, not just powder filled into capsule.
- Active form: monohydrochloride monohydrate of a single specified chemical entity.
- Excipients: “at least one” excipient in intimate mixture; not limited to specific excipient types beyond surfactant and lubricant.
- Surfactant range: inclusive 0% through 1%.
- Lubricant ceiling: <= 1%.
What claim 1 deliberately avoids
- It does not name diluents/disintegrants/glidants in the claim text of claim 1.
- It does not cap the number or identity of “at least one” other excipient besides surfactant and lubricant.
- It does not require the surfactant to be a particular chemical class (unless dependent claims apply).
Practical claim-1 risk zone for a generic formulary:
- If the generic uses the same API salt form and monohydrate, and maintains surfactant at or under 1% and lubricant at or under 1% in the final capsule composition, it stays closer to claim scope.
- If the generic exceeds 1% lubricant or exceeds 1% surfactant, it moves outside the numeric limits of claim 1 (subject to doctrine-of-equivalents analysis in litigation, which turns on claim construction).
Dependent Claims 2-4: Lock-in to Specific Excipient Identities
Claim 2
- Lubricant is magnesium stearate.
Effect on scope: claim 2 narrows claim 1 to products where lubricant is magnesium stearate. A product using a different lubricant can still fall under claim 1 if lubricant level stays <= 1%, but claim 2 will not be met.
Claim 3
Effect on scope: narrows claim 1 to poloxamer-containing formulations, excluding non-poloxamer surfactants.
Claim 4
- Poloxamer is poloxamer 188.
Effect on scope: narrows further to poloxamer 188 specifically.
Interpretation for portfolio mapping:
- A competitor can attempt to design around by using a surfactant outside poloxamer (escaping claim 3) or using a different poloxamer than 188 (escaping claim 4), while still potentially falling into claim 1 if the generic preserves the numeric surfactant and lubricant caps.
Claim 5: Process Limitation on Granulation and Drying
Claim 5 depends from claim 1 and adds:
- Therapeutic compound and excipients are combined to form granules
- The granules are further dried to form a powder blend of granules
Effect on scope:
- This clause can narrow infringement to manufacturing methods where a drying step produces a powder blend of granules prior to capsule filling.
- If the final product composition matches claim 1 but the manufacturing route differs, claim 5 can be harder to assert unless claim 5 is interpreted as a product-by-process limitation tied to the product structure created by drying.
Claim 6: Numerical Formulation Capture Including Water-Granulation External Phase
Claim 6 is the most operationally useful claim because it hard-codes a formulation. It recites:
Capsule containing a mixture of:
- 55.2% by weight of the monohydrochloride salt API monohydrate
- 0.8% by weight surfactant
- 19.6% by weight diluent
- 4% by weight disintegrant
External phase further comprising:
- 19.4% by weight diluent
- 0.5% by weight glidant
- 0.5% by weight lubricant
- and water, where water is used as a granulation liquid
What claim 6 covers with certainty
- It covers products where the capsule formulation matches the exact percentage breakdown and includes water during granulation used as granulation liquid.
- It covers the presence of an external phase with a separate diluent/glidant/lubricant makeup.
How claim 6 relates to claim 1
- Surfactant in claim 6 is 0.8%, inside claim 1’s 0 to 1% cap.
- Lubricant is 0.5%, inside claim 1’s <= 1% ceiling.
- Claim 6 therefore sits inside claim 1 for any product using those percentages. The key distinction is that claim 6 also requires a specific excipient set and a specific quantitative makeup.
Design-around logic:
- To avoid claim 6, a generic typically must materially change one or more of the specified weight percentages, the use of water as granulation liquid, or the external-phase design.
Breadth Assessment: What Does This Patent Likely Cover in Practice?
Strongest protection points
- API form is fixed: “monohydrochloride salt” and “as a monohydrate.”
- Dosage form is fixed: capsule containing granules.
- Excipients are constrained by concentration: surfactant 0-1%; lubricant <=1%.
- Some excipients are nailed down in dependents: magnesium stearate; poloxamer; poloxamer 188.
- A “numerical recipe” exists in claim 6: exact weight percentages and external phase with water as granulation liquid.
Likely weaker points
- Claim 1 uses broad phrasing for excipients: “at least one pharmaceutically acceptable excipient” and does not require specific identities besides surfactant and lubricant.
- The surfactant range in claim 1 is permissive (0 to 1%).
- If a competitor stays within claim 1’s numeric windows but changes excipient identities (except when dependent claims require poloxamer 188 or magnesium stearate), it may still remain within claim 1.
Patent Landscape: How This Claim Set Typically Sits Against Generic Competition
You provided only the claims but not the patent’s bibliographic fields (assignee, filing date, priority dates, expiration, CPC/US classification, related continuations, or listed references). Without those, a complete landscape mapping across families, continuations, and citation-based validity risk cannot be produced.
What the landscape analysis would normally include (and that you cannot infer from claim text alone)
- Whether US 8,501,760 is part of a larger formulation family with multiple continuations (common for salt form + solid state + excipient/process variants).
- Whether there are earlier patents on the API salt form and hydrate itself, which would shift the landscape from formulation patents to composition-of-matter.
- Whether there are later patents around:
- different granulation granule sizes
- alternative poloxamers or lubricants
- alternative external phase compositions
- capsule fill mass or disintegration profiles
- Whether the claims align with typical ANDA paragraph IV strategies for excipient composition patents.
Since no bibliographic data was provided, this response limits itself to scope mechanics and claim-driven competitive implications.
Actionable Competitive Implications (Formulation Strategy vs Claim Boundaries)
1) Surfactant selection and loading
- Claim 1 allows surfactant at 0 to 1%. Claim 6 uses 0.8%.
- Dependent claims require poloxamer and then poloxamer 188 (claims 3-4) if those dependents are asserted.
Net effect: switching surfactant away from poloxamer can exit claims 3-4 while still risking claim 1 if surfactant remains within 0-1%.
2) Lubricant selection and loading
- Claim 1: lubricant <= 1%.
- Claim 2: lubricant fixed to magnesium stearate.
- Claim 6: lubricant fixed to 0.5% (and paired with external phase).
Net effect: changing lubricant identity may exit claims 2, but a lubricant mass fraction exceeding 1% can be a straightforward numeric carve-out from claim 1.
3) Matching the “numerical recipe” (claim 6)
- Claim 6’s infringement likelihood rises sharply if a generic copies:
- 55.2% API monohydrochloride monohydrate
- 0.8% surfactant
- 19.6% + 19.4% diluents split between internal and external phases
- 4% disintegrant
- 0.5% glidant
- 0.5% lubricant
- water as granulation liquid
Even a small deviation from one of these percentages can avoid claim 6, but it may still fall under claim 1 unless it violates numeric constraints or depends on excipient identities.
Key Takeaways
- US 8,501,760 protects an oral capsule granule formulation of a single defined API salt form: monohydrochloride monohydrate of the specified benzamide heteroaryl compound.
- Claim 1 is the primary scope claim: surfactant 0-1% and lubricant <=1% in the capsule composition, with broad “at least one” other excipient permitted.
- Claims 2-4 narrow to magnesium stearate (lubricant) and then poloxamer 188 (surfactant), reducing design-around by excipient class and identity.
- Claim 6 is a high-value formulation claim that locks in exact weight percentages and an external phase using water as granulation liquid.
- For competitive product development, the most direct claim-1 and claim-6 avoidance levers are (i) surfactant and lubricant levels, (ii) surfactant identity, (iii) lubricant identity, and (iv) adherence to the exact formulation recipe in claim 6.
FAQs
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Does claim 1 require a specific diluent or disintegrant?
No. Claim 1 requires an intimate mixture with “at least one pharmaceutically acceptable excipient,” plus surfactant (0 to 1% by weight) and lubricant (<= 1% by weight). It does not specify diluent or disintegrant identities.
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Can a product avoid claim 4 while still falling under claim 1?
Yes. Claim 4 requires poloxamer 188. A formulation using a different surfactant could avoid claim 4 while still meeting claim 1 if it maintains surfactant within 0 to 1% and lubricant within <=1%, with the same API monohydrochloride monohydrate in capsule granules.
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What is the most exacting claim in this set for formulation copying?
Claim 6. It lists multiple exact percentages and an external phase with water used as granulation liquid.
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Does claim 5 protect a manufacturing step or only the final product?
Claim 5 adds a limitation about combining to form granules and drying to form a powder blend of granules, tying infringement to that manufacturing pathway as written (a product-by-process style limitation).
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If lubricant is magnesium stearate but at <=1%, is the formulation within claim 1?
If other claim 1 elements are met (capsule, granule, API monohydrochloride monohydrate, surfactant 0 to 1%), then lubricant identity as magnesium stearate does not remove coverage because claim 1 only requires lubricant concentration <=1% (identity is fixed in claim 2, not claim 1).
References
No sources cited because the patent number’s bibliographic record, assignee, filing/priority dates, and full patent text were not provided beyond the claim excerpts.
