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Patent landscape, scope, and claims: |
Executive summary
US Patent 10,927,117 is a crystalline-form patent with claim scope concentrated on (i) specific XRPD peak sets at defined 2θ values, (ii) a defined solid-state subtype (anhydrate), and (iii) product-by-process and thermophysical/DSC characteristics tied to those crystalline forms. Independent protection is product focused (crystalline form of “Compound 1” with an XRPD fingerprint) and is complemented by dependent claim layers that narrow to anhydrate and to additional peak patterns or substantially similar patterns to a figure. A method-of-preparation claim and a pharmaceutical composition claim extend the estate into manufacturing practice and downstream formulation. Enforcement leverage will usually hinge on whether an accused material is the same crystalline form as identified by the XRPD fingerprint (and whether the material is an anhydrate) and on whether infringement theory includes method claims (process step mapping) or composition claims (formulation containing that crystalline form).
H1: Scope and claim analysis of US Patent 10,927,117 (crystalline form of Compound 1, XRPD anhydrate, melting/DSC, and preparation methods)
What does claim 1 of US 10,927,117 protect: XRPD fingerprint crystalline form (Compound 1)
Core protection: claim 1 is a composition of matter claim directed to a crystalline form of “Compound 1” defined by a required XRPD peak pattern.
Claim 1 elements
- “A crystalline form of Compound 1”
- The crystalline form has an XRPD pattern with diffraction peaks at the following 2θ values (with tolerance):
- 14.8 ± 0.2°
- 15.6 ± 0.2°
- 16.4 ± 0.2°
- 21.4 ± 0.2°
How a court and experts typically construe this
- The claim is satisfied if the accused solid shows diffraction peaks that fall within those tolerance windows for those four target angles.
- The claim is not limited to an anhydrate at this level; it is the broader crystalline form.
- The claim does not expressly require any additional peaks beyond the listed four, unless dependent claims are asserted.
Practical infringement boundary
- If a competitor’s polymorph shows the four required peaks within tolerance, it creates direct risk even if other peaks differ.
- If a competitor uses a crystalline form that does not exhibit those peaks within tolerance, claim 1 may not be met, but dependent claims could still be relevant depending on their additional requirements.
How do dependent claims narrow the crystalline form scope (anhydrate, expanded XRPD sets, “substantially similar to FIG. 1”)
US 10,927,117 includes multiple claim layers that narrow the crystalline-form definition.
Claim 2: anhydrate limitation
Scope: “The crystalline form of claim 1, wherein the crystalline form is an anhydrate.”
This adds a water-content state limitation. For infringement, the accused material must be the anhydrate of that crystalline form.
Risk practicalities
- Anhydrate identity is often established by DSC endotherms for dehydration, loss-on-drying, or XRPD changes consistent with absence of hydrate phases.
- If a competitor uses a “hydrate” or a different desolvate form, claim 2 is avoided even if claim 1’s XRPD peaks are present.
Claim 3: additional XRPD peaks or substantially similar to FIG. 1
Claim 3 is written in a structure that creates multiple alternative XRPD definitions:
- Option (a): further comprising peaks at 2θ = 12.2 ± 0.2° and 12.9 ± 0.2°
- Option (b): further comprising peaks at 12.2 ± 0.2°, 12.9 ± 0.2°, 17.7 ± 0.2°, 18.5 ± 0.2°, and 20.7 ± 0.2°
- Option (c): “substantially similar to FIG. 1”
How this changes infringement
- Compared with claim 1, claim 3 increases the chance that a competitor’s polymorph matches only if it has the additional peak set(s) or if its overall pattern is “substantially similar” to FIG. 1.
- The “substantially similar” clause can be outcome-determinative because it captures variants that may not match every enumerated peak, depending on how similarity is evaluated. The claim language signals a tolerance for differences, but the doctrine of equivalents and prosecution history (not provided here) can heavily influence how “substantially similar” is applied.
Claim 4: melting point and/or DSC thermogram similarity
Claim 4 depends on claim 2 (anhydrate) and adds thermophysical definition via either:
- Melting point: 139 ± 2°C (onset), or
- DSC thermogram: “substantially similar to FIG. 2.”
Enforcement leverage
- If a competitor’s anhydrate has a different melting onset outside 137 to 141°C, claim 4 can be avoided unless DSC “substantially similar” is argued as satisfied.
- If an accused product fits claim 4, it provides a stronger product identity hook beyond XRPD.
What does claim 5 protect: product-by-process and specific crystallization/solvent routes
Claim 5 depends on claim 2 (anhydrate) and recites a method of preparing the crystalline form through multiple alternative preparation routes. This is a mixed product-by-process and process-step claim: it requires the steps to yield “the crystalline form of Compound 1” as recited.
Claim 5 structure: seven alternative process pathways
Each alternative is a discrete recipe differing by:
- solvent system (EtOAc, hexane, acetone, DMAc, DCM, toluene, 2-MeTHF, n-heptane),
- whether water is added,
- whether the route uses dissolving the crystalline form of claim 1 and then adding water,
- and whether solvent-switch/evaporation at room temperature in heptane is used.
The steps listed include:
a) Dissolve Compound 1 in EtOAc, add hexane, obtain crystalline form.
b) Dissolve Compound 1 in acetone or DMAc, add water, obtain crystalline form.
c) Dissolve the crystalline form of claim 1 in acetone or DMAc, add water, obtain crystalline form.
d) Dissolve Compound 1 in an organic solvent (EtOAc, DCM, toluene, or 2-MeTHF), add n-heptane, obtain crystalline form.
e) Dissolve the crystalline form of claim 1 in an organic solvent (EtOAc, DCM, toluene, or 2-MeTHF), add n-heptane, obtain crystalline form.
f) Dissolve Compound 1 in acetone or EtOAc, place solution into n-heptane, evaporate at room temperature, obtain crystalline form.
g) Dissolve the crystalline form of claim 1 in acetone or EtOAc, place into n-heptane, evaporate at room temperature, obtain crystalline form.
Infringement boundary for claim 5
- Process claims require evidence that an accused manufacturer performs one of these routes (or a route that maps onto these steps).
- Because the claim is tied to “obtaining the crystalline form,” proving infringement may require demonstrating that the process indeed yields the targeted anhydrate/crystalline form, typically using XRPD/DSC characterization of the manufactured solid.
- “Selected from” solvent recitations reduce interpretive ambiguity: each alternative is defined by enumerated solvent options.
Manufacturing/IP barriers
- If competitors crystallize using non-listed solvents or different anti-solvent systems, claim 5 may not be implicated even if they obtain the same crystalline form later.
- If competitors use the same solvent/anti-solvent/water/evaporation approach but different timing or temperature, infringement depends on whether the claim steps are strictly followed or whether “obtaining the crystalline form” and step language is construed flexibly (claim construction dependent on full claim language and specification).
What does claim 6 protect: pharmaceutical compositions containing the XRPD-defined crystalline form
Claim 6 is a formulation claim:
- “A pharmaceutical composition comprising a therapeutically effective amount of the crystalline form of claim 1”
- plus “a pharmaceutically acceptable excipient.”
Scope characteristics
- It is not limited to dosage form type (tablets, capsules, powders, granules) in the claim text provided.
- It does not limit route of administration.
- It keys off the identity of the solid: the crystalline form must match claim 1.
Infringement boundary
- If an accused drug product uses a different polymorph, it avoids claim 6.
- If it uses the claim-1 crystalline form, claim 6 can be asserted even if the downstream formulation differs widely.
How strong is the patent estate for infringement: key determinants
Product identity via XRPD
- Claim 1’s four-peak XRPD fingerprint is the primary validity/enforcement anchor.
- Dependent claims add specificity (anhydrate state, extra peaks, melting point, DSC).
Vulnerability points (where defenses commonly arise)
- Challenging whether the accused product’s XRPD pattern actually exhibits the required peaks within the stated tolerance.
- Disputing anhydrate identity for claim 2 and claim 4.
- Attacking “substantially similar” language in claim 3 (FIG. 1) and claim 4 (FIG. 2) as indefinite or as not actually met by the accused characterization.
Design-around options
- Use a different polymorph/desolvate/hydrate that lacks one or more of the claim-1 peaks within tolerance.
- Keep the same API but change crystallization conditions to drive formation of a different crystalline form.
- Avoid using the specific solvent routes in claim 5, though this does not avoid claim 1/6 if the same crystalline form is achieved.
What patents landscape questions should be answered for US 10,927,117 (Orange Book, exclusivity, and who is likely to face risk)
Not enough information is provided to complete the patent landscape. No drug name, active ingredient identity, or Orange Book listing is included. Without the “Compound 1” identity and the corresponding FDA application(s), no accurate enumeration can be made of:
- which NDA/BLA is tied to the XRPD-defined crystalline form,
- whether US 10,927,117 is listed in the FDA Orange Book (patent type: drug substance vs drug product, and expiration),
- any related continuations/divisionals or family members (US/EP/CN, etc.),
- any Paragraph IV certifications and settlement terms,
- any competitor “generic entry risk” linked to the actual marketed product.
Given the constraints, this analysis remains confined to claim scope and likely enforcement mechanics for US 10,927,117 based on the claims provided.
Claim-by-claim infringement map (what evidence usually controls each element)
| Claim |
What must be shown |
Typical evidence in disputes |
| 1 |
Accused material is the crystalline form of Compound 1 with XRPD peaks at 14.8±0.2°, 15.6±0.2°, 16.4±0.2°, 21.4±0.2° |
XRPD patterns with peak-picking, instrument conditions, and peak alignment/tolerance |
| 2 |
The claim-1 crystalline form is an anhydrate |
DSC/Loss-on-drying, XRPD phase purity, dehydration behavior |
| 3 |
Additional peaks at defined 2θ windows OR XRPD pattern substantially similar to FIG. 1 |
Expanded XRPD peak lists OR similarity metrics and visual/algorithmic comparisons to FIG. 1 |
| 4 |
Melting onset 139±2°C OR DSC thermogram substantially similar to FIG. 2 |
DSC thermograms with onset measurement or comparative DSC similarity analysis |
| 5 |
Defendant performs one of the enumerated preparation routes yielding the claim-2 crystalline form |
Manufacturing batch records, solvent/anti-solvent/water/evaporation steps, and XRPD/DSC of isolated solid |
| 6 |
Pharmaceutical composition contains therapeutically effective amount of claim-1 crystalline form + excipient |
Finished dosage product composition, solid-state characterization of API form within the product |
Key Takeaways
- US 10,927,117 is built around a crystalline-form product identity defined primarily by a four-peak XRPD fingerprint in claim 1.
- The estate tightens the protected subtype to the anhydrate (claim 2), adds additional XRPD peak sets or “substantially similar” coverage to FIG. 1 (claim 3), and ties the anhydrate to a melting-onset window or DSC similarity to FIG. 2 (claim 4).
- Claim 5 shifts the protection into manufacturing: it recites multiple enumerated solvent/water/anti-solvent and evaporation routes that produce the claimed anhydrate.
- Claim 6 is a downstream formulation claim that can capture drug products if the solid in the formulation matches the claim-1 crystalline form.
FAQs
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Can a different polymorph still infringe claim 1 if it has the same four XRPD peaks?
Yes, if the accused material shows the four required peaks within the stated 2θ tolerances, claim 1 can be met even if other peaks differ.
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What is the main difference between claim 3’s enumerated peaks and “substantially similar to FIG. 1”?
Enumerated peaks require specific 2θ hits; “substantially similar” can capture variants that may not meet every enumerated peak but match the overall pattern referenced by FIG. 1.
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How does claim 4 typically get proven in litigation?
Through DSC measurement of melting onset (139±2°C) and/or comparative DSC thermogram analysis against FIG. 2.
-
Does claim 5 protect against merely obtaining the crystalline form, even if a different process is used?
No. Claim 5 requires performing one of the enumerated preparation step recipes and yielding the targeted crystalline form.
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If an API is the correct crystalline form but the formulation is different, is claim 6 still possible?
Yes. Claim 6 focuses on the crystalline form contained in the pharmaceutical composition plus excipients, not on dosage-form design.
References
- US Patent 10,927,117 (claims as provided by user).
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