US Patent 11,117,902: What Is Claimed, How Broad It Is, and Where It Sits in the US Patent Landscape
United States Patent 11,117,902 claims crystalline forms of a specific chemical entity (a compound defined by a formula with R1/R2 substituents where one substituent is Cl, F, —CF3, or —CH3 and the other is H) plus pharmaceutically acceptable salts and compositions and methods for cancer treatment. The differentiator across the claim set is XRPD-defined crystal forms, including (i) a parent crystalline form defined by an XRPD peak at 2θ 19.8±0.2 and selected additional peaks and (ii) salt crystalline forms defined by XRPD peaks at 2θ 20.5±0.2 (benzenesulfonate) and 2θ 20.1±0.2 (4-methylbenzenesulfonate). The therapeutic claims cover multiple solid tumors, with added dependent claims specifying ER-positive variants for select cancers.
What exactly is the claim scope (independent vs dependent)?
Independent claims in the set
Claim 1 (core crystalline form):
- A crystalline form of “the compound of the formula” where either R1 or R2 is selected independently from Cl, F, —CF3, —CH3, and the other is hydrogen, or a pharmaceutically acceptable salt.
Claim 3 (XRPD-defined specific crystalline form):
- Depends from claim 2 (salt context), and recites an XRPD pattern with:
- a peak at 2θ = 19.8±0.2, and
- plus one or more additional peaks selected from:
- 6.8±0.2
- 16.0±0.2
- 22.1±0.2
Claim 4 (XRPD spectrum list for the benzenesulfonate? see below):
- Depends from claim 2 and recites an XRPD pattern as a table including a dominant peak at 19.8°2θ (100%) and a set of other peaks (e.g., 6.8°, 16.0°, 17.4°, 18.1°, 21.1°, 22.1°, 24.9°, 25.4°).
- In the text you provided, claims 6-10 introduce the other salts and their XRPD patterns, so claim 4 is best read as the principal XRPD fingerprint for the crystalline form of the claim-1 compound or its salts in that branch.
Claim 6 / 7 / 9 / 10 (salt-specific XRPD embodiments):
- Claim 6: XRPD with 2θ = 20.5±0.2 plus one or more additional peaks from 12.3±0.2, 22.2±0.2, 23.1±0.2.
- Claim 7: full XRPD peak list with the most intense at 20.5°2θ (100%) and other peaks including 7.6°, 10.6°, 12.3°, 12.6°, 17.7°, 19.2°, 22.2°, 23.1°, 24.2°.
- Claim 9: XRPD with 2θ = 20.1±0.2 plus one or more additional peaks from 12.8±0.2, 19.5±0.2, 22.8±0.2.
- Claim 10: full XRPD list with most intense at 20.1°2θ (100%) and other peaks including 7.6°, 12.4°, 12.8°, 18.9°, 19.5°, 20.9°, 21.8°, 22.8°, 25.4°.
Claim 11 (composition):
- A pharmaceutical composition comprising the compound or its salt from claim 1, plus a pharmaceutically acceptable excipient/carrier/diluent.
Claim 13 (method of treatment):
- A method of treating a defined set of cancers (breast, ovarian, endometrial, prostate, uterine, gastric, lung) by administering an effective amount of the compound or its salt from claim 1.
How wide is the chemical scope? (R-group and salt coverage)
R-group breadth (substituent freedom, but only at one position class)
The chemical entity in claim 1 is constrained by:
- R1 or R2 is independently selected from: Cl, F, —CF3, —CH3
- The “other” position is H
That means the claim set covers a small discrete set of substitution patterns, not a full Markush of arbitrary groups. The independent selection language indicates that both variants (e.g., substituent at R1 with H at R2 and substituent at R2 with H at R1) are within scope, but the substituent set is limited to four groups.
Salt breadth (two specific sulfonate salts + generic pharmaceutically acceptable salts)
- Claim 1 already includes “or a pharmaceutically acceptable salt thereof.”
- Claim 5 narrows to benzenesulfonic acid salt.
- Claim 8 narrows to 4-methylbenzenesulfonic acid salt.
Practical implication: even with the generic “pharmaceutically acceptable salt” language, the strongest enforcement hooks in this patent are the XRPD fingerprints recited in claims 3-4 (general crystalline form / one XRPD pattern) and in claims 6-7 and 9-10 (two specific sulfonate salts with distinct XRPD maxima).
Where the claim set draws legal boundaries: crystalline form defined by XRPD
The patent relies on crystallinity and XRPD peak positions as the exclusivity mechanism. Key boundaries:
Crystalline form XRPD fingerprint (claim branch centered on 19.8°2θ)
Claim 3 requires:
- Peak at 19.8±0.2 (2θ) plus at least one additional peak from:
- 6.8±0.2
- 16.0±0.2
- 22.1±0.2
Claim 4 recites a full peak list with:
- Most intense peak: 19.8°2θ at 100%
- Additional peaks at approx.:
- 6.8° (29.40%)
- 16.0° (20.10%)
- 17.4° (7.60%)
- 18.1° (16.00%)
- 21.1° (14.60%)
- 22.1° (28.90%)
- 24.9° (16.40%)
- 25.4° (21.90%)
Benzenesulfonate crystalline form fingerprint (claims 6-7; max at 20.5°2θ)
Claim 6 requires:
- Peak at 20.5±0.2 plus one or more additional peaks from:
- 12.3±0.2
- 22.2±0.2
- 23.1±0.2
Claim 7 recites full peak list with:
- Most intense: 20.5°2θ (100%)
- Additional peaks:
- 7.6° (27.10%)
- 10.6° (34.50%)
- 12.3° (42.10%)
- 12.6° (32.30%)
- 17.7° (32.80%)
- 19.2° (26.70%)
- 22.2° (45.50%)
- 23.1° (36.30%)
- 24.2° (29.80%)
4-methylbenzenesulfonate crystalline form fingerprint (claims 9-10; max at 20.1°2θ)
Claim 9 requires:
- Peak at 20.1±0.2 plus one or more additional peaks from:
- 12.8±0.2
- 19.5±0.2
- 22.8±0.2
Claim 10 recites full peak list with:
- Most intense: 20.1°2θ (100%)
- Additional peaks:
- 7.6° (25.70%)
- 12.4° (27.90%)
- 12.8° (36.80%)
- 18.9° (26.50%)
- 19.5° (56.90%)
- 20.9° (41.50%)
- 21.8° (40.90%)
- 22.8° (39.40%)
- 25.4° (29.70%)
Enforcement posture: To infringe claims 3-4, 6-7, or 9-10, an accused solid must match the specified crystalline form identity through the XRPD pattern. The explicit use of tight peak tolerances (±0.2°) and explicit additional-peak alternatives creates definable infringement and a clear testing protocol in practice.
How strong is the composition claim?
Claim 11 is a conventional formulation claim:
- Pharmaceutical composition containing the compound or salt from claim 1
- plus pharmaceutically acceptable excipient/carrier/diluent
Claim 12 broadens to include one or more other therapeutic agents.
Enforcement posture: composition claims often extend well beyond solid-form manufacture because they attach to dosage product composition. However, the scope still depends on the drug entity being the same “compound or salt” and, in practice, the XRPD-defined form may determine whether the marketed material reads on the claimed “crystalline form” embodiments.
How broad is the therapeutic method scope?
Core method claim (claim 13)
Cancers explicitly listed:
- breast
- ovarian
- endometrial
- prostate
- uterine
- gastric
- lung
Mechanism is not recited; the claim is “administering an effective amount of the compound or pharmaceutically acceptable salt thereof” (from claim 1).
Dependent ER-positive carveouts
- Claim 14: ER-positive breast cancer
- Claim 15: ER-positive gastric cancer
- Claim 16: ER-positive lung cancer
Scope reality: If “ER-positive” is critical for claim 14-16, those dependent claims narrow the population. The independent method claim 13 already covers breast, gastric, and lung without the ER-positive limitation, so the ER-positive language primarily adds narrower coverage.
XRPD-driven claim architecture: what it means for freedom to operate (FTO)
Three practical “design-around” routes implied by the claim set
- Use a different solid form that does not match the XRPD peaks within the recited windows.
- Use a different salt other than benzenesulfonic acid and 4-methylbenzenesulfonic acid, or a different polymorph form of those salts not matching the claimed XRPD fingerprint.
- Avoid the claimed compound substitution pattern (R-group restriction to Cl/F/CF3/CH3 with the other position as H).
Why XRPD matters
The claims are written to require:
- specific 2θ peak locations,
- specific tolerance bands (±0.2°),
- a defined intensity-based fingerprint in the “full list” claims (claims 4, 7, 10).
That gives a relatively objective infringement test, which typically intensifies the importance of analytical characterizations in disputes and licensing.
US patent landscape: how 11,117,902 likely positions against neighboring rights
No prosecution history, family members, related continuations, or citing/cited documents are provided in the input. A complete landscape requires patent-document identifiers (publication numbers, assignee, CPC classes, forward citations, and legal status). Without those, a full “who else owns what” mapping cannot be constructed from the provided text alone.
What can be concluded from the claims themselves is the likely landscape segmentation:
1) Solid-form exclusivity layer
- Crystalline form claims with XRPD patterns are typically positioned against:
- prior polymorph disclosures of the same compound,
- other salt forms (including other sulfonates),
- amorphous or hydrate forms,
- solvates.
2) Salt-specific solid-form layer
- Two sulfonate salts are explicitly claimed with distinct XRPD maxima:
- benzenesulfonate (20.5°2θ)
- 4-methylbenzenesulfonate (20.1°2θ)
3) Product/therapy layer
- The composition and method claims extend the protection from manufacturing solids to marketed drug products and therapeutic use.
Net effect: this patent is engineered to block both (i) a competitor’s crystalline form entry into the same substitution/salt territory and (ii) downstream product commercialization for the listed indications, even if the competitor tries to formulate without changing the chemical entity.
Claim-by-claim scope map (quick read)
| Claim |
What is claimed |
Key defining elements |
| 1 |
Crystalline form of formula compound (or pharmaceutically acceptable salt) |
R1 or R2 in {Cl, F, —CF3, —CH3}; other is H |
| 2 |
Crystalline form where compound is salt |
Depends on claim 1 |
| 3 |
Crystalline form salt with XRPD fingerprint |
Peak at 19.8±0.2 plus one or more from 6.8±0.2 / 16.0±0.2 / 22.1±0.2 |
| 4 |
Crystalline form salt with full XRPD list |
Dominant 19.8°2θ (100%) plus listed secondary peaks |
| 5 |
Salt identity |
Benzenesulfonic acid salt |
| 6 |
Benzenesulfonate XRPD with partial pattern |
Peak at 20.5±0.2 plus one or more of 12.3±0.2 / 22.2±0.2 / 23.1±0.2 |
| 7 |
Benzenesulfonate XRPD with full list |
Dominant 20.5°2θ (100%) plus listed peaks |
| 8 |
Salt identity |
4-methylbenzenesulfonic acid salt |
| 9 |
4-methylbenzenesulfonate XRPD with partial pattern |
Peak at 20.1±0.2 plus one or more of 12.8±0.2 / 19.5±0.2 / 22.8±0.2 |
| 10 |
4-methylbenzenesulfonate XRPD with full list |
Dominant 20.1°2θ (100%) plus listed peaks |
| 11 |
Pharmaceutical composition |
Compound/salt from claim 1 + acceptable excipient/carrier/diluent |
| 12 |
Composition with added therapies |
Adds “one or more other therapeutic agents” |
| 13 |
Method of treating listed cancers |
Administer effective amount of compound/salt from claim 1 |
| 14 |
ER-positive breast cancer |
Dependent on claim 13 |
| 15 |
ER-positive gastric cancer |
Dependent on claim 13 |
| 16 |
ER-positive lung cancer |
Dependent on claim 13 |
Key Takeaways
- Core protection is solid-form specific: the patent claims crystalline forms identified through XRPD peak positions with tight tolerances (±0.2°), including full peak lists with intensity ratios.
- Chemical breadth is constrained to a small substituent set: Cl, F, —CF3, —CH3 with the other position as H.
- Salt breadth is staged: generic “pharmaceutically acceptable salt” in claim 1, with strong, explicit XRPD embodiments for benzenesulfonate and 4-methylbenzenesulfonate.
- Downstream coverage spans product and use: composition claims and a multi-indication oncology method claim extend the asset beyond the crystalline form itself.
- Landscape mapping cannot be completed from the provided excerpt: no assignee, family, prosecution history, or citation network is included, so a true US “patent landscape” (who owns what nearby and what is invalidating) cannot be stated.
FAQs
1) Does infringement depend on the XRPD peak match?
Yes for the crystalline-form claims that recite XRPD requirements (claims 3-4, 6-7, 9-10). Those claims tie scope to specific diffraction peak locations and, in some claims, a broader peak list with relative intensities.
2) Are benzenesulfonate and 4-methylbenzenesulfonate both covered?
Yes. Claim 5/6/7 cover benzenesulfonic acid salt with XRPD max at 20.5°2θ; claim 8/9/10 cover 4-methylbenzenesulfonic acid salt with XRPD max at 20.1°2θ.
3) Can a competitor avoid by using another salt?
If the competitor uses a salt not matching the claimed XRPD-defined embodiments, it may avoid the narrower salt crystalline-form claims. Claim 1 still includes “pharmaceutically acceptable salts,” but the enforceable crystal-form scope is anchored to the XRPD patterns in the dependent claims.
4) Are the indications limited to ER-positive cancers?
No. Claim 13 covers multiple cancers without ER limitation. ER-positive versions are added via dependent claims 14-16 for breast, gastric, and lung.
5) Does the patent cover just the solid or also marketed formulations?
It covers both: claim 11 is a pharmaceutical composition claim with excipients/carriers, and claim 12 includes combinations with other therapies.
References
[1] United States Patent 11,117,902 (claim text provided in prompt).
