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Patent landscape, scope, and claims: |
United States Patent 10,093,654 (IDH2 Inhibitor Crystalline Forms): Scope, Claims, and Patent Landscape
What does US 10,093,654 claim in scope?
US 10,093,654 covers pharmaceutical compositions that use specific crystalline forms of a single active ingredient and, separately, methods of treating IDH2-mutant advanced hematologic malignancies by administering those compositions. The claim set is structurally built around (1) X-ray powder diffraction (XRPD) peak-defined crystals for the free base and for methanesulfonate salt, (2) route of administration limited to oral, and (3) dosage form limited to tablet, then (4) therapeutic use for IDH2-mutant advanced hematologic malignancies with AML subsetting to relapsed or primary refractory.
Core active ingredient recited throughout
All composition claims recite the same molecular entity:
2-methyl-1-[(4-[6-(trifluoromethyl)pyridin-2-yl]-6-{[2-(trifluoromethyl)pyridin-4-yl]amino}-1,3,5-triazin-2-yl)amino]propan-2-ol
Some claims further recite this compound as a methanesulfonate salt.
Crystal definition method (claim-critical)
The crystalline forms are defined exclusively by XRPD peaks at specific 2θ angles, with tolerance:
- Peak lists of 2θ values
- ±0.2° tolerance on each peak value
- Additional dependency: crystalline form “substantially similar to FIG. [number]”
This is the main infringement gate: practicing a composition outside these XRPD peak sets risks falling outside the literal claim scope.
How are the composition claims structured?
The patent includes multiple “sets” of claims that correspond to different crystalline polymorphs and salts. Each set follows the same hierarchy:
- Independent composition claim: crystalline form + pharmaceutically acceptable carrier/adjuvant + XRPD peak list
- Dependent claim: crystalline form “substantially similar to” a figure
- Dependent claim: oral administration
- Dependent claim: tablet
Composition claims (free base crystalline forms)
These are claims where the XRPD peaks correspond to the crystalline form of the free base (not methanesulfonate).
| Claim No. |
Compound form |
XRPD peaks (2θ, degrees) with ±0.2° |
| 1 |
Free base |
6.8, 10.6, 13.6, 14.2, 19.2 |
| 5 |
Free base |
8.9, 13.0, 18.9, 23.8, 28.1 |
| 9 |
Free base |
12.7, 17.1, 19.2, 23.0, 24.2 |
| 29 |
Free base |
7.2, 13.6, 18.5, 19.3, 21.9, 23.5 |
| 33 |
Free base |
6.4, 8.4, 9.8, 17.8, 19.7 |
| 37 |
Free base |
8.1, 14.1, 16.4, 17.3, 20.5, 24.1 |
Each has dependent “FIG similarity” and then oral/tablet dependencies:
- Claim 2 depends on claim 1 (FIG. 34)
- Claim 6 depends on claim 5 (FIG. 1)
- Claim 10 depends on claim 9 (FIG. 2)
- Claim 30 depends on claim 29 (FIG. 37)
- Claim 34 depends on claim 33 (FIG. 38)
- Claim 38 depends on claim 37 (FIG. 39)
Route and dosage:
- Oral administration: claims 3, 7, 11, 31, 35, 39
- Tablet: claims 4, 8, 12, 32, 36, 40
Composition claims (methanesulfonate crystalline forms)
These claims are for the crystalline form of the methanesulfonate salt and are defined by different XRPD peak lists.
| Claim No. |
Compound form |
XRPD peaks (2θ, degrees) with ±0.2° |
| 13 |
Methanesulfonate |
7.5, 9.3, 14.5, 18.8, 21.3, 24.8 |
| 17 |
Methanesulfonate |
14.1, 19.1, 21.8, 23.5, 25.7 |
| 21 |
Methanesulfonate |
9.0, 9.2, 21.9, 22.1, 24.2, 24.6 |
| 25 |
Methanesulfonate |
6.5, 19.6, 20.1, 21.6 |
Each has dependent “FIG similarity” and then oral/tablet dependencies:
- Claim 16 depends on claim 13 (FIG. 5)
- Claim 18 depends on claim 17 (FIG. 15)
- Claim 22 depends on claim 21 (FIG. 17)
- Claim 26 depends on claim 25 (FIG. 19)
Route and dosage:
- Oral administration: claims 14, 19, 23, 27
- Tablet: claims 15, 20, 24, 28
How are the therapeutic method claims limited?
The method claims are tied to the crystalline-form composition claims. The claim architecture is:
- Independent method claim: administering the composition of a referenced composition claim to treat a defined malignancy class with a specified biomarker state (mutant allele of IDH2).
- Dependent method claims: narrow the cancer type to AML and narrow the AML status to relapsed or primary refractory.
Malignancy class and biomarker requirement (method-scope limiter)
Each method claim uses the same disease template:
- Advanced hematologic malignancy selected from:
AML, MDS, CMML, myeloid sarcoma, multiple myeloma, and lymphoma
- Each malignancy is “characterized by the presence of a mutant allele of IDH2.”
Composition-to-method mapping
Each set corresponds to the relevant composition claim:
| Method claim base |
Administers composition claim(s) |
Oral/tablet requirement? |
| 41 |
claim 1 |
Not required explicitly; method references claim 1 composition |
| 44 |
claim 5 |
Not required explicitly; method references claim 5 composition |
| 47 |
claim 9 |
Not required explicitly; method references claim 9 composition |
| 50 |
claim 13 |
Not required explicitly; method references claim 13 composition |
| 53 |
claim 17 |
Not required explicitly; method references claim 17 composition |
| 56 |
claim 21 |
Not required explicitly; method references claim 21 composition |
| 59 |
claim 25 |
Not required explicitly; method references claim 25 composition |
| 62 |
claim 29 |
Not required explicitly; method references claim 29 composition |
| 65 |
claim 33 |
Not required explicitly; method references claim 33 composition |
| 68 |
claim 37 |
Not required explicitly; method references claim 37 composition |
Cancer narrowing and clinical status narrowing
All method sets include:
- Dependent claim narrowing advanced malignancy to acute myelogenous leukemia (AML)
- Another dependent narrowing AML to relapsed or primary refractory
Examples (pattern shown):
- Claim 41 (IDH2-mutant advanced malignancy) → claim 42 (AML) → claim 43 (AML relapsed or primary refractory)
- Claim 44 → claim 45 → claim 46
- Claim 47 → claim 48 → claim 49
- … continuing through claim 70
What is the practical claim scope for infringement risk?
US 10,093,654 is a crystalline-form patent: infringement risk tracks production and formulation rather than broad mechanism-of-action.
Key literal-scope anchors
- XRPD peak set match
Independent composition claims require a crystalline form defined by specific 2θ peak lists with ±0.2° tolerances.
- Compound identity is fixed
The active ingredient is fixed as the exact named IDH2 inhibitor structure (free base or methanesulfonate).
- Carrier/adjuvant presence is generic
“At least one pharmaceutically acceptable carrier or adjuvant” is broad and is unlikely to avoid infringement.
- Oral and tablet are additional claim dependencies
If a product uses an accused crystalline form but is not oral or not a tablet, that may avoid some dependent claim paths, but not necessarily the independent method claims that reference the base composition claims.
“Substantially similar to FIG.” dependency effect
Dependent claims add a second crystalline-form qualifier: “substantially similar to FIG. [n].” This typically operates as an evidentiary reinforcement of crystallinity identity, not a separate ingredient requirement.
What is the patent landscape implied by this filing strategy?
Without adding external records, the internal structure of US 10,093,654 itself indicates the landscape posture:
Defensive coverage pattern: polymorph and salt layering
The patent stacks coverage across:
- Multiple free-base crystalline forms (at least 6 distinct XRPD peak sets)
- Multiple salt crystalline forms (at least 4 distinct XRPD peak sets)
- Multiple formulation interfaces (carrier-based oral tablet in dependent claims)
- Multiple therapeutic labels within an IDH2-mutant bucket (6 malignancy categories + AML refinements)
This is the typical “cluster” approach: it reduces the design-around space by offering multiple XRPD “targets” that can cover alternative process outcomes (different crystallization conditions) and alternative solid-state presentations (polymorph and salt forms).
Design-around levers that remain inside the claims
A competitor can only avoid literal capture by altering at least one of the claim anchors:
- Use a different solid state form whose XRPD peaks are not within the recited peak lists (and not “substantially similar” to the cited figures in dependent claims).
- Use a different salt form (not methanesulfonate) if solid form is the crystallinity trigger.
- Avoid the exact administration route/dosage form if only dependent tablet/oral claims are asserted, though the method claims already target administration of the composition referenced by independent composition claims.
Claim-by-claim “what you must practice” checklist
The following shows the minimum practice requirements per claim family.
Family A: Free base crystalline forms
- To practice claim 1: formulate the named free-base compound as a crystalline form having XRPD peaks at 6.8, 10.6, 13.6, 14.2, 19.2° ±0.2°, plus carrier/adjuvant.
- To practice claim 3: do the same for claim 1 composition, with oral administration.
- To practice claim 4: do the same for claim 3 composition, with a tablet dosage form.
Repeat analogous “practice requirements” for:
- claim 5 / 7 / 8 using 8.9, 13.0, 18.9, 23.8, 28.1
- claim 9 / 11 / 12 using 12.7, 17.1, 19.2, 23.0, 24.2
- claim 29 / 31 / 32 using 7.2, 13.6, 18.5, 19.3, 21.9, 23.5
- claim 33 / 35 / 36 using 6.4, 8.4, 9.8, 17.8, 19.7
- claim 37 / 39 / 40 using 8.1, 14.1, 16.4, 17.3, 20.5, 24.1
Family B: Methanesulfonate crystalline forms
- To practice claim 13: formulate the methanesulfonate as crystalline form with XRPD peaks at 7.5, 9.3, 14.5, 18.8, 21.3, 24.8° ±0.2°, plus carrier/adjuvant.
- To practice claim 14: that composition for oral administration.
- To practice claim 15: that composition as a tablet.
Repeat for:
- claim 17 / 19 / 20 using 14.1, 19.1, 21.8, 23.5, 25.7
- claim 21 / 23 / 24 using 9.0, 9.2, 21.9, 22.1, 24.2, 24.6
- claim 25 / 27 / 28 using 6.5, 19.6, 20.1, 21.6
Therapeutic method families (administering the claimed compositions)
- To practice claim 41: administer the claim 1 composition to treat an advanced malignancy in the enumerated set that is characterized by a mutant allele of IDH2.
- To practice claim 42 / 43: narrow the treated condition to AML, and further to relapsed or primary refractory.
Repeat analogous mappings for each base composition reference:
- 44-46 (claim 5)
- 47-49 (claim 9)
- 50-52 (claim 13)
- 53-55 (claim 17)
- 56-58 (claim 21)
- 59-61 (claim 25)
- 62-64 (claim 29)
- 65-67 (claim 33)
- 68-70 (claim 37)
Key takeaways
- US 10,093,654 is a solid-state (XRPD) centered patent with coverage anchored to specific 2θ peak sets (±0.2°) for both free-base and methanesulfonate crystalline forms.
- The independent claims protect crystalline-form compositions generically with carriers/adjuvants; dependent claims add oral administration and tablet.
- The method claims are biomarker- and disease-bucket limited: advanced AML/MDS/CMML/myeloid sarcoma/multiple myeloma/lymphoma with IDH2 mutant allele, with dependent narrowing to AML relapsed or primary refractory.
- Design-around is driven primarily by whether a competitor’s solid form matches (or is “substantially similar to”) the recited XRPD peak profiles; the liquid or carrier formulation typically does not provide meaningful escape if the crystalline form is captured.
FAQs
1) Are the composition claims limited to tablets?
Yes, tablet is explicitly required only in the dependent claims (claims 4, 8, 12, 15, 20, 24, 28, 32, 36, 40). The independent composition claims (e.g., claims 1, 5, 9, 13, 17, 21, 25, 29, 33, 37) do not require tablet.
2) What is the single most important technical element to assess for infringement?
The claimed XRPD 2θ peak lists for the crystalline form (with ±0.2° tolerance) that appear in each independent composition claim.
3) Does the patent cover both the free base and a salt?
Yes. Free base crystalline forms are covered in claims 1, 5, 9, 29, 33, and 37. Methanesulfonate crystalline forms are covered in claims 13, 17, 21, and 25.
4) Does the method claim require oral dosing?
The method claims reference specific composition claims but do not repeat the “oral administration” limitation; oral is a feature of the dependent composition claims, not a stated limiter in the method claim text provided.
5) Which patient populations are explicitly covered?
Advanced hematologic malignancies including AML, MDS, CMML, myeloid sarcoma, multiple myeloma, and lymphoma, each specified as having a mutant allele of IDH2, with dependent claims narrowing to AML relapsed or primary refractory.
References
[1] United States Patent 10,093,654 (claims provided in prompt): “Pharmaceutical compositions comprising crystalline forms of 2-methyl-1-[(4-[6-(trifluoromethyl)pyridin-2-yl]-6-{[2-(trifluoromethyl)pyridin-4-yl]amino}-1,3,5-triazin-2-yl)amino]propan-2-ol and methods of treatment.”
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