United States Patent 11,827,635: Scope of Claims and KRAS G12C Landscape Impacts
What does U.S. Patent 11,827,635 claim, in force-of-right terms?
U.S. Patent 11,827,635 is directed to a specific drug substance and its use in a defined pharmaceutical and method-of-treatment set.
Claim 1: substance identity + crystallinity + XRD fingerprints
Claim 1 defines a compound as:
- Crystalline, anhydrous form of the M atropisomer of a specified structure (labeled “Compound 1”) with defined substituents and stereochemistry, including:
- “M atropisomer”
- pyrido[2,3-d]pyrimidin-2(1H)-one core
- 6-fluoro and 7-(2-fluoro-6-hydroxyphenyl) substitution
- a substituted pyridine element including “4-methyl-2-(2-propanyl)-3-pyridinyl”
- a piperazine sidechain substituent containing (2S)-2-methyl-4-(2-propenoyl)-1-piperazinyl
- Characterized by XRPD (powder) with an explicit peak:
- 9.0 ± 0.2 degrees 2θ, using Cu Kα wavelength 1.54 Å
This claim is not a generic “compound class” claim. It is a formulation-limited substance claim anchored to:
1) a particular atropisomer designation (M),
2) anhydrous crystallinity, and
3) a numerical XRPD peak at a defined 2θ window.
Claims 2–7: alternative XRPD peak variants layered on the same substance scaffold
Claims 2–7 keep the same core structure definition as Claim 1 but expand “characterized by” XRPD to include additional single-peak requirements at different 2θ positions:
- Claim 2: peak at 12.0 ± 0.2° 2θ (1.54 Å)
- Claim 3: peak at 12.6 ± 0.2° 2θ (1.54 Å)
- Claim 4: peak at 12.6 ± 0.2° 2θ, depends from Claim 2 but still locks to the same XRPD peak position set
- Claim 5: peak at 19.0 ± 0.2° 2θ (1.54 Å)
- Claim 6: peak at 19.0 ± 0.2° 2θ (depends from Claim 2)
- Claim 7: peak at 19.0 ± 0.2° 2θ (depends from Claim 3)
Practical reading: the claim set is structured to cover at least multiple XRPD-anchored crystalline “variants” of the same underlying compound definition by specifying different single diagnostic peaks.
Claim 8–10: composition + tablet + 120 mg unit dose
- Claim 8: a pharmaceutical composition containing the compound of Claims 1–7 plus a pharmaceutically acceptable excipient.
- Claim 9: composition is a tablet.
- Claim 10: the tablet comprises 120 mg of the compound.
This part of the patent narrows beyond “any formulation” and creates a stronger position for solid oral dosage at a specific unit content.
Claims 11–16: method of treating KRAS G12C mutation cancers
- Claim 11: administering a therapeutically effective amount to treat cancer having a KRAS G12C mutation.
- Claim 11 tumor scope includes an extensive list across solid tumors and some hematologic categories:
- non-small cell lung cancer (NSCLC), small cell lung cancer
- small intestine, appendix
- colorectal
- endometrial
- pancreatic, pancreatic neuroendocrine tumor
- liver, bile duct
- gastric
- cervical, ovarian, germ cell tumor
- head and neck, esophageal
- bladder
- myelodysplastic/myeloproliferative neoplasms
- malignant mesothelioma
- thyroid, skin, nasal cavity
- soft tissue sarcoma
- plus others in the claim list
- Claim 12: further narrows to a subset list.
- Claim 13: narrows to NSCLC or colorectal.
- Claim 14: narrows to pancreatic or colorectal.
- Claim 15: administration to an adult.
- Claim 16: repeats dependency from Claim 13, also requiring adult.
Key scope characteristic: this is a broad therapeutic use claim centered on KRAS G12C while simultaneously specifying eligible indications (many cancer types) rather than only a single tumor.
How broad is the patent in infringement terms? (substance vs. use vs. formulation)
1) Substance scope is constrained to a crystalline anhydrous form with M-atropisomer identity
A challenger must engage all three pillars of Claim 1:
- correct compound identity (M atropisomer of the specified chemical structure),
- correct solid-state requirement (crystalline, anhydrous),
- XRPD “characterization” match (diagnostic peak at the specified 2θ window, 1.54 Å).
Implication: variants that change polymorph form, hydration state, or atropisomeric composition may fall outside if they do not present the required XRPD peak under the same measurement conditions.
2) XRPD claims 2–7 expand the “characterization” possibilities
Claims 2–7 create multiple entry points into infringement by allowing a match to different peak positions (12.0, 12.6, 19.0, in addition to the 9.0 peak in Claim 1). Under claim construction, this often supports arguments that different batches or forms that show one of the specified diagnostic peaks can still map to the “characterized by” limitation.
3) Composition scope narrows to tablet dosing and unit strength
Even if the substance is covered, Claim 8–10 require:
- pharmaceutical composition,
- tablet dosage form,
- 120 mg content per tablet (Claim 10).
Implication: generic or competitor development often screens exposure by avoiding exact strength/form content matching, though they would still face Claim 8 and Claim 11–16 if they use the claimed compound for KRAS G12C treatment.
4) Method claims are wide on indication but anchored on KRAS G12C
The method of treating is not limited to a single cancer type. It is broad across numerous tumor types, but constrained by the biological marker: KRAS G12C.
What is the practical claim hierarchy and where is the strongest “fencing”?
Claim hierarchy summary
| Claim |
Category |
Main limiting elements |
| 1 |
Drug substance |
M atropisomer + crystalline anhydrous + XRPD peak 9.0 ±0.2° 2θ (1.54 Å) |
| 2 |
Substance variant |
XRPD peak 12.0 ±0.2° 2θ (1.54 Å) |
| 3 |
Substance variant |
XRPD peak 12.6 ±0.2° 2θ (1.54 Å) |
| 4 |
Variant dependency |
XRPD peak 12.6 ±0.2° 2θ (1.54 Å) |
| 5 |
Substance variant |
XRPD peak 19.0 ±0.2° 2θ (1.54 Å) |
| 6 |
Variant dependency |
XRPD peak 19.0 ±0.2° 2θ (1.54 Å) |
| 7 |
Variant dependency |
XRPD peak 19.0 ±0.2° 2θ (1.54 Å) |
| 8 |
Composition |
composition with excipient |
| 9 |
Composition |
tablet form |
| 10 |
Composition |
tablet contains 120 mg |
| 11 |
Method of use |
KRAS G12C cancers list + administration |
| 12–14 |
Method narrowing |
subsets of tumor types |
| 15–16 |
Method narrowing |
adult patient |
Where the “fence” is strongest
- Substance fence (Claims 1–7): solid-state + atropisomer + XRPD measurement window. This is the hardest element to design around without changing the active.
- Formulation fence (Claims 8–10): tablet + exact 120 mg unit.
- Use fence (Claims 11–16): KRAS G12C treatment across many tumor indications. In practice, if a competitor uses the covered compound, they face method exposure even if their tablet strength differs, unless the infringement analysis is limited to the specific strength claims only.
What does this imply for the patent landscape around KRAS G12C covalent inhibitors and solid-form IP?
Even without the full specification details, the claim architecture indicates this patent is built as a solid-form and dosing/use hedge around a KRAS G12C small-molecule inhibitor scaffold.
Landscape impact points (business and R&D relevance)
1) Polymorph and XRPD strategy matters
- The patent uses single-peak XRPD characterizations. Competitors often respond by developing alternative polymorphs and verifying XRPD patterns under matching measurement conditions.
- If the competitor’s solid form lacks the specified peaks at the specified tolerance (±0.2°), it may avoid Claim 1–7 limitations.
2) Atropisomer control is an additional lock
- The requirement of “M atropisomer” adds a stereochemical axis for design-around or product differentiation. If a competitor uses a different atropisomeric distribution or purification approach leading to a different atropisomeric identity, it can affect infringement mapping.
3) Unit dose matters for tablet commercialization
- The explicit “120 mg tablet” (Claim 10) creates a clear commercial hook. A competitor may still be exposed under Claim 8 and Claims 11–16 if they use the same compound for KRAS G12C treatment, but Claim 10 provides a clearer, strength-specific pathway.
4) Indication breadth increases enforcement reach
- The method claims enumerate many cancer types. That reduces the need for a brand to prove indication-by-indication marker coverage within the listed set.
What is the likely scope of enforceable rights within the KRAS G12C market?
Enforceable rights by scenario
-
Scenario A: covered crystalline anhydrous M-atropisomer compound is used
- Likely falls within Claims 1–7 if XRPD matches at least one of the specified peak windows.
- If it is also made into a tablet and dosed at 120 mg, Claim 10 is implicated.
-
Scenario B: competitor uses the same active but different solid form
- Potentially outside Claims 1–7 if XRPD peaks do not match.
- If their product is still treated as “compound of Claims 1–7,” the litigation will pivot on XRPD and solid-state characterization.
-
Scenario C: competitor uses a non-anhydrous or different polymorph
- The claim specifies “crystalline anhydrous form,” which can provide a strong boundary condition if the competitor’s material is hydrated or otherwise does not meet the anhydrous crystallinity requirement.
-
Scenario D: competitor sells tablets of different mg strength
- Claim 10 likely avoids strength mismatch, but Claim 8 and Claims 11–16 can still be relevant if the compound is covered.
Key Takeaways
- U.S. Patent 11,827,635 is a solid-form and use patent: it claims a crystalline anhydrous M-atropisomer active with XRPD peak characterizations at 9.0 ±0.2°, plus 12.0 ±0.2°, 12.6 ±0.2°, and 19.0 ±0.2° (all measured at 1.54 Å).
- The substance claims (1–7) are the core enforcement lever; the XRPD and anhydrous crystallinity limitations are the primary design-around variables.
- The composition claims narrow to tablets and include a specific unit dose: 120 mg.
- The method claims cover KRAS G12C cancers across a broad, enumerated indication set, with narrowing dependent claims for NSCLC, colorectal, and pancreatic/colorectal, and an adult patient limitation.
FAQs
1) Does the patent claim a free-standing chemical structure regardless of solid form?
No. Claim 1 ties the invention to a crystalline anhydrous material and requires XRPD peak presence at defined 2θ values.
2) Are multiple XRPD peaks covered under the same overall patent?
Yes. Claims 1–7 cover different diagnostic peaks: 9.0 ±0.2°, 12.0 ±0.2°, 12.6 ±0.2°, and 19.0 ±0.2° (1.54 Å).
3) What formulation elements are required for infringement of the composition claims?
Claim 8 requires an excipient composition; Claim 9 requires a tablet; Claim 10 requires a tablet with 120 mg of the compound.
4) Is the method-of-use limited to one cancer type?
No. Claim 11 enumerates a broad list of KRAS G12C mutation cancers; dependent claims further narrow to subsets.
5) What is the most likely “design-around” axis for competitors?
The most direct is solid-state mapping: producing a material whose XRPD pattern does not show the specified peaks (or fails the anhydrous crystallinity requirement) under the claimed measurement conditions.
References
[1] United States Patent No. 11,827,635, “Crystalline anhydrous form of M atropisomer of Compound 1 and methods of use,” claim text as provided.
