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Patent landscape, scope, and claims: |
Executive summary
US patent 9,980,961 claims a method of activating mutant pyruvate kinase (PKR) by administering a broad structural class of small-molecule compounds of formula (I) (plus salts) with extensive substituent latitude over multiple defined fragments (notably W/X/Y/Z, D/D1, A, L, R1, and R3/Rd). Claim 24 narrows the claimed target to specific mutant PKR alleles. Dependent claims further narrow certain variables (examples include W/X/Y/Z = CH, D = NRb and D1 = bond, Rb = H/methyl/ethyl, and selected linker L such as bond or —(CRcRc)m—). Practically, this is a broad functional “method” claim anchored to a chemistry genus, with scope likely shaped most by the formula (I) variable definitions and by prosecution history related to mutant-selectivity/activation.
What is US Patent 9,980,961 (scope and claims) for mutant pyruvate kinase activation?
Direct answer: US 9,980,961 is a US method-of-treatment patent that covers activating a mutant pyruvate kinase (mutant PKR) in a subject using a compound of formula (I) (or salt). It is not a composition standalone claim; its infringement theory is administering the claimed compound(s) to treat/activate mutant PKR in vivo.
Core independent claim (Claim 1) architecture
Claim 1 is structured as:
- Purpose/biological function: “activating a mutant pyruvate kinase R in a subject…”
- Treatment act: “administering a therapeutically effective amount…”
- Drug structure: “a compound of formula (I) or a pharmaceutically acceptable salt thereof”
- High-dimensional substituent variables: the variables W, X, Y, Z, D, D1, A, L, R1, R3, Ra, Rb, Rc, Rd, n, m, h, g collectively define a chemistry genus.
Because Claim 1’s infringement depends on both administration and use against mutant PKR, the scope is typically interpreted through:
- the chemistry boundary of formula (I), and
- the match between the treated patient’s mutant PKR and the claim’s mutant activation concept (explicitly enumerated in Claim 24).
Dependent claims narrow along three axes
- Variable instantiation
- Claim 2: h = 1 and g = 1
- Claim 3: W = X = Y = Z = CH
- Claims 4–6: D = NRb, D1 = bond, Rb = H/methyl/ethyl, and specific linker options for L
- Linker and substituent constraints
- Claim 6 and 7: L limited to a set, including —(CRcRc)m—
- Claims 8–10: restrictions on R class and R1 class, plus L = —CH2— and n = 0
- Drug sub-type selection
- Claims 11–22: “selected from” and multiple “structural formula” dependencies
- Claim 24: restricts target mutant PKR types to enumerated residues.
Mutant PKR scope (Claim 24)
Claim 24 states the mutant PKR is selected from:
- G332S, G364D, T384M, R479H, R479K, R486W, R532W, R510Q, and R490W
This is a material scope limiter for “mutant PKR activation” in the dependent layer, and likely anchors infringement arguments in litigations on patient genotype.
How broad are the claims in US 9,980,961’s formula (I) genus?
Direct answer: Claim 1’s genus is broad at the formula level and only narrowed in dependent claims. The breadth comes from parallel choice sets for multiple scaffold positions, including heteroatom/heterocycle compatibility and multiple substitution patterns.
Claim 1 variable map (what each lever does)
Below is a practical scope readout of the claim’s defined variable clusters.
1) Ring/heteroatom positions: W, X, Y, Z
- Each independently CH or N
- Dependent Claim 3 sets all four to CH, signaling that the application likely disclosed specific heteroatom/aza variations and then captured them.
Claim strategy implication: Competitors can attempt to design around by changing the count/type of N atoms in the relevant positions, but only if the resulting structure falls outside formula (I)’s W/X/Y/Z definition.
2) D and D1 connectivity: bond vs NRb
- Each independently bond or NRb
- Dependent Claim 4 sets D = NRb and D1 = bond
- Dependent Claim 5 sets Rb = H, methyl, ethyl
Scope impact: These variables control an amine/amine-adjacent feature (an exocyclic/hetero-connector) that can influence binding and potency. If a competitor shifts that connectivity outside bond/NRb limits, they may avoid Claim 1.
3) A: optionally substituted aryl / optionally substituted heteroaryl
- A can be a broad aromatic/heteroaromatic head group.
Scope impact: This variable alone can cover multiple marketed/scaffold-like fragments if they are aryl/heteroaryl and optionally substituted.
4) Linker L: enumerated functional forms
L can be one of several defined structures, including:
- bond
- —C(O)—
- —(CRcRc)m—
- —OC(O)—
- —(CRcRc)m—OC(O)—
- —(CRcRc)m—C(O)—
- —NRbC(S)—
- —NRbC(O)—
Dependent Claim 7 narrows to —(CRcRc)m—; Claim 6 lists other permitted options.
Scope impact: L captures multiple linker chemistries (alkyl-like, carbonyl-containing, sulfidic/amidic variants). Design-arounds often target the exact linker family to step outside the enumerated options.
5) R1: substitutable group with 0–5 Rd substituents
- R1 is alkyl, cycloalkyl, aryl, heteroaryl, or heterocyclyl
- R1 has 0–5 occurrences of Rd
- Each Rd is selected from a broad set including halogenated and heterocycle-forming substituents (and functional groups like cyano, nitro, hydroxyl, carbonyl-containing, thio, amino/alkoxy variants), or two Rd together form an optionally substituted heterocyclyl.
Scope impact: This is a significant breadth lever. Even if R1 is constrained to particular base categories, Rd provides wide variation of peripheral functionalization.
6) R3: surface substituents or fused ring closure
- Each R3 independently halo, haloalkyl, alkyl, hydroxyl, or —ORa
- Or two adjacent R3 can cyclize with the carbon atoms to form an optionally substituted heterocyclyl.
Scope impact: This supports both substitution and ring-fusion strategies. Competitors often manage design-arounds here by removing the possibility of meeting the exact cyclization/substitution pattern.
7) Ra and Rb: small alkyl vs hetero-connectivity
- Ra: alkyl, acyl, hydroxyalkyl, haloalkyl
- Rb: hydrogen or alkyl
Dependent Claim 5 narrows Rb to H/methyl/ethyl.
8) Rc: multi-allowable substituents on repeating unit
- Rc: hydrogen, halo, alkyl, alkoxy, haloalkoxy, or two Rc together form an optionally substituted cycloalkyl.
Scope impact: Particularly relevant to L = —(CRcRc)m— where the repeating unit bears Rc substitutions.
9) Integers n, m, h, g
- n ∈ {0,1,2}
- m ∈ {1,2,3}
- h ∈ {0,1,2}
- g ∈ {0,1,2}
Dependent Claims 2 and 10 pin these in some cases:
- Claim 2: h=1, g=1
- Claim 10: L=—CH2— and n=0 (implies linker simplification and substitution position change)
Bottom line on breadth
Claim 1’s formula (I) is a substantive genus claim with:
- a large set of allowed linker chemistries,
- flexible aromatic/heteroaromatic A,
- flexible R1 scaffolds,
- wide allowable substituent families (Rd/R3/Ra/Rb/Rc),
- and multi-valued indices (n/m/h/g).
Dependent claims then carve narrower embodiments, but they do not fully negate the overall coverage of Claim 1.
What patents protect mutant pyruvate kinase activators like those claimed in US 9,980,961?
Direct answer: Based on the claim text provided, US 9,980,961 itself protects:
- the method of activating mutant PKR using a compound that matches formula (I),
- including embodiments with particular variable instantiations and mutant allele selections in dependent claims.
A “patents protect…” landscape for additional patents (family members, continuations, divisionals, related compounds, or process claims) cannot be constructed accurately from the claim snippet alone, because you did not provide:
- the patent’s full bibliographic data (publication numbers, priority, family members),
- the specification’s specific compound examples tied to the dependent “structural formula” claims,
- or any citation list from the patent’s face.
When does US 9,980,961 lose exclusivity or expire?
Direct answer: Expiration timing for US 9,980,961 depends on:
- its filing dates and priority chain,
- PTA (patent term adjustment) and any terminal disclaimer,
- and whether it is part of a term-restored regime linked to an FDA approval.
The expiration date cannot be computed from the claim text alone without the patent’s front-page data.
What is the Orange Book status of US 9,980,961?
Direct answer: Orange Book listing requires linkage to an FDA-approved drug product and associated NDA/ANDA references. The claim text does not identify the marketed product name or the approved code(s) that would tie this patent to the Orange Book. Without that, Orange Book status cannot be stated accurately.
What formulations are protected by US 9,980,961?
Direct answer: The claims are method-of-activation and are anchored to a compound of formula (I) or salt. The claim set you provided does not contain explicit formulation claim limitations (e.g., specific dosage forms, excipients, sustained-release matrices, or tablet/composition parameters). As written, protection centers on:
- the administered chemical entity within the formula (I) scope, and
- the therapeutic administration context.
If the dependent “structural formula” claims (11–23) specify particular chemical structures, those chemical entities are protected as administered in the method context.
How strong is the patent estate for activating mutant pyruvate kinase under US 9,980,961?
Direct answer: Strength here comes from two features present in Claim 1:
- A large genus defined by explicit allowable substituent and linker options.
- A functional target (“activating a mutant pyruvate kinase R”) paired with dependent mutant allele enumeration.
Main strength factors:
- Literal coverage likelihood: A product or candidate that falls inside formula (I) variable definitions can be captured directly by Claim 1, assuming the method is practiced.
- Target linkage (mutants): Claim 24’s enumerated mutants provide a clear genotype-to-method mapping, aiding enforcement that depends on mutant-selective patient targeting.
Main fragility factors:
- Genus interpretation: Broad claims with many “optionally substituted” terms can become narrowing in construction through prosecution record or specification definitions. This can reduce effective capture if competitors argue the “optionally substituted” limits are not met by their actual structure.
- Method proof: Even if a compound matches formula (I), infringement hinges on administering it in a context that satisfies the claim method (activation of mutant PKR). Litigation often turns on evidentiary proof of the method being performed.
Which companies are challenging US 9,980,961 via Paragraph IV or biosimilar pathways?
Direct answer: Not computable from the provided content. Paragraph IV challenges require Orange Book listing and notice details (e.g., from FDA or litigation dockets). Biosimilar pathways are also irrelevant here because the claims are for small molecules.
What generic entry risks exist for US 9,980,961?
Direct answer: Generic or follow-on risk depends on:
- whether a marketed product using these compounds exists,
- whether that product’s active ingredient matches formula (I),
- and whether the FDA approval is bound to this patent in the Orange Book.
No product identity or FDA linkage is provided in the prompt.
How does US 9,980,961 compare with other PK activator patents (scope, claim type, and design-around surface)?
Direct answer: Comparable assessment is not possible from the prompt alone. A comparison requires:
- additional patent claims from other PK activator families,
- the specific chemistry examples in the “structural formula” dependencies (claims 12–23),
- and the actual structures/compound names used by competitors.
Key claim scope takeaways (what to map for freedom-to-operate)
- Match the chemistry boundary first: formula (I) is the gating limitation. Every design-around must change at least one of the enumerated variable categories such that the final structure is outside W/X/Y/Z, D/D1, L, A, R1/Rd, and/or R3/Ra/Rb/Rc constraints.
- Then map the method boundary: even a covered compound must be administered to activate mutant PKR.
- If targeting enforcement leverage, focus on mutant alleles: Claim 24 lists nine PKR mutations (G332S, G364D, T384M, R479H, R479K, R486W, R532W, R510Q, R490W). If a competitor’s clinical program targets patients outside this set, that can narrow the method-to-patent alignment at the dependent layer.
Key Takeaways
- US 9,980,961 is a method-of-treatment patent covering activation of mutant pyruvate kinase R by administering a compound of formula (I) (or salt).
- Claim 1’s scope is defined by broad, explicit chemical genus options across multiple variable definitions, especially L (linker family), R1/Rd (core + substitution), and W/X/Y/Z and D/D1 (heteroatom and connectivity).
- Dependent claims narrow parameter values (e.g., W/X/Y/Z = CH, D = NRb, Rb = H/methyl/ethyl, L = —(CRcRc)m—, h=g=1, and L = —CH2— with n=0).
- Claim 24 anchors mutant targeting to nine specific PKR mutations.
- Freedom-to-operate work should treat formula (I) literal boundaries and patient mutant alignment as the two primary infringement determinants.
FAQs
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Does US 9,980,961 claim a specific marketed drug product or only a chemical genus?
It claims administration of compounds matching formula (I) or salts, not a named product in the claim text provided.
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Are linker variations (L) a main design-around target for US 9,980,961?
Yes. L is enumerated with multiple permitted families, and dependent claims further restrict L in some embodiments.
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How do dependent claims like h=1 and g=1 affect infringement risk?
They narrow specific embodiments; however, Claim 1 remains broad, so infringement can still occur without meeting the dependent parameter constraints if Claim 1’s genus is met.
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Is the mutant PKR genotype required for all claims or only Claim 24?
The independent claim requires “a mutant pyruvate kinase R,” while Claim 24 specifies which mutants; the dependent limitation is relevant to strengthening genotype-specific allegations.
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What evidence typically matters most for proving infringement of a method claim like this?
Demonstrating that the accused product’s active compound falls within formula (I) and that it was administered to activate mutant PKR in a way consistent with the claim’s method limitations.
References
- United States Patent 9,980,961 (claim text provided in prompt).
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