Scope and claim-strength analysis for US Patent 10,072,013 (method-of-treatment using (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one)
US Patent 10,072,013 claims a branded-style, drug-dispositive method-of-treatment estate built around a single stereodefined small-molecule structure (including a defined active stereoisomer) and then expands disease coverage and combination therapy breadth. Claim scope is driven primarily by (i) the identity of the administered compound or salt, (ii) the therapeutic populations enumerated (lymphoid and related myeloid/hematologic malignancies), and (iii) optional “add-on” language that allows co-administration of “at least one other anti-cancer agent.” Dependent claims add (a) the specific 4-methylbenzenesulfonate salt form and (b) additional specific tumor-type mappings.
This is not a claim set that protects a manufacturing process, device, dosing regimen schedule, or biomarker-defined subgroup on its face. The independent method claims are broad in therapeutic intent and broad in the universe of concomitant anticancer agents, which is the key legal and commercial lever for clearance and for Paragraph IV risk triage.
What does US 10,072,013 protect: method-of-treatment claims, active ingredient, and salt scope?
Answer: The patent protects methods of treating a defined list of lymphoid and selected hematologic malignancies by administering an effective amount of a specific (S)-enantiomer of a specific chromen-4-one scaffold, including “a pharmaceutically acceptable salt thereof,” with dependent claims adding coverage specifically for the 4-methylbenzenesulfonate (tosylate) salt.
Core chemical definition that controls infringement
All independent claims are anchored to the same active ingredient:
- (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one
- plus “pharmaceutically acceptable salt thereof”
The “(S)” stereochemical limitation is important for scope. Any product design that eliminates the claimed stereoisomer (e.g., racemate or different-enantiomer predominance) would still need to be evaluated claim-by-claim for whether the formulation delivers the claimed (S)-isomer in an “effective amount” under the claim language.
Salt coverage split: “any pharmaceutically acceptable salt” vs specific tosylate
- Independent claims include “pharmaceutically acceptable salt thereof” (very broad salt class language).
- Dependent claims 11-20 specifically recite:
- …4-methylbenzenesulfonate (a specific salt form)
Practical implication: The claim set simultaneously captures (i) salt-agnostic formulations (via the independent salt language) and (ii) a concrete, likely commercial candidate (tosylate) via the dependent salt claims. That makes “salt switching” a weaker design-around unless the candidate avoids both (a) the exact scaffold/stereoisomer and (b) delivery of the claimed compound as a pharmaceutically acceptable salt.
Therapeutic intent is the only functional element
The claims do not require a biomarker, line of therapy, stage, dosing interval, or duration. The functional language is “method for the treatment of … in a subject in need thereof” plus administering an “effective amount.” That is typically sufficient to sweep in clinician-directed use so long as the indication falls within the enumerated diseases.
How broad are the disease indications in US 10,072,013 claims?
Answer: The estate is built on a broad lymphoid malignancy basket in independent Claim 1, expanded further in Claim 2 to include hematopoietic tumors of myeloid lineage and multiple myeloma spectrum, and then narrowed/reshaped in Claim 3 into an even larger multi-myeloma and indolent lymphoma set. Dependent claims then map to B-cell lymphoma, T-cell lymphoma, Hodgkin’s lymphoma, and multiple myeloma, with an additional dependent layer tying the same treatment bundle to the tosylate salt.
Claim 1: lymphoid lineage plus selected lymphomas
Claim 1 covers methods for:
- lymphoid lineage
- B-cell lymphoma
- T-cell lymphoma
- Hodgkin’s lymphoma
- hairy cell lymphoma
- Burkitt’s lymphoma
The language “lymphoid lineage” is a broad umbrella that can create interpretive leverage even before reaching named lymphoma types.
Claim 2: adds myeloid tumors and multiple myeloma spectrum
Claim 2 covers:
- lymphoid lineage
- B-cell lymphoma
- T-cell lymphoma
- Hodgkin’s lymphoma
- hairy cell lymphoma
- Burkitt’s lymphoma
- hematopoietic tumors of myeloid lineage
- multiple myelomas
- smoldering multiple myeloma
- nonsecretory myeloma
- osteosclerotic myeloma
- plasma cell leukemia
- solitary plasmacytoma
- extramedullary plasmacytoma
Claim 2 is the broadest “population canvas” in your list.
Claim 3: broad multi-myeloma + multiple NHL items + WM
Claim 3 covers:
- Multiple Myeloma (MM)
- Small Lymphocytic Lymphoma (SLL)
- Indolent Non-Hodgkin's Lymphoma (I-NHL)
- mantle cell lymphoma (MCL)
- follicular lymphoma
- Waldenstrom's macroglobulinemia (WM)
- T-cell lymphoma
- B-cell lymphoma
Key scope note: Claim 3 mixes “indolent NHL” (class-level) with multiple named NHL subtypes, plus WM. This combination increases the surface area for generic challenge in method-of-use and for off-label clinician use in practice, depending on how the Orange Book and label align.
Does US 10,072,013 cover combination therapy with other anticancer agents?
Answer: Yes. Claims 4-6 extend each independent claim (1-3 respectively) by requiring that the method further comprises administering “simultaneously or sequentially” at least one other anti-cancer agent.
Combination claim mechanics
- Claim 4 depends on Claim 1 and adds co-administration of “at least one other anti-cancer agent.”
- Claim 5 depends on Claim 2 with the same addition.
- Claim 6 depends on Claim 3 with the same addition.
Legal and commercial effect: This is broad language: it does not limit the partner drug class (chemo, immunotherapy, BTK inhibitor, IMiD, anti-CD20, anti-CD38, checkpoint inhibitor, etc.). It also does not constrain the partner mechanism of action, line of therapy, or regimen sequence beyond “simultaneously or sequentially.”
From a freedom-to-operate perspective, any regimen in an enumerated indication that includes the claimed active compound and a second anticancer agent can fall into these dependent claims, even if the primary driver is monotherapy.
How does the tosylate salt (4-methylbenzenesulfonate) affect claim coverage?
Answer: Claims 11-20 are salt-specific overlays that attach the same therapeutic methods to the compound delivered as 4-methylbenzenesulfonate.
Dependent salt claims mapping
- Claims 11-16 correspond to Claims 1-6 respectively, each with the tosylate salt limitation.
- Claims 17-19 correspond to dependent disease mapping claims 7-9 respectively, each with the tosylate limitation.
- Claim 20 corresponds to Claim 10 with tosylate.
Implication for design-around
A competitor cannot avoid these dependent claims simply by using another salt if independent “pharmaceutically acceptable salt” language already covers the competitor formulation. Conversely, even if a competitor avoids tosylate, they can still infringe independent claims if they administer the same compound (as any pharmaceutically acceptable salt) for any enumerated indication.
So the tosylate claims strengthen the estate against product-specific formulations while not being the sole infringement pathway.
What is the likely infringement theory against a generic or new formulation?
Answer: The likely theory is direct method-of-treatment infringement based on prescribing/administering the claimed active compound (as a salt) for one of the enumerated malignancies, with or without another anticancer agent.
Because the claims are administration-based methods (not formulation composition claims in the strict sense), litigation often centers on:
- label and intended use
- prescribing patterns
- marketing representations
- evidence of administration for the claimed diseases
The claim set’s lack of dosing schedule and lack of biomarker conditions makes the “effective amount” standard typically easier to satisfy for clinician use in labeled indications.
What patent landscape exists beyond US 10,072,013: how should the estate be mapped?
Answer: A complete landscape requires the related patent family and all US continuations/divisionals, plus the Orange Book reference product and listed patents. Your prompt provides only the claims text and the patent number, not the bibliographic metadata (assignee, filing dates, priority dates, publication numbers, family members) and not the Orange Book listing. Without that, the full landscape cannot be produced accurately.
Accordingly, no additional landscape assertions are provided here.
When does US 10,072,013 lose exclusivity: what are the expiration drivers?
Answer: This cannot be determined from the claim text alone. Expiration depends on filing/priority dates, any patent term adjustment, and whether there are statutory or regulatory exclusivity interactions tied to the reference product.
Accordingly, no exclusivity timeline is provided here.
What is the Orange Book status of US 10,072,013 and what generic entry risks exist?
Answer: Orange Book status and generic entry risk require the FDA Reference Listed Drug (RLD), NDA/BLA number, and the list of Orange Book patents referencing US 10,072,013. Those facts are not provided.
Accordingly, no Orange Book status is provided here.
How strong is the patent estate for US 10,072,013 given claim drafting?
Answer: Strength is primarily a function of breadth and enforceability features in the claim language you provided: disease breadth, salt breadth, stereochemical anchoring, and combination co-administration breadth.
Strength factors
- Broad disease coverage: multiple lymphoma types plus multiple myeloma spectrum and WM. This increases infringement likelihood across indications.
- Broad salt coverage in independents: “pharmaceutically acceptable salt” reduces salt-formulation avoidance routes.
- Combination language is permissive: “at least one other anti-cancer agent” is not class-limited.
- No dosing regimen constraints: easier to meet “effective amount” in routine clinical practice than regimen-specific claims.
Weakness factors (relative)
- Stereochemistry and structure specificity: infringement requires the specific (S) enantiomer and the exact scaffold (or a salt delivering the claimed compound). This can support clearer invalidity arguments if prior art teaches the same (S) compound or if there are obviousness gaps in the underlying chemistry. That analysis requires the written description and file history, not provided.
- No biomarker or line-of-therapy limitation: this can be a double-edged sword. It expands coverage, but it also makes anticipation/obviousness easier to argue if prior art broadly teaches treating those malignancies with the same compound class.
Net
On face-value claim drafting, the estate is designed for high enforcement practicality: it tracks how oncology drugs are prescribed and administered rather than how they are manufactured.
Key Takeaways
- US 10,072,013 claims administration-based methods that turn on a single stereodefined small molecule scaffold, including “pharmaceutically acceptable salt” and a specific 4-methylbenzenesulfonate salt.
- The disease scope is broad across lymphoid malignancies and extends to multiple myeloma spectrum and selected myeloid lineage tumors.
- Combination coverage is wide: adding “simultaneously or sequentially at least one other anti-cancer agent” without class limits.
- The claim set lacks dosing schedule, biomarker, or regimen constraints, which increases real-world infringement probability.
- A full business-ready landscape (expiration dates, Orange Book listing, family members, Paragraph IV risks, litigation posture) cannot be produced from claim text alone.
FAQs
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Would a formulation that is not tosylate still infringe US 10,072,013?
Yes, if it delivers the same (S)-compound and falls within the enumerated treatment methods because the independents cover “pharmaceutically acceptable salts.”
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Does US 10,072,013 require monotherapy or does it include combination regimens?
It includes both. The independents cover monotherapy by administering the claimed compound; dependent Claims 4-6 add combination co-administration.
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Can US 10,072,013 be avoided by treating a malignancy not listed in Claims 1-3?
Yes, if the therapeutic use is outside the enumerated disease list, because the claims require treatment for those specific malignancies/umbrella categories.
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Does the patent claim any specific dosing schedule or treatment duration?
No. The claims require an “effective amount” but do not specify timing, dose levels, or duration.
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Is there any claim coverage for methods using different stereoisomers?
The independent claims specify the (S) enantiomer. Coverage turns on administering that stereodefined compound (or salt of that compound).
References
- United States Patent 10,072,013 (claim text provided in prompt).
