US Patent 9,388,415: What Is Claimed and How Broad Is the Telomerase Inhibition Scope?
US Drug Patent 9,388,415 is directed to methods of inhibiting telomerase activity by contacting telomerase (and, in dependent claims, cells and patients) with a specific nucleoside-linked oligomer structure defined by a thiophosphoramidate (nps) linkage that connects nucleosides via a 3′-to-5′ bond. The claims are written to cover both in vitro and in vivo use, with broad dependent language capturing many cancer indications, including differentiated sub-classes of hematologic cancers.
What Is the Core Claim Construct? (Single-Structure, Multiple Contexts)
Across the independent claims (1, 2, 4), the operative element is the compound structure whose defining connection is:
- “nps” represents a thiophosphoramidate linkage
- Linkage described as: —NH—P(═O)(SH)—O—
- Connectivity described as: connects the 3′-carbon of one nucleoside to the 5′-carbon of the adjacent nucleoside
Claims then cover use in three escalating settings:
- Telomerase enzyme (Claim 1)
- Telomerase in a cell (Claim 2)
- Telomerase in a patient, via administration of a pharmaceutical composition (Claim 4)
Claim scope is therefore structure-first (the compound definition drives coverage) and route/context second (enzyme vs cell vs patient).
What Do Claims 1 and 2 Cover? (Enzyme and Cellular Inhibition)
Claim 1 (Method; telomerase enzyme)
- Inhibiting activity of a telomerase enzyme
- By contacting the telomerase enzyme with:
- A compound having the specified thiophosphoramidate-linked nucleoside structure
- Or a pharmaceutically acceptable salt
Claim 2 (Method; telomerase in a cell)
- Same compound structure requirement as Claim 1
- Adds in a cell:
- Contacting the cell with the compound
Practical scope implications
Because both Claims 1 and 2 are method claims that hinge on the presence of the same compound structure, the key infringement question is whether an accused product is a compound (or salt) that contains the claimed thiophosphoramidate (“nps”) linkage and the 3′-to-5′ adjacent nucleoside connection. Non-identical linkage chemistries or different nucleoside connectivity patterns fall outside literal scope as written.
How Broad Is the Patient/Composition Coverage? (Claim 4 and the Administering Step)
Claim 4 (Method; patient in need)
- Inhibiting telomerase activity in a patient in need thereof
- By administering a pharmaceutical composition comprising:
- The same specified compound structure (or salt)
This claim ties coverage to:
- A patient “in need” of telomerase inhibition (functional disease nexus is later restricted by dependent claims)
- An administration step of a composition containing the compound
Scope profile
Claim 4 is broader than an indication-limited formulation claim because it is not limited to a specific regimen, route, dosing schedule, or cancer type in the independent claim itself. Those limitations come through dependent claims (Claims 5 to 10).
What Indications Are Captured? (Cancer Lists and Hematologic Sub-Classes)
Dependent claims narrow the patient population to enumerated cancers.
Claim 3 (Cell type)
- Claim 2 wherein the cell is a cancer cell
Claim 5 (Patient cancer)
- Claim 4 wherein the patient has cancer
Claim 6 (Cancer list; very broad enumerated scope)
Claim 6 lists cancer categories including:
- Skin cancer
- Connective tissue cancer
- Adipose cancer
- Breast cancer
- Lung cancer
- Stomach cancer
- Pancreas cancer
- Ovary cancer
- Cervix cancer
- Uterus cancer
- Kidney cancer
- Bladder cancer
- Colon cancer
- Prostate cancer
- Central nervous system (CNS) cancer
- Retina cancer
- Hematologic cancer
Claims 7 to 10 (Additional granularity within Claim 6)
- Claim 7: cancer is lung cancer
- Claim 8: cancer is hematologic cancer
- Claim 9: hematologic cancer is myeloma, leukemia, or lymphoma
- Claim 10: cancer is breast cancer
Scope implications
The claims operate like a coverage lattice:
- Independent: telomerase inhibition by the compound structure
- Dependent: applied to cancer patients
- Further dependent: expands across many cancer types and then narrows to lung, hematologic, and breast, with hematologic sub-types.
This structure creates multiple, parallel infringement “hooks” for a single compound-family if it is used in any listed cancer type.
Scope Mapping: What Must an Accused Product Have to Land in These Claims?
A. Chemical structure requirements
To fall within Claims 1/2/4, an accused compound (or salt) must satisfy:
- A thiophosphoramidate (“nps”) linkage
- Linkage described as —NH—P(═O)(SH)—O—
- 3′-to-5′ connection between adjacent nucleosides
B. Functional use requirements
Depending on the claim:
- Claim 1: contacting telomerase enzyme
- Claim 2: contacting a cell that contains telomerase activity (expressed/functional in context)
- Claim 3: the cell is a cancer cell
- Claim 4: administering a composition to a patient in need (telomerase inhibition context)
- Claim 5: the patient has cancer
- Claims 6 to 10: patient cancer type must match the list and sub-class restrictions
C. Composition requirement
For Claim 4, the accused must be delivered as a pharmaceutical composition comprising the compound (even if the composition itself has additional excipients).
Claim Strategy and Patent Landscape Signals (From Claim Drafting Alone)
Even without the full specification text, the claim architecture signals a landscape around:
- Nucleoside conjugates/oligomers with thiophosphoramidate backbone chemistry
- Telomerase inhibition for broad oncology use
- Multiple levels of method claims (enzyme, cell, patient)
For a business or R&D risk assessment, this is a “compound-chemistry anchored” patent: most design-around efforts that attempt to avoid infringement would need to change at least one of the backbone linkage identity or adjacency connectivity described in the claims.
Where This Patent Likely Sits Relative to Typical Telomerase Inhibitor Patents
Telomerase inhibition patent families often cluster into a few categories:
- Direct telomerase inhibitors with defined small molecules
- Nucleic acid / oligonucleotide approaches including telomeric targeting
- Backbone-modified nucleoside oligomers where linkage chemistry (e.g., phosphoramidate variants) is central
US 9,388,415 is clearly in category 3, with linkage chemistry (“nps” thiophosphoramidate) and 3′-to-5′ adjacent nucleoside connection being the decisive element. That placement matters because many competitors either:
- Use different backbone linkages (e.g., phosphates, phosphonates, phosphorothioates, other amidates), or
- Use different nucleoside connectivity (e.g., different backbone geometry or different positioning of the linkage)
If those differences alter either the thiophosphoramidate linkage or the 3′-to-5′ adjacency connection terms, they reduce literal coverage.
Actionable Infringement Screening Checklist (Claim-Driven)
Use the following as a direct filter against candidate structures and label indications:
Structure screen (Claims 1/2/4)
- Does the candidate compound include the thiophosphoramidate (“nps”) linkage described as —NH—P(═O)(SH)—O—?
- Does it connect adjacent nucleosides via 3′-carbon of one to 5′-carbon of the adjacent?
If either answer is “no,” the candidate is outside the literal scope of the provided claims.
Use/setting screen (Claims 1 to 10)
- Is it used to contact telomerase (enzyme or cell context)?
- Is it administered to cancer patients (Claim 5)?
- If the product is targeted to a specific indication, does the indication match any of:
- Lung cancer (Claim 7)
- Hematologic cancer (Claim 8)
- Myeloma/leukemia/lymphoma (Claim 9)
- Breast cancer (Claim 10)
- Any listed cancer in Claim 6 (wide set)
Composition screen (Claim 4)
- Is there a pharmaceutical composition that comprises the claimed compound for patient administration?
Key Takeaways
- US 9,388,415 claims telomerase inhibition driven by a specific nucleoside linkage chemistry: thiophosphoramidate (“nps”) with —NH—P(═O)(SH)—O— connecting adjacent nucleosides via 3′-to-5′ connectivity.
- Coverage spans enzyme (Claim 1), cell (Claim 2), and patient administration via a pharmaceutical composition (Claim 4).
- Indication scope is broad through dependent claims, listing many cancer types (Claim 6) and narrowing to lung cancer, hematologic cancer (with myeloma/leukemia/lymphoma), and breast cancer (Claims 7, 8, 9, 10).
- For competitive strategy, the highest-leverage design-around lever is the backbone/connection definition because each independent claim is anchored to that structure; changing linkage identity or adjacency connectivity is the most direct way to avoid literal coverage.
- For regulatory and launch planning, the largest practical exposure is that a single compound-family meeting the structure definition can map to multiple oncology indications in the dependent claim chain.
FAQs
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Is the patent limited to a single cancer indication?
No. Claim 6 enumerates many cancer types, and additional dependent claims target lung, hematologic (with myeloma/leukemia/lymphoma), and breast.
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What is the decisive element for infringement risk: indication or chemistry?
Chemistry. Claims 1, 2, and 4 all require the specific nucleoside linkage defined by the thiophosphoramidate (“nps”) description and 3′-to-5′ nucleoside adjacency connection.
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Does the patent cover both enzyme-level and clinical-level use?
Yes. Claim 1 covers contacting telomerase enzyme; Claim 2 covers contacting cells; Claim 4 covers administering a pharmaceutical composition to a patient.
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If an accused compound differs in linkage chemistry but still inhibits telomerase, is it within the literal claims?
The provided claim language requires the specific thiophosphoramidate (“nps”) linkage and described connectivity, so a different linkage chemistry would not satisfy the claim’s structural limitation.
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Do the dependent claims broaden or narrow the patient scope?
They narrow. They restrict the patient and cell populations by requiring the presence of cancer and specifying which cancer types apply.
References
[1] United States Patent No. 9,388,415. “Method of inhibiting the activity of a telomerase enzyme” (claims as provided).
