US Drug Patent 9,814,722: Scope, Claim Architecture, and US Landscape
US Patent 9,814,722 (Drug method claims) is directed to treating two transplant-immunology indications using a single defined small molecule: 3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile (and pharmaceutically acceptable salts). The patent’s scope is anchored by (i) rigid chemical identity and (ii) downstream method and formulation permutations for graft versus host disease (GVHD) and allograft rejection.
What does the patent claim, in plain scope terms?
Core independent claim coverage
Patent 9,814,722 provides two independent-style claim pathways:
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Method of treatment (independent “method” claim set)
- Treat a disease selected from allograft rejection and GVHD
- Administer the defined compound (or salt)
- Independent structure begins with claim 1, with narrowing in subsequent claims.
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Method of treatment using a pharmaceutical composition (independent “composition/method” claim set)
- Treat a disease selected from allograft rejection and GVHD
- Administer a pharmaceutical composition with therapeutically effective amount of the defined compound (or salt)
- Composition sub-scope then narrows by route and dosage form (oral/tablet).
Absolute chemical identity lock
Across the claim set you provided, every operative claim requires the same active:
- 3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or pharmaceutically acceptable salt.
- Claims then optionally narrow to the (3R) stereoisomer.
This is the key determinant of infringement risk: the claims do not cover “a class of related compounds” or “substantially similar analogs.” They require the claimed chemical (or salts).
How broad is claim coverage on indications, dosing, and combinations?
Indication breadth
The patent limits use to two disease states:
There is no claim language for other immunologic endpoints (e.g., transplant vasculopathy, organ rejection broadly, autoimmune indications). Indication scope is therefore narrow at the disease level but explicit at the transplant level.
Dosing breadth
Claims provide a wide numeric dosing window in dependent claims:
- About 5 mg to about 1000 mg per administration/usage as written (claims 4 and 14).
This is operationally broad for commercial dosing formats because it covers typical oral/systemic ranges once the regimen maps into “about” and the mg relates to administered compound or salt as claimed.
Combination therapy breadth
A large portion of claim weight is on adding another therapy:
- Claims 5-12 for the GVHD branch (via claim dependency chain from claim 3)
- Claims 15-22 for the allograft rejection branch (via claim dependency chain from claim 13)
Combination therapy is not limited to one immunosuppressant; it is structured as:
- “Further comprising administering at least one additional therapeutic agent”
- The agent can be an immunosuppressant (claims 7 and 17)
- Or a steroid / corticosteroid (claims 8-12 and 18-22)
- Or specifically dexamethasone or prednisone (claims 10-12 and 20-22)
The combination is also not limited to concurrent administration:
- The therapeutic agent can be given simultaneously or sequentially (claims 6 and 16)
Route and dosage form limitations (composition claims)
The composition-based claim sub-scope narrows to:
- Oral administration (claim 25)
- Tablet form (claims 26, then indication-specific follow-ons: claims 27-30)
This creates a second infringement surface for a developer: even if a product uses non-tablet oral forms, or parenteral forms, the tablet/oral dependent claims may not read. The method claims without route/dosage-form limitations remain the broader basis.
Claim-by-claim scope map (what each claim adds or narrows)
A. Independent claim 1: Method of treating GVHD or allograft rejection
- Claim 1: Treat disease selected from allograft rejection and GVHD by administering the defined compound or salt.
Scope effect: This is the central broadest claim you provided for method use.
B. Claim 2: Stereochemical narrowing
- Claim 2: Compound is (3R) enantiomer or salt.
Scope effect: This narrows chemical identity to the (3R) stereoisomer. If a product uses racemate or other enantiomer, claim 2 may not read, but claim 1 can still read if the product includes the claimed compound definition as used in claim 1. (Your claim set indicates claim 1 uses the generic compound name without explicitly limiting to (3R), so claim 1 likely covers any embodiment using the compound as named, while claim 2 is a refinement.)
C. Claims 3-4: Indication selection and dosing band
- Claim 3: Disease is GVHD.
- Claim 4: About 5-1000 mg administered.
Scope effect: Claim 3 selects the indication; claim 4 adds a numerical dosing range.
D. Claims 5-12: Combination with immunosuppressant/steroids and specific corticosteroids (GVHD path)
- Claim 5: Further comprising at least one additional therapeutic agent.
- Claim 6: Agent administered simultaneously or sequentially.
- Claim 7: Agent is an immunosuppressant.
- Claim 8: Agent is a steroid.
- Claim 9: Agent is a corticosteroid.
- Claim 10: Corticosteroid is dexamethasone or prednisone.
- Claim 11: Corticosteroid is dexamethasone.
- Claim 12: Corticosteroid is prednisone.
Scope effect: Strong coverage for standard transplant regimens that include corticosteroids, including common agents by name.
E. Claims 13-14: Indication selection and dosing band (allograft rejection path)
- Claim 13: Disease is allograft rejection.
- Claim 14: About 5-1000 mg administered.
Scope effect: Mirrors the GVHD dosing branch for allograft rejection.
F. Claims 15-22: Combination with immunosuppressant/steroids and specific corticosteroids (allograft rejection path)
- Claim 15: Further comprising at least one additional therapeutic agent.
- Claim 16: Agent administered simultaneously or sequentially.
- Claim 17: Agent is an immunosuppressant.
- Claim 18: Agent is a steroid.
- Claim 19: Agent is a corticosteroid.
- Claim 20: Corticosteroid is dexamethasone or prednisone.
- Claim 21: Corticosteroid is dexamethasone.
- Claim 22: Corticosteroid is prednisone.
G. Claim 23: Composition-based method (composition includes compound or salt)
- Claim 23: Treat GVHD or allograft rejection by administering a pharmaceutical composition with therapeutically effective amount of the defined compound or salt.
Scope effect: Adds “composition” framing but still requires the same active ingredient and same indications.
H. Claims 24-30: Composition route/dosage form narrowing
- Claim 24: Compound is (3R) or salt.
- Claim 25: Composition is suitable for oral administration.
- Claim 26: Composition in tablet form.
- Claim 27-28: Indication-specific (GVHD and allograft rejection) for the tablet branch.
- Claim 29-30: Duplicative indication-specific dependences (still tied to claim 24/tablet/oral structure as provided).
Scope effect: Creates narrower “product form” claim capture for oral tablets using the (3R) compound.
What is the practical infringement surface? (Where claims bite hardest)
1) The drug identity gate
Any product must use the exact chemical entity as claimed (or a pharmaceutically acceptable salt). This is typically the most litigated gate because it determines whether analog “design-arounds” exist.
2) Indication gate (transplant immunology only)
A developer designing for other immunology endpoints would not automatically trigger these claims. However, most transplant clinical use in GVHD/allograft rejection includes immunosuppressants, which the claims explicitly anticipate.
3) Combination therapy gate is very permissive
Even if a developer tries to avoid independent monotherapy coverage by changing co-therapies, the combination claims already cover:
- any additional “immunosuppressant”
- or “steroids/corticosteroids”
- and specifically dexamethasone and prednisone
- with either simultaneous or sequential dosing
In practice, a large share of real-world regimens for GVHD and rejection will map onto these dependent claim patterns.
4) Oral tablets narrow scope only in the composition claims
Tablet/oral limitations apply only to the dependent composition claims (25-30). The method claims (1-22) are not constrained to oral or tablet form based on what you provided.
Patent landscape: what other patents does this likely intersect in the US?
Without the rest of the patent record (filing dates, family members, specification, related US continuations, and prosecution history), the landscape can only be mapped at a structural level based on what is claimable here.
Landscape hotspots created by this claim set
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Chemical entity patents
- The claims are specific to a defined compound name and (3R) stereoisomer.
- This typically sits on top of a broader “compound” patent family, plus salt form and synthetic routes.
-
Method-of-treatment patents for transplant immunology
- The use limitation is to GVHD and allograft rejection.
- That usually overlaps with prior art or later patents covering:
- JAK/kinase inhibitors (if mechanistically related)
- immunomodulators used post-transplant
- combinational immunosuppressive regimens
-
Combination regimens with corticosteroids
- The dependent claims named:
- These often appear in multiple patent families as “standard of care” anchors, which can create obviousness intersections if an earlier disclosure teaches the same compound in transplant settings with steroids.
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Formulation patents
- The tablet/oral dependent claims create another overlap surface:
- oral solid dosage forms
- stereochemistry-specific formulation preferences
- pharmaceutically acceptable salt formulation
How to read the landscape for freedom to operate (FTO)
A typical US FTO workflow for a compound like this looks for four overlapping layers:
| Layer |
What 9,814,722 would typically constrain |
Main design-around levers |
| API identity |
The exact compound (and salts), plus (3R) in dependent claims |
Use a non-identical chemical entity or non-covered salt/enantiomer profile |
| Indication |
GVHD and allograft rejection |
Avoid those indications (or new endpoints) |
| Regimen |
Co-therapy with immunosuppressants/steroids/corticosteroids, with dexamethasone/prednisone |
Use a combination not falling within the dependent patterns (hard because “immunosuppressant” is broad) |
| Dosage form |
Oral tablet form in dependent composition claims |
Use non-tablet oral, non-oral, or avoid the (3R)/oral tablet mapping in a composition strategy |
Scope comparisons inside the claim set
Method vs composition claims
- Claims 1-22: “administering a compound” (method-based) without explicit route/dosage form.
- Claims 23-30: “administering a pharmaceutical composition” and specifically oral/tablet in dependent claims.
Net effect: If a commercial product is oral tablets of the (3R) compound, it likely creates exposure across both method and composition claim sets. If it is a parenteral or non-tablet oral form, exposure shifts toward claims 1-22.
Indication split mirrors regimen split
- GVHD: claims 3-12
- Allograft rejection: claims 13-22
The combination logic is structurally identical across the two branches, which means an alleged “indication workaround” by changing between GVHD and allograft rejection would not remove combination coverage if the disease still fits the claim definition.
Key Takeaways
- US 9,814,722 is a transplant immunology method patent focused on GVHD and allograft rejection using one specifically named small molecule (3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile], including salts).
- The claim set is broad on combinations because it explicitly includes immunosuppressants and corticosteroids, with named agents dexamethasone and prednisone, and allows simultaneous or sequential administration.
- The claim set is broad on dosing in dependent claims via about 5 mg to about 1000 mg.
- The claim set is narrow only in formulation-dependent branches: oral and tablet appear only in the composition claims (25-30).
- Freedom-to-operate exposure in the US is most sensitive to the exact API identity, use in GVHD or allograft rejection, and co-therapy choice.
FAQs
1) Does the patent cover both GVHD and allograft rejection?
Yes. The disease is explicitly “selected from allograft rejection and graft versus host disease” in the base method/composition claims and then narrowed in dependent claims.
2) Is (3R) required for all claim coverage?
No. The (3R) restriction appears in dependent claims (2, 24) and in the composition/tablet chain. The base method claim (1) is not written as (3R)-limited in the claim text you provided.
3) Is co-administration with corticosteroids covered?
Yes. Dependent claims explicitly include corticosteroids and name dexamethasone and prednisone, with either simultaneous or sequential dosing.
4) Does the patent require oral administration?
No. Oral/tablet limitations appear only in the composition dependent claims (25-30). The broader method claims do not state a route in the claim text provided.
5) What is the dosing range in the claims you provided?
Dependent dosing is stated as about 5 to about 1000 mg (claims 4 and 14).
References
[1] US Patent 9,814,722, claims as provided by the user (claim text).
