Patent: 10,471,140

Summary for Patent: 10,471,140

Title:	Composition for enhancing induction of humoral immunity, and vaccine pharmaceutical composition
Abstract:	The present invention aims to provide a composition for promoting humoral immunity induction and a vaccine pharmaceutical composition that can be universally used for various antigens in inducing humoral immunity to antigens, contain a Th2 reaction promoter, and exerts a high humoral immunity inducing effect. The present invention relates to a vaccine pharmaceutical composition containing an antigen for humoral immunity induction and at least one Th2 reaction promoter.
Inventor(s):	Shishido; Takuya (Osaka, JP), Asari; Daisuke (Osaka, JP), Matsushita; Kyohei (Osaka, JP), Hori; Mitsuhiko (Osaka, JP)
Assignee:	NOTTO DENKO CORPORATION (Osaka, JP)
Application Number:	16/388,266
Patent Claims:	see list of patent claims

United States Patent 10,471,140: Claim Critique and US Patent Landscape for Gi- and Gq-GPCR Antagonist–Based Antigen Compositions

What does US 10,471,140 actually claim?

US 10,471,140 claims a pharmaceutical composition that combines (i) an antigen and (ii) a G protein-coupled receptor ligand that is at least one selected from: a Gi-coupled GPCR antagonist and a Gq-coupled GPCR antagonist. The independent claim sets the core combination; dependent claims constrain administration routes and antagonist receptor classes.

Claim set provided (verbatim meaning preserved)

Claim 1 (core):
A pharmaceutical composition comprising:

• an antigen; and
• a G protein-coupled receptor ligand that is at least one selected from:
  • an antagonist for a Gi-coupled GPCR and
  • an antagonist for a Gq-coupled GPCR.

Claim 2 (administration location):
Configured to be administered to a body surface.

Claim 3 (administration route):
Configured for intradermal injection, subcutaneous injection, or intramuscular injection.

Claim 4 (antagonist class examples):
Antagonist is selected from:

• adrenergic receptor antagonist
• muscarinic receptor antagonist
• dopamine receptor antagonist
• histamine receptor antagonist
• serotonin receptor antagonist
• PAF receptor antagonist
• purine receptor antagonist
• vasopressin receptor antagonist
• opioid receptor antagonist
• leukotriene receptor antagonist
• angiotensin receptor antagonist.

Claim architecture and what it implies

The claim is structured as a combination claim: antigen + GPCR antagonist(s). It does not claim a specific antigen, dose, formulation excipients, mechanism-by-proving, or a target disease. It also does not require any particular number of GPCR antagonists beyond “at least one” from the Gi and Gq antagonist categories.

That construction creates a broad scope but also concentrates risk: infringement depends on whether the accused product contains an antigen and includes at least one Gi-coupled GPCR antagonist and/or Gq-coupled GPCR antagonist, within the definitional boundaries of the receptor coupling classification.

How broad are the independent claims, practically?

Claim 1 is broad along four axes:

1. Antigen breadth: Any antigen can fall inside the claim, including proteins, peptides, nucleic acids encoding antigens, or fragments, depending on how “antigen” is interpreted in the patent. The claim language you provided does not limit antigen type.
2. GPCR antagonist breadth: It covers “antagonist for Gi-coupled” and “antagonist for Gq-coupled” GPCRs. Many marketed receptor antagonists map to these coupling states, so the category is wide.
3. Combination flexibility: The ligand is “at least one selected from” the two antagonist categories. This wording can cover:
   • a composition containing only a Gi antagonist, or
   • only a Gq antagonist, or
   • both, depending on the patent’s construction of “at least one selected from.”
4. Administration not in Claim 1: Routes and location appear in dependent claims, allowing Claim 1 to be asserted beyond the specific injection routes if the formulation is administered “as a pharmaceutical composition” with the antigen and antagonist categories.

Claim 4 further broadens receptor coverage by listing many receptor classes. Even if any given listed receptor is debated for exact coupling (Gi vs Gq), the claim’s receptor-class list increases the odds that many prior arts and product formulations will be argued to fall within scope.

What are the main patentability pressure points for Claim 1?

The central question for validity is whether prior art already disclosed antigen + GPCR antagonist(s) compositions or vaccination/adjuvant strategies that pair antigens with antagonists targeting Gi/Gq GPCR pathways.

1) Antigen + “antagonist” combination is the key novelty battleground

Because Claim 1 only requires:

• an antigen
• plus at least one Gi-coupled GPCR antagonist and/or Gq-coupled GPCR antagonist

it is vulnerable to obviousness if prior art shows:

• use of GPCR ligands or receptor antagonists as immunomodulators or vaccine adjuvants; and
• use of combinations of immune modulators with antigens.

If a prior art reference teaches GPCR antagonist-mediated immune modulation in the presence of an antigen, the remaining argument is often whether it explicitly or implicitly identifies Gi-coupled vs Gq-coupled GPCR antagonists, and whether a person of ordinary skill would have combined them.

2) “Gi-coupled” and “Gq-coupled” classifications can be attacked as taught rather than invented

Coupling of GPCRs to Gi or Gq is a known pharmacology dimension. If prior art references characterize particular receptor antagonists as acting through Gi or Gq pathways to modulate immune cell signaling, then mapping those agents into the claim’s categories becomes an obvious step.

3) Claim 1’s “at least one selected from” phrasing increases anticipation risk

In many claim constructions, “at least one of A and B” language can be interpreted broadly depending on the exact written patent claims. If a prior art composition contains:

• only a Gi-coupled GPCR antagonist with an antigen, that can be argued to satisfy Claim 1 if the claim is interpreted to allow “at least one selected from” to mean “at least one of the listed ligand types,” rather than “at least one from each category.”

That construction risk cuts both ways: it can broaden infringement and broaden invalidity attack.

4) Dependent claims can be anticipated in combination or by route-specific vaccine disclosures

• Claim 2 (body surface administration) is a common vaccination framing.
• Claim 3 (intradermal, subcutaneous, intramuscular injection) is standard for many vaccine products. If any single prior art discloses a vaccine composition using the same or overlapping antagonist categories for immune modulation, the administration constraints may not rescue patentability.

5) Claim 4’s receptor list helps scope, but also helps prior art mapping

Claim 4 identifies multiple receptor antagonist classes. This makes it easier for an examiner or challenger to cite prior art that uses common antagonists:

• adrenergic antagonists
• muscarinic antagonists
• H1 antihistamines (histamine receptor antagonists)
• 5-HT receptor antagonists
• dopamine receptor antagonists
• leukotriene receptor antagonists
• angiotensin receptor antagonists
• opioid receptor antagonists
• vasopressin receptor antagonists
• PAF receptor antagonists
• purine receptor antagonists

Even if the prior art does not say “Gi-coupled” or “Gq-coupled,” challengers can use pharmacology to map each receptor to the coupling family. If that mapping is supported in conventional references, Claim 4 can be attacked as an obvious aggregation.

How does the dependent claim set change infringement and validity exposure?

Claim 2: “administered to a body surface”

This can be satisfied by topical or transcutaneous delivery approaches. However, Claim 3 already narrows to injection routes. If a product is only injectable, Claim 2 might not be met depending on construction of “body surface” versus injection into tissue.

From a business perspective, Claim 2 is less likely to be a limiting hook than Claim 3. It is more likely to be used tactically in enforcement where delivery is topical or where the specification broadens “body surface” to include injection at/near the surface.

Claim 3: intradermal/subcutaneous/intramuscular injection

This is the most operational limitation. Many commercial vaccines and immune modulators use these routes. If Claim 1 is met, Claim 3 can often be met by routine administration, so it is not a strong differentiator unless the prior art is tied to non-injection routes.

Claim 4: receptor class selection

Claim 4 can be both:

• a scope-limiting narrowing (helps novelty if the key antagonist class was not known for vaccine modulation), and
• a scope-expanding risk (helps mapping prior art by listing many receptor families).

If the antagonist used by an accused product is among these listed receptor classes and is a known antagonist, Claim 4 may become a straightforward infringement hook. It also makes invalidity easier for a challenger.

What is the likely technical theory underlying the claim?

The claims suggest a vaccine-adjuvant or immune-modulatory concept built on GPCR signaling modulation:

• Antagonizing Gi-coupled GPCR signaling and Gq-coupled GPCR signaling in the context of delivering an antigen.
• The chosen receptor classes in Claim 4 align with immune-relevant signaling pathways (inflammatory mediators and neurotransmitter/peptide receptor systems also participate in immune cell regulation).

Because the provided claims do not state mechanism, the theory becomes secondary in validity. The prior art landscape will focus on whether any earlier document teaches using GPCR antagonists with antigens to modulate immune responses.

What does this mean for the US patent landscape?

A proper landscape requires a set of citations, priority families, and claim charting against known vaccine adjuvants and immunomodulators that use GPCR-targeting antagonists. However, your input provides only the claim text, not:

• the patent bibliographic data,
• publication numbers or priority dates,
• the specification’s described embodiments,
• prosecution history, or
• related family members.

Under these constraints, an accurate, citation-backed landscape cannot be produced without risking fabricated mapping to specific US applications or patents.

Where will challengers focus their invalidity arguments?

Even without additional record data, the claim language dictates standard attack vectors:

1. Antigen + immunomodulatory drug combinations: prior art that discloses antigen compositions combined with agents that modulate immune cell activation.
2. GPCR antagonists as immunomodulators/adjuvants: any disclosure tying receptor antagonism to immune response enhancement or suppression in vaccination contexts.
3. Pharmacological mapping to Gi/Gq: use of standard GPCR coupling references to argue that the disclosed antagonists are Gi- or Gq-coupled.
4. Combination obviousness: if separate references show antigen-administration and GPCR antagonist-driven immune modulation, challengers argue routine combination.
5. Anticipation by broad genus disclosures: Claim 4’s receptor list increases the probability that prior art discloses at least one listed antagonist class used in similar compositions.

Where will enforceability issues arise for potential licensees or competitors?

Competitors can design around by targeting one missing element:

• Exclude “antigen” (for example, use carrier-only or non-antigen constructs if claim construction is strict).
• Use GPCR agonists instead of antagonists.
• Target GPCRs coupled to pathways other than Gi and Gq (or avoid those categories).
• Use non-injection routes where Claim 3 is asserted, while still delivering a formulation that meets Claim 1’s scope ambiguities.

However, the broadness of Claim 1 makes design-around harder unless antagonists are clearly removed.

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Key Takeaways

• Claim 1 is a broad antigen + Gi/Gq GPCR antagonist combination without dose, antigen type, or formulation limitations in the claim text you provided.
• Claim 2 and Claim 3 are administration constraints that are common in vaccination, so they may not provide meaningful novelty over many prior art vaccine compositions.
• Claim 4’s receptor-class list materially expands scope and accelerates prior art mapping by enumerating many familiar antagonists (adrenergic, muscarinic, histamine, serotonin, leukotriene, angiotensin, opioid, etc.).
• Validity risk concentrates on whether prior art already taught antigen compositions using GPCR antagonists and whether those receptors were identifiable as Gi- or Gq-coupled using established pharmacology.
• Landscape analysis cannot be completed to a defensible standard from claim text alone because no bibliographic identifiers, priority data, or citation record are available in the prompt.

FAQs

1) What is the only independent claim element that can carry novelty?
The novelty must sit in the combination of an antigen with at least one Gi-coupled GPCR antagonist and/or Gq-coupled GPCR antagonist, because administration and specific antagonist classes are placed in dependent claims.

2) Does Claim 1 require both Gi and Gq antagonists?
The language “at least one selected from” can be construed to require only one category depending on construction. As written, it does not explicitly state “both,” so enforceability and validity both hinge on claim construction.

3) Are the dependent injection routes likely to limit prior art?
Often they do not, because intradermal, subcutaneous, and intramuscular routes are standard for many vaccine and immunotherapy products.

4) Why does Claim 4 matter for freedom-to-operate?
It names many receptor antagonist families that overlap with marketed drugs, making it easier to argue an accused product falls inside the listed antagonist scope.

5) What prior art categories are most dangerous against this patent?
Documents that disclose vaccine or antigen formulations combined with GPCR antagonists (or immunomodulators acting through Gi/Gq GPCR pathways) and documents that can map those antagonists to Gi or Gq coupling.

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References

[1] US 10,471,140 claim text as provided in the prompt.

Details for Patent 10,471,140

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Jubilant Hollisterstier Llc	N/A	positive skin test control-histamine	Injection	103891	March 13, 1924		2039-04-18