Details for Patent: 9,289,446

Summary for Patent: 9,289,446

Title:	Myocardial perfusion imaging methods and compositions
Abstract:	A myocardial imaging method that is accomplished by administering one or more adenosine A2A adenosine receptor agonist to a human undergoing myocardial imaging as well as pharmaceutical compositions comprising at least one A2a receptor agonist, at least one liquid carrier, and at least one co-solvent.
Inventor(s):	Luiz Belardinelli, Mitchell Rosner
Assignee:	Gilead Sciences Inc
Application Number:	US14/533,025
Patent Claim Types: see list of patent claims	Use; Composition; Device;

Patent 9,289,446 (US) Claim Scope and US Patent Landscape: What Do the Formulation, Kit, and IV Bolus Coronary Vasodilation Claims Cover?

US Patent 9,289,446 centers on a specific liquid formulation and downstream kit and use claims for IV bolus administration in coronary vasodilation and myocardial perfusion imaging (MPI) when paired with a radionuclide. The claims are tight on: (i) a ~400 µg dose of a defined “compound” (formula unspecified in the claim text you provided), (ii) propylene glycol at ~15% (w:v), (iii) a sodium phosphate buffer at ~100 mM and pH 6–8 (preferred pH ~7), and (iv) EDTA (0.1% in the explicit examples). The patent estate’s practical boundary is therefore largely defined by whether an accused product matches the buffering system, propylene glycol level, EDTA presence, and pH window and by whether the accused method performs IV bolus dosing for coronary vasodilation or MPI with the stated effect-time relationship (claims 17–18).

What exactly are the independent and dependent claims in US 9,289,446?

Claim 1 (core formulation)

Claim 1 is the only independent claim you provided that is directed to a drug product composition. Its scope is defined by all of the following elements in combination:

• Dose/amount: “about 400 μg” of a compound having a specified chemical formula.
• Liquid carrier(s): at least one selected from water, saline, buffer, or combinations.
• Buffer: at least one sodium phosphate buffer.
• Chelator: EDTA.
• Co-solvent: propylene glycol at about 15% (w:v).
• pH: composition pH is about 6 to about 8.

This claim is a classic “parameter constrained” liquid formulation: it is not simply “a phosphate-buffered EDTA solution,” it explicitly requires propylene glycol at ~15% (w:v) and pH 6–8.

Claims 2–7 (formula narrowing)

These add specific subranges and preferred embodiments:

• Claim 2: pH is about 7.
• Claim 3–4: water is distilled or de-ionized.
• Claim 5: explicit formulation match: 15% (w:v) propylene glycol; 100 mM phosphate buffer at pH 7; 0.1% EDTA.
• Claim 6: sodium phosphate buffer concentration about 100 mM.
• Claim 7: duplicates claim 5.

Note claims 5 and 7 are the same “tight” exemplar and will matter for infringement analysis and for how broadly courts interpret the “about” language around those numeric targets.

Claims 8–11 (kit / container closure)

These are composition plus packaging:

• Claim 8: a kit with a vessel formed from type I glass or plastic, containing the claim 1 composition.
• Claim 9: vessel formed from plastic.
• Claim 10: a kit containing claim 3 composition (water selection narrowed) with vessel type I glass or plastic.
• Claim 11: vessel formed from plastic.

The kit claims are not about the chemical formulation beyond what is imported from the composition claims. They instead constrain container material (type I glass vs plastic).

Claims 12–13 (method: coronary vasodilation)

• Claim 12: administer by IV bolus the claim 1 composition to a human.
• Claim 13: same but using claim 3 composition (water selection narrowed).

These are direct method-of-use claims tied to the formulation defined in claims 1 and 3.

Claims 14–16 (method: MPI with radionuclide)

• Claim 14: IV bolus administration of claim 1 composition plus a radionuclide, then examine myocardium for insufficient blood flow following administration of both.
• Claim 15: composition and radionuclide administered separately.
• Claim 16: composition and radionuclide administered simultaneously.

These claims require both:

1. the formulation delivery method (IV bolus), and
2. the imaging workflow pairing with a radionuclide.

Claims 17–18 (timing/effect constraint)

• Claim 17: causes at least 2.5-fold increase in coronary blood flow for less than ~5 minutes.
• Claim 18: same but for less than ~3 minutes.

These are functional limitations that can materially narrow infringement exposure by imposing a performance window. For most litigation, these claims create the need for evidence tied to pharmacodynamics in the accused regimen.

Claims 19–20 (MPI with claim 3 formulation)

• Claim 19: like claim 14 but with claim 3 composition.
• Claim 20: separate administration.

Which formulation elements are the “high-risk” infringement anchors?

The claim language imports multiple constraints that act as “hard stops” for design-around:

1. Propylene glycol at about 15% (w:v)
   This is the most distinctive excipient constraint. Many liquid formulations could be phosphate buffered and contain EDTA, but fewer will be tuned to ~15% (w:v) propylene glycol.

2. Sodium phosphate buffer
   Claim 1 requires “at least one sodium phosphate buffer.” Replacing phosphate with a different buffer system is the cleanest design-around, unless the product still contains sodium phosphate as one component.

3. EDTA present
   EDTA is explicitly required. Formulations that omit EDTA should fall outside claim 1.

4. pH window 6–8 (preferred ~7)
   If an accused composition is outside “about 6 to about 8,” it may avoid literal claim 1, though the risk depends on how “about” is interpreted.

5. ~400 µg dose per administration
   The composition claim is tied to “about 400 μg” of the compound. If an accused product delivers a materially different dose, it may not satisfy the claim as written.

In practice, the tightest “match test” for composition infringement is whether an accused IV bolus drug uses:

• ~15% w:v propylene glycol,
• 100 mM sodium phosphate buffer near pH 7,
• EDTA near 0.1%, and
• delivers the compound at about 400 µg.

How do the claims treat “about” ranges and preferred embodiments?

The claim set includes explicit numerics (claims 5–7: 15%, 100 mM, pH 7, 0.1% EDTA) plus broader ranges (claim 1: pH 6–8, “about 400 μg,” and “about 15%”). This structure usually means:

• The broader independent claim 1 is the primary litigation target because it captures a range.
• Dependent claims 5–7 function as “exact-configuration” anchors that reduce disputes over whether a formulation is within the broader boundaries.

For infringement analysis, the numeric dependent claims (5–7) are typically the most persuasive because they define a specific target formulation that an accused product either matches or does not.

What patents or patent families typically surround a formulation + IV bolus MPI use claim?

US 9,289,446’s structure suggests it belongs to a family targeting multiple layers:

• Drug substance definition (the compound defined by formula in claim 1, which you did not provide in the text).
• Specific liquid formulation including excipients and pH/buffer system (core scope).
• Container/closure (type I glass vs plastic) via kit claims.
• Method of use for:
  • coronary vasodilation by IV bolus, and
  • myocardial perfusion imaging in combination with radionuclide,
  • including an effect timing limitation.

However, without the patent header details (assignee, inventors, filing dates, related applications, continuation/divisional status) and without the full specification text, a complete landscape map (priority chain, related US continuations, foreign equivalents, and the full set of family members) cannot be produced accurately.

What is the legal scope of the kit claims (type I glass or plastic)?

Claims 8–11 impose a container constraint:

• Vessel must be formed from either type I glass or plastic (claims 8 and 10).
• Vessel formed from plastic (claims 9 and 11).

The practical implication for freedom-to-operate (FTO) is that changing container material could avoid these kit claims if the accused vessel is outside “type I glass or plastic.” But in practice, most marketed parenteral products use plastic infusion/administration components or glass vials, so the container element may not offer strong design-around value unless a nonconforming container system is used.

What does the MPI method-of-use claim require, procedurally and technically?

Claim 14 and claim 19 require a combined regimen:

• administering the formulation by IV bolus to a human in need thereof, and
• administering a radionuclide, with imaging to examine myocardium for areas of insufficient blood flow following administration of both.

Claims 15–16 further require the administration schedule:

• separate vs simultaneous.

These are “workflow” constraints rather than formulation constraints. They can be avoided if the competitor performs MPI using a different route (not IV bolus), not pairing with the radionuclide as required by the claim, or altering administration timing such that a narrower interpretation of the “simultaneous” or “separately” terms is not met.

How risky are the performance window claims (2.5-fold increase for <5 minutes/<3 minutes)?

Claims 17–18 add functional requirements that depend on pharmacology and study evidence:

• at least 2.5-fold increase in coronary blood flow, and
• duration less than ~5 minutes or less than ~3 minutes.

These constraints can be harder to enforce than pure composition elements because infringement depends on the accused product’s measured effect in the claimed context (human, IV bolus, imaging workflow, etc.). Still, if the accused drug is intended for the same clinical use, it is likely to be tested in a comparable model and could create evidentiary alignment with the claimed performance.

When does US 9,289,446 expire (and what else may extend exclusivity)?

A full exclusivity and patent expiration timeline cannot be stated from the claim text alone. Expiration depends on:

• earliest US filing date,
• whether the patent is subject to PTA (35 U.S.C. 154),
• terminal disclaimers,
• and the presence of related continuations.

Also, any data exclusivity and/or regulatory exclusivity under the FD&C Act (e.g., for new chemical entities or other categories) are not inferable from the claim excerpt.

Where is the design-around space likely concentrated?

Based on the claim constraints alone, the most plausible design-arounds are:

1. Change excipient system

   • omit EDTA,
   • replace sodium phosphate with a non-sodium phosphate buffer,
   • reduce or eliminate propylene glycol, or use a substantially different proportion (e.g., not about 15% w:v).

2. Change pH

   • move outside pH 6–8.

3. Change dose

   • administer a materially different amount than about 400 µg.

4. Change administration method

   • not by IV bolus (if a non-bolus route is used), or structure the protocol so it does not match claim 14/19.

5. Change imaging workflow pairing

   • not pairing with radionuclide in the claimed sequence/schedule.

Container/material design-around may reduce exposure to the kit claims if the vessel is outside the claim’s glass/plastic boundary, but it does not avoid composition and method claims.

Key Takeaways

• US 9,289,446 is primarily a liquid formulation patent with downstream IV bolus coronary vasodilation and MPI with radionuclide method claims.
• The highest-signal infringement anchors in claim 1 are propylene glycol (~15% w:v), sodium phosphate buffer, EDTA, pH 6–8, and ~400 µg dose.
• Claims 5–7 define a tight preferred embodiment that is likely central to enforcement.
• Kit claims narrow container type (type I glass or plastic; plastic in dependent claims).
• MPI claims add operational constraints (radionuclide pairing; separate vs simultaneous dosing).
• Performance-window claims (claims 17–18) can narrow the scope but rely on human efficacy measurements.

FAQs

Which parts of US 9,289,446 are composition claims vs method claims?

Composition claims: 1–11 (including kit). Method claims: 12–7? (12–13 coronary vasodilation; 14–16 and 19–20 MPI workflows; 17–18 performance duration elements).

Can a formulation avoid infringement by changing EDTA concentration?

Claim 1 requires EDTA to be present; dependent claim 5 ties to 0.1% EDTA. Removing EDTA or using a nonconforming formulation could avoid literal scope, depending on how “about” is interpreted.

Does using a non-IV bolus administration route avoid claims 12–20?

Claims 12–20 explicitly require IV bolus administration. A non-bolus regimen is a direct pathway to avoidance of those method claims.

What must be paired with the radionuclide for MPI claims to read on a competitor?

Claims 14/19 require IV bolus administration of the formulation and administration of a radionuclide, followed by imaging for insufficient blood flow.

Do the kit claims provide additional protection beyond the composition claims?

Yes. Claims 8–11 add the vessel material constraint (type I glass or plastic) to the kit concept, but they do not replace composition or method limitations.

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References

1. US Patent No. 9,289,446. United States Patent and Trademark Office. (Cited from the claim text provided in the prompt.)

Drugs Protected by US Patent 9,289,446

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

International Family Members for US Patent 9,289,446

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2003259264
Canada	2492855
China	1671399
European Patent Office	1524984
Israel	166555
Japan	2005538190
South Korea	20050026546