PTAB

IPR2025-00466

Padagis US LLC v. Neurelis Inc

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Key Events
Petition
petition

1. Case Identification

2. Patent Overview

  • Title: Administration Of Benzodiazepine Compositions
  • Brief Description: The ’786 patent describes pharmaceutical compositions for the intranasal administration of benzodiazepine drugs. The invention is a solution comprising a benzodiazepine (e.g., diazepam), tocopherols or tocotrienols (Vitamin E), one or more alcohols including benzyl alcohol, and an alkyl glycoside (n-dodecyl beta-D-maltoside) to improve solubility and bioavailability.

3. Grounds for Unpatentability

Ground 1: Obviousness over Gwozdz and Meezan - Claims 1-25 are obvious over Gwozdz in view of Meezan.

  • Prior Art Relied Upon: Gwozdz (WO 2009/120933) and Meezan (Application # 2006/0046962).
  • Core Argument for this Ground:
    • Prior Art Mapping: Petitioner argued that Gwozdz taught the core formulation for solubilizing a benzodiazepine like diazepam for nasal administration. Gwozdz disclosed using a combination of tocopherols (e.g., alpha-tocopherol) in amounts of 30-99% (w/w) and one or more alcohols (including ethanol and benzyl alcohol) in amounts of 1-70% (w/w). Petitioner asserted that Meezan taught the missing element: adding an alkyl glycoside, specifically dodecyl maltoside, as a permeation enhancer to increase the absorption and bioavailability of drugs administered intranasally.
    • Motivation to Combine: A person of ordinary skill in the art (POSITA) would combine Gwozdz's solubilizing formulation with Meezan's absorption enhancer to solve the known problem of poor benzodiazepine solubility and improve overall efficacy. Gwozdz expressly suggested that its formulations could incorporate additional additives to improve drug delivery. A POSITA would look to known enhancers like those in Meezan to achieve this predictable improvement.
    • Expectation of Success: A POSITA would have a reasonable expectation of success because Gwozdz demonstrated that its solvent system was effective for diazepam, and Meezan showed that alkyl glycosides were effective permeation enhancers in non-aqueous, alcohol-based solvent systems. The combination was a predictable optimization of a known formulation strategy.

Ground 2: Obviousness over Gwozdz, Meezan, and Cartt - Claims 20-21 are obvious over Gwozdz in view of Meezan, further in view of Cartt.

  • Prior Art Relied Upon: Gwozdz (WO 2009/120933), Meezan (Application # 2006/0046962), and Cartt (Application # 2008/0279784).
  • Core Argument for this Ground:
    • Prior Art Mapping: This ground built upon the combination of Gwozdz and Meezan to establish the base formulation. Cartt was introduced to teach the specific dosage limitations recited in claims 20 (5-20 mg) and 21 (1-20 mg). Petitioner argued that Cartt explicitly disclosed delivering diazepam nasally in therapeutic doses ranging from about 1 to 20 mg per dose.
    • Motivation to Combine: A POSITA, having developed the base formulation from Gwozdz and Meezan, would be motivated to consult a reference like Cartt—which is directed to the same field of benzodiazepine nasal sprays—to determine a clinically appropriate and effective dosage range. This represents a routine step in pharmaceutical product development.
    • Expectation of Success: Integrating a known therapeutic dose from Cartt into the solubilized and absorption-enhanced formulation from Gwozdz and Meezan would have been a predictable step with a high expectation of success.

Ground 3: Obviousness over Gwozdz, Meezan, and USP 23/NF 18 - Claims 26-27 are obvious over Gwozdz in view of Meezan, further in view of USP 23/NF 18.

  • Prior Art Relied Upon: Gwozdz (WO 2009/120933), Meezan (Application # 2006/0046962), and USP 23/NF 18 (a 1995 compendium of standards).
  • Core Argument for this Ground:
    • Prior Art Mapping: This ground also built upon the base formulation from Gwozdz and Meezan. It introduced USP 23/NF 18 to teach the limitation in claims 26 and 27 that the α-tocopherol must be "Vitamin E USP." USP 23/NF 18 provided the official monograph for Vitamin E, defining it as a form of alpha tocopherol and setting the standard for its pharmaceutical grade.
    • Motivation to Combine: A POSITA would be motivated to use USP-grade ingredients as a matter of standard industry practice to ensure quality, purity, and regulatory compliance. USP 23/NF 18 was the internationally recognized standard for pharmaceutical ingredients.
    • Expectation of Success: A POSITA would have a clear expectation of success, as using the official USP grade of a known ingredient (α-tocopherol) would not alter its chemical properties but would simply ensure it met established pharmaceutical standards.

4. Key Claim Construction Positions

  • Petitioner argued that the term "Vitamin E," recited in claims 10, 26, and 27, should be construed according to its express definition in the ’786 patent specification: "any of the natural or synthetic tocopherols, tocotrienols, any isomers thereof, any esters thereof, any analogs or derivatives thereof, or any combinations thereof." This construction allows Gwozdz's disclosure of tocopherols to map directly onto the claims.

5. Key Technical Contentions (Beyond Claim Construction)

  • Priority Date Entitlement: A central contention was that the ’786 patent is not entitled to the March 28, 2008 filing date of its earliest provisional application (the ’558 provisional). Petitioner argued the ’558 provisional failed to provide adequate written description support for the "alkyl glycoside" limitation, which first appeared in the March 27, 2009 non-provisional application (the ’439 application). This later priority date is critical because it establishes Gwozdz (March 28, 2008 priority) and Cartt (May 7, 2007 priority) as prior art under pre-AIA 35 U.S.C. §102(e).

6. Arguments Regarding Discretionary Denial

  • Petitioner argued the Board should not exercise its discretion to deny institution under §314(a) or §325(d). The petition asserted that the arguments and specific prior art combinations were not considered by the Examiner during prosecution. Crucially, Petitioner highlighted that the Board, in a Final Written Decision for a related case (IPR2019-00451) against the parent ’876 patent, found nearly identical claims unpatentable over the same core prior art (Gwozdz, Meezan, and Cartt). This prior decision demonstrates both the Examiner's error and the strength of the petition's merits. To address Fintiv concerns, Petitioner stipulated that it would not pursue the same grounds or any grounds that could have been reasonably raised in a parallel district court proceeding if the inter partes review (IPR) is instituted.

7. Relief Requested

  • Petitioner requested institution of an IPR and cancellation of claims 1-27 of the ’786 patent as unpatentable.