Padagis US LLC v. Neurelis Inc

1. Case Identification

• Case #: IPR2025-00464
• Patent #: 8,895,546
• Filed: January 17, 2025
• Petitioner(s): Padagis US LLC
• Patent Owner(s): Neurelis, Inc.
• Challenged Claims: 1-22

2. Patent Overview

• Title: Administration Of Benzodiazepine Compositions
• Brief Description: The ’546 patent describes pharmaceutical solutions for the intranasal administration of benzodiazepine drugs. The claimed solutions consist of a benzodiazepine, one or more tocopherols (e.g., vitamin E), a combination of ethanol and benzyl alcohol, and an alkyl glycoside as a penetration enhancer.

3. Grounds for Unpatentability

Ground 1: Obviousness over Gwozdz and Meezan - Claims 1-22 are obvious over Gwozdz in view of Meezan.

• Prior Art Relied Upon: Gwozdz (International Publication No. WO 2009/120933) and Meezan (Application # 2006/0046962).
• Core Argument for this Ground:
  • Prior Art Mapping: Petitioner argued that the combination of Gwozdz and Meezan taught all limitations of the challenged claims. Gwozdz disclosed pharmaceutical solutions for nasal administration containing a benzodiazepine (e.g., diazepam), a tocopherol carrier, and a combination of alcohols including ethanol and benzyl alcohol. The concentration ranges for these components disclosed in Gwozdz were argued to overlap with or render obvious the ranges recited in the claims. Meezan was cited for its teaching of adding an alkyl glycoside (e.g., dodecyl maltoside) as a penetration enhancer to improve the bioavailability of drugs administered to a mucosal surface. Petitioner contended that adding Meezan’s alkyl glycoside to Gwozdz's base formulation would result in the claimed invention. The arguments for dependent claims followed from the teachings for independent claim 1, with Gwozdz and Meezan allegedly disclosing or suggesting the more specific components and concentration ranges.
  • Motivation to Combine: Petitioner asserted a person of ordinary skill in the art (POSITA) would combine Gwozdz and Meezan to solve the known problem of limited solubility and bioavailability of benzodiazepine drugs for non-oral administration. Gwozdz provided a base formulation for solubilizing benzodiazepines in a tocopherol and alcohol solvent system suitable for nasal delivery. Gwozdz further taught that its formulations could be improved by adding other excipients, including "penetration enhancers." A POSITA would have looked to references like Meezan, which explicitly taught using alkyl glycosides as penetration enhancers to increase the absorption and bioavailability of drugs. The combination was presented as a predictable application of known technologies to achieve an improved result.
  • Expectation of Success: A POSITA would have a reasonable expectation of success in combining the references. Gwozdz demonstrated that its formulation successfully solubilized diazepam. Meezan showed that alkyl glycosides were effective and compatible with alcohol-based systems and successfully increased the bioavailability of other drugs. Therefore, a POSITA would expect that adding the known enhancer from Meezan to the known solubilizing formulation from Gwozdz would predictably improve the drug’s overall performance.
  • Key Aspects: A central pillar of the petition is the argument that the Patent Owner is collaterally estopped from contesting the obviousness of this combination. Petitioner highlighted that in a prior inter partes review (IPR), IPR2019-00451, the Board found all claims of a related patent (Patent 9,763,876) unpatentable over the same Gwozdz and Meezan combination. Petitioner argued the claims of the ’546 patent are materially identical to the previously invalidated claims, differing only in reciting the pharmaceutical solution itself rather than a method of using it.

4. Key Claim Construction Positions

• "vitamin E": Petitioner argued the Board should construe "vitamin E" according to the patent's explicit definition, which means "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 aligns the term with the broader "tocopherols or tocotrienols" language found in independent claim 1.

5. Key Technical Contentions (Beyond Claim Construction)

• Priority Date Entitlement: Petitioner contended that the ’546 patent is not entitled to its earliest claimed priority date from the ’558 provisional application (filed March 28, 2008). The argument was that the ’558 provisional failed to provide adequate written description for the critical "alkyl glycoside" limitation, as this term was first introduced in the later ’439 application (filed March 27, 2009). This technical argument is crucial, as establishing the later priority date makes Gwozdz, which claims priority to a March 28, 2008 provisional, valid prior art under 35 U.S.C. §102(e). Petitioner noted the Board reached this same conclusion in the related IPR2019-00451.

6. Arguments Regarding Discretionary Denial

• §325(d) (Advanced Bionics factors): Petitioner argued against discretionary denial because, although Gwozdz and Meezan were cited in an Information Disclosure Statement (IDS) during prosecution, the examiner never issued a rejection based on the combination or substantively addressed their combined teachings. Petitioner asserted that the final written decision in IPR2019-00451, which invalidated a related patent on the same art, demonstrates that the examiner erred in a manner material to patentability.
• §314(a) (Fintiv factors): To preempt discretionary denial based on parallel district court litigation, Petitioner stipulated that if the Board institutes this IPR, it will not pursue the same grounds, or any grounds that could have reasonably been raised in the petition, in the co-pending district court case.

7. Relief Requested

• Petitioner requests institution of an IPR and cancellation of claims 1-22 of Patent 8,895,546 as unpatentable.