Novartis Pharmaceuticals Corp v. Regents Of University Of Michigan

1. Case Identification

• Case #: IPR2023-01346
• Patent #: 10,633,344
• Filed: August 28, 2023
• Petitioner(s): Novartis Pharmaceuticals Corporation
• Patent Owner(s): Regents of the University of Michigan and University of South Florida
• Challenged Claims: 10, 11, and 18

2. Patent Overview

• Title: Multiple-Component Solid Phases Containing At Least One Active Pharmaceutical Ingredient
• Brief Description: The ’344 patent relates to pharmaceutical compositions comprising co-crystals. The claimed co-crystals are formed from an active pharmaceutical ingredient (API) with a specific chemical functionality (e.g., carboxamide) and a complementary co-former, which are joined by non-covalent hydrogen bonds to form supramolecular synthons.

3. Grounds for Unpatentability

Ground 1: Anticipation of Claims 10, 11, and 18 under 35 U.S.C. §102 over Hickey

• Prior Art Relied Upon: Hickey, "Performance comparison of a co-crystal of carbamazepine with marketed product," European Journal of Pharmaceutics and Biopharmaceutics (2007).
• Core Argument for this Ground:
  • Prior Art Mapping: Petitioner argued that Hickey discloses every limitation of the challenged claims. Hickey described a pharmaceutical composition containing a 1:1 co-crystal of carbamazepine (the API) and saccharin (the co-former) with lactose as a pharmaceutically acceptable carrier. Petitioner asserted that carbamazepine meets the claimed API limitations, as it is an anti-epileptic agent with a carboxamide functional group that inherently forms homosynthons in its pure form. Saccharin was identified as a solid co-former with a complementary chemical functionality that forms non-covalent hydrogen bonds with carbamazepine to create supramolecular synthons. For claim 11, Petitioner contended the interaction between the different functionalities of carbamazepine and saccharin forms the required heterosynthon dimer. The composition was administered to dogs in a therapeutically effective amount to evaluate bioavailability.

Ground 2: Anticipation or Obviousness of Claims 10, 11, and 18 under §§102/103 over Almarsson, alone or in combination with Hickey and Martindale

• Prior Art Relied Upon: Almarsson (Patent 7,927,613), Hickey (a 2007 journal article), and Martindale (The Complete Drug Reference).
• Core Argument for this Ground:
  • Prior Art Mapping: Petitioner contended that Almarsson, which is related to the ’344 patent, anticipates or renders obvious the challenged claims. Almarsson discloses the same 1:1 carbamazepine/saccharin co-crystal (in its Example 32) within a pharmaceutical composition comprising a carrier. Almarsson explicitly teaches the co-crystal structure, the API (carbamazepine), the co-former (saccharin), and their formation of supramolecular synthons via hydrogen bonding, mapping to most claim limitations. Petitioner argued Almarsson’s disclosure of using a "desired amount of API per dose unit" teaches or makes obvious the "therapeutically effective amount" limitation.
  • Motivation to Combine (for §103 grounds): If Almarsson alone was deemed insufficient to teach a "therapeutically effective amount," Petitioner argued a person of ordinary skill in the art (POSA) would combine Almarsson with Hickey and Martindale. A POSA, knowing from Almarsson that the co-crystal has improved properties, would have been motivated to consult a standard drug reference like Martindale for established carbamazepine dosages and a practical example like Hickey, which details a successful formulation using a specific effective amount. The overlapping subject matter—all three references concern carbamazepine for treating epilepsy—provides a strong motivation to combine their teachings.
  • Expectation of Success (for §103 grounds): A POSA would have had a high expectation of success in formulating a therapeutically effective composition, as Hickey successfully prepared and tested the exact co-crystal composition and demonstrated its viability.

4. Key Technical Contentions (Beyond Claim Construction)

• Invalid Priority Claim: The central technical contention underpinning all grounds was that the ’344 patent is not entitled to its claimed 2002/2003 priority dates. Petitioner argued the priority applications fail to provide adequate written description and enablement for the full, broad scope of the challenged genus claims, as required by 35 U.S.C. §112.
  • Lack of Written Description: The claims cover a vast and "limitless" number of potential co-crystals. The priority applications, however, disclose at most ten relevant examples using only three different APIs, which Petitioner argued is not a representative number of species to support the broad genus.
  • Lack of Enablement: Petitioner asserted that co-crystal formation was widely recognized as unpredictable and required "trial and error." The limited examples in the priority applications were insufficient to enable a POSA to practice the full scope of the claims without undue experimentation. This conclusion was supported by prosecution histories of related applications where examiners rejected similar broad claims on enablement and written description grounds.
• Effective Filing Date: As a result of the invalid priority claim, Petitioner argued the effective filing date for the challenged claims is February 13, 2014, making Hickey (2007) and Almarsson (2011) valid prior art.

5. Arguments Regarding Discretionary Denial

• Petitioner argued that the Board should not exercise its discretion to deny institution under either 35 U.S.C. §314(a) (Fintiv) or 35 U.S.C. §325(d).
  • Arguments against Fintiv Denial: Petitioner provided a Sotera-style stipulation, agreeing not to pursue in the parallel district court litigation any ground raised or that reasonably could have been raised in the inter partes review (IPR). Petitioner also argued that other Fintiv factors favored institution, as no trial date had been set in the parallel litigation and substantial work remained to be completed.
  • Arguments against §325(d) Denial: Petitioner contended that the arguments and evidence presented were not previously or substantively considered by the patent office. The primary reference Hickey was never cited during prosecution. The other primary reference, Almarsson, was merely included in a large Information Disclosure Statement (IDS) with hundreds of other references and was not substantively discussed by the examiner. Furthermore, the examiner never considered the critical priority date challenge that enables the use of this art.

6. Relief Requested

• Petitioner requested institution of an IPR and cancellation of claims 10, 11, and 18 of the ’344 patent as unpatentable.