Argentum Pharmaceuticals LLC v. Cosmo Technologies Ltd

1. Case Identification

• Case #: IPR2018-00080
• Patent #: 9,320,716
• Filed: October 20, 2017
• Petitioner(s): Argentum Pharmaceuticals LLC
• Patent Owner(s): Cosmo Technologies Limited
• Challenged Claims: 1-29

2. Patent Overview

• Title: Controlled Release and Taste Masking Oral Pharmaceutical Compositions
• Brief Description: The ’716 patent describes controlled-release oral pharmaceutical compositions for treating intestinal inflammatory disease. The invention comprises a core tablet containing the active ingredient budesonide, a "macroscopically homogenous" structure of at least one lipophilic and one hydrophilic compound to control drug release, and a gastro-resistant coating to prevent release in the stomach.

3. Grounds for Unpatentability

Ground 1: Anticipation of Claims 1-29 - Claims are anticipated under 35 U.S.C. §102 by Savastano.

• Prior Art Relied Upon: Savastano (Patent 5,681,584).
• Core Argument for this Ground:
  • Prior Art Mapping: Petitioner argued that Savastano, entitled "Controlled Release Drug Delivery Device," discloses every element of the challenged claims. Savastano explicitly teaches time-controlled tablets containing budesonide for treating inflammatory bowel diseases like Crohn's disease. The core formulation in Savastano was asserted to meet the "macroscopically homogenous structure" limitation by disclosing the mixing of all core components, including lipophilic lubricants (e.g., stearic acid, magnesium stearate) and hydrophilic binders (e.g., hydroxyethyl cellulose). Furthermore, Savastano discloses an enteric, gastro-resistant coating (e.g., methacrylic acid copolymer NF) to prevent drug release in the stomach.
  • Key Aspects: Petitioner contended that Savastano's disclosure of lists of suitable excipients (lubricants, binders) anticipates the claims, as a person of ordinary skill in the art (POSA) would understand that selecting one from each category is necessary to form a functional tablet.

Ground 2: Obviousness of Claims 1-29 - Claims are obvious under 35 U.S.C. §103 over Friend.

• Prior Art Relied Upon: Friend (Patent 5,811,388).
• Core Argument for this Ground:
  • Prior Art Mapping: Petitioner asserted that Friend, which teaches drug delivery to the lower GI tract, renders the claims obvious. Friend discloses uniform matrix tablets containing budesonide for treating inflammatory bowel disease. It teaches using lipophilic lubricants (magnesium stearate) and hydrophilic cellulosic derivatives (HPMC is preferred), which allegedly meet the limitations for the macroscopically homogenous core. Friend also explicitly teaches applying an enteric coating to the tablet to prevent stomach degradation. For claims requiring an amphiphilic compound, Friend discloses detergents like lysolectin (lysolecithin).
  • Motivation to Combine (for single-reference obviousness): The motivation stemmed from combining known elements for their predictable functions. A POSA would have been motivated to formulate a tablet with budesonide using standard, well-known excipients like magnesium stearate (lubricant) and HPMC (binder) to create a standard uniform matrix tablet, and apply a standard enteric coating for delivery to the colon, all as taught by Friend.
  • Expectation of Success: A POSA would have had a high expectation of success because Friend teaches combining conventional components using standard tableting techniques to achieve the predictable result of a controlled-release formulation for treating inflammatory bowel disease.

Ground 3: Obviousness of Claims 8, 10, 18, and 20 - Claims are obvious over Friend in view of Savastano.

• Prior Art Relied Upon: Friend (Patent 5,811,388) and Savastano (Patent 5,681,584).

• Core Argument for this Ground:

  • Prior Art Mapping: This ground specifically targeted claims reciting lecithin (claims 8, 18) and stearic acid (claims 10, 20). Petitioner argued that Friend teaches the foundational controlled-release budesonide formulation, including the use of a related amphiphilic compound (lysolecithin) and a related lipophilic lubricant (magnesium stearate). Savastano explicitly discloses the use of both lecithin and stearic acid in its own controlled-release budesonide formulation.
  • Motivation to Combine: A POSA, starting with Friend's formulation, would have been motivated to consult Savastano, as both patents address the same problem (controlled release of budesonide) using overlapping excipients. To optimize Friend's formulation, a POSA would have looked to Savastano and found express teachings to use lecithin (a known wetting agent useful for the poorly soluble budesonide) and stearic acid (a well-known, interchangeable alternative to magnesium stearate).
  • Expectation of Success: The combination would have yielded predictable results, as it involved substituting known, interchangeable excipients (magnesium stearate for stearic acid) or adding a known functional excipient (lecithin) into a conventional formulation for its established purpose.

• Additional Grounds: Petitioner asserted additional challenges, including that claims 1-29 are obvious over Savastano alone (Ground 2) and that various claims are anticipated by Friend (Ground 3). These grounds relied on similar arguments that the prior art's disclosure of conventional drug formulation techniques and lists of standard excipients inherently taught or rendered obvious the claimed compositions.

4. Key Claim Construction Positions

• Petitioner referenced and relied upon claim constructions from a Markman Order in a related district court litigation (Cosmo Technologies Limited v. Alvogen Pine Brook, LLC).
• The construction for "macroscopically homogeneous composition" as "A composition of uniform structure throughout, as as observed by the naked eye" was central to Petitioner's arguments. Petitioner contended that this limitation is met by the standard blending and mixing techniques for preparing uniform matrix tablets, which are explicitly disclosed in both the Savastano and Friend prior art references.
• Petitioner argued these constructions were consistent with the broadest reasonable interpretation and supported its mapping of the prior art onto the claims.

5. Key Technical Contentions (Beyond Claim Construction)

• Excipients are not "Optional": Petitioner argued that although prior art references like Savastano may list excipients such as lubricants and binders as "additional" or part of a list of possibilities, a POSA would understand these components are functional necessities for creating a viable, manufacturable tablet. Therefore, a disclosure listing them is a disclosure of their use.
• Latent Properties Do Not Confer Patentability: Petitioner contended that to the extent the ’716 patent relies on a specific dissolution profile ("controls the release") as the point of novelty, this is merely the discovery of a latent, inherent property of an otherwise obvious formulation. An obvious combination of known ingredients is not rendered non-obvious simply by identifying and claiming its inherent, predictable performance characteristics.

6. Arguments Regarding Discretionary Denial

• Petitioner argued that institution should not be denied under §325(d), even though the primary prior art references (Savastano and Friend) were cited to the examiner during prosecution of the ’716 patent or related applications.
• The petition asserted that it presented the art in a new light, supported by a detailed expert declaration from Dr. Hartmut Derendorf, and provided arguments and evidence beyond what the examiner previously considered.

7. Relief Requested

• Petitioner requested institution of an inter partes review and cancellation of claims 1-29 of Patent 9,320,716 as unpatentable.