Gene Co Pty Ltd v. Trustees Of Columbia University In City Of New York

1. Case Identification

• Case #: IPR2024-00312
• Patent #: 9,486,432
• Filed: December 19, 2023
• Petitioner(s): Gene Company Pty Ltd
• Patent Owner(s): The Trustees of Columbia University in the City of New York
• Challenged Claims: 1-28

2. Patent Overview

• Title: Pharmaceutical Compositions Comprising Deuterated Retinoids
• Brief Description: The ’432 patent relates to pharmaceutical compositions containing vitamin A derivatives (retinoids) where hydrogen atoms at the C20 position are replaced with deuterium. These compositions are intended for treating or preventing eye diseases, such as macular degeneration, by slowing the formation of toxic lipofuscin pigments.

3. Grounds for Unpatentability

Ground 1: Obviousness over Olson 1988 and Olson 1989 - Claims 1-6 and 28 are obvious over Olson 1988 in view of Olson 1989.

• Prior Art Relied Upon: Olson 1988 (a 1988 journal article on the synthesis of deuterated Vitamin A) and Olson 1989 (a 1989 journal article on Vitamin A concentration assays).
• Core Argument for this Ground:
  • Prior Art Mapping: Petitioner argued that Olson 1988 expressly discloses the synthesis and purification of the claimed C20-D3-retinol and C20-D3-retinol acetate for use in biological studies. While Olson 1988 does not explicitly mention a carrier, Petitioner asserted that Olson 1989, from the same research group, demonstrates the conventional step of formulating a different deuterated vitamin A (retinyl acetate) in a pharmaceutically acceptable carrier (corn oil) for administration to humans in biological studies. Claims 5, 6, and 28, which recite the functional property of reduced A2E formation, were argued to be inherent properties of C20 deuteration due to the well-known kinetic isotope effect.
  • Motivation to Combine: A POSA would have been motivated to formulate the C20-deuterated compounds of Olson 1988 in a carrier because they were explicitly created for "biological studies," which necessitates a delivery vehicle. Olson 1989 corroborated that this was a routine, conventional, and successful practice for the same research group.
  • Expectation of Success: Petitioner contended there was a high expectation of success, as Olson 1989 showed the successful formulation of a similar deuterated vitamin A. Further, the ’432 patent itself allegedly admits that such formulation is conventional and well within the ordinary skill in the art.

Ground 2: Obviousness over Ortho Pharma and Olson 1988 - Claims 1-6, 8-23, 25, and 27-28 are obvious over Ortho Pharma and Olson 1988.

• Prior Art Relied Upon: Ortho Pharma (a 2007 German patent application) and Olson 1988 (a 1988 journal article).
• Core Argument for this Ground:
  • Prior Art Mapping: Ortho Pharma allegedly disclosed pharmaceutical compositions containing standard (non-deuterated) vitamin A, a carrier, and various additives (e.g., vitamins C, D, E, zinc, carotenoids) for treating macular degeneration. Olson 1988 disclosed the claimed C20-deuterated vitamin A. Petitioner argued it would have been obvious to substitute the known C20-deuterated vitamin A from Olson 1988 for the standard vitamin A in Ortho Pharma’s therapeutic formulation to achieve an improved treatment. This combination allegedly teaches claim 1 and the various dependent claims reciting specific additives.
  • Motivation to Combine: The motivation was to improve the treatment for macular degeneration taught by Ortho Pharma. Petitioner asserted that other prior art (Mata) had identified that the formation of toxic A2E pigment involved a reaction at the C20 position of vitamin A. A POSA, knowing the deuterium kinetic isotope effect, would have been motivated to substitute the C20-deuterated compound from Olson 1988 to specifically slow this known, undesirable byproduct formation.
  • Expectation of Success: Success was reasonably expected because it involved substituting a known compound into a conventional formulation to leverage a predictable scientific principle (the kinetic isotope effect) to solve a known problem (A2E formation).

Ground 3: Obviousness over Ground 2 and Widder - Claims 7, 24, and 26 are obvious over the combination in Ground 2 in further view of Widder.

• Prior Art Relied Upon: Ortho Pharma (a 2007 German patent application), Olson 1988 (a 1988 journal article), and Widder (a 2006 WO publication).
• Core Argument for this Ground:
  • Prior Art Mapping: This ground builds on the base composition from Ground 2. Petitioner argued that Widder teaches further improving vitamin A therapies for macular degeneration by adding specific supplements. Widder allegedly discloses adding fenretinide (recited in claim 7), adding negatively-charged phospholipids like cardiolipin (recited in claim 24), and preparing the composition for direct ocular administration (recited in claim 26).
  • Motivation to Combine: A POSA seeking to create a more effective treatment for macular degeneration would have been motivated to incorporate the beneficial agents and administration routes taught by Widder into the base composition of Ground 2. Widder provided the express rationale for including these elements to reduce lipofuscin formation and treat ocular diseases.
  • Expectation of Success: Petitioner argued for a high expectation of success, as Widder teaches that these combinations are effective and can be formulated using conventional methods, which is consistent with the admissions in the ’432 patent.

4. Key Technical Contentions

• Petitioner’s argument centered on the assertion that the scientific basis for the invention was already established in the prior art. The core contention was that Mata (a 2000 journal article) identified the biochemical pathway for toxic A2E formation as involving hydrogen removal from the C20 position of vitamin A. A POSA would have immediately recognized that substituting this hydrogen with deuterium—using the exact C20-D3-retinoids disclosed in Olson 1988—would predictably slow this undesirable reaction due to the well-known deuterium kinetic isotope effect.

5. Arguments Regarding Discretionary Denial

• Petitioner argued that institution is warranted under §325(d) because the key prior art and arguments are materially different from those considered during prosecution. The ’432 patent was allowed with no prior art rejections. Critically, the primary references relied upon in the petition—Olson 1988, Olson 1989, Ortho Pharma, and Mata—were never before the Examiner. Petitioner contended the applicant overcame prosecution in a parent case by arguing the prior art did not disclose C20-deuterated retinoids, a statement directly contradicted by Olson 1988, thus constituting a material error.

6. Relief Requested

• Petitioner requests institution of an inter partes review and cancellation of claims 1-28 of the ’432 patent as unpatentable.