PTAB

IPR2018-01143

Mylan Pharmaceuticals Inc. v. Bayer Intellectual Property GmbH

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1. Case Identification

2. Patent Overview

  • Title: Prevention and Treatment of Thromboembolic Disorders
  • Brief Description: The ’218 patent is directed to a method of treating thromboembolic disorders, such as pulmonary embolism (PE), deep vein thrombosis (DVT), or stroke. The method comprises administering the factor Xa inhibitor rivaroxaban no more than once daily for at least five consecutive days in a rapid-release tablet.

3. Grounds for Unpatentability

Ground 1: Claims 1-4 are obvious over the '610 Publication and Kubitza Abstracts.

  • Prior Art Relied Upon: The ’610 Publication (Application # 2003/0153610) and Kubitza Abstracts (a 2003 abstract book from the American Society of Hematology).
  • Core Argument for this Ground:
    • Prior Art Mapping: Petitioner asserted that the combination of these references discloses all elements of the challenged claims. The ’610 publication teaches using rivaroxaban for the prophylaxis and therapy of thromboembolic disorders, including PE, DVT, and stroke, and suggests formulating it into tablets for oral administration. The Kubitza Abstracts report on Phase I clinical trials of rivaroxaban, disclosing a once-daily dosing regimen for five consecutive days and administration in tablet form. Petitioner contended that a person of ordinary skill in the art (POSITA) would understand the "tablet" disclosed in Kubitza to be a conventional, rapid-release tablet, as this is the default formulation unless otherwise specified.
    • Motivation to Combine: A POSITA would combine the teachings because both references concern the same compound (rivaroxaban) for the same therapeutic purpose. It would have been a natural progression to consult the foundational disclosure of a compound in the ’610 publication alongside later clinical trial data on that same compound from the Kubitza Abstracts to determine an appropriate treatment regimen.
    • Expectation of Success: The Kubitza Abstracts demonstrated that a once-daily, five-day regimen of rivaroxaban was safe, well-tolerated, and effective in producing an antithrombotic effect. Given that the ’610 publication already identified tablets as a preferred oral dosage form, a POSITA would have had a high expectation of success in administering rivaroxaban according to the claimed method.

Ground 2: Claims 1-4 are obvious over the '610 Publication, Kubitza Abstracts, and Forsman.

  • Prior Art Relied Upon: The ’610 Publication (Application # 2003/0153610), Kubitza Abstracts (a 2003 abstract book), and Forsman (WO 2000/013671).
  • Core Argument for this Ground:
    • Prior Art Mapping: This ground presents an alternative argument in the event the term "rapid-release tablet" is construed narrowly to require a specific dissolution profile (e.g., a Q value of 75% dissolution in 30 minutes). While Petitioner maintained the teachings of the ’610 publication and Kubitza Abstracts render the claims obvious as argued in Ground 1, Forsman is added to explicitly teach this feature. Forsman discloses immediate-release (IR) tablet formulations for anticoagulants used to treat thromboembolism that release more than 85% of the active ingredient within 30 minutes, thereby meeting the more stringent dissolution requirement.
    • Motivation to Combine: A POSITA would combine Forsman with the other references to optimize the rivaroxaban tablet formulation. The Kubitza Abstracts showed that a liquid oral solution of rivaroxaban achieved maximal plasma concentration faster than a tablet, suggesting a benefit to rapid drug release. A POSITA seeking to develop a tablet with the fastest possible onset of action would look to known techniques for creating such formulations. Forsman provides a clear, successful example of an immediate-release tablet for anticoagulants that achieves this goal.
    • Expectation of Success: Forsman demonstrated a successful, conventional method for manufacturing fast-dissolving tablets for a similar class of drugs. This provided a clear roadmap and a strong expectation that applying these established formulation principles to rivaroxaban would predictably result in a rapid-release tablet meeting the claimed dissolution profile without undue experimentation.

4. Key Claim Construction Positions

  • "rapid-release tablet": Petitioner argued this term should be construed broadly to mean a conventional tablet that has not been specifically formulated for modified (e.g., extended or delayed) release. This construction is based on the patent’s specification, which distinguishes between tablets releasing the compound "rapidly" and those releasing it in a "modified manner." Petitioner supported this with extrinsic evidence, including FDA guidance and pharmaceutical textbooks, which categorize tablets as either "conventional/immediate-release" or "modified-release." This construction is central to Ground 1, as it allows the standard tablets disclosed in Kubitza to meet the claim limitation.

5. Arguments Regarding Discretionary Denial

  • Petitioner argued that discretionary denial under 35 U.S.C. §325(d) would be inappropriate. The core reason provided was that the petition presents new evidence and arguments not considered by the USPTO during prosecution. Specifically, the petition relies on new prior art (Forsman), expert declarations (from Drs. Benet and Doherty), and new arguments explaining why the tablets in Kubitza constitute "rapid-release" tablets. Petitioner contended that during prosecution, the Examiner lacked this evidence and explanation, which led to the allowance of the claims. Therefore, the Board should not defer to the Examiner's prior determination and should institute review to correct this alleged error.

6. Relief Requested

  • Petitioner requested institution of an inter partes review and cancellation of claims 1-4 of the ’218 patent as unpatentable under 35 U.S.C. §103.