Mylan Pharmaceuticals Inc v. Boehringer Ingelheim Pharmaceuticals Inc

1. Case Identification

• Case #: IPR2016-01563
• Patent #: 8,673,927
• Filed: August 10, 2016
• Petitioner(s): Mylan Pharmaceuticals Inc.
• Patent Owner(s): Boehringer Ingelheim International GMBH
• Challenged Claims: 1-26

2. Patent Overview

• Title: Uses of DPP-IV Inhibitors
• Brief Description: The ’927 patent is directed to methods for treating type II diabetes mellitus by administering a combination of metformin and linagliptin, which is a dipeptidyl peptidase-IV (DPP-IV) inhibitor. The claims recite specific oral dosage amounts and ranges for both active ingredients.

3. Grounds for Unpatentability

Ground 1: Anticipation of Claims 18-26 under §102(b)

• Prior Art Relied Upon: Himmelsbach (Application # 2004/0097510), referred to as the ’510 publication.
• Core Argument for this Ground:
  • Prior Art Mapping: Petitioner argued that the ’510 publication discloses every element of independent claims 18-20 and their dependent claims 21-26. The ’510 publication teaches using DPP-IV inhibitors, specifically identifying linagliptin, for treating type II diabetes. It explicitly discloses combining linagliptin with other antidiabetic agents, including metformin. Critically, Petitioner asserted that the publication’s disclosed oral dosage range for linagliptin (1 mg to 1000 mg, preferably 1 mg to 100 mg daily) anticipates the specific ranges recited in the claims, such as the 2.5 mg to 10 mg daily dose of claim 18 and the 5 mg daily dose of claim 19.
  • Key Aspects: This ground asserted that a single prior art reference published more than a year before the patent's priority date contained all limitations of claims 18-26, including the specific compound (linagliptin), its use in combination with metformin for treating type II diabetes, and the claimed oral dosage ranges for linagliptin.

Ground 2: Obviousness of Claims 1-26 under §103

• Prior Art Relied Upon: Himmelsbach (’510 publication) and the Glucophage Label (2001 FDA-approved prescribing information).
• Core Argument for this Ground:
  • Prior Art Mapping: The petition contended that while the ’510 publication teaches combining linagliptin with a "pharmaceutically effective amount" of metformin, it does not disclose the specific metformin dosage ranges recited in claims 1-17. The Glucophage Label, which provides standard dosing for metformin monotherapy, remedies this deficiency. Petitioner argued the label discloses standard doses (e.g., starting at 500 mg twice a day or 850 mg once a day) that fall squarely within the ranges claimed in the ’927 patent, such as the 300 mg to 1000 mg once or twice a day recited in claim 1.
  • Motivation to Combine: A POSITA would combine the references because the ’510 publication expressly teaches the combination of linagliptin and metformin. To implement this combination, a POSITA would naturally and logically look to the well-established, FDA-approved standard dosages for metformin as provided in the Glucophage Label. The petition noted that other DPP-IV inhibitors were already being combined with metformin using these same standard monotherapy doses.
  • Expectation of Success: A POSITA would have a high expectation of success. Both linagliptin and metformin were known to be safe and effective treatments for type II diabetes. Combining them using known effective doses for each drug would predictably result in an effective combination therapy for reducing blood glucose levels.

Ground 3: Obviousness of Claims 1-26 under §103

• Prior Art Relied Upon: Himmelsbach (’510 publication) in view of Ahrén (a 2004 journal article), Hughes (WO 2005/117861), and/or Brazg (a 2005 journal abstract).
• Core Argument for this Ground:
  • Prior Art Mapping: This ground presented an argument of obvious substitution. The ’510 publication taught that linagliptin is a potent DPP-IV inhibitor suitable for combination with metformin. The secondary references (Ahrén, Hughes, and Brazg) each independently demonstrated the safety and enhanced efficacy of combining other DPP-IV inhibitors (vildagliptin and sitagliptin) with standard therapeutic doses of metformin. These references provided clinical data showing that such combinations were more effective at controlling blood glucose than metformin monotherapy.
  • Motivation to Combine: A POSITA would be motivated to substitute linagliptin for the vildagliptin or sitagliptin used in the combinations described by Ahrén, Hughes, and Brazg. Linagliptin was a known member of the same drug class with the same mechanism of action. The ’510 publication taught that linagliptin was particularly potent, providing a further incentive for a POSITA to try it in an already-proven combination therapy strategy to achieve even better results or use smaller doses.
  • Expectation of Success: The expectation of success would be high because a POSITA would expect one DPP-IV inhibitor to function similarly to another in combination with metformin. Given that linagliptin shared its mechanism of action with the DPP-IV inhibitors already proven effective in combination with metformin, success in treating type II diabetes was predictable.

4. Relief Requested

• Petitioner requests institution of an inter partes review and cancellation of claims 1-26 of Patent 8,673,927 as unpatentable.