PTAB

IPR2017-00631

Complex Innovations LLC v. AstraZeneca Ab

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1. Case Identification

2. Patent Overview

  • Title: Pharmaceutical Compositions
  • Brief Description: The ’328 patent relates to a stable pharmaceutical aerosol formulation for inhalation. The formulation comprises the active ingredients formoterol and budesonide, a hydrofluoroalkane (HFA) propellant, and the excipients polyvinylpyrrolidone (PVP) and polyethylene glycol (PEG) to achieve enhanced physical suspension stability.

3. Grounds for Unpatentability

Ground 1: Anticipation by Mistry - Claims 1 and 4-15 are anticipated under 35 U.S.C. § 102 by Mistry.

  • Prior Art Relied Upon: Mistry (Patent 6,123,924).
  • Core Argument for this Ground:
    • Prior Art Mapping: Petitioner argued that Mistry teaches every element of the challenged claims. Mistry discloses a stable, pressurized aerosol formulation for treating respiratory diseases, specifically teaching the use of HFA 227 as a preferred propellant. It identifies both formoterol (and its salts, like formoterol fumarate dihydrate) and budesonide as suitable medicaments and explicitly teaches combining a bronchodilator with a prophylactic agent. Critically, Mistry teaches using PVP with K-values between 15 and 120 (which encompasses the claimed K-value of 25) at a concentration of at least 0.001% w/w. It also teaches using PEG as a valve lubricant with a preferred molecular weight range of 400 to 2000 (encompassing the claimed 1000) and a concentration range of 0.1% to 2% w/w (encompassing the claimed 0.3%). Mistry further discloses treating “reversible obstructive airways diseases,” which a POSITA would understand to include asthma, rhinitis, and COPD (claims 4-7).

Ground 2: Obviousness over Mistry, Rogueda, and Carling - Claims 1 and 4-15 are obvious over Mistry in view of Rogueda and Carling.

  • Prior Art Relied Upon: Mistry (Patent 6,123,924), Rogueda (WO 02/03958), and Carling (Patent 5,674,860).
  • Core Argument for this Ground:
    • Prior Art Mapping: Petitioner asserted that Carling first taught the combination of the active ingredients formoterol and budesonide for treating respiratory disorders, but in an older chlorofluorocarbon (CFC) based formulation. Mistry taught a general solution for creating a stable, non-CFC formulation using an HFA propellant (HFA 227) with the same active ingredients and the same classes of excipients (PVP for stability and PEG for lubrication). Rogueda then provided the exact, optimized parameters for commercialization, teaching the specific PVP K25 and PEG 1000 at the precise concentrations of 0.001% and 0.3% w/w, respectively, as recited in the ’328 patent claims.
    • Motivation to Combine: A POSITA would be motivated by regulatory pressure (the Montreal Protocol phasing out CFCs) and commercial interest to reformulate the successful drug combination from Carling into a modern, non-CFC inhaler. A POSITA would look to Mistry for a known, stable HFA-based platform for these drugs. To avoid time-consuming and routine experimentation, the POSITA would then consult Rogueda, which discloses specific, successful formulations and control samples, to arrive at the precise, optimized formulation.
    • Expectation of Success: A POSITA would have a high expectation of success, as combining these references involved using known components for their predictable and intended functions: replacing a CFC propellant with a known HFA alternative, using a known stabilizer (PVP), and adding a known lubricant (PEG) at concentrations shown to be effective in the art.

Ground 3: Obviousness of Isomer Claims - Claims 2 and 3 are obvious over Mistry and Rogueda in view of Meade and Lewis.

  • Prior Art Relied Upon: Mistry (Patent 6,123,924), Rogueda (WO 02/03958), Meade (Application # 2003/0018019), and Lewis (Patent 8,142,763).

  • Core Argument for this Ground:

    • Prior Art Mapping: Petitioner contended that claims 2 and 3, which specify particular stereoisomers of the active ingredients, were obvious improvements upon the base formulation disclosed by Mistry and Rogueda. Meade explicitly teaches that the R,R-enantiomer of formoterol (recited in claim 2) provides therapeutic benefits with decreased side effects. Similarly, Lewis teaches that using the 22R-epimer of budesonide (recited in claim 3) results in a more stable formulation due to reduced interaction with the interior walls of the inhaler canister.
    • Motivation to Combine: A POSITA, having developed the stable base formulation from Mistry and Rogueda, would be motivated to seek further improvements in stability and safety profile. The Meade and Lewis references provide known, specific solutions for improving the formulation by substituting the standard active ingredients with their known, more stable, and effective stereoisomers.
    • Expectation of Success: Success would be expected, as this modification involves the simple substitution of a known, improved version of an active ingredient into an established formulation to achieve its known, predictable benefits of enhanced stability and efficacy.

  • Additional Grounds: Petitioner also asserted that claims 1 and 4-15 are anticipated by Rogueda (WO 02/03958), which allegedly discloses a Symbicort HFA formulation with the exact same components and concentrations as the challenged claims.

4. Relief Requested

  • Petitioner requests institution of an inter partes review and cancellation of claims 1-15 of Patent 7,759,328 as unpatentable.