PTAB

IPR2013-00015

Apotex Inc v. Alcon

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1. Case Identification

2. Patent Overview

  • Title: Method of Treating Ophthalmic Infections with Moxifloxacin Compositions
  • Brief Description: The ’070 patent discloses methods for treating ophthalmic infections. The methods comprise topically applying to the eye a pharmaceutical composition containing moxifloxacin in a concentration of 0.1 to 1.0 wt. % in a pharmaceutically acceptable vehicle.

3. Grounds for Unpatentability

Ground 1: Anticipation Over ’942 Patent - Claims 1, 15, and 17-19 are anticipated by the ’942 patent.

  • Prior Art Relied Upon: Patent 5,607,942 (’942 patent).
  • Core Argument for this Ground:
    • Prior Art Mapping: Petitioner argued that the ’942 patent disclosed every element of the challenged claims. The ’942 patent taught using moxifloxacin to treat "eye infections" by formulating it in ophthalmological preparations like "eye ointments or drops" for "local therapy." The ’942 patent’s disclosed concentration range of "about 0.1 to 99.5%" by weight entirely subsumed the ’070 patent’s claimed range of 0.1 to 1.0 wt. %. Petitioner contended this subsumed range was not critical and therefore anticipated. For dependent claims, the ’942 patent disclosed treating infections caused by pathogens known to cause conjunctivitis (e.g., S. aureus, S. epidermidis), thereby inherently disclosing the treatment of conjunctivitis.
    • Key Aspects: The central argument was that the claimed concentration range was merely a selection from a broader, explicitly disclosed range in the prior art without any evidence of criticality or unexpected results, which under controlling case law constitutes anticipation.

Ground 2: Obviousness over ’942 patent and OCUFLOX® PDR - Claim 1 and its dependent claims are obvious over the ’942 patent in view of OCUFLOX® PDR.

  • Prior Art Relied Upon: ’942 patent and OCUFLOX® PDR (product information for Ofloxacin ophthalmic solution 0.3% from the 1996 Physician's Desk Reference).
  • Core Argument for this Ground:
    • Prior Art Mapping: The ’942 patent established moxifloxacin as a known antibacterial compound suitable for treating eye infections in ophthalmic formulations. OCUFLOX® PDR disclosed a commercially successful sterile ophthalmic solution for treating eye infections that used ofloxacin, a fluoroquinolone from the same class as moxifloxacin. The OCUFLOX® product had a concentration of 0.3%, which fell directly within the ’070 patent’s claimed range of 0.1 to 1.0 wt. %.
    • Motivation to Combine: A person of ordinary skill in the art (POSITA) would combine the teachings to develop an improved or alternative topical ophthalmic therapy. Knowing from the ’942 patent that moxifloxacin was a potent antibacterial, a POSITA would look to existing, successful formulations like OCUFLOX® as a template. A POSITA would have been motivated to substitute the known compound moxifloxacin for ofloxacin to create an alternative therapy effective against Gram-positive and Gram-negative bacteria. The 0.3% concentration of OCUFLOX® provided a clear reason to formulate moxifloxacin at a similar concentration.
    • Expectation of Success: A POSITA would have had a high expectation of success. The ’942 patent taught moxifloxacin’s suitability for ophthalmic use, and OCUFLOX® PDR demonstrated that a fluoroquinolone could be safely and effectively formulated as a 0.3% topical ophthalmic solution. Therefore, creating a similar formulation with moxifloxacin would have been a routine and predictable endeavor.

Ground 3: Obviousness over ’942 patent and CILOXAN® PDR - Claim 1 and its dependent claims are obvious over the ’942 patent in view of CILOXAN® PDR.

  • Prior Art Relied Upon: ’942 patent and CILOXAN® PDR (product information for Ciprofloxacin HCl ophthalmic solution 0.3% from the 1996 Physician's Desk Reference).

  • Core Argument for this Ground:

    • Prior Art Mapping: This ground presented a parallel argument to Ground 2. The ’942 patent provided the base teaching of using moxifloxacin for eye infections. CILOXAN® PDR disclosed another commercially successful 0.3% ophthalmic solution using ciprofloxacin, a different but structurally similar fluoroquinolone.
    • Motivation to Combine: The motivation was identical to that in Ground 2: to develop an alternative topical therapy. A POSITA would substitute moxifloxacin for ciprofloxacin, using the successful CILOXAN® product as a guide for formulation and concentration.
    • Expectation of Success: The expectation of success was similarly high. CILOXAN® provided further evidence that 0.3% was a safe and effective concentration for a topical fluoroquinolone antibacterial, making the successful formulation of moxifloxacin at that concentration predictable.

  • Additional Grounds: Petitioner asserted additional obviousness challenges based on combinations including Petersen Abstract (a 1996 publication disclosing moxifloxacin's high aqueous solubility, further enhancing the expectation of success) and Dalhoff (a 1996 article disclosing moxifloxacin as a potent, broad-spectrum antibiotic superior to ciprofloxacin against certain bacteria). These references were combined with the ’942 patent, OCUFLOX® PDR, and CILOXAN® PDR to reinforce the primary obviousness arguments. The dependent claims were argued to be obvious as they recited routine and predictable formulation parameters (e.g., pH, tonicity, preservatives) disclosed in the commercial OCUFLOX® and CILOXAN® products.

4. Relief Requested

  • Petitioner requests institution of IPR and cancellation of claims 1, 15, 17-20, 22-32, and 34-41 as unpatentable.