PTAB

IPR2020-00369

GlaxoSmithKline Consumer Healthcare Holdings US LLC v. Cipla Ltd

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Key Events
Petition
petition

1. Case Identification

2. Patent Overview

  • Title: Pharmaceutical Formulations Comprising Azelastine and Fluticasone
  • Brief Description: The ’620 patent relates to pharmaceutical formulations for nasal administration that combine azelastine (an antihistamine) and fluticasone (a corticosteroid). The formulations are intended for treating conditions such as allergic rhinitis.

3. Grounds for Unpatentability

Ground 1: Obviousness over PDR 1999 and Segal - Claims 1-18, 21-22, 24-26, 28-29, 31, 33, and 35-47 are obvious over PDR 1999 in view of Segal.

  • Prior Art Relied Upon: PDR 1999 (the 1999 Physicians' Desk Reference), Segal (International Publication No. WO 98/48839).
  • Core Argument for this Ground:
    • Prior Art Mapping: Petitioner argued that PDR 1999 disclosed all necessary components of the claimed invention, albeit in separate commercial products. Specifically, PDR 1999 described Astelin®, an FDA-approved nasal spray containing azelastine hydrochloride, and Flonase®, an FDA-approved aqueous nasal spray containing fluticasone propionate. Segal taught combining a topical anti-inflammatory agent (like fluticasone) with at least one other therapeutic agent (explicitly naming azelastine) into a single formulation for nasal administration. The combination of these references, Petitioner asserted, disclosed every limitation of the independent claims.
    • Motivation to Combine: A POSITA would combine the well-known, effective products from PDR 1999 based on the explicit teachings of Segal. Segal provided multiple rationales, including achieving convenient administration in a single composition, providing additive and synergistic effects, and overcoming the known disadvantages of separate administration, such as patient inconvenience and compromised compliance. Further motivation stemmed from the known complementary mechanisms of action, where azelastine targets the early-phase allergic reaction and fluticasone targets the late-phase reaction.
    • Expectation of Success: A POSITA would have a high expectation of success because both azelastine and fluticasone were known to be safe and effective for nasal administration, as confirmed by their FDA approval noted in PDR 1999. Segal's disclosure of their combined use, coupled with the general knowledge of standard pharmaceutical formulation techniques, would lead a POSITA to reasonably expect a successful and useful co-formulation.
    • Key Aspects: Petitioner contended that various dependent claim limitations were also rendered obvious. These included specific concentrations, aqueous suspension forms, particle sizes (<10 µm), pH ranges, and the use of common excipients (surfactants, preservatives, thickening agents), all of which were either disclosed in the PDR 1999 descriptions of Astelin® and Flonase® or were well-known and predictable choices for a formulator.

Ground 2: Obviousness over PDR 1999, Segal, and Hettche - Claim 48 is obvious over PDR 1999 in view of Segal and Hettche.

  • Prior Art Relied Upon: PDR 1999, Segal, and Hettche (Patent 5,164,194).
  • Core Argument for this Ground:
    • Prior Art Mapping: This ground specifically targeted claim 48, which differs from other claims by reciting a precise concentration of "1% (weight/weight) of azelastine hydrochloride." The core argument mirrored Ground 1, establishing the general obviousness of the combination. The additional reference, Hettche, was introduced to specifically teach azelastine formulations with a concentration range that explicitly encompassed the claimed 1% value.
    • Motivation to Combine: The motivation was identical to that in Ground 1, with Hettche providing a specific teaching that would have guided a POSITA to select the concentration recited in claim 48.
    • Expectation of Success: The expectation of success was based on the same reasoning as Ground 1, strengthened by Hettche's disclosure of a viable concentration.

Ground 3: Obviousness over Cramer and PDR 1999 - Claims 1-18, 21-22, 24-26, 28-29, 31, 33, and 35-48 are obvious over Cramer in view of PDR 1999.

  • Prior Art Relied Upon: Cramer (European Application # EP 0,780,127), PDR 1999.
  • Core Argument for this Ground:
    • Prior Art Mapping: Petitioner argued that Cramer alone taught the core invention by disclosing pharmaceutical formulations for nasal administration comprising a glucocorticoid (explicitly naming fluticasone) and a leukotriene-inhibiting antihistamine (explicitly naming azelastine). PDR 1999 provided the specific, well-known, and commercially successful forms of these active ingredients: azelastine hydrochloride (Astelin®) and fluticasone propionate (Flonase®). Together, these references disclosed all limitations of the challenged claims.
    • Motivation to Combine: The primary motivation was derived directly from Cramer, which taught that combining these specific drug classes results in "improved intranasal compositions... providing improved relief of symptoms." A POSITA, seeking to implement Cramer's combination therapy, would have been motivated to use the specific, FDA-approved salt and ester forms detailed in PDR 1999 as a reliable and effective starting point.
    • Expectation of Success: A POSITA would have a strong expectation of success because Cramer taught the therapeutic benefits of the combination, and PDR 1999 demonstrated that the individual components were safe and effective. Cramer further taught that the combined formulation could be prepared using conventional mixing techniques, reinforcing the predictability of the outcome.

4. Arguments Regarding Discretionary Denial

  • Petitioner argued that discretionary denial under 35 U.S.C. §325(d) would be inappropriate. Although the examiner had considered Cramer during prosecution, the rejection was overcome based solely on alleged objective indicia of nonobviousness. Petitioner contended this evidence was flawed and did not actually demonstrate nonobviousness, meaning the substance of the primary obviousness case over Cramer had not been fully and properly evaluated on its merits.

5. Relief Requested

  • Petitioner requests institution of an inter partes review and cancellation of claims 1-18, 21-22, 24-26, 28-29, 31, 33, and 35-48 of the ’620 patent as unpatentable.