Olopatadine - USA

On Mar. 01, 2018, Judge Gregory M. Sleet of Delaware held that Defendants failed to present a primafacie case that the asserted claims of the patents-in-suit are invalid as obvious in Pazeo® Hatch-Waxman litigation.

In this patent infringement action, Alcon Research, Ltd. alleged that Watson Labs., Inc., Lupin Ltd., and Lupin Pharma. Inc., (collectively, "the Defendants") infringed the asserted claims of the patents-in-suit. Alcon has asserted claims 4-6, 8-10, 12-14, and 20-27 of US 8,791,154 Patent. The US’154 relates to "High Concentration Olopatadine Ophthalmic Composition”. The court held a four-day bench trial in this matter beginning on October 2, 2017. Presently before the court are the parties' post-trial proposed findings of fact and conclusions of law concerning the validity of the patents-in-suit, specifically whether the asserted claims are invalid as obvious under 35 U.S.C. § 103.

The obviousness analysis hinges on the core elements of the independent claims asserted, 8 and 21 which require: (1) an aqueous ophthalmic solution for treatment of ocular allergic conjunctivitis comprising; (2) at least 0.67 w/v% but no greater that 1.0 w/v % olopatadine dissolved in the solution; (3) 2.0 w/v% to 1.0 w/v% PEG having a molecular weight of 300 to 500; (4) 2.0 w/v% to 6.0 w/v% polyvinylpyrrolidone ("PVP") at least 0.5 w/v% but no greater than 2.0 w/v% hydroxypropyl-y cyclodextrin ("HPyCD"); and (5) water.

Defendants argued that the asserted claims were obvious for six reasons:  

(1) that it would have been obvious to select a concentration of 0.67% to 1.0% w/v olopatadine;

(2) a POSA would have been motivated to develop a solution;

(3) a POSA would have known how to achieve a 0.67 to 1.0% olopatadine solution;

( 4) it was well within the level of ordinary skill to determine suitable amounts of the solubilizing agents for use with olopatadine;

(5) Dr. Olejnik's opinions are conclusory and unsupported; and

(6) claims 9 and 21- 24 require only standard ophthalmic excipients and physical properties that would have been obvious to a POSA.

It was clear after a recitation of the prior art, a 0.67-1.0% w/v olopatadine concentration at a near-neutral pH was not disclosed in the references that pre-date the patent-in-suit. Defendants argued that a combination of Hayakawa, Yanni 2002, and Yanni 2008 would make the selection of 0.67 to 1.0 % w/v olopatadine at a near neutral pH obvious to a POSA. The court however, disagreed & found that persons having ordinary skill in the art would not have selected a concentration of 0.67 to 1.0% w/v olopatatdine to treat allergic conjunctivitis in light of the asserted prior art because reference does not teach an ophthalmic solution with at least 0.67% olopatadine. Court further said that while Defendants suggested that the POSA would have been motivated to formulate a solution in order to improve upon the efficacy of Pataday® between 16 and 24 hours, they presented no evidence that the POSA recognized such a need. The court found that a POSA would be concerned that a more than three-fold increase in the concentration from 0.2% (as in Pataday®) to at least 0.67% would increase redness.

Court further held that with only general teachings and no disclosures in the art of the claimed ternary system, the POSA would have had no guidance to choose the correct combination of excipients, at the proper concentrations, to solubilize 0 .67-1.0% olopatadine at near-neutral pH. Court concluded that routine optimization would not lead a POSA to develop the claimed solution given the complexity of ophthalmic formulation. More specifically, the POSA would not have been motivated, based on what was known in the prior art, to make the claimed solution by combining all of the elements of the claims in the particular way they are recited, and have a reasonable expectation of success in doing so.

In sum, Defendants have failed to present a primafacie case that the asserted claims of the patents-in-suit are invalid as obvious. Additionally, the court found that the secondary, objective indicia point towards a finding of non-obviousness. Thus, the asserted claims were not invalid as obvious.