IPR2015-00988 (U.S. Pat. No. 6,773,720 B1)
Final Written Decision
October 5, 2016
Brief Summary: CAD’s obviousness arguments regarding Shire’s US 6,773,720B1 relating to Lialda (5-ASA; used to treat Crohn’s disease and ulcerative colitis) found not to meet the preponderance of evidence standard.
Summary: US 6,773,720B1 is the only patent listed on the OB for Shire’s Lialda for treating Crohn’s disease and ulcerative colitis (Mesalamine (5-amino salicylic acid (5-ASA); NDA N022000). CAD argued the ‘720 claims (1-4) would have been obvious over two prior art references (EP 0375063A1 (“Groenendaal”) and US 3,965,256 (“Leslie”)). Each Party submitted expert delcarations in support of their respective positions. Mulitple related litigations were identified. Independent claim 1 is directed to “[c]ontrolled-release oral…compositions” of “95% by weight” 5-ASA”, “comprising…an inner lipophilic matrix consisting of” particular substances, “an outer hydrophilic matrix…consisting of” particular substances in which “the lipophilic matrix is dispersed”, “optionally other excipients”, where the 5-ASA is “dispersed” in “both” matrices. Claim 2 depends on claim 1 and requires the 5-ASA to be “dispersed in a molten lipophilic matrix by kneading, extrusion and/or granulation.” Claim 3 requires the composition of claim 1 to be “in the form of tablets, capsules, [or] minitablets.” Claim 4 is directed to a melt granulation-based process for preparing the compositions of claim 1. The PTAB found the level of skill in the art to be one with a Bachelor’s degree in pharmacy and at least two years experience in the field. The claims of this unexpired patent were given their “broadest reasonable construction” (In re Cuozzo, US 2016) and accepted the Petitioner’s construction of “matrix” and the “consisting of” terms. The term “waxes” was construed (based on intrinsic and extrinsic evidence) as requested by Cosmo to “refer to esters of alcohols and fatty acids, and…not…higher alcohols that are not in ester form” (not cetyl alcohol or cetostearyl alcohol). This was important to the obviousness analysis since “Petitioner contend[ed] that cetyl alcohol…is a wax, and therefore qualifies as a lipophilic matrix” and was disclosed in the prior art (cetostearyl alcohol was also argued to be a wax and disclosed by Leslie). As such, the Board concluded, “Petitioner does not establish sufficiently that Leslie discloses the ‘inner lipophilic matrix’ of claim 1” or that “the combination [of Leslie and Groenendaal] would result in the compositions recited in claim 1.” It explained that Petitioner, “[r]ather than picking ‘known options’ from a ‘finite number of identified, predictable solutions’ [KSR], Petitioner’s obviousness challenge is more akin to ‘merely throw[ing] metaphorical darts at a board filled with combinatorial prior art possibilities’ when the prior art gave little or conflicting indications as to which parameters were critical or which of the many possible choices were likely to be successful” (In re Kubin, FC 2009; In re O’Farrell (FC 1988) (e.g., “Petitioner does not explain adequately…why one ‘would have been motivated to look to Leslie’ in particular to ‘improve’ the 5-ASA compositions disclosed in Groenendaal when one takes into account the crowded art of controlled release formulations generally.”)) It stated that “[a]t best for Petitioner, the record before us indicates a close call, but certainly not a strong case, regarding…the preponderance of evidence” and “the burden of persuasion is on Petitioner” (In re Magnum Oil Tools, FC 2016). And evidence of secondary considerations (e.g., long-felt but unresolved need, commercial success) were “not insubstantial”.