Trials@uspto.gov
`571-272-7822
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` Paper No. 9
`Filed: June 29, 2016
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`UNITED STATES PATENT AND TRADEMARK OFFICE
`____________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`____________
`
`LUPIN LIMITED and LUPIN PHARMACEUTICALS INC.,
`Petitioner,
`
`v.
`
` iCEUTICA PTY LTD.,
`Patent Owner.
`____________
`
`Case IPR2016-00397
`Patent 8,999,387 B2
`____________
`
`
`Before TONI R. SCHEINER, SHERIDAN K. SNEDDEN, and
`ZHENYU YANG, Administrative Patent Judges.
`
`YANG, Administrative Patent Judge.
`
`
`
`
`DECISION
`Denying Institution of Inter Partes Review
`37 C.F.R. § 42.108
`
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`571-272-7822
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` Paper No. 9
`Filed: June 29, 2016
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`
`
`
`
`
`
`UNITED STATES PATENT AND TRADEMARK OFFICE
`____________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`____________
`
`LUPIN LIMITED and LUPIN PHARMACEUTICALS INC.,
`Petitioner,
`
`v.
`
` iCEUTICA PTY LTD.,
`Patent Owner.
`____________
`
`Case IPR2016-00397
`Patent 8,999,387 B2
`____________
`
`
`Before TONI R. SCHEINER, SHERIDAN K. SNEDDEN, and
`ZHENYU YANG, Administrative Patent Judges.
`
`YANG, Administrative Patent Judge.
`
`
`
`
`DECISION
`Denying Institution of Inter Partes Review
`37 C.F.R. § 42.108
`
`
`
`
`
`
`
`
`
`
`IPR2016-00397
`Patent 8,999,387 B2
`
`
`INTRODUCTION
`Lupin Limited and Lupin Pharmaceuticals, Inc. (collectively
`“Petitioner”) filed a Petition for an inter partes review of claims 1–24 of
`U.S. Patent No. 8,999,387 B2 (Ex. 1001, “the ’387 patent”). Paper 1
`(“Pet.”). iCeutica Pty Ltd. (“Patent Owner”) filed a Preliminary Response.
`Paper 8 (“Prelim. Resp.”). We review the Petition under 35 U.S.C. § 314.
`Based on this record, we determine Petitioner has not established a
`reasonable likelihood that it would prevail in showing the unpatentability of
`at least one challenged claim. See 35 U.S.C. § 314(a). Therefore, we deny
`the Petition for an inter partes review.
`Related Proceedings
`According to the parties, Patent Owner previously asserted the
`’387 patent against Petitioner in iCeutica Pty Ltd. v. Lupin Limited, No.
`1:14-cv-01515 (D. Del.). Pet. 1; Paper 5, 3.
`Petitioner also concurrently filed a petition in IPR2016-00399,
`seeking an inter partes review of U.S. Patent No. 9,017,721 B2, a patent in
`the same family as the ’387 patent. Pet. 1–2; Paper 5, 3.
`The ’387 Patent
`The ’387 patent relates to methods for producing particles of
`diclofenac using dry milling processes and methods for treating pain using a
`therapeutically effective amount of diclofenac in particulate form. Ex. 1001,
`Abstract, 1:16–22.
`The ’387 patent discloses that diclofenac, a pain medication, “is a
`poorly water soluble drug so dissolution and absor[p]tion to the body is
`slow.” Id. at 3:6–10. At the time of the ’387 patent invention, it was known
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`IPR2016-00397
`Patent 8,999,387 B2
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`that decreasing particle size increases the surface area of a particulate drug,
`which in turn increases the rate of its dissolution. Id. at 1:43–45. According
`to the ’387 patent, then-existing dry milling techniques used to reduce
`particle size, however, have various drawbacks. Id. at 1:49–59, 2:65–66.
`The ’387 patent purportedly discloses a milling process that overcomes such
`problems. Id. at 2:66–3:3. Diclofenac made by this process has improved
`dissolution and faster absorption, which result in a more rapid onset of the
`therapeutic effect. Id. at 3:9–13.
`Illustrative Claims
`Among the challenged claims, claims 1 and 11 are independent. They
`are reproduced below:
`1.
`A method for treating pain comprising administering a
`solid oral unit dose of a pharmaceutical composition containing
`18 mg of diclofenac acid, wherein the diclofenac acid has a
`median particle size, on a volume average basis, of less than
`1000 nm and greater than 25 nm, wherein the unit dose, when
`tested in vitro by USP Apparatus I (Basket) method of
`U.S. Pharmacopoeia at 100 rpm, at 37º C. in 900 ml of 0.05%
`sodium lauryl sulfate in citric acid solution buffered to pH 5.75,
`has a dissolution rate of diclofenac acid such that at least 94%,
`by weight, is released by 75 minutes.
`11. A method for treating pain comprising administering a
`solid oral unit dose of a pharmaceutical composition containing
`35 mg of diclofenac acid, wherein the diclofenac acid has a
`median particle size, on a volume average basis, of less than
`1000 nm and greater than 25 nm, wherein the unit dose, when
`tested in vitro by USP Apparatus I (Basket) method of
`U.S. Pharmacopoeia at 100 rpm, at 37º C. in 900 ml of 0.05%
`sodium lauryl sulfate in citric acid solution buffered to pH 5.75,
`has a dissolution rate of diclofenac acid such that at least 95%,
`by weight, is released by 75 minutes.
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`IPR2016-00397
`Patent 8,999,387 B2
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`
`Asserted Grounds of Unpatentability
`Petitioner asserts the following grounds, each of which challenges the
`patentability of claims 1–24:
`References
`Basis
`Meiser1 and Norvatis Package Insert2
`§ 103
`Meiser, Norvatis Package Insert, USP,3 and Chuasuwan4
`§ 103
`§ 103 Meiser, Norvatis Package Insert, USP, Chuasuwan, and Reiner5
`
`In support of its patentability challenge, Petitioner relies on the
`Declaration of Dr. Mansoor M. Amiji. Ex. 1002.
`ANALYSIS
`Claim Construction
`In an inter partes review, the Board interprets a claim term in an
`unexpired patent according to its broadest reasonable construction in light of
`the specification of the patent in which it appears. 37 C.F.R. § 42.100(b);
`Cuozzo Speed Techs., LLC v. Lee, No. 15-446, 2016 WL 3369425 (U.S.
`June 20, 2016).
`
`
`1 Meiser et al., International Pub. No. WO2008/000042, published
`January 3, 2008 (Ex. 1005, “Meiser”).
`2 Novartis Package Insert for Cataflam®, Voltaren®, and Voltaren®-XR,
`dated May 2000 (Ex. 1006, “Norvatis Package Insert”).
`3 United States Pharmacopeia 30, Sections <711> and <1092>, dated
`May 2007 (Exs. 1007, 1008, collectively “USP”).
`4 Chuasuwan et al., Biowaiver Monographs for Immediate Release Solid
`Oral Dosage Forms Diclofenac Sodium and Diclofenac Potassium, 98 J.
`PHARM. SCIS. 1206–19 (2009) (Ex. 1009, “Chuasuwan”).
`5 Reiner et al., International Pub. No. WO2006/133954, published
`December 21, 2006 (Ex. 1010, “Reiner”).
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`IPR2016-00397
`Patent 8,999,387 B2
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`Petitioner contends that the “wherein . . . when tested” clause recited
`in each independent claim, i.e., “wherein the unit dose, when tested in vitro
`by USP Apparatus I (Basket) method of U.S. Pharmacopoeia at 100 rpm, at
`37º C. in 900 ml of 0.05% sodium lauryl sulfate in citric acid solution
`buffered to pH 5.75, has a dissolution rate of diclofenac acid such that at
`least 94% [/95%], by weight, is released by 75 minutes,” deserves no
`patentable weight. Pet. 32–36. Patent Owner disagrees, arguing that the
`clause is entitled to patentable weight. Prelim. Resp. 17–28.
`Claim terms need only be construed to the extent necessary to resolve
`the controversy. Wellman, Inc. v. Eastman Chem. Co., 642 F.3d 1355, 1361
`(Fed. Cir. 2011). On this record and for purposes of this Decision, we see no
`need to construe any term expressly.
`Prior Art Disclosures
`Meiser teaches improving the solubility of diclofenac acid by dry
`milling to obtain nanoparticles. Ex. 1005, 68–69, 71–72. According to
`Meiser, drugs in nanoparticulate form have advantages over conventional
`compounds, including more rapid therapeutic action and achieving a given
`therapeutic effect with a lower dose. Id. at 7.
`Norvatis Package Insert teaches tablets of diclofenac, in the form of
`sodium or potassium salt, for treating pain. Ex. 1006, 2.
`USP teaches performing the dissolution procedure in Apparatus 1 at
`37ºC. Ex. 1007, 278, 282; Ex. 1008, 581. It suggests the agitation speed,
`volume, surfactants, pH range, and time points for measuring the
`dissolution. Ex. 1008, 580–81.
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`Patent 8,999,387 B2
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`Chuasuwan reviews the solubility of diclofenac salts. Ex. 1009, 8.
`According to Chuasuwan, at “below pH 4.5 (or pH 5.8, depending on the
`tablet strength),” diclofenac salts are not highly soluble. Id. at 9.
`Reiner teaches performing the USP dissolution test to determine
`dissolution times for diclofenac sodium tablet and capsule to dissolve “90 or
`95 wt.% of the drug substance.” Ex. 1010, 22. In a preferred embodiment,
`Reiner teaches the dissolution profile is “not less than 85, 90 or 95% after
`15 minutes in simulated intestinal fluid (i.e. water) at pH=6.8.” Id.
`Obviousness over Meiser and Norvatis Package Insert
`Petitioner contends that the combination of Meiser and Norvatis
`Package Insert renders claims 1–24 obvious. Pet. 37–47. Based on the
`record before us, and for at least the following reasons, we determine
`Petitioner has not established a reasonable likelihood that it would prevail in
`this assertion.
`For this ground of unpatentability, Petitioner asserts that the “wherein
`. . . when tested” clauses of the independent claims should not be given
`patentable weight. Pet. 32–36, 38. Patent Owner challenges this assertion.
`Prelim. Resp. 17–28. We do not need to resolve this issue. Even assuming
`we accord the “wherein . . . when tested” clauses no patentable weight, we
`are not persuaded that the combination of Meiser and Norvatis Package
`Insert renders the challenged claims obvious, because Petitioner has not
`sufficiently addressed the claimed dosage of diclofenac acid.
`Petitioner refers to Norvatis Package Insert for teaching tablets of
`25 mg, 50 mg, and 75 mg diclofenac sodium. Id. at 38–39; Ex. 1006, 2.
`According to Petitioner, diclofenac, like other non-steroidal anti-
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`Patent 8,999,387 B2
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`inflammatory drugs (NSAIDs), has been associated with some side effects.
`Pet. 4–5 (citing Ex. 1009, 1208). Petitioner argues, “one of ordinary skill
`knew at the time of the ’387 patent that reducing the required dose of
`NSAIDs, such as diclofenac, would reduce the known negative side-effects
`of NSAIDs.” Id. at 5.
`Petitioner then refers to Meiser where it teaches improving the
`solubility of diclofenac acid by dry milling to obtain nanoparticles. Id. at 9
`(citing Ex. 1005, 6–7, 27–28). Petitioner points out that compounds in
`nonparticulate form “exhibit advantages over conventional compounds by
`way of, for example, more rapid therapeutic action or lower dose.” Id. at 39
`(citing Ex. 1005, 7).
`Petitioner concludes an ordinary artisan “would have been motivated
`to combine the prior art dosages in the Novartis Package Insert with the
`teachings of Meiser to develop a formulation containing a dosage lower than
`the prior art dosages.” Id. at 39. Specifically, according to Petitioner,
`“starting from the 25 mg disclosed the Novartis Package Insert,” the claimed
`dose of 18 mg of diclofenac acid in claim 1 “would have been the result of
`merely routine optimization.” Id. For claim 11, Petitioner argues that “it
`would have been obvious to lower the 50 mg dose described in the Novartis
`Package Insert to 35 mg to reduce the [side effects] of diclofenac acid.” Id.
`at 44 (citing Ex. 1002 ¶ 111). We are not persuaded.
`The challenged claims are directed to methods of treating pain with a
`pharmaceutical composition containing diclofenac acid. The Novartis
`Package Insert, however, provides information on diclofenac salts. See
`Ex. 1006, 1 (describing diclofenac “as the sodium or potassium salt”), 2
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`IPR2016-00397
`Patent 8,999,387 B2
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`(providing diclofenac sodium tablets in the doses of 25 mg, 50 mg, and
`75 mg). Formulating water-soluble salts and reducing drug particle size
`through milling are two independent methods to improve the solubility of a
`poorly soluble drug. Ex. 1001, 1:63–65, 2:32–35. Petitioner acknowledges
`so. Pet. 6. Petitioner also acknowledges the drawbacks of the salt approach.
`Id. Petitioner further appears to recognize that diclofenac salt and diclofenac
`acid have different properties. See, e.g., Pet. 58 (stating that the formulation
`in Reiner, a prior art reference not relied on in this obviousness challenge,
`“includes diclofenac sodium, not diclofenac acid”). Yet, Petitioner does not
`point to credible evidence or otherwise explain why an ordinary artisan
`would have modified 25 mg and 50 mg of diclofenac sodium taught in the
`Novartis Package Insert to reach 18 mg and 35 mg of diclofenac acid recited
`in claims 1 and 11, respectively. Thus, we are not persuaded that the
`combination of the Novartis Package Insert and Meiser teaches or suggests
`the claimed dosage.
`In sum, based on the record before us, we determine that Petitioner
`has not shown a reasonable likelihood that it would prevail in showing the
`challenged claims would have been obvious over Meiser and the Novartis
`Package Insert.
`
`Other Obviousness Grounds
`Petitioner argues that that the combination of Meiser, the Norvatis
`Package Insert, USP, and Chuasuwan renders claims 1–24 obvious. Pet. 47–
`57. Petitioner also contends that combination, further in view of Reiner,
`renders claims 1–24 obvious. Pet. 57–58. Based on the record before us, we
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`IPR2016-00397
`Patent 8,999,387 B2
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`determine Petitioner has not established a reasonable likelihood that it would
`prevail in either assertion.
`In these two obviousness challenges, Petitioner repeats that the
`combination of Meiser and the Novartis Package Insert suggests using 18
`and 35 mg of diclofenac acid, as recited in claims 1 and 11, respectively.
`Pet. 50. Petitioner relies on USP, Chuasuwan, and Reiner to address the
`dissolution profile recited in the “wherein . . . when tested” clauses. See
`Pet. 51–55, 57–58. In other words, the additional prior art references do not
`remedy the deficiency of Meiser and the Novartis Package Insert, as
`discussed above. As a result, we determine that Petitioner has not shown a
`reasonable likelihood that it would prevail in either of the additional
`obviousness challenges.
`
`CONCLUSION
`On this record, Petitioner has not demonstrated a reasonable
`likelihood of prevailing on its challenges to the patentability of any
`challenged claim of the ’387 patent on the grounds asserted in the Petition.
`ORDER
`
`Accordingly, it is
`ORDERED that Petitioner’s request for an inter partes review of
`claims 1–24 of the ’387 patent is denied and no inter partes review is
`instituted.
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`IPR2016-00397
`Patent 8,999,387 B2
`
`PETITIONER:
`
`Christy Lea
`Kerry Taylor
`Benjamin Anger
`KNOBBE, MARTENS, OLSON & BEAR, LLP
`2cgl@knobbe.com
`2kst@knobbe.com
`2bba@knobbe.com
`
`
`PATENT OWNER:
`
`Dorothy Whelan
`Martina Tyreus Hufnal
`FISH & RICHARDSON P.C.
`IPR31215-0011IP3@fr.com
`PTAB-Inbound@fr.com
`
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`10
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