Trials@uspto.gov
`571.272.7822
`
`
`
`
`
`
`
`
` Paper No. 13
`
` Entered: November 9, 2016
`
`
`
`UNITED STATES PATENT AND TRADEMARK OFFICE
`____________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`____________
`
`AMNEAL PHARMACEUTICALS, LLC,
`Petitioner,
`
`v.
`
`PURDUE PHARMA L.P.,
`THE P.F. LABORATORIES, INC., and
`PURDUE PHARMACEUTICALS L.P.,
`Patent Owner.
`____________
`
`Case IPR2016-01027
`Patent 9,060,976 B2
`____________
`
`
`Before MICHAEL P. TIERNEY, LORA M. GREEN, and
`CHRISTOPHER G. PAULRAJ, Administrative Patent Judges.
`
`GREEN, Administrative Patent Judge.
`
`
`
`DECISION
`Institution of Inter Partes Review
`37 C.F.R. § 42.108
`
`
`
`
`
`
`
`
`KASHIV1054
`IPR of Patent No. 9,492,392
`
`

`

`IPR2016-01027
`Patent 9,060,976 B2
`
`
`INTRODUCTION
`
`Amneal Pharmaceuticals LLC (“Petitioner”) filed a Petition
`requesting an inter partes review of claim 1 of U.S. Patent No. 9,060,976 B2
`(Ex. 1001, “the ’976 patent”). Paper 2 (“Pet.”). Purdue Pharma L.P., The
`P.F. Laboratories, Inc., and Purdue Pharmaceuticals L.P. (collectively,
`“Patent Owner”) filed a Preliminary Response to the Petition. Paper 9
`(“Prelim. Resp.”).
`Institution of an inter partes review is authorized by statute when “the
`information presented in the petition . . . and any response . . . shows that
`there is a reasonable likelihood that the petitioner would prevail with respect
`to at least 1 of the claims challenged in the petition.” 35 U.S.C. § 314; see
`37 C.F.R. §§ 42.4, 42.108. Upon considering the Petition and the
`Preliminary Response, we determine that Petitioner has demonstrated a
`reasonable likelihood that it would prevail in showing the unpatentability of
`claim 1. Accordingly, we institute an inter partes review of that claim.
`Related Proceedings
`A.
`Petitioner states that the ’976 patent is asserted against it “in two civil
`actions pending in the United States District Court for the District of
`Delaware captioned Purdue Pharma L.P. et al. v. Amneal Pharmaceuticals
`LLC, 15-cv-831, filed September 17, 2015 (Ex. 1007), and Purdue Pharma
`L.P. et al. v. Amneal Pharmaceuticals LLC, 15-cv-1152, filed December 15,
`2015 (Ex. 1008).” Pet. 1.
`
`Petitioner states further that the claims of U.S. Patent No. 8,337,888
`B2 (Ex. 1002, the ’888 patent), of which the ’976 patent is a continuation
`(Ex. 1001), were also asserted against it, and were “held invalid in a district
`court proceeding in the Southern District of New York captioned Purdue
`
`2
`
`KASHIV1054
`IPR of Patent No. 9,492,392
`
`

`

`IPR2016-01027
`Patent 9,060,976 B2
`
`Pharma L.P. et al. v. Amneal Pharmaceuticals LLC, No. 13-cv-3372 (‘the
`SDNY Litigation’). The Federal Circuit upheld the invalidity of those
`claims on April 8, 2016 [Ex. 1004].” Pet. 1‒2.
`
`Finally, Petitioner notes that it filed a second Petition challenging the
`validity of claim 1 of the ’976 patent, IPR2016-01028. Id. at 2. IPR2016-
`01028 is being decided concurrently with the instant proceeding.
`The ’976 Patent (Ex. 1001)
`B.
`The ’976 patent issued on June 23, 2015, with Curtis Wright,
`
`Benjamin Oshlack, and Christopher Breder as the listed co-inventors.
`Ex. 1001. The ’976 patent is a continuation of application number
`13/349,449, which issued as the ’888 patent. Id.
`
`The ’976 patent notes that opioid analgesics may sometimes be
`subject to abuse. Id. at 1:17. According to the ’976 patent, the opioid
`analgesic may be more potent when injected after mixing with a suitable
`vehicle, or when crushed and administered orally or nasally. Id. at 1:18‒29.
`The ’976 patent discloses that “[o]pioid antagonists have been combined
`with certain opioid agonists in order to deter the parenteral abuse of opioid
`agonists,” but states that there is still a need of opioid dosage forms that are
`less subject to abuse Id. at 1:32‒34, 2:9‒11.
`
`Thus, the ’976 patent discloses “oral dosage forms . . . comprising an
`opioid analgesic; and an aversive agent or agents as a component(s) of the
`dosage form helps to prevent injection, inhalation, and/or oral abuse by
`decreasing the ‘attractiveness’ of the dosage form to a potential abuser.” Id.
`at 2:42‒47. The ’976 patent defines “aversive agent” as “a bittering agent,
`an irritant, a gelling agent, or combinations thereof.” Id. at 4:12‒14.
`
`3
`
`KASHIV1054
`IPR of Patent No. 9,492,392
`
`

`

`IPR2016-01027
`Patent 9,060,976 B2
`
`
`
`According to the ’976 patent:
`In certain embodiments of the present invention, the
`dosage form comprises an aversive agent such as a gelling agent
`to discourage an abuser from tampering with the dosage form
`and thereafter inhaling, injecting, and/or swallowing the
`tampered dosage form. Preferably, the gelling agent is released
`when the dosage form is tampered with and provides a gellike
`quality to the tampered dosage form which slows the absorption
`of the opioid analgesic such that an abuser is less likely to obtain
`a rapid “high”. In certain preferred embodiments, when the
`dosage form is tampered with and exposed to a small amount
`(e.g., less than about 10 ml) of an aqueous liquid (e.g., water),
`the dosage form will be unsuitable for injection and/or inhalation.
`Upon the addition of the aqueous liquid, the tampered dosage
`form preferably becomes thick and viscous, rendering it
`unsuitable for injection.
`Id. at 2:64‒3:11. Moreover, upon contact with the mucous membranes of
`the nasal passages the gelling agent may also become a gel, which sticks to
`the nasal passage, minimizing absorption of the opioid. Id. at 3:25‒30.
`
`The ’976 teaches as to the gelling agent:
`In certain embodiments of the present invention wherein
`the dosage form includes an aversive agent comprising a gelling
`agent, various gelling agents can be employed including, for
`example and without limitation, sugars or sugar derived alcohols,
`such as mannitol, sorbitol, and the like, starch and starch
`derivatives, cellulose derivatives, such as microcrystalline
`cellulose, sodium cahoxymethyl cellulose, methylcellulose,
`ethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose,
`and hydroxypropyl methylcellulose, attapulgites, bentonites,
`dextrins, alginates, carrageenan, gum tragacanth, gum acacia,
`guar gum, xanthan gum, pectin, gelatin, kaolin, lecithin,
`magnesium aluminum silicate, the carbomers and carbopols,
`polyvinylpyrrolidone, polyethylene glycol [PEG], polyethylene
`oxide [PEO], polyvinyl alcohol, silicon dioxide, surfactants,
`mixed surfactant/wetting agent systems, emulsifiers, other
`polymeric materials, and mixtures thereof, etc. In certain
`preferred embodiments, the gelling agent is xanthan gum. In
`
`4
`
`KASHIV1054
`IPR of Patent No. 9,492,392
`
`

`

`IPR2016-01027
`Patent 9,060,976 B2
`
`
`other preferred embodiments, the gelling agent of the present
`invention is pectin.
`Id. at 6:45‒63 (emphasis added).
`
`The ’976 patent teaches further:
`A gelling agent may be added to the formulation in a ratio of
`gelling agent to opioid agonist of from about 1:40 to about 40:1
`by weight, preferably from about 1:1 to about 30:1 by weight,
`and more preferably from about 2:1 to about 10:1 by weight of
`the opioid agonist. In certain alternative embodiments, the
`gelling agent may be present in a ratio to the opioid agonist of
`from about 1:15 to about 15:1, preferably in a ratio of from about
`1:8 to about 8:1, and more preferably from about 1:3 to about 3:1
`by weight of the opioid agonist.
`Id. at 7:12‒20.
`
`The ’976 patent teaches:
`The opioid analgesic formulation in combination with one
`or more aversive agents can be formulated as an immediate
`release formulation or controlled release oral formulation in any
`suitable tablet, coated tablet or multiparticulate formulation
`known to those skilled in the art. The controlled release dosage
`form may include a controlled release material which is
`incorporated into a matrix along with the opioid analgesic. In
`addition, the aversive agent may be separate from the matrix, or
`incorporated into the matrix.
`Id. at 12:29‒37.
`C. District Court Proceeding Involving the ’888 patent
`According to the district court in the SDNY Litigation, the ’888 patent
`relates to “a controlled release oral dosage form containing oxycodone that
`forms a gel when dissolved in an aqueous liquid,” wherein the “gelling
`properties . . . enable it to resist abuse by injection, snorting, and oral
`ingestion.” Ex. 1003, 1. Claim 1 of the ’888 patent is reproduced below:
`
`
`
`5
`
`KASHIV1054
`IPR of Patent No. 9,492,392
`
`

`

`IPR2016-01027
`Patent 9,060,976 B2
`
`
`A controlled release oral dosage form comprising:
`1.
`from about 2.5 mg to about 320 mg oxycodone or a
`pharmaceutically acceptable salt thereof; and
`a gelling agent comprising polyethylene oxide in an effective
`amount to impart a viscosity of at least about 10 cP when the
`dosage form is subjected to tampering by dissolution in from
`about 0.5 to about 10 ml of an aqueous liquid;
`the dosage form providing a therapeutic effect for at least about
`12 hours when orally administered to a human patient.
`Ex. 1002, 40:22‒32.
`
`The district court concluded that the ’888 patent was invalid as
`obvious. Ex. 1003, 40. Specifically, the district court found that the prior
`art teaches that gelling agents prevent potential abuse (id. at 41), and that the
`prior art teaches that PEO acts both as an agent to control the rate of release
`in sustained release dosage forms and as a gelling agent (id. at 43).
`
`The Court of Appeals for the Federal Circuit, our reviewing court,
`affirmed the decision of the district court in a short per curium order. Ex.
`1004. Specifically, the Federal Circuit held:
`The judgment of the United States District Court for the Southern
`District of New York is affirmed on the ground that the court did
`not err in concluding that the asserted claims of U.S. Patent No.
`8,337,888 would have been obvious.
`Id. at 2.
`
`Challenged Claim
`D.
`Petitioner challenges claim 1, the only claim of the ’976 patent, which
`is reproduced below:
`1.
`An extended release abuse deterrent dosage form comprising:
`a. a core matrix comprising a blended mixture of:
`(a) PEO having a molecular weight of from about
`300,000 daltons to about 5,000,000 daltons;
`
`6
`
`KASHIV1054
`IPR of Patent No. 9,492,392
`
`

`

`IPR2016-01027
`Patent 9,060,976 B2
`
`
`(b) magnesium stearate; and
`(c) oxycodone or a pharmaceutically acceptable salt
`thereof;
`wherein the core matrix is heated to melt at least a portion of
`the PEO included in the core matrix during preparation of the
`dosage form; and
`b. PEG applied onto the core matrix;
`wherein the dosage form provides extended release of the
`drug.
`Ex. 1001, 40:35–48.
`The Asserted Grounds of Unpatentability
`E.
`Petitioner challenges the patentability of claim 1 of the ’976 patent on
`the following grounds (Pet. 4):
`References
`Kumar1
`McGinity,2
`Joshi,3 and Palermo4
`
`Petitioner relies also on the Declaration of Anthony Palmieri III,
`Ph.D. (Ex. 1009).
`
`Basis
`§ 102
`§ 103
`
`Claims Challenged
`1
`1
`
`
`1 Kumar et al., Pub. No. US 2010/0216829 A2, published Aug. 26, 2010
`(Ex. 1006) (“Kumar”).
`2 McGinity et al, WO 97/49384, published Dec. 31, 1997 (Ex. 1013)
`(“McGinity”).
`3 Joshi et al., Pub. No. US 2002/0187192 A1, published Dec. 12, 2002
`(Ex. 1014) (“Joshi”).
`4 Palermo et al, WO 99/32120, published Jul. 1, 1999 (Ex. 1011)
`(“Palermo”).
`
`7
`
`KASHIV1054
`IPR of Patent No. 9,492,392
`
`

`

`IPR2016-01027
`Patent 9,060,976 B2
`
`
`Patent Owner relies on the Declaration of Stephen Byrn, Ph.D. (Ex.
`2007), as well as the Declaration of Eric M. Gaier, Ph.D. (Ex. 2041),
`submitted with its Preliminary Response.
`ANALYSIS
`
`Claim Construction
`A.
`In an inter partes review, claim terms in an unexpired patent are
`interpreted according to their broadest reasonable construction in light of the
`specification of the patent in which they appear. See 37 C.F.R. §42.100(b);
`Cuozzo Speed Techs., LLC v. Lee, 136 S. Ct. 2131, 2144–45 (2016)
`(upholding the use of the broadest reasonable interpretation standard).
`Under the broadest reasonable construction standard, claim terms are
`presumed to have their ordinary and customary meaning, as would be
`understood by one of ordinary skill in the art in the context of the entire
`disclosure. In re Translogic Tech., Inc., 504 F.3d 1249, 1257 (Fed. Cir.
`2007).
`Petitioner offers explicit constructions of several claim terms (Pet. 25‒
`29), as does Patent Owner (Prelim. Resp. 24‒30). On the present record, we
`determine that only the following claim terms require explicit construction
`for purposes of this Decision. See, e.g., Wellman, Inc. v. Eastman Chem.
`Co., 642 F.3d 1355, 1361 (Fed. Cir. 2011) (“[C]laim terms need only be
`construed ‘to the extent necessary to resolve the controversy.’”) (quoting
`Vivid Techs, Inc. v. Am. Sci. & Eng’g, Inc., 200 F.3d 795, 803 (Fed. Cir.
`1999)).
`
`“extended release”
`i.
`Petitioner contends that the term “extended release” does not appear
`in the Specification, rather the Specification uses the terms “sustained
`
`8
`
`KASHIV1054
`IPR of Patent No. 9,492,392
`
`

`

`IPR2016-01027
`Patent 9,060,976 B2
`
`release” and “controlled release.” Pet. 25. The Specification, Petitioner
`asserts, defines “controlled release” as “release of the opioid analgesic from
`the oral dosage form at a rate such that blood (e.g., plasma) concentrations
`(levels) are maintained within the therapeutic range but below toxic levels
`over an extended period of time.” Id. at 25‒26 (quoting Ex.1001, 4:56-60).
`Petitioner asserts further that although the Specification provides examples
`of 12 to 24 hours, it “does not suggest that such a period of release defines
`the concept.” Id. at 26 (citing Ex. 1001, 4:61‒62). Thus, Petitioner argues
`that “the broadest reasonable interpretation of extended release is the above
`phrase wherein ‘over an extended period of time’ means a period of time
`other than that of an immediate release of the opioid analgesic.” Id. (citing
`Ex.1009 ¶ 23).
`Patent Owner responds that Petitioner’s definition “is incomplete as it
`fails to include the rest of the sentence of the specification’s definition,
`which provides ‘, e.g., from about 12 to about 24 hours as compared to an
`immediate release product.’” Prelim. Resp. 24‒25 (quoting Ex. 1001, 4:61).
`
`As Patent Owner itself recognizes, however, the use of “e.g.”
`describes an exemplary embodiment. See id. at 29 (noting that “e.g.” in
`reference to how the sustained release matrix may be prepared is only
`describing exemplary embodiments). Thus, we decline to limit the claim
`term as Patent Owner would have us do. Rather, for purposes of this
`Decision, we construe “extended release” as “release of the opioid analgesic
`from the oral dosage form at a rate such that blood (e.g., plasma)
`concentrations (levels) are maintained within the therapeutic range but
`below toxic levels over a period of time longer than that of an immediate
`release of the opioid analgesic.”
`
`9
`
`KASHIV1054
`IPR of Patent No. 9,492,392
`
`

`

`IPR2016-01027
`Patent 9,060,976 B2
`
`
`“abuse deterrent”
`ii.
`Petitioner contends that the claim term “abuse deterrent” appears only
`in the preamble, and, thus, should not be limiting. Pet. 26. Specifically,
`Petitioner asserts “the preamble term ‘abuse deterrent’ should be nonlimiting
`because the claim body describes a structurally complete pharmaceutical
`dosage form and does not attribute abuse deterrence to any particular
`element.” Id. (citing Ex. 1009 ¶ 24).
`Patent Owner responds that “abuse deterrent” in the preamble should
`be limiting, as “it recites essential structure or steps, or if it is ‘necessary to
`give life, meaning, and vitality’ to the claim.” Prelim. Resp. 25 (quoting
`Glaxo Wellcome, Inc. v. Impax Labs., Inc., 356 F.3d 1348, 1353 (Fed. Cir.
`2004) (explaining preamble term “sustained release tablet” was limiting)).
`According to Patent owner, the language “breathes life into the claim by
`reciting a function of the PEO: deterring abuse and thereby achieving the
`goal of the invention described in the specification and prosecution history.”
`Id. at 26 (citing Ex. 2007 ¶ 89).
`
`If the claim preamble, when read in the context of the
`entire claim, recites limitations of the claim, or, if the preamble
`is “necessary to give life, meaning, and vitality” to the claim,
`then the claim preamble should be construed as if in the balance
`of the claim. . . . If, however, the body of the claim fully and
`intrinsically sets forth the complete invention, including all of its
`limitations, and the preamble offers no distinct definition of any
`of the claimed invention’s limitations, but rather merely states,
`for example, the purpose or intended use of the invention, then
`the preamble is of no significance to claim construction because
`it cannot be said to constitute or explain a claim limitation.
`Pitney Bowes, Inc. v. Hewlett Packard Co., 182 F.3d 1298, 1305 (Fed. Cir.
`1999) (citations omitted).
`
`10
`
`KASHIV1054
`IPR of Patent No. 9,492,392
`
`

`

`IPR2016-01027
`Patent 9,060,976 B2
`
`Claim 1 is drawn to a dosage form—a composition. Patent Owner
`
`does not point out how the statement of “abuse deterrent” modifies the
`structurally complete dosage form recited in the body of claim 1. We
`conclude on the record currently before us, therefore, that the statement of
`“abuse deterrent” in the preamble, is a goal of the invention, that is, it is
`merely a statement of intended use.
`“PEG applied onto the core matrix”
`iii.
`Petitioner argues that the ordinary artisan “would understand this term
`to mean the [polyethylene glycol, “PEG”] is placed on or in contact with the
`core matrix,” which “can occur before, during, or after the core matrix is
`heated.” Pet. 29 (citing Ex.1009 ¶ 28).
`Patent Owner contends that the broadest reasonable construction of
`this claim term is “PEG coating the core matrix.” Prelim. Resp. 30.
`According to Patent Owner, Petitioner’s construction of “in contact” with
`the core matrix suggests that the PEG may be contained within the core
`matrix. Id.
`
`We agree with Patent Owner that the broadest reasonable construction
`of “PEG applied onto the core matrix” is a “PEG coating of the core matrix.”
`Petitioner’s proposed construction would read “applied onto the core matrix”
`(emphasis added) out of the claim, which we decline to do. See Bicon, Inc.
`v. Straumann Co., 441 F.3d 945, 951 (Fed. Cir. 2006) (noting that claim
`language “should not [be] treated as meaningless”).
`
`
`Anticipation by Kumar (Ex. 1006)
`B.
`Petitioner asserts that claims 1 is anticipated by Kumar (Pet. 29–40),
`and presents a claim chart for claim 1 (id. at 39‒40).
`
`11
`
`KASHIV1054
`IPR of Patent No. 9,492,392
`
`

`

`IPR2016-01027
`Patent 9,060,976 B2
`
`
`Analysis
`Petitioner contends that claim 1 of the ’976 patent “is not entitled to
`
`the benefit of priority to the Provisional Application or any of the Related
`Applications, as those applications all fail to disclose the claimed subject
`matter in a manner sufficient to satisfy the written description requirement of
`35 U.S.C. § 112, first paragraph.” Pet. 32. In particular, Petitioner argues
`that the limitation of the “PEO having a molecular weight of from about
`300,000 daltons to about 5,000,000 daltons” is not supported by any priority
`application. Id. In that regard, Petitioner notes that claim was copied from
`the Kumar patent (Ex. 1005) during prosecution in order to provoke an
`interference. Id.
`
`Patent Owner responds that in asserting that challenged claim 1 is
`anticipated by Kumar, Petitioner is “rehash[ing] an old priority contest,” as
`“the Kumar assignee conceded the ’976 inventors invented first.” Prelim.
`Resp. 1. According to Patent Owner, the Patent and Trademark Office
`“granted the ’976 patent after Purdue settled an interference involving the
`Kumar Patent, and the Kumar assignee requested entry of adverse
`judgment.” Id. Specifically, Patent Owner notes that shortly after institution
`on the interference between the assignees of the Kumar patent and the
`inventors of the ’976 patent, “the Kumar Patent assignee requested entry of
`adverse judgment in favor of Purdue,” and “the [Board of Patent Appeals
`and Interferences (“BPAI”)] granted Purdue priority,” allowing the ’976
`patent to issue. Id. at 17 (citing Exs. 2001, 2003). Patent Owner asserts,
`therefore, that the anticipation challenge should be denied under 35 U.S.C.
`§ 325(d) as the “same . . . arguments previously were presented to the
`Office.” Id. at 31. (alteration in original) (quoting 35 U.S.C. § 325(d)).
`
`12
`
`KASHIV1054
`IPR of Patent No. 9,492,392
`
`

`

`IPR2016-01027
`Patent 9,060,976 B2
`
`Under 35 U.S.C. § 325(d), the Board has discretion to reject a petition
`
`for inter partes review because “the same or substantially the same prior art
`or arguments previously were presented to the Office.” Id. Under the facts
`and circumstances of this proceeding, we decline to institute the anticipation
`challenge over Kumar. Specifically, we find substantially the same
`argument regarding priority over Kumar was previously presented to the
`Office, including to the Board in the prior interference proceeding, Patent
`Interference No. 106,004. In particular, as Patent Owner notes (Prelim.
`Resp. 16), the Board awarded priority to Patent Owner over the junior party,
`i.e., the Kumar Patent assignee (Ex. 2003). We recognize that priority was
`awarded based on a request for adverse judgment by the Kumar Patent
`assignee rather than a decision “on the merits” as to whether the application
`that issued as the ’976 patent was in fact entitled to priority. Nonetheless,
`the basis for our exercise of discretion under § 325(d) is not necessarily
`limited to only those arguments that were previously decided “on the
`merits.” Rather, the statute specifies only that we may deny institution in
`view of arguments that were previously “presented” to the Office. 35 U.S.C.
`§ 325(d). Thus, we decline to revisit an issue that has already been before
`the Board in the interference proceeding.
`
`Accordingly, we decline to institute the anticipation challenge over
`Kumar.
`
`C. Obviousness over McGinity, Joshi, and Palermo
`Petitioner asserts that claim 1 is rendered obvious by the combination
`of McGinity, Joshi, and Palermo. Pet. 40‒55. Petitioner presents a claim
`chart for claim 1. Id. at 52‒55. Patent Owner contends that Petitioner has
`not established a reasonable likelihood that claim 1 is rendered obvious by
`
`13
`
`KASHIV1054
`IPR of Patent No. 9,492,392
`
`

`

`IPR2016-01027
`Patent 9,060,976 B2
`
`the combination of references relied upon by Petitioner. Prelim. Resp. 20‒
`24, 39‒55.
`
`Overview of McGinity (Ex. 1013)
`i.
`McGinity discloses pharmaceutical formulations in which the
`formulation has been prepared “by hot-melt extrusion of mixtures containing
`high molecular weight [polyethylene oxide (‘PEO’)] and a therapeutic
`compound for use in controlled release drug delivery.” Ex. 1013, 1:8‒12.
`According to McGinity, “[i]t [had] not been appreciated that a high
`molecular weight PEO based therapeutic compound containing composition
`can be hot melt extruded without significant degradation or decomposition
`of either the PEO or therapeutic compound.” Id. at 2:15‒17.
`McGinity teaches that the PEO may have an average molecular
`weight of from about 1,000,000 to 10,000,000, with the PEO not exceeding
`99.99% by weight of the formulation. Id. at 5:2‒4, 11‒12. The formulation
`of McGinity may also contain a plasticizer, wherein the plasticizer may be a
`low molecular weight PEO having a molecular weight less than 500,000. Id.
`at 6:4‒27.
`
`With respect to the therapeutic compound, McGinity teaches that the
`structure of that compound is not critical, as long as it can diffuse from the
`formulation upon exposure to a biological fluid. Id. at 7:20‒24. McGinity
`specifically teaches that the therapeutic compound may be “analgesics such
`as aspirin, acetaminophen, deflunisal and the like.” Id. at 8:18‒20.
`ii.
`Overview of Joshi (Ex. 1014)
`Joshi is drawn to a pharmaceutical composition that reduces drug
`
`abuse, wherein the composition comprises a central nervous system
`stimulant and a gel forming polymer. Ex. 1014 ¶ 1. According to Joshi,
`
`14
`
`KASHIV1054
`IPR of Patent No. 9,492,392
`
`

`

`IPR2016-01027
`Patent 9,060,976 B2
`
`adding a gel forming polymer to the composition “reduces or eliminates
`potential drug abuse by swelling in the presence of moisture which is, for
`example, present in the dermis layer of skin and mucous membrane, and
`thus, prevents nasal absorption and injectability of the drug.” Id. ¶ 9.
`Joshi teaches that PEO is a preferred gel forming polymer, and that
`the polymer may have a molecular weight “from about 70,000 to about
`2,000,000.” Id. ¶¶ 21‒22. The gel forming polymer is from about 2 to about
`40 weight percent of the composition. Id. ¶ 23. The tablets are prepared, for
`example, by forcing the solid ingredients through a mesh, blending the solid
`ingredients, and compressing them into a tablet. Id. ¶ 37. Joshi teaches also
`that additional agents that are commonly used to prepare oral pharmaceutical
`dosage forms may also be used, such as enteric coatings. Id. ¶ 26.
`Joshi references WO 97/33566 in its “Background of the Invention,”
`which teaches an opioid composition that deters abuse, wherein an opioid
`antagonist is incorporated into the system to reduce the effect of the opioid.
`Id. ¶ 6.
`
`iii. Overview of Palermo (Ex. 1011)
`Palermo discloses an opioid oral dosage form that is less subject to
`
`potential parenteral or oral abuse. Ex. 1011, 6:1‒9. The potential for abuse
`is reduced by “combining an analgesically effective amount of an opioid
`agonist together with an opioid antagonist into an oral dosage form.” Id. at
`6:10‒16. The opioid may be oxycodone hydrochloride, with the antagonist
`being naltrexone hydrochloride. Id. at 6:25‒28.
`
`Palermo discloses further that the dosage form may be a sustained
`release formulation, which may be accomplished by incorporating a
`sustained release carrier into the matrix containing the opioid and its
`
`15
`
`KASHIV1054
`IPR of Patent No. 9,492,392
`
`

`

`IPR2016-01027
`Patent 9,060,976 B2
`
`antagonist, as well as using a sustained release coating. Id. at 8:1‒6.
`Specifically, Palermo teaches that the “tablets may be uncoated or they may
`be coated by known techniques for elegance or to delay release of the active
`ingredients.” Id. at 18:3‒5.
`
`Palermo teaches that in preferred embodiments the substrate, that is
`the matrix particle, is coated with a hydrophobic material. Id. at 22:6‒9.
`According to Palermo, the inclusion of a plasticizer in the aqueous
`dispersion of the hydrophobic material used in the coating will improve the
`physical properties of the sustained release coating. Id. at 24:25‒29. An
`example of a plasticizer that may improve the elasticity of acrylic films that
`comprise the hydrophobic coating includes polyethylene glycol (“PEG”).
`Id. at 25:11‒17.
`
`Palermo also discloses the use of melt-granulation or melt-extrusion
`techniques to form sustained release matrices. Id. at 32:11‒12. Palermo
`teaches that sustained release dosage form formed by melt-extrusion may be
`coated with a sustained release coating, such as those discussed above. Id. at
`34:25‒27.
`
`Analysis
`iv.
`Petitioner relies on McGinity for teaching “hot-melt extrudable
`pharmaceutical formulations that include a therapeutic compound and a high
`molecular weight PEO.” Pet. 42 (citing Ex. 1013, Abstract, 1:9‒12; Ex.
`1009 ¶¶ 42, 66). Petitioner notes that McGinity teaches that the matrix may
`be a blended mixture of the PEO and a therapeutic compound, and teaches
`also that the PEO may have “an average molecular weight of between about
`1,000,000 to about 10,000,000, a range that overlaps with much of the
`300,000 to 5,000,000 range claimed in the ’976 Patent.” Id. (citing Ex.
`
`16
`
`KASHIV1054
`IPR of Patent No. 9,492,392
`
`

`

`IPR2016-01027
`Patent 9,060,976 B2
`
`1013, 5:1‒4, 8:6‒7, 18:15‒30 (Example 3); Ex. 1009 ¶¶ 42, 43, 66, 68).
`Petitioner notes further that McGinity teaches that other formulation
`components, such as lubricants, may be added to the dosage form, and may
`be included in the PEO and active ingredient in the extruder. Id. at 43
`(citing Ex. 1013, 9:33‒10:2, 11:18‒21, 13:26‒30; Ex. 1009 ¶¶ 43‒45, 66,
`68, 69).
`As to the use of oxycodone, Petitioner contends:
`McGinity teaches that the therapeutic agent may be
`“analgesics . . . and the like.” (Exs.1013, at 8:20; 1009 ¶¶ 43,
`67.) As discussed . . . above, the court in the SDNY Litigation
`held that in the context of abuse-prone drugs, McGinity’s
`disclosure of “analgesics . . . and the like” includes controlled
`release oxycodone. (Ex.1003, at 37.) This was affirmed, twice.
`(Exs. 1004, 1017.) Accordingly, McGinity teaches that the
`therapeutic agent may be controlled release oxycodone.
`(Ex. 1009 ¶ 43, 67.) But even were this not the case, oxycodone
`is one of the preferred drugs formulated in Palermo. (Exs. 1011,
`at 7:5-6; 1009 ¶ 35, 72.)
`
`Id.
`According to Petitioner, Joshi “is directed to a pharmaceutical
`
`composition that reduces or eliminates the drug abuse potential of central
`nervous stimulants, such as Ritalin®.” Id. at 44 (citing Ex. 1014, Abstract).
`Petitioner notes that in discussing the need to prevent potential drug abuse,
`Joshi points to WO 97/33566, which, Petitioner asserts, discusses “an abuse-
`deterrent dosage form containing an opioid.” Id. (citing Ex. 1014 ¶ 6;
`Ex. 1009 ¶ 54). Petitioner further relies on Joshi for teaching that PEO, the
`same gel forming polymer of McGinity, when combined with the drug,
`reduces the ability to absorb the drug nasally and also reduces its
`injectability, and teaches also that the gel forming polymer may have a
`molecular weight of from about 70,000 to 2,000,000, which also overlaps
`
`17
`
`KASHIV1054
`IPR of Patent No. 9,492,392
`
`

`

`IPR2016-01027
`Patent 9,060,976 B2
`
`with the range required by challenged claim 1. Id. at 44‒45 (citing Ex. 1014
`¶¶ 8, 21, 22; Ex. 1009 ¶¶ 55, 70).
`
`As to Palermo, Petitioner argues that the reference “teaches a method
`for preventing abuse of sustained release dosage forms.” Id. at 45 (citing
`Ex. 1011, Abstract, 8:1‒2; Ex. 1009 ¶¶ 56‒57). Petitioner also relies on
`Palermo for teaching “a matrix that may include gelling agents or a
`hydrophilic material capable of providing extended release and capable of
`melting or softening.” Id. at 45‒46 (citing Ex. 1011, 6:31, 28:21‒22; Ex.
`1009 ¶¶ 56, 57). According to Petitioner, “PEO is a hydrophilic material
`and a well-known gelling agent.” Id. at 46 (citing Ex. 1009 ¶¶ 46‒52).
`Petitioner further relies on Palermo for its teaching that the matrix may
`contain oxycodone and magnesium stearate, and may be formed by melt-
`granulation or melt-extrusion techniques. Id. (citing Ex. 1011, 31:13‒14,
`32:10‒21; Ex. 1009 ¶¶ 57, 72). In addition, Petitioner depends on Palermo
`for teaching that “the matrix may be coated for protection or to regulate the
`release of materials, and that the coatings may include well-known
`plasticizers,” such as PEG. Id. (citing Ex. 1011, 18:3‒5, 21:18‒22:17,
`25:13‒15; Ex. 1009 ¶¶ 57, 73).
`
`Petitioner acknowledges that McGinity is silent as to the use of its
`dosage form to deter abuse, but contends that “Joshi teaches that it was
`known that opioids were susceptible to abuse and that abuse deterrence of
`drugs was desirable.” Id. at 47 (citing Ex. 1014 ¶¶ 1, 5, 6). Moreover,
`Petitioner asserts that the ordinary artisan would have been aware “of the
`growing concern for oxycodone abuse.” Id. (citing Ex. 1018; Ex. 1019; Ex.
`1009 ¶¶ 29, 31, 74). Petitioner contends further that the “fact that both the
`McGinity and Joshi references teach very similar compositions using high
`
`18
`
`KASHIV1054
`IPR of Patent No. 9,492,392
`
`

`

`IPR2016-01027
`Patent 9,060,976 B2
`
`molecular weight PEO gelling agents within the claimed range would only
`serve to reinforce a reasonable expectation that what McGinity was already
`doing would impart some measure of abuse resistance identified by Joshi,”
`as well as provide a reason to combine the references. Id. at 48 (citing Ex.
`1009 ¶¶ 70, 75, 77).
`
`As to the requirement of claim 1 that the drug is oxycodone, Petitioner
`contends that although McGinity does not specifically mention oxycodone,
`“the court in the SDNY Litigation has already found that McGinity’s
`teaching of an analgesic and the like was su