Trials@uspto.gov
`571-272-7822
`
`
`
`
`
`
`
`
`
`
`
` Paper 8
`
`
` Entered: April 18, 2016
`
`
`
`
`UNITED STATES PATENT AND TRADEMARK OFFICE
`____________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`____________
`
`AMERIGEN PHARMACEUTICALS LIMITED,
`Petitioner,
`
`v.
`
`SHIRE LLC,
`Patent Owner.
`
`
`Case IPR2015-02009
`Patent RE42,096 E
`
`
`
`Before TONI R. SCHEINER, LORA M. GREEN, and
`SHERIDAN K. SNEDDEN, Administrative Patent Judges.
`
`SCHEINER, Administrative Patent Judge.
`
`
`
`
`
`
`DECISION
`Institution of Inter Partes Review
`37 C.F.R. § 42.108
`
`
`
`
`
`Page 1
`
`SHIRE EX. 2047
`KVK v. SHIRE
`IPR2018-00293
`
`
`571-272-7822
`
`
`
`
`
`
`
`
`
`
`
` Paper 8
`
`
` Entered: April 18, 2016
`
`
`
`
`UNITED STATES PATENT AND TRADEMARK OFFICE
`____________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`____________
`
`AMERIGEN PHARMACEUTICALS LIMITED,
`Petitioner,
`
`v.
`
`SHIRE LLC,
`Patent Owner.
`
`
`Case IPR2015-02009
`Patent RE42,096 E
`
`
`
`Before TONI R. SCHEINER, LORA M. GREEN, and
`SHERIDAN K. SNEDDEN, Administrative Patent Judges.
`
`SCHEINER, Administrative Patent Judge.
`
`
`
`
`
`
`DECISION
`Institution of Inter Partes Review
`37 C.F.R. § 42.108
`
`
`
`
`
`Page 1
`
`SHIRE EX. 2047
`KVK v. SHIRE
`IPR2018-00293
`
`
`
`IPR2015-02009
`Patent RE42,096 E
`
`
`I. INTRODUCTION
`Amerigen Pharmaceuticals Limited ( “Petitioner”) filed a Petition
`(Paper 1, “Pet.”) on October 1, 2015, requesting an inter partes review of
`claims 1–3, 5, 8, 9, 11, 18–21, 23, and 25 of U.S. Patent No. RE42,096 E
`(Ex. 1001, “the ’096 patent”). Shire LLC (“Shire” or “Patent Owner”) filed
`a Preliminary Response (Paper 7, “Prelim. Resp.”) on January 19, 2016. We
`have jurisdiction under 35 U.S.C. § 314, which provides that an inter partes
`review may not be instituted “unless . . . there is a reasonable likelihood that
`the petitioner would prevail with respect to at least 1 of the claims
`challenged in the petition.”
`Upon consideration of the information presented in the Petition and
`the Preliminary Response, we are persuaded that Petitioner has established a
`reasonable likelihood that it would prevail in its challenges to claims 18–21,
`23, and 25 of the ’096 patent. Accordingly, we institute an inter partes
`review of those claims.
`
`A. Related Proceedings
`Petitioner informs us of the following related judicial matters: Shire
`
`LLC v. Amerigen Pharms. Ltd., 14-cv-6095 (D.N.J. Oct. 1, 2014); Shire LLC
`v. Corepharma LLC, 14-05694 (D.N.J. Sept. 12, 2014); Shire LLC v. Par
`Pharm. Inc., 15-cv-01454 (D.N.J. Feb. 26, 2015). Pet. 1. Patent Owner
`
`2
`
`
`Page 2
`
`
`
`IPR2015-02009
`Patent RE42,096 E
`
`identifies the same related matters in its Mandatory Notices under 37 C.F.R.
`§ 42.8(a)(2).1 Paper 6, 1.
`
`B. The Asserted Grounds of Unpatentability
`Petitioner asserts the challenged claims are unpatentable on the
`
`following grounds. Pet. 4–8, 17–60.2
`
`References
`
`Mehta3
`
`Mehta and Adderall PDR4
`Mehta, Adderall PDR, and
`Rosen5
`
`Basis
`
`Claims Challenged
`
`§ 102(e)
`
`§ 103(a)
`
`§ 103(a)
`
`1–3, 5, 8, 9, 11, 18–
`21, 23, and 25
`1–3, 5, 18–21, 23,
`and 25
`8, 9, and 11
`
`
`1 Patent Owner informs us of a number of additional related judicial and
`administrative matters. Prelim. Resp. 2–7. We are not persuaded that
`Petitioner’s failure to include those matters in its mandatory notices warrants
`dismissal of the Petition, and decline to do so on that basis.
`2 Petitioner supports its challenges with the Declaration of Edmund J. Elder,
`Jr., Ph.D., R.Ph., executed September 30, 2015 (“Elder Declaration”)
`(Ex. 1006).
`3 U.S. Patent No. 5,837,284, issued November 17, 1998, to Mehta et al.
`(“Mehta”) (Ex. 1003).
`4 PHYSICIANS’ DESK REFERENCE 331, 2209–11 (51st ed. 1997) (“Adderall
`PDR”) (Ex. 1004).
`5 Earl Rosen et al., Absorption and Excretion of Radioactively Tagged
`Dextroamphetamine Sulfate from a Sustained-Release Preparation, 194
`JAMA 145–147 (1965). (“Rosen”) (Ex. 1015).
`3
`
`
`Page 3
`
`
`
`IPR2015-02009
`Patent RE42,096 E
`
`
`C. The ’096 Patent (Ex. 1001)
`The ’096 patent, titled “ORAL PULSED DOSE DRUG DELIVERY
`SYSTEM,” is a reissue of U.S. Patent 6,322,819,6 and “is listed in the FDA’s
`‘Orange Book’ of approved drug products for Adderall XR®, which is
`indicated for Attention Deficit Hyperactivity Disorder (ADHD).” Prelim.
`Resp. 1.
`The ’096 patent teaches that ADHD in children conventionally is
`treated by administering two separate doses of medication, “one in the
`morning, and one approximately 4–6 hours later, commonly away from
`home under other than parental supervision.” Ex. 1001, 3:20–13.
`Administering two separate doses, however, “is time consuming,
`inconvenient, and may be problematic for those children having difficulties
`in swallowing tablet formulations.” Id. at 3:14–17.
`The ’096 patent, thus, discloses a pharmaceutical composition
`comprising “an oral multiple pulsed dose delivery system for amphetamine
`salts and mixtures thereof” (id. at 3:22–24), “in which there is immediate
`release of drug and enteric release of drug wherein the enteric release is a
`pulsed release and wherein the drug includes one or more amphetamine salts
`and mixtures thereof” (id. at 3:53–57). In other words, “[t]he immediate
`release component releases the pharmaceutical agent in a pulsed dose upon
`oral administration of the delivery system” (id. at 3:58–60), while “[t]he
`
`
`6 U.S. Patent No. 6,322,819, issued November 7, 2001 to Burnside et al.
`(“the ’819 patent”) (Ex. 1017).
`
`4
`
`
`Page 4
`
`
`
`IPR2015-02009
`Patent RE42,096 E
`
`enteric release coating layer retards or delays the release of the
`pharmaceutical active or drug for a specified time period (“lag time”) until a
`predetermined time, at which time the release of the drug is rapid and
`complete” (id. at 3:61–64).
`In accordance with a preferred embodiment . . . there is
`provided a pharmaceutical composition for delivering one or
`more pharmaceutically active amphetamine salts that includes:
`(a) one or more pharmaceutically active amphetamine
`salts that are covered with an immediate release coating,
`and
`(b) one or more pharmaceutically active amphetamine
`salts that are covered with an enteric release coating
`wherein (1) the enteric release coating has a defined
`minimum thickness and/or (2) there is a protective layer
`between
`the at
`least one pharmaceutically active
`amphetamine salt and the enteric release coating and/or (3)
`there is a protective layer over the enteric release coating.
`Id. at 3:28–42.
`According to the ’096 patent, plasma levels of the pharmaceutically
`active amphetamine salts “will reach a peak fairly rapidly after about 2
`hours, and after about 4 hours a second pulse dose is released, wherein a
`second fairly rapid additive increase of plasma drug levels occurs which
`slowly decreases over the course of the next 12 hours.” Id. at 10:4–9. Thus,
`“the multiple dosage form of the . . . invention can deliver rapid and
`complete dosages of pharmaceutically active amphetamine salts to achieve
`the desired levels of the drug in a recipient over the course of about 8 hours
`with a single oral administration.” Id. at 9:66–10:3.
`
`5
`
`
`Page 5
`
`
`
`IPR2015-02009
`Patent RE42,096 E
`
`
`Finally, the ’096 patent teaches that
`Pharmaceutical active amphetamine salts contemplated to be
`within the scope of the present invention include amphetamine
`base, all chemical and chiral derivatives and salts thereof;
`methylphenidate, all chemical and chiral derivatives and salts
`thereof; phenylpropanolamine and its salts; and all other
`compounds indicated for the treatment of attention deficit
`hyperactivity disorder (ADHD).
`Id. at 7:50–57.
`
`D. Illustrative Claims
`Petitioner challenges claims 1–3, 5, 8, 9, 11, 18–21, 23, and 25 of the
`’096 patent, of which claims 1, 2, 5, 8, 11, and 18 are independent claims.
`Claims 1 and 18, reproduced below, are illustrative.
`1. A pharmaceutical composition for delivery of one or more
`pharmaceutically active amphetamine salts, comprising:
`(a) one or more pharmaceutically active amphetamine
`salts covered with an immediate release coating;
`(b) one or more pharmaceutically active amphetamine
`salts that are covered with an enteric release coating that
`provides for delayed pulsed enteric release,
`wherein said enteric release coating releases essentially
`all of said one or more pharmaceutically active amphetamine
`salts coated with said enteric coating within about 60 minutes
`after initiation of said delayed pulsed enteric release;
`wherein the pharmaceutically active amphetamine salts
`in (a) and (b) comprise mixed amphetamine salts.
`Ex. 1001, 12:53–67.
`
`6
`
`
`Page 6
`
`
`
`IPR2015-02009
`Patent RE42,096 E
`
`
`18. A pharmaceutical composition for delivery of one or more
`pharmaceutically active amphetamine salts comprising:
`(a) one or more pharmaceutically active amphetamine
`salts covered with an immediate release coating;
`(b) one or more pharmaceutically active amphetamine
`salts that are covered with an enteric release coating that
`provides for delayed pulsed enteric release, wherein said
`enteric release coating releases said one or more
`pharmaceutically active amphetamine salts coated with
`said enteric coating within about 60 minutes after
`initiation of said delayed pulsed enteric release; and
`(c) a protective layer between the at least one
`pharmaceutically active amphetamine salt and the enteric
`release coating.
`Ex. 1001, 14:63–15:11.
`
`II. ANALYSIS
`
`A. Claim Construction
`In an inter partes review, claim terms in an unexpired patent are given
`their broadest reasonable interpretation in light of the specification of the
`patent in which they appear. 37 C.F.R. § 42.100(b). Under this standard, we
`presume that a claim term carries its “ordinary and customary meaning,”
`which “is the meaning the term would have to a person of ordinary skill in
`the art in question” at the time of the invention. In re Translogic Tech., Inc.,
`504 F.3d 1249, 1257 (Fed. Cir. 2007). See also Trivascular, Inc. v. Samuels,
`812 F.3d 1056, 1062 (Fed. Cir. 2016) (“Under a broadest reasonable
`interpretation, words of the claim must be given their plain meaning, unless
`such meaning is inconsistent with the specification and prosecution
`7
`
`
`Page 7
`
`
`
`IPR2015-02009
`Patent RE42,096 E
`
`history.”). Any special definition for a claim term must be set forth in the
`specification with reasonable clarity, deliberateness, and precision. In re
`Paulsen, 30 F.3d 1475, 1480 (Fed. Cir. 1994). Finally, only terms which are
`in controversy need to be construed, and then only to the extent necessary to
`resolve the controversy. Vivid Techs., Inc. v. Am. Sci. & Eng’g. Inc., 200
`F.3d 795, 803 (Fed. Cir. 1999).
`For purposes of this Decision, and on this record, only the following
`terms require explicit construction.
`1. “pharmaceutically active amphetamine salts,”
`“amphetamine salt,” and “mixed amphetamine salts”
`The parties agree that the term “pharmaceutically active amphetamine
`salts” is explicitly defined in the ’096 patent, at column 7, lines 51–58. Pet.
`9–10; Prelim. Resp. 18–19. That explicit definition is as follows:
`Pharmaceutical[ly] active amphetamine salts contemplated to be
`within the scope of the present invention include amphetamine
`base, all chemical and chiral derivatives and salts thereof;
`methylphenidate, all chemical and chiral derivatives and salts
`thereof; phenylpropanolamine and its salts; and all other
`compounds indicated for the treatment of attention deficit
`hyperactivity disorder (ADHD).
`Ex. 1001, 7:50–57.
`
`Given the specification’s explicit definition, we agree with the parties
`that the term “pharmaceutically active amphetamine salts” includes non-
`salts, such as “amphetamine base” and “methylphenidate,” as well as salts of
`amphetamine base and methylphenidate.
`
`8
`
`
`Page 8
`
`
`
`IPR2015-02009
`Patent RE42,096 E
`
`The term “amphetamine salt(s)” appears in several places in the
`
`specification of the ’096 patent, without the adjacent language
`“pharmaceutically active,” but is not separately defined. See e.g., id. at 1:9,
`10, 4:17–18, 22–23, 51. In at least one instance, the term “amphetamine
`salts” is closely followed by the term “pharmaceutically active amphetamine
`salts”:
`
`in view of a need for successfully
`Accordingly,
`administering a multiple pulsed dose of amphetamine salts and
`mixtures thereof, the present invention provides an oral multiple
`pulsed dose delivery system for amphetamine salts and mixtures
`thereof. FIG. 1 illustrates the desired target plasma level profile
`of the pharmaceutical active contained within the delivery
`system.
`In accordance with a preferred embodiment of the present
`invention, there is provided a pharmaceutical composition for
`delivering one or more pharmaceutically active amphetamine
`salts that includes:
`(a) one or more pharmaceutically active
`amphetamine salts that are covered with an immediate
`release coating, and
`(b) one or more pharmaceutically active
`amphetamine salts that are covered with an enteric release
`coating . . .
`Id. at 3:20–36 (emphases added).
`Having consulted the specification, we find little guidance as to the
`difference in scope, if any, between “pharmaceutically active amphetamine
`salts” and “amphetamine salts.” We next look to evidence of how a person
`of ordinary skill in the art would understand the relationship between these
`terms. Petitioner’s witness, Dr. Elder, testifies that one of ordinary skill in
`9
`
`
`Page 9
`
`
`
`IPR2015-02009
`Patent RE42,096 E
`
`the art “would construe amphetamine salt to mean pharmaceutically active
`amphetamine salt” because “the ’096 patent uses ‘amphetamine base’ to
`describe the compound commonly referred to as amphetamine; on [sic] the
`way the terms are used in describing the features of the disclosure relative to
`how they appear in the claims” (Pet. 9–10 (citing Ex. 1005 ¶¶ 108–135));
`and because “the term ‘amphetamine salt(s)’ refers back to the term
`‘pharmaceutically active amphetamine salts’ as an antecedent” in claims 8,
`11, and 20 of the ’096 patent. Pet. 9 (citing Ex. 1026, 9 n.5); see, e.g., Ex.
`1001, 13:45–63, 15:15–17. Alternatively, Dr. Elder testifies that one of
`ordinary skill in the art would have understood that “amphetamine salts is
`used more broadly than pharmaceutically active amphetamine salts in
`several locations.” Pet. 11 (citing Ex. 1001, 3:20–25; Ex. 1005 ¶ 122).
`For purposes of this decision, we need not determine whether
`“amphetamine salts” is broader than “pharmaceutically active amphetamine
`salts,” or whether the two terms are coextensive. Rather, for purposes of this
`decision, it is enough that we are persuaded by Dr. Elder’s testimony that the
`ordinary artisan would not have understood “amphetamine salts” to be
`narrower than “pharmaceutically active amphetamine salts.” Thus, we also
`are persuaded that the ordinary artisan would have understood the term
`“amphetamine salts,” like the term “pharmaceutically active amphetamine
`salts,” to include “amphetamine base” and “methylphenidate,” as well as
`salts of amphetamine base and methylphenidate.
`
`10
`
`
`Page 10
`
`
`
`IPR2015-02009
`Patent RE42,096 E
`
`The term “mixed amphetamine salts” also is not separately defined in
`
`the specification of the ’096 patent, and apart from the claims, appears only
`in Examples 1 and 2, with no further elaboration (Ex. 1001, 10:21, 32, 43–
`44). However, the term “amphetamine salts” appears several times without
`the adjacent language “pharmaceutically active,” but followed immediately
`by the words “and mixtures thereof.” See, e.g., id. at 3:21, 23, 56–57.
`Petitioner contends that we “should find mixed amphetamine salts to
`
`mean ‘made up of pharmaceutically active amphetamine salts of more than
`one kind.’” Pet. 12.
`Patent Owner argues that “‘[m]ixed amphetamine salts” means a
`combination of two or more salts of α-methylphenethylamine” (Prelim.
`Resp. 20), and Petitioner’s proposal “is unreasonably broad” (id. at 21).
`Patent Owner contends that “[t]he separate set of ‘pharmaceutically active
`amphetamine salts’ comprising . . . methylphenidate, is not imported into the
`narrower set of ‘mixed amphetamine salts.’” Id. at 20–21. Patent Owner
`contends that unlike the term “pharmaceutically active amphetamine salts,”
`the terms “amphetamine” and “mixed” were “not redefined . . . to include
`methylphenidate” (id.), and should be given their ordinary meaning—that is
`to say that “‘Amphetamine’ has its ordinary meaning: one or both
`enantiomers of α-methylphenethylamine” (id. at 20), and two salts “are
`‘mixed,’ when one or both of the acid and base components of the salt are
`different” (id.).
`
`11
`
`
`Page 11
`
`
`
`IPR2015-02009
`Patent RE42,096 E
`
`
`Patent Owner is correct in that a patentee, to act as a lexicographer
`“must clearly set forth a definition of the disputed term other than its plain
`and ordinary meaning,” or in other words, “must clearly express an intent to
`redefine the term.” Aventis Pharma S.A. v. Hospira, Inc., 675 F.3d 1324,
`1330 (Fed. Cir. 2012).
`
`Moreover, we agree that nothing in the specification sets forth a
`special definition for the naked term “amphetamine salts” or “mixed
`amphetamine salts.” The problem is that the Applicants of the ’096 patent,
`having set out a definition of “pharmaceutically active amphetamine salts”
`in the specification that included, among other things, amphetamine base
`and salts thereof and methylphenidate and salts thereof, did not then make it
`clear that modifying the term “amphetamine salts” with the word “mixed”
`instead of “pharmaceutically active” meant that methylphenidate salts were
`excluded. Dr. Elder testifies to that effect. Ex. 1005 ¶¶ 106–115, 122,
`154–161. We agree with Dr. Elder that one of ordinary skill in the art,
`reading the specification, would have understood the term “amphetamine
`salt” to be at least as broad as “pharmaceutically active amphetamine salts,”
`and to include both amphetamine base and methylphenidate (as well as their
`salts). Logically, then, we are persuaded that one of ordinary skill in the art
`would have understood the term “amphetamine salts and mixtures thereof”
`to include pharmaceutically active amphetamine salts and mixtures thereof,
`and “mixed amphetamine salts” to be a simple rearrangement of the term
`“amphetamine salts and mixtures thereof.”
`
`12
`
`
`Page 12
`
`
`
`IPR2015-02009
`Patent RE42,096 E
`
`
`That, in and of itself, does not settle the matter. We still must
`consider Patent Owner’s contention that its construction is supported by the
`prosecution history. DePuy Spine, Inc. v. Medtronic Sofamor Danek, Inc.,
`469 F.3d 1005, 1014 (Fed. Cir. 2006) (“In determining the meaning of the
`disputed claim limitation, we look principally to the intrinsic evidence of
`record, examining the claim language itself, the written description, and the
`prosecution history, if in evidence.”); Microsoft Corp. v. Proxyconn, Inc.,
`789 F.3d 1292, 1298 (Fed. Cir. 2015) (instructing the PTO to consider
`prosecution history in inter partes review).
`Patent Owner directs us to two statements in the prosecution history
`of the ’096 patent. The first is a statement accompanying an amendment
`dated May 18, 2007 and a Supplemental Reissue Declaration, and identifies
`an amendment to original independent claim 1 as the basis for reissue. The
`first statement is as follows: “This amendment narrows claim 1 by the added
`limitation: ‘wherein the pharmaceutically active amphetamine salts comprise
`mixed amphetamine salts (MASL).’ . . . This is an error correctable by
`reissue because original claim 1 may be too broad, and the amendment
`accordingly narrows the claim.” Ex. 2012, 134. The second is a statement
`in support of nearly identical amendment to claim 1 dated March 6, 2008:
`“Further, ‘mixed amphetamine salts’ is a subgroup of drugs falling within
`‘pharmaceutically active amphetamine salts.” Ex. 2012, 217.
`We agree that these amendments narrowed the claims, but are not
`persuaded that either of these statements unambiguously supports Patent
`
`13
`
`
`Page 13
`
`
`
`IPR2015-02009
`Patent RE42,096 E
`
`Owner’s proposed construction. The clause “wherein the pharmaceutically
`active amphetamine salts in (a) and (b) comprise mixed amphetamine salts”
`refers back to “one or more pharmaceutically active amphetamine salts.”
`The “one or more” requirement can be satisfied by a single pharmaceutically
`active amphetamine salt, or by more than one. “Mixed amphetamine salts”
`can be interpreted as requiring more than a single pharmaceutically active
`amphetamine salt.
`
`Thus, at this stage of the proceeding, we are not persuaded that
`Petitioner’s proposed construction is unreasonably broad. Accordingly, for
`purposes of this decision, we construe “mixed amphetamine salts” to mean
`made up of pharmaceutically active amphetamine salts of more than one
`kind.
`
`2. enteric release coating
`Petitioner contends that “[t]he broadest reasonable construction of
`enteric coating, based on the ordinary and customary meaning of this term,
`is ‘a layer of material that protects medication in the stomach and releases
`medicine in the intestines.’” Pet. 13.
`Patent Owner proposes a similar construction:
`A drug release is “enteric” when the release happens after
`a delay, when the drug has passed through the stomach.
`“Covered with an enteric coating” means covered with a coating
`that is intended to delay release of drug until the drug has passed
`through the stomach.”
`The ordinary meaning of ‘enteric’ is: ‘of, referring to, or
`being within the intestines . . . which in context means a
`
`14
`
`
`Page 14
`
`
`
`IPR2015-02009
`Patent RE42,096 E
`
`
`composition designed to pass through the stomach and reach the
`intestines.
`Prelim. Resp. 24 (citing Ex. 1012, 4; Ex. 1008, 19–20).
`Apart from Patent Owner’s use of the words “intended” or
`“designed,” the constructions are essentially the same. For our purposes, we
`need not resolve the nuances of the two constructions, it is enough that we
`are persuaded that “enteric release coating” refers to a coating that will delay
`release of a drug until the drug has passed through the stomach and reached
`the intestines.
`We further note that the specification of the ’096 patent teaches that
`the enteric coating may comprise pH-dependent polymers, which will not
`dissolve “in the acidic stomach environment of approximately below pH 4.5,
`but [are] not limited to this value.” Ex. 1001, 8:12–19. According to the
`specification, “[t]he pharmaceutical active should become available when
`the pH-sensitive layer dissolves at the greater pH, after a certain delayed
`time, or after the unit passes through the stomach” and “[t]he preferred delay
`time is in the range of two to six hours.” Id. at 8:20–24. In addition, the
`specification teaches “[i]n a preferred embodiment, the lag time period is
`only time-dependent, i.e., pH independent” and “[t]he lag time is preferably
`within 4 to 6 hours after oral administration of the delivery system.” Id. at
`3:61–4:8. Finally, the ’096 patent discloses and claims a composition
`“wherein said enteric release coating is a non-pH dependent enteric release
`coating.” Id. at 13:43–44.
`
`15
`
`
`Page 15
`
`
`
`IPR2015-02009
`Patent RE42,096 E
`
`
`3. “essentially all”
`The term “essentially all” is not defined in the ’096 patent. Petitioner
`and Patent Owner agree that “essentially all” means “less than 100%, and
`not less than 80%.” Pet. 17 (citing Ex. 1026, 21; Ex. 1010, 7); Prelim. Resp.
`28 (citing Ex. 2030, 6, 8, 12 (describing dissolution testing “until either 80%
`of the drug from the drug product is released or an asymptote is reached.”).7
`At this stage of the proceeding, we see nothing in the specification or
`prosecution history of the ’096 patent inconsistent with this construction,
`and are persuaded, for purposes of this decision, that one of ordinary skill in
`the art would understand “essentially all” to mean “less than 100%, and not
`less than 80%.”
`
`B. Patent Owner’s Argument under § 325(d)
`Patent Owner argues that we should decline to institute an inter partes
`review pursuant to 35 U.S.C. § 325(d), which gives the Board authority to
`reject a petition that presents the same or substantially the same prior art or
`arguments as were previously presented to the Office. See Prelim. Resp. 7–
`12.
`
`Patent Owner contends that Mehta, the Adderall PDR, and Rosen
`(Exs. 1003, 1004, and 1015) appear on the face of the ‘096 patent, and the
`Examiner acknowledged them. Prelim. Resp. 8 (citing Ex. 1001 [56]; Ex.
`
`
`7 The preliminary Response incorrectly cites Exhibit 2032 for this
`parenthetical. The correct exhibit is Exhibit 2032—SUPAC-MR: Modified
`Release Solid Oral Dosage Forms (1997) (“1997 FDA Guidance).
`16
`
`
`Page 16
`
`
`
`IPR2015-02009
`Patent RE42,096 E
`
`2012, 81, 82). Patent Owner further contends that Mehta was a principal
`reference, and was overcome, during prosecution of the original ’819 patent
`and the ’096 patent upon reissue. Id. Patent Owner contends that the
`Petition depends on arguments about Mehta that already were considered in
`the original prosecution and upon reissue. Id. at 1.
`Under § 325(d), “the Director may take into account whether, and
`reject the petition . . . because, the same or substantially the same prior art or
`arguments previously were presented to the Office.” The permissive
`language in the statute signals that we are not required to reject a petition
`simply because it relies on art that was cited to the Office previously, and we
`decline to do so in this case, at least in part because our preliminary claim
`constructions differ in certain respects from those advanced during
`prosecution.
`
`C. Claims 1–3, 5, 8, 9, 11, 18–21, 23, and 25—
`Asserted Anticipation by Mehta
`1. Mehta (Ex. 1003)
`Mehta discloses that methylphenidate hydrochloride, “available
`
`commercially as, e.g., Ritalin®,” is commonly used to treat the symptoms of
`attention deficit disorder (ADD) and ADHD in children. Ex. 1003, 1:35–42.
`
`Mehta teaches that methylphenidate exists as four separate optical
`isomers—l-threo, d-threo, l-erythro, and d-erythro—and that “the threo pair
`of enantiomers of methylphenidate hydrochloride [the dl-threo racemate] is
`generally administered for the treatment of ADD and ADHD.” Id. at 1:48–
`
`17
`
`
`Page 17
`
`
`
`IPR2015-02009
`Patent RE42,096 E
`
`65, 2:5–7. Mehta teaches that the dl-threo racemate “is a mild central
`nervous system stimulant with pharmacological activity qualitatively similar
`to that of amphetamines” (id. at 2:14–16), and “is a Schedule II controlled
`substance [that] produces a euphoric effect when administered through . . .
`ingestion, and thus carries a high potential for abuse.” Id. at 2:19–22.8
`
`Further according to Mehta:
`An additional problem is that children being treated with
`dl-threo methylphenidate must generally take one or more doses
`during the day. This creates a problem for school administrators
`who must store a controlled substance on school premises, with
`the associated risk that it may be stolen for illicit use.
`Furthermore, children may be traumatized by ridicule from peers
`when they must take medication at school.
`Id. at 2:34–41.
`
`Mehta notes that
`Sustained release formulations of dl-threo methylphenidate have
`been developed, which provide for slow release of the drug over
`the course of the day. However, it has been observed that peak
`plasma concentrations of the drug are lower when sustained
`release formulations are used. In some studies, sustained release
`formulations of methylphenidate have been shown to have lower
`efficacy than conventional dosage forms.
`Id. at 2:42–49.
`
`
`8 Mehta also notes that the dl-threo racemate of methylphenidate is
`associated with “[u]ndesirable side effects . . . includ[ing] anorexia, weight
`loss, insomnia, dizziness and dysphoria.” Ex. 1003, 2:16–18.
`
`
`18
`
`
`Page 18
`
`
`
`IPR2015-02009
`Patent RE42,096 E
`
`
`In order to “eliminate the risk of theft or loss of the second dose,
`while minimizing undesirable side effects and maximizing ease of
`administration” (id. at 2:56–58), Mehta proposes “administer[ing] only the
`active d-threo form of the drug” (id. at 2:29–32), in “a dosage form which
`provides, in one administration, an initial release followed, at a predictable
`delay, by a second release, of maximally effective methylphenidate” (id. at
`2:53–56). Though Mehta emphasizes the advantages of administering a
`composition comprising only the d-threo isomer of methylphenidate
`hydrochloride, the administration of the dl-threo racemate is also disclosed.
`See e.g., Ex. 1003, 15:5–10, 16:10–11.
`
`Mehta teaches that “[t]he release of the first dose preferably occurs
`substantially immediately; for example, within about 30 minutes following
`administration.” Id. at 5:31–33. Then, “[f]ollowing a period of little or
`substantially no drug release, the second dose is released.” Id. at 5: 33–35.
`The period of delay between the first and second doses is “from about 2
`hours to about 7 hours following ingestion before release of the second
`dose.” Id. at 3:18–19. According to Mehta, “the two releases can be
`referred to as ‘pulses’, and such a release profile can be referred to as
`‘pulsatile’.” Id. at 5:35–36. Moreover, Mehta distinguishes between
`“sustained delivery . . . i.e., for the relatively constant administration of a
`drug,” and “pulsatile release of the drug, a very distinct phenomenon.” Id. at
`7:53–60.
`
`19
`
`
`Page 19
`
`
`
`IPR2015-02009
`Patent RE42,096 E
`
`
`
`Mehta further specifies that:
`“Immediate release” . . . means release within about a half
`hour following ingestion, preferably about 15 minutes, and more
`preferably within about 5 minutes following ingestion. “Delayed
`release” . . . refers to a drug release profile which includes a
`period during which no more than about 10 percent of the drug
`in a particular dosage form is released, followed by a period of
`from about 0.5 hour to about 2.5 hours, preferably about 1.5
`hours, more preferably about 1 hour, in which no less than about
`70 percent, preferably no less than about 80 percent, and more
`preferably no less than about 90 percent, of the drug is released.
`Id. at 6:5–16.
`Mehta discloses preparation of layered pellets containing d-threo-
`methylphenidate (d-MPD) cores, coated with a sealant comprising
`hydroxypropyl methylcellulose, and further coated with varying amounts
`and ratios of ammoniomethacrylate polymers (Eudragit® RS30D and
`Eudragit® RL30D) in Examples 1–3, or with Eudragit® NE30D in Example
`4. Ex. 1003, 12:50–14:10. The results of the dissolution measurements are
`presented in Table 1, reproduced below.
`
`20
`
`
`Page 20
`
`
`
`IPR2015-02009
`Patent RE42,096 E
`
`
`
`
`Ex. 1003, 14:21–45. Table 1 presents results of dissolution measurements
`for the various types of layered and coated pellets produced in Mehta’s
`Examples 1–3. Trial 1 is the pellet of Example 4—in which “no delay was
`observed; substantially all of the drug was released within approximately
`one hour.” Id. at 14:8–10. Trials 2–21 are delayed release formulations.
`According to Mehta, “[t]he results indicate that the amount of drug released
`is influenced by: amount of coating, ratio of the two polymers, amount of
`talc, and curing time.” Id. at 13:58–60.
`
`Finally, Mehta teaches that particles (pellets) providing substantially
`immediate release and particles providing delayed release can be combined
`in a capsule, or the two groups of particles can be compressed into a tablet.
`21
`
`
`Page 21
`
`
`
`IPR2015-02009
`Patent RE42,096 E
`
`Id. at 11:55–60. Alternatively, Mehta discloses a layered dosage form
`comprising “a single group of particles providing both a substantially
`immediate dose of a methylphenidate drug, and a delayed dose.” Id. at
`11:66–12:10, 15:57–16:9.
`
`3. Analysis
`Petitioner contends that the subject matter of claims 1–3, 5, 8, 9, 11,
`
`18–21, 23, and 25 is anticipated by Mehta. Pet. 17–35. Patent Owner
`disagrees. Prelim. Resp. 29–35.
`Claims 1–3, 5, 8, 9, and 11
`
`
`Claims 1–3, 5, 8, 9, and 11 are directed to a pharmaceutical
`composition comprising, in relevant part, one or more pharmaceutically
`active amphetamine salts covered with an immediate release coating, and
`one or more “pharmaceutically active amphetamine salts that are covered
`with an enteric release coating” that provides “a delayed pulsed enteric
`release,” “wherein said enteric release coating releases essentially all of said
`one or more pharmaceutically active amphetamine salts coated with said
`enteric coating within about 60 minutes after initiation of said delayed
`pulse[d] enteric release.” Ex. 1001, 12:53–15:8.
`
`Petitioner contends that “Mehta teaches delivery of two time-
`separated releases of methylphenidate drug.” Pet. 20 (citing Ex. 1005,
`¶¶ 183–186). According to Petitioner, “Mehta describes a ‘first dose’ that is
`‘immediate,’ followed by ‘a period of . . . substantiall
Accessing this document will incur an additional charge of $.
After purchase, you can access this document again without charge.
Accept $ Charge
Still Working On It
This document is taking longer than usual to download. This can happen if we need to contact the court directly to obtain the document and their servers are running slowly.
Give it another minute or two to complete, and then try the refresh button.
A few More Minutes ... Still Working
It can take up to 5 minutes for us to download a document if the court servers are running slowly.
Thank you for your continued patience.
This document could not be displayed.
We could not find this document within its docket. Please go back to the docket page and check the link. If that does not work, go back to the docket and refresh it to pull the newest information.
Your account does not support viewing this document.
You need a Paid Account to view this document. Click here to change your account type.
Your account does not support viewing this document.
Set your membership
status to view this document.
With a Docket Alarm membership, you'll
get a whole lot more, including:
- Up-to-date information for this case.
- Email alerts whenever there is an update.
- Full text search for other cases.
- Get email alerts whenever a new case matches your search.
One Moment Please
The filing “” is large (MB) and is being downloaded.
Please refresh this page in a few minutes to see if the filing has been downloaded. The filing will also be emailed to you when the download completes.
Your document is on its way!
If you do not receive the document in five minutes, contact support at support@docketalarm.com.
Sealed Document
We are unable to display this document, it may be under a court ordered seal.
If you have proper credentials to access the file, you may proceed directly to the court's system using your government issued username and password.
Access Government Site
