Trials@uspto.gov
`571-272-7822
`
`Paper No. 15
`Entered: February 3, 2017
`
`UNITED STATES PATENT AND TRADEMARK OFFICE
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`
`MYLAN PHARMACEUTICALSINC.,
`Petitioner,
`
`V.
`
`BOEHRINGER INGELHEIM INTERNATIONAL GMBH,
`Patent Owner.
`
`Case IPR2016-01566
`Patent 9,173,859 B2
`
`Before TONI R. SCHEINER, BRIAN P.MURPHY,and
`ZHENYU YANG,Administrative Patent Judges.
`
`YANG, Administrative Patent Judge.
`
`DECISION
`DenyingInstitution of Inter Partes Review
`37 CFR. § 42.108
`
`
`571-272-7822
`
`Paper No. 15
`Entered: February 3, 2017
`
`UNITED STATES PATENT AND TRADEMARK OFFICE
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`
`MYLAN PHARMACEUTICALSINC.,
`Petitioner,
`
`V.
`
`BOEHRINGER INGELHEIM INTERNATIONAL GMBH,
`Patent Owner.
`
`Case IPR2016-01566
`Patent 9,173,859 B2
`
`Before TONI R. SCHEINER, BRIAN P.MURPHY,and
`ZHENYU YANG,Administrative Patent Judges.
`
`YANG, Administrative Patent Judge.
`
`DECISION
`DenyingInstitution of Inter Partes Review
`37 CFR. § 42.108
`
`
`
`IPR2016-01566
`Patent 9,173,859 B2
`
`INTRODUCTION
`
`Mylan Pharmaceuticals Inc. (“Petitioner”) filed a Petition for an inter
`
`partes review of claims 1-22 of U.S. Patent No. 9,173,859 B2 (“the 859
`
`patent,” Ex. 1001). Paper 2 (“Pet.”). Boehringer Ingelheim International
`
`GmbH (“Patent Owner”) timely filed a Preliminary Response. Paper 9
`
`(“Prelim. Resp.”). We review the Petition under 35 U.S.C. § 314.
`
`Based on this record, we determine Petitioner has not established a
`
`reasonablelikelihood that it would prevail in showing the unpatentability of
`
`at least one challenged claim. Therefore, we decline to institute an inter
`
`partes review of claims 1—22 of the ’859 patent. See 35 U.S.C. § 314(a).
`
`Related Proceedings
`
`Patent Ownerinformsusthat it has asserted the ’859 patent against
`
`Petitioner in Boehringer Ingelheim Pharm. Inc. v. Mylan Pharm. Inc., Case
`
`No. 1:15-cv-00145 (N.D.W.Va.), which is currently inactive. Paper6, 3.
`
`Accordingto the parties, the 7859 patentis the subject of several other
`
`casesin district courts, which have been consolidated into Boehringer
`
`Ingelheim Pharm. Inc. v. HEC Pharm Group, Case No. 3:15-cv-05982
`
`(D.N.J.). Pet. 5; Paper 6, 2. In that case, Patent Owneralso asserted U.S.
`
`Patent Nos. 8,673,927, 8,846,695, and 8,853,156. Pet. 5. Petitioner has
`
`concurrently filed IPR2016-01563, IPR2016-01564, and IPR2016-01565,
`
`challenging those patents respectively. Id.
`
`The ’859 Patent
`
`The ’859 patent describes selected DPP-4 inhibitors that are useful for
`
`treating various diseases, including type 2 diabetes. Ex. 1001, 3:66-4:20,
`
`16:45-17:2. Specifically, the ’859 patent identifies DPP-4 inhibitor 1-[(4-
`2
`
`
`
`IPR2016-01566
`Patent 9,173,859 B2
`
`methy!-quinazolin-2-yl)methy]]-3-methyl-7-(2-butyn-| -yl)-8-(3-(R)-amino-
`
`piperidin-1-yl)-xanthine, also known as BI 1356 orlinagliptin, as
`
`“particularly preferred.” Jd. at 5:20—35.
`
`DPP-4 inhibitors “influence the plasma level of bioactive peptides
`including the peptide GLP-1 andare highly promising molecules for the
`treatment of diabetes mellitus.” Jd. at 1:21-23. The ’859 patent states that
`
`the DPP-4 inhibitors disclosed therein may be used in conjunction with other
`
`antidiabetic agents, such as metformin,“either in a free combination or in a
`
`fixed combination in a tablet.” Jd. at 8:60-9:11, 20:25—51. According to the
`
`°859 patent:
`
`A particularly preferred example of an antidiabetic combination
`partner is metformin in doses of about 100 mg to 500 mgor 200
`mg to 850 mg (1-3 times a day), or about 300 mg to 1000 mg
`once or twice a day, or delayed-release metformin in doses of
`about 100 mg to 1000 mgorpreferably 500 mg to 1000 mg once
`or twice a day or about 500 mg to 2000 mg oncea day.
`
`Id. at 14:6—12.
`
`Illustrative Claims
`
`Amongthe challenged claims, claims 1, 13, 14, and 16-18 are
`
`independent. Claims 1 and 14 are representative and are reproduced below:
`
`l.
`
`A methodoftreating type 2 diabetes comprising
`
`administering to a patient in need thereof (a) 1-[(4-methyl-
`quinazolin-2-yl)methy]]-3-methyl-7-(2-butyn- 1-yl)-8-(3-(R)-a-
`mino-piperidin-1-yl)-xanthine, or a therapeutically active salt
`thereof, in an oral dosage of 2.5 mg or 5 mg, and (b) metformin
`
`wherein the dose of metformin is 100 mg to 500 mg or 200 mg
`to 850 mg (1-3 times a day), or 300 mg to 1000 mg onceor twice
`a day, or as delayed-release metformin in a dose of 500 mg to
`
`3
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`
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`IPR2016-01566
`Patent 9,173,859 B2
`
`1000 mg.onceor twice a day, or 500 mg to 2000 mg once a day,
`-Or
`
`wherein the dose of metformin is 500 mg, 850 mg or 1000 mg as
`a single dose with a total daily dose of metformin of 500-2850
`mg, or 500 mg, 1000 mg, 1500 mg or 2000 mg metformin in
`delayed release form, or
`
`wherein the dose of metforminis 500 mg to 1000 mg.
`
`formulation comprising 1-[(4-methyl-
`tablet
`14. An oral
`quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-a-
`mino-piperidin-1-yl)-xanthine in an amount of 2.5 mg or 5 mg
`optionally
`in
`combination with metformin,
`and
`a
`pharmaceutically acceptable carrier or diluent.
`Asserted Grounds of Unpatentability
`
`Petitioner asserts the following grounds of unpatentability:
`
`Ahrén,* Hughes,‘ and/or Brazg°
`
`The 7510 publication and Glucophage® Label?
`The ’510 Publication and
`
`' Himmelsbachetal., U.S. Patent Publication No. 2004/0097510, published
`May20, 2004 (Ex. 1003).
`2 Glucophage® and Glucophage® XR Label (Ex. 1004).
`3 Ahrén et al., Twelve and 52-Week Efficacy ofthe Dipeptidase IV Inhibitor
`LAF237 in Metformin-Treated Patients with Type 2 Diabetes, DIABETES
`CARE 27:2874—80 (2004) (Ex. 1005).
`4 Hughes, Int’! Pub. No. WO 2005/117861, published December 15, 2005
`(Ex. 1006).
`> Brazg, et al., Effect ofAdding MK-0431 to On-going Metformin Therapy in
`Type 2 Diabetic Patients Who Have Inadequate Glycemic Control on
`Metformin, DIABETES 54 (Suppl. 1):A3 (2005) (Ex. 1007).
`4
`
`
`
`IPR2016-01566
`Patent 9,173,859 B2
`
`In support ofits patentability challenge, Petitioner relies on the
`
`Declaration of Dr. Mayer B. Davidson. Ex. 1002.
`
`ANALYSIS
`
`Claim Construction
`
`In an inter partes review, the Board interprets a claim term in an
`
`unexpired patent accordingto its broadest reasonable constructionin light of
`
`the specification of the patent in which it appears. 37 C.F.R. § 42.100(b);
`
`Cuozzo Speed Techs., LLC v. Lee, 136 S. Ct. 2131, 214446 (2016). Under
`
`that standard, and absent any special definitions, we assign claim termstheir
`
`ordinary and customary meaning, as would be understood by oneof ordinary
`
`skill in the art at the time of the invention,in the context of the entire patent
`
`disclosure. In re Translogic Tech., Inc., 504 F.3d 1249, 1257 (Fed. Cir.
`
`2007).
`
`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.
`
`Anticipation by the ’510 Publication
`
`Petitioner asserts that the °510 publication anticipates claims 14 and
`
`20. Pet. 30-31. Based on the current record, we determinePetitioner has
`
`not established a reasonable likelihood that it would prevail in this assertion.
`
`The ’510 publication discloses a genus of substituted xanthine
`
`compoundsthat act as DPP-IV inhibitors, particularly for the prevention and
`
`treatment of type 2 diabetes. Ex. 1003, Abstract, FJ 3, 4. It discloses
`
`linagliptin as one in a series of 30 “[m]Jost particularly preferred” substituted
`5
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`
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`IPR2016-01566
`Patent 9,173,859 B2
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`xanthine compounds. Jd. F§ 232, 245. It also lists the ICso values of nearly
`50 DPP-IV inhibitor compounds,includinglinagliptin.® Id. § 295.
`
`Linagliptin is one of six compoundslisted as having the highest potency in
`
`the group, with the lowest ICs value of 1 nM. Jd.
`
`According to the ’510 publication, the substituted xanthine
`
`compoundsdisclosed therein, dueto their “ability to inhibit DPP-IV
`activity,” are expected to be suitable “for the prevention or treatment of
`
`diseases or conditions such as type | and type 2 diabetes mellitus.” Jd.
`
`{ 297. The ’510 publication discloses that “[t]he compounds according to
`
`the invention mayalso be used in conjunction with other active substances,”
`
`including antidiabetics, such as metformin. Jd. { 298.
`
`Claim 14 of the ’859 patent recites “[a]n oral tablet formulation
`
`comprising [linagliptin] in an amount of 2.5 mg or 5 mg optionally in
`
`combination with metformin, and a pharmaceutically acceptable carrier or
`
`diluent.” Claim 20 recites “[a] method oftreating type 2 diabetes
`
`comprising administering to a patient in need thereofthe oral tablet of claim
`
`14, wherein the daily oral amountof[linagliptin] administered to said
`
`patient is 5 mg.”
`
`Petitioner refers to the ’510 publication for disclosing that the
`
`substituted xanthine compounds thereof may beorally administered in the
`
`amountof “1 to 1000 mg, preferably 1 to 100 mg,in each case 1 to 4 times
`
`therein a day,” to achieve a therapeutic effect. Pet. 22 (citing Ex. 1003
`
`{ 300). According to Petitioner, because the 510 publication discloses “the
`
`6 Linagliptin is Example 2 (142)). Ex. 1003 ff] 1933-1937, 2400.
`6
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`IPR2016-01566
`Patent 9,173,859 B2
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`most preferable oral dosage range for linagliptin” that encompasses the
`
`dosesrecited in claims 14 and 20, it anticipates those claims. Jd. at 22, 30.
`
`Weare not persuaded.
`
`To anticipate a claim, a single prior art reference must discloseall
`
`limitations “arranged as in the claim,” either expressly or inherently.
`
`Connell v. Sears, Roebuck & Co., 722 F.2d 1542, 1548 (Fed. Cir. 1983). To
`
`be “arrangedasin the claim,” the anticipatory reference must “showall of
`
`the limitations of the claims arranged or combined in the same way as
`
`recited in the claims, not merely in a particular order.” NetMoneyln,Inc. v.
`
`Verisign, Inc., 545 F.3d 1359, 1369 (Fed. Cir. 2008). Whether a generic
`
`disclosure necessarily anticipates everything within the genus depends on
`
`the factual aspects of the specific disclosure and the particular products at
`
`issue. Sanofi-Synthelabo v. Apotex, Inc., 550 F.3d 1075, 1083 (Fed.Cir.
`
`2008).
`
`The Federal Circuit’s opinion in OSRAM Sylvania, Inc. v. Am.
`
`Induction Techs., Inc., 701 F.3d 698 (Fed. Cir. 2012) is instructive. In that
`case, the dispute centered on whetherthe priorart disclosure of
`“approximately 1 torr or less” anticipates the limitation “less than 0.5 torr”
`
`in the challenged claim. Jd. at 706. The Federal Circuit reversed the district
`court’s granting of summary judgmentof anticipation. Jd. Accordingto the
`
`Federal Circuit, the patent challenger there relied on “the conclusory claim
`
`that less than 0.5 torr necessarily falls within ‘approximately 1 torr or less’
`as a matter of fact.” Jd. The court explained:
`.
`
`While true, the inquiry does not end there. How oneofordinary
`skill in the art would understand the scope of the disclosure or,
`
`7
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`IPR2016-01566
`Patent 9,173,859 B2
`
`stated differently, how one of ordinary skill in the art would
`understand the relative size of a genus or species in a particular
`technologyis of critical importance.
`
`Id.
`
`The facts in this case are similar to those in OSRAM. Here,Petitioner
`
`relies on a conclusory statementthat “the most preferable oral dosage range
`
`for linagliptin [disclosed in the ’510 publication] encompassesand thus
`
`anticipates the claimed dose recited” in the challenged claims. Pet. 22, 30;
`
`see also Ex. 1002 4 51 (stating the same). But, Dr. Davidson does not
`
`testify, and Petitioner does not argue, that an ordinary artisan would
`
`understand any dosage within the preferred dose of 1 to 100 mg
`
`administered “1 to 4 times a day” disclosed in the 7510 publication to be
`
`efficacious.
`
`We emphasize that in an inter parte review,Petitioner has the ultimate
`
`burden of persuasion to prove unpatentability by a preponderance ofthe
`
`evidence. 35 U.S.C. § 316(e); Dynamic Drinkware, LLC v. Nat’l Graphics,
`
`Inc., 800 F.3d 1375, 1378-79 (Fed. Cir. 2015). Here, the only evidence
`
`Petitioner relies on is a broad rangeofpotential linagliptin dosages. That
`
`does not amount to a preponderanceof the evidence.
`
`Petitioner cites Perricone v. Medicis Pharma. Corp., 432 F.3d 1368
`(Fed. Cir. 2005). Pet. 22,25. The facts in this case are distinguishable from
`
`those in Perricone. There, the prior art discloses a composition having an
`
`active ingredient in a concentration range that not only encompasses, but
`
`also “does not significantly deviate from,” the claimed ranges. Perricone,
`
`432 F.3d at 1377. In contrast, in the present case, the dosage range disclosed
`
`
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`IPR2016-01566
`Patent 9,173,859 B2
`
`in the prior art is from 20% to 160 times the claimed dosages(1.e., 1 mg in
`the ’510 publication versus 5 mg claimed (20%), and 400 mgin the *510
`publication versus 2.5 mg claimed (160 times)). Petitioner does not explain
`
`why, based on the disclosure of a genus of dosage ranges for DPP-4
`
`inhibitors, a person of skill in the art would immediately envisage
`
`administering linagliptin in the dosage amounts recited in the challenged
`
`claims 14 and 20. See OSRAM, 701 F.3d at 706 (explaining that “priorart’s
`
`teaching of a broad genus does not necessarily disclose every species within
`
`that genus”).
`
`As a result, we determine Petitioner has not shown a reasonable
`
`likelihood of prevailing in its assertion that the °510 publication anticipates
`
`claims 14 and 20 of the ’859 patent.
`
`Obviousness over the ’510 Publication and Glucophage® Label
`
`Petitioner asserts that claims 1-22 would have been obviousoverthe
`
`combination of the ’510 publication and Glucophage® Label. Pet. 18-30.
`
`Basedon the current record, we determinePetitioner has not established a
`
`reasonable likelihood that it would prevail in this assertion.
`
`Claims 1-13, 15-19, 21, and 22
`
`
`The Glucophage® Label provided by Petitioner as Exhibit 1004
`
`includes a coverpagestating it is the “FINAL PRINTED LABELING?”for
`
`application number 20-357/S019 at the Food and Drug Administration
`
`(“FDA”) Center for Drug Evaluation and Research. Ex. 1004, 1.
`
`Glucophage® is described in the document as metformin hydrochloride
`
`tablets and Glucophage® XR is described as metformin hydrochloride
`
`extended release tablets, both indicated for the treatment of type 2 diabetes.
`
`9
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`IPR2016-01566
`Patent 9,173,859 B2
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`Id. at 2. The Glucophage® Label contains a date “Revised January 2001.”
`
`Id. at 7.
`
`Relying on the Davidson Declaration, Petitioner contendsthat the
`
`Glucophage® Label qualifies as prior art under 35 U.S.C. §102(b) becauseit
`
`wasapproved and published by the FDA for treating type 2 diabetes in
`
`February 2001. Pet. 19 (citing Ex. 1002 § 48). Patent Owner counters
`
`Mylan has not met its burden to show that Exhibit 1004, “purporting to be
`
`the Glucophage label as-approved,is, in fact, a printed package insert, much
`
`less one that was publically available prior to” the priority date of the °510
`
`patent. Prelim. Resp. 14-17. We agree with Patent Owner.
`
`Under 35 U.S.C. § 311(b), a petitioner in an inter partes review may
`
`only challenge the claims of a patent based on “prior art consisting of patents
`
`or printed publications.” 35 U.S.C. § 311(b). Petitioner has the ultimate
`
`burden of persuasion to prove unpatentability by a preponderanceofthe
`
`evidence. Dynamic Drinkware, LLC v. Nat’l Graphics, Inc., 800 F.3d 1375,
`
`1378-79 (Fed. Cir. 2015). Petitioner also bears the initial burden of
`
`production to establish the existence ofprior art that renders the claims
`
`unpatentable. Jd. To satisfy the initial burden of production, we have often
`
`required a petitioner to make a threshold showingthat the reference relied
`
`upon waspublicly accessible as a printed publication prior to the effective
`
`filing date of a challenged patent. See, e.g., Frontier Therapeutics, LLCv.
`
`Medac. Gesellschaft Fur Klinische Spezialpraparate MBH, Case IPR2016-
`
`00649, slip op. at 22 (PTAB September 1, 2016) (Paper 10) (finding that an
`
`alleged “printed package insert” was not a printed publication); Symantec
`
`Corp. v. Trs. of Columbia Univ., Case IPR2015-00371, slip op. at 5—9
`10
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`
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`IPR2016-01566
`Patent 9,173,859 B2
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`(PTAB June 17, 2015) (Paper 13); Temporal Power, Ltd. v. Beacon Power,
`
`LLC, Case IPR2015-00146,slip op. at 8-11 (PTAB Apr. 27, 2015) (Paper
`
`10); Dell, Inc. v. Selene Comm’n Techs., LLC, Case IPR2014-01411, slip op.
`
`at 21-22 (PTAB Feb. 26, 2015) (Paper 23).
`
`“A given referenceis “publicly accessible” upona satisfactory
`
`showing that such document has been disseminated or otherwise made
`
`available to the extent that persons interested and ordinarily skilled in the
`
`subject matter or art exercising reasonable diligence, can locateit.”
`
`Bruckelmyer v. Ground Heaters, Inc., 445 F.3d 1374, 1378 (Fed. Cir. 2006).
`
`Here, the Glucophage® Label does not contain any source identifying
`
`information, e.g. as an FDA-approvedlabel, or other indicia of when the
`
`document becamepublicly available. See Prelim. Resp. 15. For example,
`
`the Glucophage® Label submitted by Petitioner contains noindiciathatit
`
`(1) is a certified copy of a public record, (2) is copied from an official 2001
`
`publication such as the United States Pharmacopoeia—National Formulary,
`
`(3) is copied from a recognized periodical published in 2001 such as the
`
`Physicians’ Desk Reference, or (4) otherwise bears the hallmarksofa self-
`
`authenticating documentpublished in 2001. See Fed. R. Evid. 902 (4){7),
`
`(11). Exhibit 1004 indicates the label was revised in January 2001, butit
`
`bears no source identifying information from the FDA, a copyright date, or
`
`any other indicia of a publication date.
`
`Dr. Davidsonstates that Glucophage® IR, a metformin hydrochloride
`
`immediate release tablet, has been available since 1994, and Glucophage®
`
`XR, a long-acting extended-release form of metformin, has been available
`
`since 2000. Ex. 1002 Ff 29, 49. He, however, cites the January 2001
`1]
`
`
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`IPR2016-01566
`Patent 9,173,859 B2
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`revision of the Glucophage® Label in support. Jd. 429. With regard to the
`
`Glucophage® Label, Dr. Davidson merely parrots the same statementin the
`
`Petition, that is, the label was approved and published by the FDA for
`
`treating type 2 diabetes in February 2001. Id. § 48.
`
`Dr. Davidson doesnot provide a sufficient explanation or foundation
`
`to establish his personal knowledge of the Glucophage® Label’s alleged
`
`publication in February 2001. The statements that Glucophage® was
`
`approved by the FDA in 1994 and Glucophage® XR in 2000, by
`
`themselves, are insufficient as a threshold showing that the Glucophage®
`
`Label wasa publicly available printed publication as of February 2001.
`
`Earlier FDA approval of the Glucophage® drug products is not co-extensive
`
`with a February 2001 publication date of the revised Glucophage® Label, on
`
`whichPetitioner relies for proof of the specific metformin dosesrecited in
`
`claims 1-13, 15-19, 21, and 22. See Pet. 21-29.
`
`In sum, Petitioner has notsatisfied its burden to show that the
`Glucophage® Label was available as a prior art printed publication.
`Therefore, we determine Petitioner has not shown a reasonable likelihood of
`
`prevailing on its assertion that claims 1-13, 15-19, 21, and 22 of the ’859
`
`patent would have been obvious overthe ’510 publication and the
`
`Glucophage® Label.
`
`Claims 14 and 20
`
`Neither claim 14 nor claim 20 recites a specific metformin dose.
`
`Nevertheless, we find Petitioner has not shown a reasonable likelihood of
`
`prevailing onits assertion that claims 14 and 20 of the ’859 patent would
`
`have been obvious overthe ’510 publication and the Glucophage® Label.
`
`12
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`Each of claims 14 and 20recites a specific linagliptin dosage. Claim
`
`14 requires an oral tablet formulation of linagliptin in an amount of 2.5 mg
`
`or 5 mg, and claim 20 requires administering linagliptin in a daily amountof
`
`5 mg. .In its obviousness challenge, Petitioner relies on the same conclusory
`
`statementof linagliptin dosageas in its anticipation argument, that is, the
`
`’510 publication discloses “the most preferable oral dosage range for
`
`linagliptin encompasses and thus anticipates the claimed dose recited”in the
`
`challenged claims. Pet. 22, 30. Again, such a single sentence, devoidof any
`further analysis, does not satisfy Petitioner’s burden to prove unpatentability
`
`by a preponderanceof the evidence. See 35 U.S.C. § 316(e).
`
`For example, Petitioner does not explain why an ordinary artisan
`
`would have had a reason to modify the teachings of the ?510 publication to
`
`arrive at the claimedlinagliptin dosage of 2.5 mg or 5 mg. Indeed, the ’510
`
`publication teaches drug formulation for oral administration with 75 mg to
`
`150 mg DPP-4 inhibitor. Ex. 1003 {J 2898-911. While this does not, as
`
`Patent Ownerasserts, amounts to teaching away from the claimedlinagliptin
`
`dosage (see Prelim. Resp. 29), Petitioner presents no credible evidence or
`
`otherwise explains why one of ordinary skill in the art, in view of such a
`
`teaching, would have had a reason to pursue a dosage morethan 10-fold
`
`lower than suggested in the ?510 publication.
`
`As a result, we determine Petitioner has not shown a reasonable
`likelihood of prevailing onits assertion that claims 14 and 20 of the ’859
`
`patent would have been obviousoverthe ’510 publication and the
`
`Glucophage® Label.
`
`13
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`Obviousness over the ’510 Publication and Ahrén, Hughes, and/or Brazg
`
`Petitioner asserts that claims 1-22 would have been obvious over the
`
`combination of the ?510 publication and Ahrén, Hughes, and/or Brazg. Pet.
`
`31-43. Based on the current record, we determine Petitioner has not
`
`established a reasonable likelihood that it would prevail in this assertion.
`
`Ahrén describesthe clinical effect of DPP-4 inhibitor LAF237
`
`(vildagliptin) when combined with metforminto treat patients with type 2
`
`diabetes. Ex. 1005, 2874-75. Ahrén compares two groupsof type 2
`
`diabetes patients treated with either metformin monotherapy (1500 to 3000
`
`mg per day), or metformin (1,500 to 3,000 mgper day) and vildagliptin (50
`
`mg once per day) combination therapy. Jd. at 2874. Ahrén showsthat
`“when added to metformin treatment, LAF237 waseffective at improving
`
`glycemic control for at least 1 year in patients with type 2 diabetes and
`
`appeared to be well tolerated.” Jd. at 2878.
`
`Like Ahrén, Hughesteaches a method oftreating patients with type 2
`
`diabetes using a combination of LAF237 (vildagliptin) and metformin over
`an extended period of time. Ex. 1006, Abstract, 3-4, 13’. It teachesthat
`
`vildagliptin may be administered in an oral daily dosage “between 1 and 100
`
`mg; preferably between 10 and 100 mg e.g. 10 mg; most preferably between
`
`25 and 100 mg e.g. 25 mg or 30 or 40 or 50, 61, 70, 90, 100 mg.” Jd. at 23.
`
`Metformin is administered at a daily dosage in the range of about 50 mg to
`
`about 3000 mg, preferably from about 500 mg to about 2000 mg,using
`
`commercially available 500 mg tablets. Jd. Hughes describesa clinical
`
`7 Page referencesare to the exhibit pages, not the internal documentpages.
`14
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`IPR2016-01566
`Patent 9,173,859 B2
`
`study treating patients with type 2 diabetes who werealready receiving
`
`metformin. Jd. at 25. In the Hughesstudy, patients were treated with
`
`vildagliptin (50 mg once daily) in addition to metformin (1500-3000 mg
`
`daily). Id. Hughesreports that the combination therapy achievedbetter
`
`clinical results when compared to metformin plus placebo treatment. Jd. at
`
`26-33.
`
`Brazg reports the efficacy of combining the DPP-4 inhibitor MK-0431
`
`(sitagliptin) with ongoing metformin therapy in type 2 diabetes patients. Ex.
`
`1007, 2. Brazg notes that “[m]etformin is a commonly usedfirst-line
`
`antihyperglycemic agent.” Jd. Brazg states that “[c]ombination treatment
`
`with MK-0431[sitagliptin] and metformin may be useful since these agents
`
`target different pathophysiologic process leading to hyperglycemiain [type
`
`II diabetes].” Jd. In the Brazg study, “the combination of MK-0431
`
`[sitagliptin] and metformin wasefficacious and generally well-tolerated as a
`
`treatment regimen” for patients with type 2 diabetes. Jd.
`
`Petitioner argues that the combination ofthe asserted prior art teaches
`
`each limitation in the challenged claims. Pet. 36-37, 40-43. Petitioner also
`
`contends that an ordinary artisan would have had a reason to combine the
`
`prior-art teachings and would have had a reasonable expectation of success
`
`in doing so. Jd. at 38-39. Patent Ownerchallenges each assertion by
`
`Petitioner. See Prelim. Resp. 17-33.
`
`For purposesof this Decision, we assume, without deciding, that one
`
`of ordinary skill in the art would have combinedthe teachingsof the prior
`
`art. Petitioner, however, has not presented credible evidence or otherwise
`
`15
`
`
`
`IPR2016-01566
`Patent 9,173,859 B2
`
`persuasively argued that such an artisan would havearrivedat the linagliptin
`
`dosagesrecited in the challenged claims.
`
`Petitioner, again, in a conclusory fashion, arguesthat the 7510
`
`publication teaches the claimed linagliptin dosages. See Pet. 36 (“The ’510
`
`Publication discloses the combination of metformin andtherecited oral
`
`doses of a DPP-IV Inhibitor (linagliptin).””); id. at 41 (“As described in Table
`
`1 above in Ground1, the °510 Publication discloses linagliptin dosages of
`
`2.5mg and 5mg.”) (citing Ex. 1003
`
`300). As explained above, based on
`
`the current record, we are not persuadedthat an ordinary artisan would have
`
`had a reason to modify the teachings of the ’510 publication—apreferred
`
`dose of 1 to 100 mg administered “1 to 4 times a day”—to arrive at the
`
`claimed linagliptin dosage of 2.5 mg or 5 mg.
`
`Wenote Petitioner’s assertion “the ’510 Publication reports that
`
`linagliptin [is] more potent than vildagliptin or sitagliptin.” Pet. 38 (citing
`
`Ex. 1002 { 85; Ex. 1003, § 295; Ex. 1011, 158). Dr. Davidson, however,
`
`testifies that “[lJinagliptin’s purported higher potency would have
`
`potentially allowed for smaller doses of DPP-IV inhibitor to be administered
`
`to the patient.” Ex. 1002 4 85. Such testimony is speculative and again,
`
`does not amountto a preponderanceof the evidence. Asa result, we
`
`determine Petitioner has not established a reasonable likelihood that it would
`
`prevail in showing claims 1—22 obvious over the combination of the ’510
`
`publication and Ahrén, Hughes, and/or Brazg.
`
`16
`
`
`
`IPR2016-01566
`Patent 9,173,859 B2
`
`CONCLUSION
`
`For the foregoing reasons, we determine that Petitioner has not shown
`
`there is a reasonable likelihood that it would prevail in proving the
`
`unpatentability of claims 1—22 of the ’859 patent.
`
`In consideration of the foregoing, it is hereby:
`
`ORDER
`
`ORDEREDthatpursuant to 35 U.S.C. § 314(a), the Petition for inter
`
`partes review of the ’859 patent is denied and notrial is instituted.
`
`PETITIONER:
`
`Thomas Parker
`thomas.parker@alston.com
`
`Chris McArdle
`chris.mcardle@alston.com
`
`Ellen Cheong
`ellen.cheong@alston.com
`
`Charles Naggar
`charles.naggar@alston.com
`
`17
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`
`
`IPR2016-01566
`Patent 9,173,859 B2
`
`PATENT OWNER:
`
`Leora Ben-Ami
`leora.benami@kirkland.com
`
`Eugene Goryunov
`egoryunov@kirkland.com
`
`Mira Mulvaney
`mira.mulvaney@kirkland.com
`
`18
`
`
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