`1201 NORTH MARKET STREET
`P.O. BOX 1347
`
`“VILMINGTON, DELAWARE 19899—1347
`
`
`JAth.Bunmlmn
`(3021 351—9291
`thimenfeld®uumcom
`
`(302) 658—9200
`(302) 658—3989 FAX
`
`September 18, 2018
`
`The Honorable Richard G. Andrews
`United States District Comt for the District of
`
`HIGHLY CONFIDENTIAL —
`PROTECTIVE ORDER MATERIAL
`
`Delaware
`
`844 North King Street
`Wilmington, DE 19801
`
`FILED UNDER SEAL
`
`Re:
`
`Bayer Intellectual Property GmbH v. Tare Pharmaceutical Industries, Ltd.
`C .A. No. 17-462 (RGA)
`
`Dear Judge Andrews:
`
`Plaintiffs Bayer Intellectual Property GmbH, Bayer AG, and Janssen Pharmaceuticals,
`Inc., (collectively, “Plaintiffs”) write to bring an additional claim construction dispute to the
`
`Couit’s attention, and to seek the Comt’s illidance on how to iroceed. ibis disiute arises from
`
`On July 3, 2018, this Corut issued a Mar/mm" Order constluing the telm “rapid-release
`tablet” in US. Patent Nlunber 9,539,218 (“the ’218 patent”). See D1. 91. The Court adopted
`Plaintiffs’ proposed construction, which was based on the express definition of the phrase
`provided in the ’2 l8 patent’s specification: “a tablet which, according to the USP release method
`using apparatus 2 (paddle), has a Q value (30 minutes) of 75%.” Id. As desc1ibed in further
`detail below, however, Plaintiffs and Mylan now dispute the meaning of the Court’s
`construction.
`
` a petition for
`
`Plaintiffs seek to file this letter under seal because Plaintiffs do not have Mylan’s permission
`1
`to share information contained in this letter with the other defendants.
`See BI. 27 at 1[ 7.2(a)
`(protective order).
`
`F M
`
`YLAN — EXHIBIT 1066
`
`Mylan Pharmaceuticals Inc. V. Bayer Intellectual Property GmbH
`IPR2018-01143
`
`PROTECTIVE ORDER MATERIAL
`
`0001
`
`
`
`The Honorable Richard G. Andrews
`
`September 18, 2018
`Page 2
`
`interpartes review of the ’218 patent asserting that a tablet that releases more than 75% of its
`active ingredient in 30 minutes satisfies the claim limitation of “a tablet which, according to the
`USP release method using apparatus 2 (paddle), has a Q value (30 minutes) of 75%.” See
`Exh. A (Mylan’s IPR Petition) at 47-48 (“Forsman Example 1a released 94% of anticoagulant at
`pH 1 and at pH 6.8. As Dr. Benet [Mylan’s expert] explains, such a tablet necessarily released
`75% within 30 minutes as well. Forsman thus demonstrated that its Example 1A rapid—release
`tablet had a Q value (30 minutes) of 75% according to the USP release method using apparatus 2
`(paddle) because it resulted in at least 75% dissolution within 30 minutes.” (citations omitted)).
`
`
`
`Mylan did not suggest— during the original claim
`construction proceedings, and Plaintiffs were imaware of it rmtil well after the Corut’s Markman
`Order had issued.
`Indeed, Mylan did not make its position known until after it had served its
`First Supplemental Objections and Responses to Plaintiffs’ Interrogatories on August 13, 2018.
`Plaintiffs then sought further clarity in a meet and confer call. Had Mylan timely raised this
`issue, the parties could have addressed it during the claim construction process.
`
`Plaintiffs are prepared to brief this issue for the Corut on an accelerated briefing schedule
`with short submissions by each side. Proceeding in this way would simplify expert discovery
`and the presentation of evidence at trial, including potentially eliminating the presentation of a
`doctrine of equivalents case in the alternative. Plaintiffs therefore proposed that the parties
`jointly seek supplemental claim construction; Mylan, however, rejected Plaintiffs proposal.
`Alternatively, the issue that Mylan has raised is straightforward and could also be addressed at
`trial rather than now, if that is the Corut’s preference.
`
`Plaintiffs are available to discuss this issue further at the Court’s convenience.
`
`Respectfully,
`
`/s/jack,$. $[umenfelif
`
`Jack B. Blumenfeld (#1014)
`
`JBB/bac
`
`Enclosure
`
`cc:
`
`Clerk of the Court (via hand delivery; w/enclosru‘e)
`Corursel of Record Mylan Pharmaceuticals Inc. (via electronic mail; w/enclosru'e)
`
`PROTECTIVE ORDER MATERIAL
`
`0002
`
`
`
`Exhibit A
`Excerpt of Petition in
`IPR2018-01143
`
`0003
`
`PROTECTIVE ORDER MATERIAL
`
`
`
`Filed on behalf of: Mylan Pharmaceuticals Inc.
`By: Steven W. Parmelee
`Michael T. Rosato
`Jad A. Mills
`Wilson Sonsini Goodrich & Rosati
`
`UNITED STATES PATENT AND TRADEMARK OFFICE
`_____________________________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`
`_____________________________
`
`MYLAN PHARMACEUTICALS INC.,
`Petitioner,
`
`v.
`
`BAYER INTELLECTUAL PROPERTY GMBH,
`Patent Owner.
`
`_____________________________
`
`Case No. IPR2018-01143
`Patent No. 9,539,218
`_____________________________
`
`PETITION FOR INTER PARTES REVIEW
`OF U.S. PATENT NO. 9,539,218
`
`0004
`
`PROTECTIVE ORDER MATERIAL
`
`
`
`TABLE OF CONTENTS
`
`I.
`
`INTRODUCTION .............................................................................................. 1
`
`A.
`
`B.
`
`C.
`
`D.
`
`Brief Overview of the ’218 Patent....................................................... 3
`
`Brief Overview of the Prosecution History ......................................... 4
`
`Brief Overview of the Scope and Content of the Prior Art .................. 6
`
`Brief Overview of the Level of Skill in the Art ................................. 11
`
`II.
`
`GROUNDS FOR STANDING ............................................................................. 13
`
`III. MANDATORY NOTICES UNDER 37 C.F.R. § 42.8 ........................................... 13
`
`IV.
`
`V.
`
`STATEMENT OF THE PRECISE RELIEF REQUESTED ......................................... 15
`
`CLAIM CONSTRUCTION ................................................................................ 15
`
`VI. BACKGROUND KNOWLEDGE IN THE ART PRIOR TO JANUARY 31, 2005 .......... 26
`
`VII. DETAILED EXPLANATION OF GROUNDS FOR UNPATENTABILITY .................... 31
`
`A.
`
`B.
`
`[Ground 1] Claims 1-4 are Obvious under 35 U.S.C. § 103 over
`the ’610 Publication and Kubitza Abstracts....................................... 31
`
`[Ground 2] Claims 1-4 are Obvious under 35 U.S.C. § 103 over
`the ’610 Publication, Kubitza Abstracts, and Forsman. ..................... 46
`
`VIII. NO UNEXPECED RESULTS ............................................................................ 50
`
`IX. CONCLUSION ............................................................................................... 55
`
`X.
`
`XI.
`
`CERTIFICATE OF COMPLIANCE ...................................................................... 56
`
`PAYMENT OF FEES UNDER 37 C.F.R. §§ 42.15(A) AND 42.103 ...................... 57
`
`XII. APPENDIX – LIST OF EXHIBITS...................................................................... 58
`
`i
`
`0005
`
`PROTECTIVE ORDER MATERIAL
`
`
`
`
`
`oral solution, maximal plasma concentration
`were observed after about 0.5 hours. . ..Lower
`
`
`
`peak concentration of approximately 50%
`were observed 2 hours after administration of
`
`
`the tablet.” EX1006 at 0015 (Abstract
`#3010); EX1002, 1198, 107—16, 118-21, 124—
`
`27; EX1003, 111177, 89.
`
`B.
`
`[Ground 2] Claims 1—4 are Obvious under 35 U.S.C. § 103 over
`the ’610 Publication, Kubitza Abstracts, and Forsman.
`
`In view of the combined teachings of the ‘610 publication, Kubitza
`
`Abstracts, and additionally Forsman, claims 1-4 further would have been obvious
`
`to a person of ordinary skill in the art before the critical date of the ‘218 patent
`
`even if the term “rapid-release tablet” were amended to require a “rapid-release
`
`tablet having a Q value of (30 minute) of 75%.” EX1002, 11133.
`
`The combined teachings of the ‘610 publication and Kubitza Abstracts are
`
`discussed in Ground 1. Forsman additionally teaches that immediate/rapid-release
`
`tablets have utility “in the prophylaxis and/or treatment of thromboembolism”
`
`EX1007, 1:6-9; EX1002, 11134; EX1003, 1195; see also EX1019 at 1300
`
`(prophylaxis and therapy of thromboembolic disorders may require a rapid onset of
`
`action); EX1032 at 1:14-16 (for “treatment or prophylaxis of thrombosis,
`
`immediate release formulations may be necessary to ensure that a sufficient
`
`amount of drug is provided in plasma ...to enable quick onset of action”); EX1006
`
`at 0015 (rivaroxaban has rapid onset of action). Forsman thus teaches methods for
`
`formulating immediate/rapid-release oral tablets for low molecular weight
`
`46
`
`PROTECTIVE ORDER MATERIAL
`
`0006
`
`
`
`anticoagulant thrombin inhibitors. In light of the disclosure in Kubitza Abstracts
`
`that the liquid oral dosage form achieved maximum blood concentrations even
`
`faster (~30 minutes) than rapid-release tablet (~2 hrs), a person of ordinary skill
`
`before January 2005 would have had good reason to develop rapid-release tablet
`
`that releases rivaroxaban as rapidly after oral administration as possible. EX1002,
`
`¶¶134-35, 141-43.
`
`Forsman’s immediate release tablets are “based on conventional
`
`manufacturing processes….that provides a dissolution which is not, or very little
`
`dependent on pH.” EX1007, 1:13:21; EX1002, ¶¶104 (discussing manufacture of
`
`Forsman Example 1a tablets), 136 (discussing EX1036 (Golub et al. 78 J.
`
`ALLERGY CLIN. IMMUNOL. (1986) 689-94) at 689, 691, 693). Forsman’s rapid-
`
`release tablets released “more than 85% [of the thrombin inhibitor] within 30
`
`minutes in acidic as well as neutral environment.” EX1007, 3:29-4:2. Indeed,
`
`Forsman Example 1a released 94% of anticoagulant at pH 1 and at pH 6.8. Id. at
`
`7:1-8:2; see also id. at FIG. 1. As Dr. Benet explains, such a tablet necessarily
`
`released 75% within 30 minutes as well. EX1002, ¶¶135, 138. Forsman thus
`
`demonstrated that its Example 1A rapid-release tablet had a Q value (30 minutes)
`
`of 75% according to the USP release method using apparatus 2 (paddle) because it
`
`resulted in at least 75% dissolution within 30 minutes. Id. at ¶¶102-03; see also
`
`EX1054 (Chapter 711 Dissolution, THE UNITED STATES PHARMACOPEIA (USP)
`
`47
`
`0007
`
`PROTECTIVE ORDER MATERIAL
`
`
`
`2000) at 1943 (“Where a single time specification is given, the test may be
`
`concluded in a shorter period if the requirement for minimum amount dissolved is
`
`met.”); EX1033 (Saccone et al., 11 DISSOLUTION TECH. (2004) 25-28) at 25.
`
`Dr. Benet confirms that a person of ordinary skill seeking to develop a rapid-
`
`release tablet formulation for rivaroxaban would have had good reason to use
`
`Forsman’s formulation, which was taught to be useful for administering thrombin
`
`inhibitors for the prophylaxis and therapy of thromboembolisms without being pH
`
`dependent, and would have had a reasonable expectation of success in doing so.
`
`EX1002, ¶¶101, 137-39.
`
`Although Dr. Benet testifies that it would have been obvious to make a
`
`rapid-release tablet with a Q value (30 minutes) of 75% for rivaroxaban and to
`
`administer it once daily to a patient in need thereof for five consecutive days as
`
`claimed by the ’218 patent, he also explains that there is no criticality to the 75% Q
`
`value. EX1002, ¶¶140-43.
`
`For each of the reasons discussed above, each of claims 1-4 would have
`
`been obvious to a person of ordinary skill in the art in view of the combined
`
`teachings of the ’610 publication, Kubitza Abstracts, and Forsman. The claim chart
`
`below provides exemplary citations where the specific elements of these claims are
`
`found in the asserted references, and where they are addressed in the
`
`accompanying declarations of Drs. Benet and Doherty.
`
`48
`
`0008
`
`PROTECTIVE ORDER MATERIAL
`
`
`
`9,539,218 Patent Claims
`
`1. A method of treating a
`thromboembolic disorder
`
`comprising administering a
`direct factor Xa inhibitor that is
`
`5-Chloro-N-({(SS)-2-oxo-3-[4-
`(3-oxo-4-morpholinyl)phenyl]-
`1 , 3 -oxazolidin—S —yl} methyl)—2-
`thiophenecarboxamide no more
`than once daily for at least five
`consecutive days in a rapid-
`release tablet to a patient in need
`thereof, wherein the
`thromboembolic disorder is
`
`selected from the group
`consisting of pulmonary
`embolisms, deep vein
`thromboses, and stroke.
`
`2. The method of claim 1,
`wherein the thromboembolic
`
`disorder is pulmonary
`embolisms.
`
`3. The method of claim 1,
`wherein the thromboembolic
`
`disorder is deep vein thrombosis.
`
`4. The method of claim 1,
`wherein the thromboembolic
`
`disorder is stroke.
`
`
`
`Obvious under U.S.C. § 103 over the ’610
`Publication (EX1005), Kubitza Abstracts
`(EX1006), and Forsman (EX1007)
`
`See claim chart above for Ground 1.
`
`“The invention relates to a solid dosage form of a
`low molecular weight thrombin inhibitor
`formulated as immediate release (IR) tablets as
`well as a process for manufacture thereof. The
`invention also relates to the medical use of the
`
`formulation in the prophylaxis and/or
`treatment of thromboembolism.” EX1007, 1:6-
`
`9; EX1002, 1111100, 134; EX1003, 195.
`
`“Tablets must release 85% or more of stated
`
`amount Within 30 min.” EX1007, 2:4-5;
`
`EX1002, 11100.
`
`“The present invention provides an immediate
`release formulation based on conventional
`
`manufacturing processes. . .that provides a
`dissolution which is not, or very little dependent
`on pH.” EX1007, 1:13-21; see also id. at 7:1-8:2
`(Example 1a); id. at FIG. 1; EX1002, 1111100-04,
`1 36—39.
`
`“[T]hrombin inhibitors...can be formulated as
`IR tablets with no or very little pH depending
`dissolution.” EX1007, 2:9—1 1; EX1002, 11101.
`
`. .pH dependent dissolution could be
`reduced. . .giving a tablet release of more than
`85% within 30 minutes in acidic as well as
`
`neutral environment[s].” EX1007, 3:29—42;
`EX1002, 11135.
`
`49
`
`PROTECTIVE ORDER MATERIAL
`
`0009
`
`