M O R R I S , N I C H O L S , A R S H T & T U N N E L L L L P
`1201 NORTH MARKET STREET
`P.O. BOX 1347
`WILMINGTON, DELAWARE 19899-1347
`
`(302) 658-9200
`(302) 658-3989 FAX
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`JACK B. BLUMENFELD
`(302) 351-9291
`jblumenfeld@mnat.com
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`
`
`
`September 18, 2018
`
`
`The Honorable Richard G. Andrews
`United States District Court for the District of
`Delaware
`844 North King Street
`Wilmington, DE 19801
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`HIGHLY CONFIDENTIAL –
`PROTECTIVE ORDER MATERIAL
`
`FILED UNDER SEAL
`
`Re:
`
`Bayer Intellectual Property GmbH v. Taro Pharmaceutical Industries, Ltd.
`C.A. No. 17-462 (RGA)
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`
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`Dear Judge Andrews:
`
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`Plaintiffs Bayer Intellectual Property GmbH, Bayer AG, and Janssen Pharmaceuticals,
`Inc., (collectively, “Plaintiffs”) write to bring an additional claim construction dispute to the
`Court’s attention, and to seek the Court’s guidance on how to proceed. This dispute arises from
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`On July 3, 2018, this Court issued a Markman Order construing the term “rapid-release
`tablet” in U.S. Patent Number 9,539,218 (“the ’218 patent”). See D.I. 91. The Court adopted
`Plaintiffs’ proposed construction, which was based on the express definition of the phrase
`provided in the ’218 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.
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`0001
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`MYLAN - EXHIBIT 1066
`Mylan Pharmaceuticals Inc. v. Bayer Intellectual Property GmbH
`IPR2018-01143
`
`

`

`The Honorable Richard G. Andrews
`September 18, 2018
`Page 2
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` during the original claim
`Mylan did not suggest
`construction proceedings, and Plaintiffs were unaware of it until well after the Court’s Markman
`Order had issued.
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`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.
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`Plaintiffs are prepared to brief this issue for the Court 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 Court’s preference.
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`Plaintiffs are available to discuss this issue further at the Court’s convenience.
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`Respectfully,
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`/s/ Jack B. Blumenfeld
`
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`Jack B. Blumenfeld (#1014)
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`JBB/bac
`Enclosure
`
`cc:
`
`Clerk of the Court (via hand delivery; w/enclosure)
`Counsel of Record Mylan Pharmaceuticals Inc. (via electronic mail; w/enclosure)
`
`0002
`
`

`

`Exhibit A
`Excerpt of Petition in
`IPR2018-01143
`
`0003
`
`

`

`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
`
`

`

`TABLE OF CONTENTS
`
`I.(cid:3)
`
`INTRODUCTION .............................................................................................. 1(cid:3)
`
`A.(cid:3)
`
`B.(cid:3)
`
`C.(cid:3)
`
`D.(cid:3)
`
`Brief Overview of the ’218 Patent....................................................... 3(cid:3)
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`Brief Overview of the Prosecution History ......................................... 4(cid:3)
`
`Brief Overview of the Scope and Content of the Prior Art .................. 6(cid:3)
`
`Brief Overview of the Level of Skill in the Art ................................. 11(cid:3)
`
`II.(cid:3)
`
`GROUNDS FOR STANDING ............................................................................. 13(cid:3)
`
`III.(cid:3) MANDATORY NOTICES UNDER 37 C.F.R. § 42.8 ........................................... 13(cid:3)
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`IV.(cid:3) STATEMENT OF THE PRECISE RELIEF REQUESTED ......................................... 15(cid:3)
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`V.(cid:3)
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`CLAIM CONSTRUCTION ................................................................................ 15(cid:3)
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`VI.(cid:3) BACKGROUND KNOWLEDGE IN THE ART PRIOR TO JANUARY 31, 2005 .......... 26(cid:3)
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`VII.(cid:3) DETAILED EXPLANATION OF GROUNDS FOR UNPATENTABILITY .................... 31(cid:3)
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`A.(cid:3)
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`B.(cid:3)
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`[Ground 1] Claims 1-4 are Obvious under 35 U.S.C. § 103 over
`the ’610 Publication and Kubitza Abstracts....................................... 31(cid:3)
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`[Ground 2] Claims 1-4 are Obvious under 35 U.S.C. § 103 over
`the ’610 Publication, Kubitza Abstracts, and Forsman. ..................... 46(cid:3)
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`VIII.(cid:3) NO UNEXPECED RESULTS ............................................................................ 50(cid:3)
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`IX.(cid:3) CONCLUSION ............................................................................................... 55(cid:3)
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`X.(cid:3)
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`CERTIFICATE OF COMPLIANCE ...................................................................... 56(cid:3)
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`XI.(cid:3) PAYMENT OF FEES UNDER 37 C.F.R. §§ 42.15(A) AND 42.103 ...................... 57(cid:3)
`
`XII.(cid:3) APPENDIX – LIST OF EXHIBITS...................................................................... 58
`
`i
`
`0005
`
`

`

`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, ¶¶98, 107-16, 118-21, 124-
`27; EX1003, ¶¶77, 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
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`even if the term “rapid-release tablet” were amended to require a “rapid-release
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`tablet having a Q value of (30 minute) of 75%.” EX1002, ¶133.
`
`The combined teachings of the ‘610 publication and Kubitza Abstracts are
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`discussed in Ground 1. Forsman additionally teaches that immediate/rapid-release
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`tablets have utility “in the prophylaxis and/or treatment of thromboembolism.”
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`EX1007, 1:6-9; EX1002, ¶134; EX1003, ¶95; see also EX1019 at 1300
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`(prophylaxis and therapy of thromboembolic disorders may require a rapid onset of
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`action); EX1032 at 1:14-16 (for “treatment or prophylaxis of thrombosis,
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`immediate release formulations may be necessary to ensure that a sufficient
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`amount of drug is provided in plasma …to enable quick onset of action.”); EX1006
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`at 0015 (rivaroxaban has rapid onset of action). Forsman thus teaches methods for
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`formulating immediate/rapid-release oral tablets for low molecular weight
`
`46
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`0006
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`

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`anticoagulant thrombin inhibitors. In light of the disclosure in Kubitza Abstracts
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`that the liquid oral dosage form achieved maximum blood concentrations even
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`faster (~30 minutes) than rapid-release tablet (~2 hrs), a person of ordinary skill
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`before January 2005 would have had good reason to develop rapid-release tablet
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`that releases rivaroxaban as rapidly after oral administration as possible. EX1002,
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`¶¶134-35, 141-43.
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`Forsman’s immediate release tablets are “based on conventional
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`manufacturing processes….that provides a dissolution which is not, or very little
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`dependent on pH.” EX1007, 1:13:21; EX1002, ¶¶104 (discussing manufacture of
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`Forsman Example 1a tablets), 136 (discussing EX1036 (Golub et al. 78 J.
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`ALLERGY CLIN. IMMUNOL. (1986) 689-94) at 689, 691, 693). Forsman’s rapid-
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`release tablets released “more than 85% [of the thrombin inhibitor] within 30
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`minutes in acidic as well as neutral environment.” EX1007, 3:29-4:2. Indeed,
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`Forsman Example 1a released 94% of anticoagulant at pH 1 and at pH 6.8. Id. at
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`7:1-8:2; see also id. at FIG. 1. As Dr. Benet explains, such a tablet necessarily
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`released 75% within 30 minutes as well. EX1002, ¶¶135, 138. Forsman thus
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`demonstrated that its Example 1A rapid-release tablet had a Q value (30 minutes)
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`of 75% according to the USP release method using apparatus 2 (paddle) because it
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`resulted in at least 75% dissolution within 30 minutes. Id. at ¶¶102-03; see also
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`EX1054 (Chapter 711 Dissolution, THE UNITED STATES PHARMACOPEIA (USP)
`
`47
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`0007
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`

`

`2000) at 1943 (“Where a single time specification is given, the test may be
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`concluded in a shorter period if the requirement for minimum amount dissolved is
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`met.”); EX1033 (Saccone et al., 11 DISSOLUTION TECH. (2004) 25-28) at 25.
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`Dr. Benet confirms that a person of ordinary skill seeking to develop a rapid-
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`release tablet formulation for rivaroxaban would have had good reason to use
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`Forsman’s formulation, which was taught to be useful for administering thrombin
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`inhibitors for the prophylaxis and therapy of thromboembolisms without being pH
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`dependent, and would have had a reasonable expectation of success in doing so.
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`EX1002, ¶¶101, 137-39.
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`Although Dr. Benet testifies that it would have been obvious to make a
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`rapid-release tablet with a Q value (30 minutes) of 75% for rivaroxaban and to
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`administer it once daily to a patient in need thereof for five consecutive days as
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`claimed by the ’218 patent, he also explains that there is no criticality to the 75% Q
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`value. EX1002, ¶¶140-43.
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`For each of the reasons discussed above, each of claims 1-4 would have
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`been obvious to a person of ordinary skill in the art in view of the combined
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`teachings of the ’610 publication, Kubitza Abstracts, and Forsman. The claim chart
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`below provides exemplary citations where the specific elements of these claims are
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`found in the asserted references, and where they are addressed in the
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`accompanying declarations of Drs. Benet and Doherty.
`
`48
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`0008
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`

`

`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-({(5S)-2-oxo-3-[4-
`(3-oxo-4-morpholinyl)phenyl]-
`1,3-oxazolidin-5-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, ¶¶100, 134; EX1003, ¶95.
`“Tablets must release 85% or more of stated
`amount within 30 min.” EX1007, 2:4-5;
`EX1002, ¶100.
`“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, ¶¶100-04,
`136-39.
`“[T]hrombin inhibitors…can be formulated as
`IR tablets with no or very little pH depending
`dissolution.” EX1007, 2:9-11; EX1002, ¶101.
`“…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, 3:29-4:2;
`EX1002, ¶135.
`
`49
`
`0009
`
`