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`UNITED STATES PATENT AND TRADEMARK OFFICE
`___________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`___________
`
`
`INITIATIVE FOR MEDICINES, ACCESS & KNOWLEDGE (I-MAK), INC.
`Petitioner
`
`v.
`
`GILEAD PHARMASSET LLC
`Patent Owner
`
`___________
`
`Case No. IPR2018-00121
`U.S. Patent No. 8,334,270
`
`___________
`
`
`
`PETITIONER’S REQUEST FOR REHEARING
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`
`
`I.
`
`
`
`INTRODUCTION
`
`Petitioner Initiative for Medicines, Access & Knowledge (I-MAK), Inc.
`
`(“Petitioner”) respectfully requests rehearing of the Board’s Decision Denying
`
`Institution of Inter Partes Review (“IPR”) of Gilead Pharmasset LLC’s (“Gilead”)
`
`U.S. Patent 8,334,270 (“the ’270 patent”) (“Decision”; Paper 10) because the
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`Board misapprehended or overlooked that a provisional application to which the
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`‘270 patent claims priority failed to satisfy the written description requirement.
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`The Board’s resulting conclusion that the ‘270 patent was entitled to the benefit of
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`the filing date of that provisional application was, thus, incorrect, as was the
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`Board’s further conclusion that two of the references cited by Petitioner in the
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`Petition did not qualify as prior art.1
`
`
`1 In IPR2018-00123 of U.S. Patent No. 8,735,372, a patent that relates to the ‘270
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`patent, the Board held that Sofia (Ex. 1004) is unavailable as a printed publication.
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`Paper 7 (June 13, 2018). However, notably, Patent Owner did not dispute there,
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`and has not disputed here, that Sofia was a printed publication as of September
`
`2007, and the Internet Archive Wayback Machine confirms it was published on the
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`website of Patent Owner’s predecessor at that time. Ex. 1016; see also
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`https://web.archive.org/web/20071005041918/http://investor.pharmasset.com:80/e
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`vents.cfm (link to “View Phosphoramidates presentation” under “Sep 10, 2007”).
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`1
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`
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`II. LEGAL STANDARD
`
`A party may request rehearing of a denial of institution by, “identify[ing] all
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`matters the party believes the Board misapprehended or overlooked, and the place
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`where each matter was previously addressed in a motion, an opposition, or a
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`reply.” 37 C.F.R. § 42.71(d). The Board reviews its decision for “abuse of
`
`discretion,” Id. at § 42.71(c), which includes basing the decision on, “an erroneous
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`conclusion of law or clearly erroneous factual finding.” PPG Indus., Inc. v.
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`Celanese Polymer Specialties Co., 840 F.2d 1565, 1567 (Fed. Cir. 1988).
`
`III. THE ‘270 PATENT IS NOT ENTITLED TO THE BENEFIT OF THE
`‘315 APPLICATION’S FILING DATE BECAUSE IT DOES NOT
`SATISFY THE WRITTEN DESCRIPTION REQUIREMENT
`
`
`
`“[A] patent application is entitled to the benefit of the filing date of an
`
`earlier filed application only if the disclosure of the earlier application provides
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`support for the claims of the later application, as required by 35 U.S.C. § 112.” In
`
`re Chu, 66 F.3d 292, 297 (Fed. Cir. 1995). “To be entitled to a parent’s effective
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`filing date, a continuation must comply with the written description requirement of
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`35 U.S.C. § 112, ¶1.” In re Owens, 710 F.3d 1362, 1366 (Fed. Cir. 2013).
`
`
`
`To satisfy the written description requirement, “the applicant must convey
`
`with reasonable clarity to those skilled in the art that, as of the filing date sought,
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`he or she was in possession of the invention, and demonstrate that by disclosure in
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`the specification of the patent.” ULF Bamberg v. Dalvey, 815 F.3d 793, 797 (Fed.
`
`2
`
`
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`Cir. 2016) (citations and internal quotation marks omitted); accord Ariad Pharms.
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`v. Eli Lilly, 598 F.3d 1336, 1351-52 (Fed. Cir. 2010) (en banc). “A disclosure in a
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`parent application that merely renders the later-claimed invention obvious is not
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`sufficient to meet the written description requirement; the disclosure must describe
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`the claimed invention with all its limitations.” Tronzo v. Biomet, 156 F.3d 1154,
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`1158 (Fed. Cir. 1998); accord Ariad, 593 F.3d at 1352.
`
`
`
`“The ‘270 patent claims the benefit of priority of two earlier-filed
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`provisional applications, 60/909,315 filed March 30, 2007 (Ex. 2013), and
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`60/982,309 filed on October 24, 2007 (Ex. 2014), respectively, “the ‘315
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`application” and “the ‘309 application”).” Paper 10, 3. In the Petition, I-MAK
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`contested that the ’270 patent is entitled to claim priority to the ’315 application.
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`Id. at 8. Specifically, although the ‘315 application discusses broad genera of
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`compounds, “it does not discuss the specific compounds and stereochemistry
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`around the phosphorous atom claimed in the ‘270 patent.” Pet. 22, 24; Ex. 1002
`
`¶ 72. As a result, the two references cited in the Petition that were published after
`
`the ‘315 application but prior to the ‘309 application constitute prior art.
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`
`
`Neither Patent Owner in its Preliminary Response, nor the Board in its
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`Decision, dispute I-MAK’s assertion that the ‘315 application fails to identify the
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`specific compounds and stereochemistry around the phosphorous atom and at the
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`amino acid ester (i.e., R3a and R3b) as claimed in the ‘270 patent. Rather, Patent
`
`3
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`
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`Owner argued, and the Board concluded, that the ’270 patent is entitled to claim
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`priority to the ‘315 application because it contains one line identifying the
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`substituents of the claimed compound (Ex. 2013, 195) and one line generically
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`stating phosphorous can be a chiral center of the disclosed compounds (Ex. 2013,
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`63). This is despite the fact that Patent Owner did not specify the stereochemistry
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`at phosphorous as claimed in the ’270 Patent. Id. (the ‘315 states that the
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`stereochemistry at phosphorous can be either R- or S-). The Patent Owner further
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`did not specify the stereochemistry at positions R3a and R3b as claimed in the ‘270
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`Patent. Id. (the ‘315 states that the stereochemistry at R3a and R3b can be either R-
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`or S-).
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`But the ‘315 application identifies 12,400 different compounds (31
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`structures each having 50 tables of 8 compounds), of which the ‘315 application
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`states that they can have various chiral centers. Thus, there are tens of thousands of
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`possible compounds each with various particular stereochemistry identified by the
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`‘315 application, and yet claims 1, 2, 10-18 and 20-25 of the ‘270 patent claim at
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`most just fifty-four specific stereoisomers of those compounds, none of which are
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`specifically described by the ‘315 application.2 Given the vast disclosure of the
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`2 Claim 1 claims 12 individual stereoisomeric compounds and claims 10-15 depend
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`therefrom. Claim 2 claims 6 individual stereoisomeric compounds. Claim 16
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`
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`4
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`
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`‘315 application and its failure to specifically disclose the compounds and
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`stereochemistry claimed in the ‘270 patent, the mere two lines cited by the Board
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`from the 645-page long document do not, “reasonably convey[] to those skilled in
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`the art
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`that
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`the
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`inventor had possession” of
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`the compounds with
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`the
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`stereochemistry claimed in the ‘270 patent. Ariad, 598 F.3d at 1351.
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`Further, the structures of many of the compounds claimed in challenged
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`claims 16, 17 and 18 are not even disclosed in any of the ‘315 application’s tables,
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`as, for example, the ‘315 application discloses only 5 of the 16 different R4 groups
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`named as esters in the ‘270 patent. Ex. 1001, 608:22-25 (2,4-Dichloro-phenoxy not
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`included in any table for R1), 608:50-53 (3,4-Dichloro-phenoxy not included in any
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`table for R1), 608:54-57 (sec-butyl ester not included in any table for R4), 608:62-
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`65 (4-methoxy-phenoxy not included in any table for R1), 609:11-15 (same),
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`609:20-23 (2,4-Dichloro-phenoxy not included in any table for R1), 609:32-35
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`(3,4-Dichloro-phenoxy not included in any table for R1); 609:40-43 (4-methoxy-
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`phenoxy not included in any table for R1), 609:44-47 (pentyl ester not included in
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`any table for R4), 610:5-24 (neither 4-fluoro-benzyl ester nor 3-methyl-butyl ester
`
`
`claims 54 individual stereoisomeric compounds and claims 20-25 depend
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`therefrom. Claims 17 and 18 claim 50 and 33 individual stereoisomeric
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`compounds, respectively.
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`5
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`
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`included in any table for R4, 2,4-Dichloro-phenoxy not included in any table for
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`R1, cyclohexyl ester not included in any table for R4, and 2-chloro-phenoxy not
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`included in any table for R1), 610:29-611:15 (cyclohexyl ester not included in any
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`table for R4, butyric acid not included in any table for R3a or R3b, 2,2-difluoro-ethyl
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`ester not included in any table for R4, 2,2,2-trifluoro-1-trifluoromethyl-ethyl ester
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`not included in any table for R4, 2-fluoro-1-fluoromethyl-ethyl ester not included in
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`any table for R4, cyclopropyl methyl ester not included in any table for R4,
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`cyclopentyl ester not included in any table for R4, 3,4,-dichloro-phenoxy not
`
`included in any table for R1, 2-fluoro-ethyl ester not included in any table for R4),
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`611:42-45, 611:66-612:6, 612:11-14, 612:28-31, 612:36-39, 612:48-51, 612:56-63,
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`613:22-37, 613:46-53, 613:58-65, 614:7-15, 614:46-49, 614:66-615:6, 615-20-23,
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`615:27-31, 615:35-43, 615:56-63, 616:1-14, and 616:19-22. Thus, the ‘315
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`application cannot even support claims 16, 17 and 18 on the basis asserted by the
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`Board, i.e. that the tables in the ‘315 application provide the substituents for the
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`claimed compounds.
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`The Board determined that Dr. Fortunak is qualified to opine from the
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`perspective of a person of ordinary skill in the art, Paper 10 at 5, and his testimony
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`was quite clear, “[t]he ‘315 provisional application does not include a description
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`of the specific compounds claimed by the ‘270 patent.” Id. at 8 (citing Ex. 1002 ¶
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`72. This testimony supports I-MAK’s position that the challenged claims of the
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`6
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`
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`‘270 patent are not entitled to claim the benefit of the ‘315 application. Patent
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`Owner could have entered evidence to contradict Dr. Fortunak’s testimony with its
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`Preliminary Response, but chose not to do so. Thus, the only evidence of record is
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`that of Dr. Fortunak’s opinion.
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`The Board cites in its Decision Fujikawa v. Warranasin, 93 F.3d 1559, 1570
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`(Fed. Cir. 1996), for the proposition that, “It is well settled that ‘ipsis verbis
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`disclosure is not necessary to satisfy the written description requirement of section
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`112.’” Paper 10, 10-11. While of course correct, that does not mean any disclosure,
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`no matter how minor, is sufficient. Here, the mere two lines of text in the ‘315
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`application cited by the Board fail to, “reasonably convey[] to those skilled in the
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`art that the inventor had possession” of the compounds with the stereochemistry
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`claimed in the ‘270 patent. Ariad, 598 F.3d at 1351.
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`The Board also cites In re Ruschig, 379 F.2d 990, 994-95 (CCPA 1967) for,
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`“[a]nalogizing the direction sufficient to identify species in a genus as ‘blaze marks
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`which single out particular trees.’” Paper 10, 11. As described by the en banc
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`Federal Circuit in Ariad, a reasonable interpretation of Ruschig is that, “the court
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`properly rejected the claim under a written description requirement separate from
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`enablement because the specification did not disclose the later-claimed compound
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`to one of skill in the art as something the inventors actually invented out of the
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`myriad of other compounds encompassed by the broad disclosure.” 598 F.3d at
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`7
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`
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`1348. Further, “the court properly affirmed the rejection because the original
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`application did not disclose the specific claimed invention, chlorpropamide, even if
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`one of skill in the art could, based on the disclosure with respect to related
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`compounds, make and use it.” Id.
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`Here, we have the same situation, a broad disclosure with no “blaze marks”
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`to identify the species claimed. Nothing in the ‘315 application tells one of
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`ordinary skill in the art that the specific stereoisomeric compounds claimed in the
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`challenged claims of the ‘270 patent are the ones to pursue. Nothing in the ‘315
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`application tells one of ordinary skill in the art that phosphorous should be
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`employed as a single chiral center (either in the Rp or Sp configuration), or as a
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`mixture of both. Such chirality at phosphorous is referred to merely as, “the
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`inventors recognize that stereochemical configurations are possible such that in a
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`staggered (or zig-zag) line structure the oxo substituent projects towards the viewer
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`while the OR1 substituent projects away from the viewer, and vice versa.
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`Therefore, the structures below include all possible stereochemical configurations
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`possible for phosphorous.” Ex. 2013, 63-64.
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`Such possible mixtures are not described as having a configuration at
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`phosphorous of either Rp or Sp; a 50:50 mixture (racemic at phosphorous); or as
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`any other ratio of chirality at phosphorous, e.g., 60:40, 80:20, 20:80, 97:3, or 3:97
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`or any other ratio. Thus, phosphorous as a chiral center is not identified as being a
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`8
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`
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`“preferred compound.” In short, there’s nothing at all in the ‘315 application
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`providing anything close to “blaze marks” that single out the particular compounds
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`and stereochemistry claimed in the ‘270 patent.
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`Further, the structures of the Tables in ‘315 possess an additional element of
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`optional stereochemistry at the carbon bearing substituents R3a and R3b. Thus, each
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`structure in the Tables amounts to possible mixtures at phosphorous, requiring a
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`further step of a selection of either R- or S- stereochemistry at the amino acid
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`center of the phosphoramidate.
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`As the Federal Circuit said en banc in Ariad, “the original application did
`
`not disclose the specific claimed invention.” 598 F.3d at 1348. Whether the ‘315
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`application enabled one of skill in the art to make and use the specific compounds
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`claimed in the ‘270 patent is irrelevant and insufficient. Id.
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`The issue here boils down to a simple question, would a POSA reading the
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`‘315 application have had a reasonably clear understanding that the applicant
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`possessed the precise compounds with stereochemistry claimed when they were
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`just a few of the many thousands of stereoisomeric compounds disclosed,
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`especially since phosphorous as a chiral center was specifically described as not
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`being preferred.
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`The only evidence of record here on that simple question is Dr. Fortunak’s
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`testimony that it was not. Ex. 1002 ¶72. The Board accorded little weight to
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`9
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`
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`Dr. Fortunak’s discussion of the issue because it was direct and to the point,
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`Paper 10, 11, but Gilead has introduced no testimony on the issue whatsoever even
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`though it could have done so with its Preliminary Response and still can do so post
`
`institution. For now, the only conclusion to draw from the evidence of record is
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`that of Dr. Fortunak, that, “[t]he ‘315 provisional application does not include a
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`description of the specific compounds claimed by the ‘270 patent.” Ex. 1002 ¶ 72.
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`As such, the ‘315 application does not satisfy the written description requirement
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`to support the challenged claims of the ‘270 patent.
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`Supporting the conclusion that the disclosure in the ‘315 application does
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`not satisfy the written description requirement is the fact that, “a description that
`
`merely renders the invention obvious does not satisfy the requirement.” Ariad, 598
`
`F.3d at 1352. Whether the claims of the ‘270 patent would be obvious in light of
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`the ‘315 application is unaddressed by both Patent Owner in its Preliminary
`
`Response and the Board in the Decision. The answer to that question is unclear.
`
`While the ‘315 application arguably teaches in separate locations all of the
`
`elements of the ‘270 patent’s claims, it does so as part of an extremely broad
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`disclosure of an incalculable number of such compounds. It does not identify the
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`specific compounds – even among the thousands of compounds listed in the Tables
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`- as being lead compounds and it does not identify phosphorous as being preferred
`
`as: 1) racemic; 2) in any specific chiral configuration (Rp or Sp); or in any
`
`10
`
`
`
`preferred non-racemic mixture of chirality. The ‘315 application further does not
`
`disclose any specific chirality (R- or S-) of the amino acid ester of the
`
`phosphoramidate. If it is uncertain whether the ‘315 application would render the
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`‘270 patent’s claims obvious, there can be no doubt that the ‘315 application fails
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`to provide written description support for the ‘270 patents claims, because even if
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`it did render those claims obvious, that is insufficient. Ariad, 598 F.3d at 1352.
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`Indeed, in the related IPR filed by Petitioner concurrently with this IPR,
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`IPR2018-00122, the Board denied institution there because it concluded that
`
`although Petitioner cited prior art disclosing a genus of compounds including that
`
`claimed by the ‘270 patent, Petitioner failed to “adequately explain why this
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`particular compound was chosen over other compounds.” IPR2018-00122, Paper
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`10, 19. The same is true for the ‘315 application. It did not explain at all why the
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`compounds with specific stereochemistry claimed in the ‘270 patent were chosen
`
`from among the tens of thousands disclosed. Thus, using the Board’s own
`
`reasoning in the related IPR, the ‘315 application fails to render the ‘270 patent’s
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`claims obvious, which means it is far from satisfying written description.
`
`This case is much different than Concert Pharm. v. Incyte Corp, PGR2017-
`
`00034, where the Board found a specification satisfied written description when it
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`(1) disclosed the precise enantiomers claimed; (2) provided a working example
`
`describing an exemplary chemical synthesis; (3) demonstrated separation of the
`
`11
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`
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`isomers, and (4) described the resulting claimed compound’s biological activity.
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`PGR2017-00034, Paper 13 (P.T.A.B. May 21, 2018). Here, the ‘315 application
`
`does none of those things. It does not disclose the enantiomers claimed in the ‘270
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`patent, it does not provide a working example describing their chemical synthesis,
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`it does not demonstrate separation of the isomers, nor does it describe the resulting
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`compound’s biological activity. Thus, the ‘315 application’s specification is
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`materially different from the specification in Concert Pharm. in several respects.
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`While not binding on the Board, it is nonetheless instructive that the
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`European Patent Office has addressed the same issues raised here and concluded,
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`like Petitioner, that the ‘315 application does not provide support for claims
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`comparable to the challenged claims of the ‘270 patent here. Specifically, in
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`resolving oppositions to related patent application EP2203462, the EPO found that
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`a claim to the (S) diastereomer at phosphorous was not sufficiently supported by
`
`the ‘315 application because:
`
`The compound of claim 1 is a racemate with two chiral centres
`whereby the chirality is defined at the carbon atom and not at the
`phosphorus atom. The specific indication is IX-25-2 where neither
`chiral centre is defined. In order to arrive at the racemate form IX-25-
`2 it is necessary to make at least two choices: firstly to define chirality
`at one, but not both, of the two possible sites and secondly to specify
`the chirality at that particular site. This represents a selection from
`within two lists. On account of this and the general teaching of
`
`12
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`
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`the standard way of
`to represent
`taken
`is
`T1046/97 which
`understanding the scope of an application which discloses compounds
`and has a reference to the (non-exemplified) enantiomers, the OD
`considers that the auxiliary request 1 is not entitled to the priority of
`D1.
`Ex. 1015, 24 (¶¶ 25.1-25.2) (D1 identified as ‘315 application on p. 3) Thus, when
`
`considering the same exact disclosure, the EPO came to the exact opposite
`
`conclusion as the Board here regarding the right to claim priority to the ‘315
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`application with respect to the specific (S) diastereomer at phosphorous. This
`
`supports a finding that the challenged claims of the ‘270 patent are not entitled to
`
`claim priority to the ‘315 application, since they each cover that stereoisomer.
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`IV. CONCLUSION
`
`
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`For the foregoing reasons, Petitioner respectfully requests that the Board
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`rehear its decision denying institution and institute a trial on all challenged claims.
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`Respectfully submitted,
`
`
`
`/Daniel B. Ravicher/
`Daniel B. Ravicher (Reg. No. 47,015)
`RAVICHER LAW FIRM PLLC
`
`Counsel for Petitioner
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`13
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`Dated: June 20, 2018
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`V. CERTIFICATE OF SERVICE
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`
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`I certify that on the date indicated below I caused a true and correct copy of
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`the foregoing PETITIONERS’ REQUEST FOR REHEARING to be served on
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`counsel for Patent Owner by filing through the PTAB – E2E system as well as by
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`electronic mail to the following email addresses:
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`Dated: June 20, 2018
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`whelan@fr.com
`kane@fr.com
`shear@fr.com
`IPR36583-0020IP4@fr.com
`PTABInbound@fr.com
`david.cavanaugh@wilmerhale.com
`emily.whelan@wilmerhale.com
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`
`
`
`/Daniel B. Ravicher/
`Daniel B. Ravicher (Reg. No. 47,015)
`RAVICHER LAW FIRM PLLC
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`Counsel for Petitioner
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`14
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