Trials@uspto.gov
`571-272-7822
`
`Paper 33
`Date: August 31, 2021
`
`UNITED STATES PATENT AND TRADEMARK OFFICE
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`
`SYNGENTA CROP PROTECTION AG,
`Petitioner,
`v.
`FMC CORPORATION,
`Patent Owner.
`
`PGR2020-00028
`Patent 10,294,202 B2
`
`
`
`
`
`
`
`
`
`Before SUSAN L. C. MITCHELL, ZHENYU YANG, and
`CYNTHIA M. HARDMAN, Administrative Patent Judges.
`HARDMAN, Administrative Patent Judge.
`
`
`
`
`
`JUDGMENT
`Final Written Decision
`Determining Some Challenged Claims Unpatentable
`35 U.S.C. § 328(a)
`Denying Petitioner’s Motions to Exclude
`37 C.F.R. § 42.64
`
`
`
`
`
`

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`PGR2020-00028
`Patent 10,294,202 B2
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`I.
`INTRODUCTION
`This is a Final Written Decision in a post grant review challenging the
`patentability of claims 1–7, 9–13, and 21–31 of U.S. Patent No. 10,294,202
`B2 (“the ’202 patent,” Ex. 1001). We have jurisdiction under 35 U.S.C. § 6.
`Petitioner has the burden of proving unpatentability of the challenged
`claims by a preponderance of the evidence. 35 U.S.C. § 326(e) (2018).
`Having reviewed the parties’ arguments and supporting evidence, for the
`reasons discussed below, we find that Petitioner has demonstrated by a
`preponderance of the evidence that claims 1–3, 9–13, and 21–30 are
`unpatentable, but has not demonstrated by a preponderance of the evidence
`that claims 4–7 and 31 are unpatentable. We also deny Petitioner’s motions
`to exclude.
`
` Procedural History
`Syngenta Crop Protection AG (“Petitioner”) filed a Petition requesting
`post-grant review of claims 1–7, 9–13, and 21–31 of the ’202 patent.
`Paper 1 (“Pet.”). FMC Corporation (“Patent Owner”) filed a Preliminary
`Response. Paper 7. Based on the Petition and Preliminary Response, we
`determined that Petitioner more likely than not would prevail in showing
`that at least one of the challenged claims was unpatentable. Thus, we
`instituted trial. Paper 8 (“Inst. Dec.”).
`After institution, Patent Owner filed a Response (Paper 15, “Resp.”),
`Petitioner filed a Reply (Paper 19, “Reply”), and Patent Owner filed a Sur-
`reply (Paper 20, “Sur-reply”). On June 16, 2021, we held an oral hearing,
`the transcript of which is of record. Paper 32 (“Tr.”).
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`Patent 10,294,202 B2
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`Petitioner filed a motion to exclude certain opinions of Patent
`Owner’s expert Dr. Dayan (Paper 24), Patent Owner filed an opposition
`(Paper 27), and Petitioner filed a reply (Paper 28).
`Petitioner also filed a motion to exclude testimony, exhibits, and
`arguments regarding patents issued to its expert Dr. Hunt (Paper 25), Patent
`Owner filed an opposition (Paper 26), and Petitioner filed a reply (Paper 29).
` Real Parties in Interest
`Petitioner identifies the real parties in interest as Syngenta Crop
`Protection AG and Syngenta AG.1 Paper 11, 1. Patent Owner identifies
`itself as the real party in interest. Paper 3, 2.
` Related Matters
`Petitioner identifies two applications to which the ’202 patent claims
`priority: (1) U.S. Provisional Application No. 61/911,324 (filed 12/3/2013);
`and (2) PCT/US2014/068073, WO2015/084796 (published June 11, 2015).
`Pet. 3–4.
`Patent Owner states that it “knows of no judicial or administrative
`matters that may affect or be affected by a decision in this proceeding.”
`Paper 3, 2.
`
`
`1 In its Preliminary Response, Patent Owner argued that the Petition “fails to
`name all real parties in interest.” Paper 7, 2, 61. We authorized Patent
`Owner to file a brief addressing real parties in interest (Paper 10, 3), but
`Patent Owner elected not to do so, stating: “In the interest of expediting the
`proceeding, FMC declined to pursue the issue further. However, FMC does
`not concede that the petition does, in fact, name all real parties in interest.”
`Resp. 4 n.4. Because Patent Owner has not raised a real party in interest
`argument during the trial, it is waived. See In re NuVasive, 842 F.3d 1376,
`1380–81 (Fed. Cir. 2016) (finding that an argument raised in preliminary
`proceedings but not raised during trial is waived).
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`PGR2020-00028
`Patent 10,294,202 B2
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` The ’202 Patent
`The ʼ202 patent, titled “Pyrrolidinones as Herbicides,” “relates to
`certain pyrrolidinones, their N-oxides and salts, and compositions and
`methods of their use for controlling undesirable vegetation.” Ex. 1001, code
`(54), 1:5–7. The Specification states that “[t]he control of undesired
`vegetation is extremely important in achieving high crop efficiency,” and
`that “[m]any products are commercially available for these purposes, but the
`need continues for new compounds that are more effective, less costly, less
`toxic, environmentally safer or have different sites of action.” Id. at 1:11–
`23.
`
`The ’202 patent provides sixteen compound synthesis schemes (id. at
`33:9–41:49) and seven example syntheses (id. at 42:44–50:35). The
`ʼ202 patent also discloses approximately 350 compounds that were
`synthesized (Index Tables A–D), 335 of which were tested for herbicidal
`effect on various crop and weed species (Tables A–H5). Id. at 173:49–54,
`174:1–182:50, 182:57–285:27.
` Illustrative Claim
`Of the challenged claims, claims 1 and 31 are independent. Claim 1,
`reproduced below, is illustrative:
`1. A compound selected from Formula I, N-oxides and
`salts thereof:
`
`
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`wherein
`Q1 is a phenyl ring optionally substituted with up to 5
`substituents independently selected from R7; or a 5- to 6-
`membered heterocyclic ring or an 8- to 10-membered
`heteroaromatic bicyclic ring system, each ring or ring
`system containing ring members selected from carbon atoms
`and 1 to 4 heteroatoms independently selected from up to 2
`O, up to 2 S and up to 4 N atoms, wherein up to 3 carbon
`ring members are independently selected from C(═O) and
`C(═S), and the sulfur atom ring members are independently
`selected from S(═O)u(═NR8)v, each ring or ring system
`optionally substituted with up to 5 substituents
`independently selected from R7 on carbon atom ring
`members and selected from R9 on nitrogen atom ring
`members;
`Q2 is a phenyl ring or a naphthalenyl ring system, each ring or
`ring system optionally substituted with up to 5 substituents
`independently selected from R10; or a 5- to 6-membered
`fully unsaturated heterocyclic ring or an 8- to 10-membered
`heteroaromatic bicyclic ring system, each ring or ring
`system containing ring members selected from carbon atoms
`and 1 to 4 heteroatoms independently selected from up to 2
`O, up to 2 S and up to 4 N atoms, wherein up to 3 carbon
`ring members are independently selected from C(═O) and
`C(═S), and the sulfur atom ring members are independently
`selected from S(═O)u(═NR8)v, each ring or ring system
`optionally substituted with up to 5 substituents
`independently selected from R10 on carbon atom ring
`members and selected from R11 on nitrogen atom ring
`members;
`Y1 and Y2 are each independently O, S or NR12;
`R1 is H, hydroxy, amino, C1-C6 alkyl, C1-C6 haloalkyl, C2-
`C6 alkenyl, C3-C6 alkynyl, C4-C8 cycloalkylalkyl, C2-
`C8 alkoxyalkyl, C2-C8 haloalkoxyalkyl, C2-C8 alkylthioalkyl,
`C2-C8 alkylsulfinylalkyl, C2-C8 alkylsulfonylalkyl, C2-
`C8 alkylcarbonyl, C2-C8 haloalkylcarbonyl, C4-
`C10 cycloalkylcarbonyl, C2-C8 alkoxycarbonyl, C2-
`C8 haloalkoxycarbonyl, C4-C10 cycloalkoxycarbonyl, C2-
`C8 alkylaminocarbonyl, C3-C10 dialkylaminocarbonyl, C4-
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`C10 cycloalkylaminocarbonyl, C1-C6 alkoxy, C1-C6 alkylthio,
`C1-C6 haloalkylthio, C3-C8 cycloalkylthio, C1-
`C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C3-
`C8 cycloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-
`C6 haloalkylsulfonyl, C3-C8 cycloalkylsulfonyl, C1-
`C6 alkylaminosulfonyl, C2-C8 dialkylaminosulfonyl, C3-
`C10 trialkylsilyl or G1;
`R2 and R3 are each independently H, halogen or C1-C4 alkyl; or
`R2 and R3 are taken together with the carbon atom to which they
`are bonded to form a C3-C7 cycloalkyl ring;
`R4 and R5 are each independently H, halogen or C1-C4 alkyl;
`R6 is H, hydroxy, amino, C1-C6 alkyl, C1-C6 haloalkyl, C2-
`C6 alkenyl, C3-C6 alkynyl, C2-C8 alkoxyalkyl, C2-
`C8 haloalkoxyalkyl, C2-C8 alkylthioalkyl, C2-
`C8 alkylsulfinylalkyl, C2-C8 alkylsulfonylalkyl, C2-
`C8 alkylcarbonyl, C2-C8 haloalkylcarbonyl, C4-
`C10 cycloalkylcarbonyl, C2-C8 alkoxycarbonyl, C2-
`C8 haloalkoxycarbonyl, C4-C10 cycloalkoxycarbonyl, C2-
`C8 alkylaminocarbonyl, C3-C10 dialkylaminocarbonyl, C4-
`C10 cycloalkylaminocarbonyl, C1-C6 alkoxy, C1-C6 alkylthio,
`C1-C6 haloalkylthio, C3-C8 cycloalkylthio, C1-
`C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C3-
`C8 cycloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-
`C6 haloalkylsulfonyl, C3-C8 cycloalkylsulfonyl, C1-
`C6 alkylaminosulfonyl, C2-C8 dialkylaminosulfonyl, C3-
`C10 trialkylsilyl or G1;
`each R7 and R10 is independently halogen, cyano, nitro, C1-
`C4 alkyl, C1-C4 haloalkyl, C2-C4 alkenyl, C2-C4 haloalkenyl
`C2-C4 alkynyl, C2-C4 haloalkynyl, C1-C4 nitroalkyl, C2-
`C4 nitroalkenyl, C2-C4 alkoxyalkyl, C2-C4 haloalkoxyalkyl,
`C3-C4 cycloalkyl, C3-C4 halocycloalkyl, cyclopropylmethyl,
`methylcyclopropyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C2-
`C4 alkenyloxy, C2-C4 haloalkenyloxy, C3-C4 alkynyloxy, C3-
`C4 haloalkynyloxy, C3-C4 cycloalkoxy, C1-C4 alkylthio, C1-
`C4 haloalkylthio, C1-C4 alkylsulfinyl, C1-
`C4 haloalkylsulfinyl, C1-C4 alkylsulfonyl, C1-
`C4 haloalkylsulfonyl, hydroxy, formyl, C2-C4 alkylcarbonyl,
`C2-C4 alkylcarbonyloxy, C1-C4 alkylsulfonyloxy, C1-
`C4 haloalkylsulfonyloxy, formylamino, C2-
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`C4 alkylcarbonylamino, —SF5, —SCN, C3-C4 trialkylsilyl,
`trimethylsilylmethyl or trimethylsilylmethoxy;
`each R8 is independently H, cyano, C2-C3 alkylcarbonyl or C2-
`C3 haloalkylcarbonyl;
`each R9 and R11 is independently cyano, C1-C3 alkyl, C2-
`C3 alkenyl, C2-C3 alkynyl, C3-C6 cycloalkyl, C2-
`C3 alkoxyalkyl, C1-C3 alkoxy, C2-C3 alkylcarbonyl, C2-
`C3 alkoxycarbonyl, C2-C3 alkylaminoalkyl or C3-
`C4 dialkylaminoalkyl;
`each R12 is independently H, cyano, C1-C4 alkyl, C1-
`C4 haloalkyl, —(C═O)CH3 or —(C═O)CF3;
`each G1 is independently phenyl, phenylmethyl,
`pyridinylmethyl, phenylcarbonyl, phenoxy, phenylethynyl,
`phenylsulfonyl or a 5- or 6-membered heteroaromatic ring,
`each optionally substituted on ring members with up to 5
`substituents independently selected from R13;
`each R13 is independently halogen, cyano, hydroxy, amino,
`nitro, —CHO, —C(═O)OH, —C(═O)NH2, —SO2NH2, C1-
`C6 alkyl, C1-C6 haloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, C2-
`C8 alkylcarbonyl, C2-C8 haloalkylcarbonyl, C2-
`C8 alkoxycarbonyl, C4-C10 cycloalkoxycarbonyl, C5-
`C12 cycloalkylalkoxycarbonyl, C2-C8 alkylaminocarbonyl,
`C3-C10 dialkylaminocarbonyl, C1-C6 alkoxy, C1-
`C6 haloalkoxy, C2-C8 alkylcarbonyloxy, C1-C6 alkylthio, C1-
`C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-
`C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-
`C6 haloalkylsulfonyl, C1-C6 alkylaminosulfonyl, C2-
`C8 dialkylaminosulfonyl, C3-C10 trialkylsilyl, C1-
`C6 alkylamino, C2-C8 dialkylamino, C2-
`C8 alkylcarbonylamino, C1-C6 alkylsulfonylamino, phenyl,
`pyridinyl or thienyl; and
`each u and v are independently 0, 1 or 2 in each instance of
`S(═O)u(═NR8)v, provided that the sum of u and v is 0, 1 or
`2;
`provided that
`(a) the compound of Formula 1 is other than N-1H-
`benzotriazol-1-yl-2-oxo-4-phenyl-3-
`pyrrolidinecarboxamide;
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`(b) when Q1 is a 3-furanyl or 3-pyridinyl ring, then said ring is
`substituted with at least one substituent selected from R7;
`(c) when Q1 is unsubstituted phenyl, and Q2 is a phenyl or
`pyridyl ring, then said Q2 ring is substituted with R10 other
`than optionally substituted phenoxy at a 2-position (relative
`to the bond of the Q2 ring to the remainder of Formula 1),
`and unsubstituted at the 5- and 6-positions (with respect to
`the 2-position), and R5 is H or halogen;
`(d) when Q1 is a phenyl ring and said ring is substituted with
`R7 at both ortho positions (relative to the bond to the
`remainder of Formula 1), then said ring is also
`independently substituted with R7 on at least one additional
`position;
`(e) Q2 is other than optionally substituted 1H-pyrazol-5-yl; and
`(f) when Q2 is a 1H-pyrazol-3-yl ring, said ring is substituted at
`the 1-position with R11.
`Ex. 1001, 285:29–288:13.
`Dependent claims 2–7 and 22–30 narrow the choices for various
`substituents on the compounds recited in claim 1. Id. at 288:14–48, 291:1–
`292:44. Independent claim 31 recites the same core compound as claim 1
`(i.e., Formula I), but recites fewer options for several of the substituents. Id.
`at 292:45–293:24.
`Claims 9–12 and 21 cover an “herbicidal composition,” an “herbicidal
`mixture,” or a “mixture” that includes a compound of claim 1. Id. at
`288:61–289:30, 290:63–67. Claim 13 covers controlling growth of
`undesired vegetation using an “herbicidally effective amount” of a
`compound of claim 1. Id. at 289:31–34.
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`
` Asserted Grounds of Unpatentability
`We instituted trial based on the following asserted grounds of
`unpatentability:2
`Reference(s)/Basis
`35 U.S.C. §
`Claim(s) Challenged
`Enablement
`§ 112(a)
`1–3, 9–13, 21–30
`Written Description
`§ 112(a)
`9–13
`Olsson3
`§ 102(a)(1)
`1–7, 22–31
`Olsson
`§ 103
`1–7, 22–31
`Inst. Dec. 52; Pet. 5. In support of its patentability challenges, Petitioner
`relies on two declarations from Dr. David Allen Hunt, Ph.D. (Ex. 1003;
`Ex. 1029), among other evidence. Patent Owner relies on a declaration from
`Franck E. Dayan, Ph.D. (Ex. 2011), among other evidence.
`II. ANALYSIS
`
`Level of Ordinary Skill in the Art
`We consider the grounds of unpatentability in view of the
`understanding of a person of ordinary skill in the art (sometimes referred to
`herein as “POSA”) as of December 2013 (the earliest possible priority date
`for the challenged claims). See Ex. 1001, code (60). Petitioner contends
`that a such a person would have had “at least a Bachelor’s degree in
`biochemistry or chemistry with several years’ experience in agrochemistry,
`or alternatively, an advanced degree (Masters or Ph.D.) in biochemistry or
`organic chemistry with emphasis in these same areas,” and “may also work
`
`
`2 Patent Owner does not dispute that the ’202 patent is eligible for post-grant
`review. Pet. 2; see generally Resp.; see also Inst. Dec. 10 (finding ’202
`patent eligible for post-grant review).
`3 Olsson et al., U.S. Patent Pub. 2007/0123508 A1, published May 31, 2007
`(“Olsson,” Ex. 1004).
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`in collaboration with other scientists and/or clinicians who have experience
`in weed science, plant pathology, or related disciplines.” Pet. 13 (citing Ex.
`1003 ¶ 66). Although Patent Owner suggests that it has offered a similar
`proposal, no proposal appears in the Patent Owner Response.4 See Resp. 50.
`In determining the level of skill in the art, we consider factors
`including the type of problems encountered in the art, prior art solutions to
`those problems, and the sophistication of the technology. Custom
`Accessories, Inc. v. Jeffrey-Allan Indus., Inc., 807 F.2d 955, 962 (Fed. Cir.
`1986). Because Petitioner’s proposed definition is consistent with the prior
`art of record and the sophistication of the technology demonstrated by the
`record, we apply it here.5
`
`4 For completeness, we note that although it is not cited in the Patent Owner
`Response, Dr. Dayan’s declaration includes the opinion that a person of
`ordinary skill in the art
`would have had a degree (Bachelor’s, Masters, or Ph.D.) in
`biology, biochemistry, or chemistry with several years’
`experience in agrochemistry, including herbicide discovery
`and development. This person may also work in
`collaboration with other scientists and/or clinicians who have
`experience in weed science, plant pathology, or related
`disciplines.
`Ex. 2011 ¶ 37. This proposal differs from Petitioner’s in adding that the
`degree can be in biology, and in requiring “experience in agrochemistry,
`including herbicide discovery and development,” regardless of degree level.
`In comparison, Petitioner’s proposal does not specify that the degree can be
`in biology, and does not require the recited “several years’ experience in
`agrochemistry” in connection with an advanced degree. Dr. Dayan states,
`however, that his opinions would not change if he were to apply Dr. Hunt’s
`proposed level of ordinary skill in the art. Id. ¶ 38.
`5 We would reach the same ultimate conclusions in this Decision under
`Dr. Dayan’s proposal. See Ex. 2011 ¶ 37.
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`Claim Construction
`We interpret a claim “using the same claim construction standard that
`would be used to construe the claim in a civil action under 35 U.S.C.
`282(b).” 37 C.F.R. § 42.100(b) (2019). Under this standard, we construe
`the claim “in accordance with the ordinary and customary meaning of such
`claim as understood by one of ordinary skill in the art and the prosecution
`history pertaining to the patent.” Id.
`Petitioner argues that claims 1 and 31 include limitations in a “when”
`clause, which “only limit[] the claim’s scope to the extent the cited condition
`occurs, and should be read as ‘if.’” Pet. 13–14. Petitioner also states that it
`has adopted definitions in the ’202 patent regarding “several terms related to
`chemical structures in 5:36–9:9 . . . [and] herbicidal mixtures at 28:61–
`33:8.” Id. at 14. Petitioner asserts that the “remaining terms are to be
`construed in accordance with their ordinary and customary meaning.” Id.
`Patent Owner asserts that “all claim terms should be given their plain
`and ordinary meaning, in light of the definitions” in the Specification, and
`does not propose any express construction for any term. Resp. 10.
`Based on the complete record developed at trial, we determine that to
`resolve the disputes herein, we do not need to expressly construe any claim
`term. See Nidec Motor Corp. v. Zhongshan Broad Ocean Motor Co., 868
`F.3d 1013, 1017 (Fed. Cir. 2017) (explaining that construction is needed
`only for disputed terms, and only as necessary to resolve the controversy).
`
`Enablement
`A patent’s specification must describe the claimed invention and “the
`manner and process of making and using it, in such full, clear, concise, and
`exact terms as to enable any person skilled in the art to which it pertains, or
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`with which it is most nearly connected, to make and use the same.” 35
`U.S.C. § 112(a). The enablement requirement asks whether “the
`specification teach[es] those in the art to make and use the invention without
`undue experimentation.” In re Wands, 858 F.2d 731, 737 (Fed. Cir. 1988).
`In analyzing whether any required experimentation is undue, we consider
`factors such as:
`(1) the quantity of experimentation necessary, (2) the amount of
`direction or guidance presented, (3) the presence or absence of
`working examples, (4) the nature of the invention, (5) the state of the
`prior art, (6) the relative skill of those in the art, (7) the predictability
`or unpredictability of the art, and (8) the breadth of the claims.
`Id. Whether a specification is enabling is determined as of the filing date of
`the application. Chiron Corp. v. Genentech Inc., 363 F.3d 1247, 1254 (Fed.
`Cir. 2004).
`Petitioner asserts that the Specification fails to enable both (1) use as
`herbicides of the full scope of the compounds encompassed by claims 1–3,
`9–13 and 21–30; and (2) how to make the full scope of the compounds
`encompassed by a subset of these claims (i.e., claims 1–3, 9–13, 21, 23, and
`27–30). Pet. 15, 32.
`On the full trial record, we determine that Petitioner has demonstrated
`by a preponderance of the evidence that the Specification fails to enable the
`use as herbicides of the full scope of compounds of claims 1–3, 9–13 and
`21–30. Because this determination reaches all claims challenged for lack of
`enablement, we need not and do not reach Petitioner’s argument that the
`Specification fails to enable how to make the full scope of the compounds of
`claims 1– 3, 9–13, 21, 23, and 27–30. See SAS Inst. Inc. v. Iancu, 138 S. Ct.
`1348, 1359 (2018) (holding a petitioner “is entitled to a final written
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`decision addressing all of the claims it has challenged”); Boston Sci. Scimed,
`Inc. v. Cook Grp. Inc., Nos. 2019-1594, -1604, -1605, 2020 WL 2071962,
`at *4 (Fed. Cir. Apr. 30, 2020) (non-precedential) (recognizing that the
`“Board need not address issues that are not necessary to the resolution of the
`proceeding” and, thus, agreeing that the Board has “discretion to decline to
`decide additional instituted grounds once the petitioner has prevailed on all
`its challenged claims”).
`We first briefly summarize the parties’ contentions, then turn to our
`analysis.
`
`Brief Overview of the Parties’ Contentions
`1.
`Petitioner asserts that claim 1 “covers over a billion[] compounds,”
`Pet. 18 (citing Ex. 1003 ¶ 139), but the ’202 patent lacks sufficient guidance
`or working examples across the full scope of claim 1 to allow a person of
`ordinary skill in the art to determine which of the claimed compounds have
`herbicidal activity without undue experimentation. Id. at 18–20 (citing
`Ex. 1003 ¶¶ 140–155; Exs. 1007, 1011–1016). According to Petitioner, the
`approximately 350 compounds tested in the Specification for herbicidal
`activity “fail[] to enumerate the majority of the substituents available at each
`position” of the claimed genus, and “indicate[] that substitutions, particularly
`at the Q1, Q2, R1, and R6 positions, can strongly impact herbicidal activity
`and even eliminate it.” Id. at 16 (citing Ex. 1003 ¶¶ 135, 136, 144, 151,
`155–172), 19–20. Petitioner asserts that small substitutions, e.g., an alkyl
`instead of a hydrogen, can dramatically affect herbicidal activity by altering
`properties such as lipophilicity, metabolism, plant uptake, and translocation,
`yet the ’202 patent fails to teach a structure-activity relationship, mode of
`action, or what enzymes or binding sites (if any) the claimed compounds
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`affect. Id. at 17, 19–20. Petitioner argues that “several of the compounds
`tested failed to exhibit any herbicidal activity at the high screening levels
`(e.g., 1000 and 500 g ai/ha), which would indicate that a POSA would not be
`able to use the claimed compounds as an herbicide without undue
`experimentation, if at all.” Id. at 16–17 (citing Ex. 1003 ¶ 137); see also id.
`at 22–30 (citing, e.g., Ex. 1003 ¶¶ 153–172).
`Patent Owner contends that Petitioner fails to distinguish between the
`legal standards for compound claims and method of use claims. Patent
`Owner argues that compound claims 1–3 and 21–30 are enabled because an
`ordinarily skilled artisan “would not have had a reason to doubt” the
`Specification’s teaching that the compounds are herbicides. Resp. 18. As to
`both these compound claims and the claims that recite use as an herbicide
`(claims 9–13), Patent Owner argues they are enabled because extensive
`screening is understood to be a normal part of herbicide development (id. at
`24), and the examples in the Specification “include sufficient variation with
`respect to at least steric and electrostatic properties . . . to allow a person of
`skill in the art to utilize standard modeling techniques . . . to guide the
`synthesis and screening of additional molecules falling within the genus”
`without undue experimentation (id. at 38 (citing Ex. 2011 ¶ 50), 43).
`2.
`Analysis
`We start with Patent Owner’s contention that the enablement standard
`is different for compound and method claims. Resp. 17; see also id. at 2.
`With respect to the compound claims, Patent Owner argues that “[a]
`disclosure of practical utility ‘must be taken as in compliance with the
`enabling requirement of . . . § 112 unless there is reason to doubt the
`objective truth of the statements contained therein,’ such as when the
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`Patent 10,294,202 B2
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`statement ‘involve[s] implausible scientific principles.’” Id. at 18 (quoting
`In re Brana, 51 F.3d 1560, 1566 & n.17 (Fed. Cir. 1995)). Patent Owner
`argues that Petitioner has presented no evidence that the Specification’s
`teaching that the compounds are herbicides6 is implausible or unreliable.
`Resp. 18; see also Ex. 2011 ¶ 47 (asserting that based on the Specification’s
`biological testing results, “a person of skill in the art would have no reason
`to doubt that compounds within the full scope of claim 1 of the ’202 patent
`would exhibit herbicidal activity”).
`Even assuming Patent Owner were correct that there is a different
`enablement standard for compound and method claims, Petitioner has raised
`reasons why persons of ordinary skill in the art would doubt that the ’202
`patent enables the full scope of the claimed compounds as herbicides. As
`will be discussed below, Petitioner has credibly established that in view of
`the breadth of the claims, the relative lack of diversity of the compounds
`actually tested, and the test results showing inactivity and trends toward
`inactivity for compounds that deviated from the narrow range of structures
`tested, a person of ordinary skill in the art has reasonable basis to doubt that
`compounds within the full scope of claim 1 of the ’202 patent exhibit
`herbicidal activity. Accordingly, we proceed to analyzing the parties’
`arguments for claims 1–3, 9–13, and 21–30 under the factors set forth in In
`re Wands. We begin with claim 1, then turn to the remaining claims.
`
`
`6 The only asserted utility taught in the Specification for the disclosed
`compounds is herbicidal activity. See, e.g., Ex. 1001, 1:5–7, 155:56–57; Ex.
`1003 ¶¶ 46–48, 130–33; Resp. 17.
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`a. Nature of the Invention, Predictability or
`Unpredictability of the Art, and Relative Skill in the Art
`The field of the invention is agrochemicals—specifically, herbicides.
`See, e.g., Ex. 1001, codes (54), (57). The parties agree that the agrochemical
`field is “well-developed and mature.” Resp. 49; Tr. 17:13–16 (Petitioner’s
`counsel acknowledging that agrochemical field is mature in some regards);
`see also Ex. 1006, 85 (discussing multibillion dollar global herbicide
`market), 86 (referencing 184 herbicides marketed between 1970 and 2005).
`The parties also agree that level of ordinary skill in the art is relatively
`high. See supra Section II.A; see also Resp. 50 (acknowledging that the
`level of skill in the art is high); Tr. 15:18 (Petitioner’s counsel
`acknowledging that the level of skill in the art is relatively high).
`The parties also agree that ordinarily skilled artisans routinely use
`field screening tests and computational modeling techniques such as
`quantitative structure-activity relationship models (“QSAR”).7 See, e.g.,
`Resp. 49; Ex. 2011 ¶¶ 20, 27, 28 (discussing common field screening tests);
`Ex. 1003 ¶ 39 (acknowledging use of screening tests in herbicide
`development); Ex. 2005, 488–89; Exs. 2017, 2022, 2024 (all relating to use
`of QSAR in herbicide development); see also Tr. 7:19–8:5 (Petitioner’s
`counsel acknowledging that QSAR is used in the field).
`Despite the maturity in the field and relatively high level of ordinary
`skill in the art, the parties agree that the art is unpredictable. See Pet. 19–20
`(discussing lack of predictability); Ex. 1003 ¶¶ 142–143; Resp. 50 (“As both
`
`
`7 Comparative molecular field analysis (“CoMFA”) is a form of QSAR.
`Ex. 1028, 39:20–21. We use the term QSAR to encompass both QSAR and
`CoMFA.
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`parties agree, and the Board recognized, chemistry and biotechnology areas
`such as the agrochemical field are generally understood to be ‘unpredictable
`arts.’”). For example, Petitioner’s expert Dr. Hunt testifies (and Patent
`Owner does not dispute) that small structural changes can result in major
`differences in biological activity, and even seemingly minor substitutions
`can have “dramatic effects on activity by altering such phenomena as
`lipophilicity, metabolism, plant uptake, and translocation.” Ex. 1003 ¶ 142
`(citing Exs. 1011, 1012); see also id. ¶ 42 (citing Ex. 1007), ¶ 43, ¶ 143
`(citing Ex. 1026).
`Based on the full record developed at trial—much of it undisputed as
`discussed above—we find that the field of invention is mature and the level
`of ordinary skill in the art is relatively high, which both weigh in favor of
`enablement, but the art is unpredictable, which weighs against enablement.
`b. Breadth of Claims
`It is undisputed that claim 1 is extremely broad, “cover[ing] more than
`a billion different compounds.” Ex. 1003 ¶ 139; see also Ex. 1029 ¶ 8
`(asserting that claim 1 covers more than 1032 compounds); Tr. 32:4–7
`(Patent Owner’s counsel acknowledging that the number of compounds
`covered by the claims is not disputed). More specifically, claim 1 recites
`“[a] compound selected from Formula I, N-oxides and salts thereof:
`
`,”
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`wherein each of ten different substituents (Q1, Q2, Y1, Y2, R1, R2, R3, R4, R5,
`and R6) are independently selected from a wide range of substituents.
`Ex. 1001, 285:29–288:13; Ex. 1003 ¶ 49. The Q1, Q2, R1, and R6 groups
`alone each recite “well over a thousand possible independent options”
`spanning a wide range of size and electrostatic properties. Ex. 1003 ¶ 49
`(citing Ex. 1001, 285:44–286:51, 286:59–287:6, 287:33–38); Reply 16–22;
`Ex. 1029 ¶¶ 34, 37, 39, 45, 49.
`We find that the breadth of the claims weighs against enablement.
`c. Direction or Guidance
`We find that despite the claim breadth, the direction or guidance in the
`Specification on how to practice the full scope of the claims is relatively
`scant. For example, Petitioner correctly notes that the Specification does not
`disclose the mode of action of the claimed compounds. Pet. 19–20 (citing
`Ex. 1003 ¶ 146). Patent Owner does not dispute this, but instead argues that
`a patent need not disclose an invention’s method of action. Resp. 44.
`Although Patent Owner is correct that a patent need not disclose an
`invention’s method of action (see, e.g., Alcon Research Ltd. v. Barr Labs.,
`Inc., 745 F.3d 1180, 1190 (Fed. Cir. 2014)), the record reflects that such
`information would have helped ordinarily skilled artisans understand how
`changes to a compound’s structure impact herbicidal activity. See, e.g.,
`Ex. 1003 ¶ 146 (discussing relationship between compound structure and
`biological activity). Without this information, by Patent Owner’s own
`admission and as will be further discussed below, to practice the full scope
`of the claims, ordinarily skilled artisans must engage in iterative QSAR
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`modeling to develop a structure-activity relationship themselves.8 See, e.g.,
`Resp. 34 (“[A] skilled artisan could have used the biological data from the
`specification to develop a structure-activity relationship, and on the basis of
`that relationship, select compounds likely to have herbicidal activity to
`synthesize and test in the field.”), 3 (referencing “common modeling
`techniques that are regularly used by persons skilled in the art when
`developing herbicides to establish structure-activity relationships”);
`Ex. 2011 ¶ 24.
`The record also reflects that knowing a mode of action would have
`assisted the QSAR modeling process. See Reply 13 n.4; Ex. 1033, 40 (“An
`understanding of a chemical mode/mechanism of action is highly sought
`when developing (Q)SARs.”); Ex. 1029 ¶ 22. Accordingly, absence of this
`information in the Specification reduces the guidance available to an
`ordinarily skilled artisan and increases the quantity of experimentation
`needed to practice the full scope of the claims. See Ex. 1029 ¶¶ 21–22; see
`
`
`8 Relying on testimony from its expert Dr. Dayan, Patent Owner also argues
`that it is “uncommon for the mechanism to be known during herbicide
`discovery” (Resp. 54 (citing Ex. 2011 ¶ 19)), and that QSAR modeling is
`“more predictive of herbicidal activity than the analysis of whether a
`particular compound binds to a target site” (id. at 8 (citing Ex. 2011 ¶¶ 22,
`25); see also id. at 43). We do not credit these arguments, because
`Dr. Dayan’s testi