BEFORE THE CONTROLLER OF PATENTS,
`
`THE PATENT OFFICE
`
`KOLKA1A
`
`in !qe na:cr .f Die Paei’Is M, 1970 as iiprdei b’v The
`Patents iAirerdn-ent Ac! 2005:
`
`In the mallet of The Ptert? Ainenc1nionI) RtiLs 200ui an
`as ;4lflerrsd fl 201(,
`
`And
`
`1 336/KOL2O13
`In The Mi:er of Patent A phciticr No.
`dated November 26, 2013 in the narie at UPL LIMITED,
`ErihUed “A METHOD FOR CQNIROLLING RUST”, havhu
`its oruicipal p12cc o b’jsines! a Agrcrhemical PIaiL
`Durqachak HaIda —721 602, Midnacn’o UI%t We1 eri!
`1111112.
`
`Applicant
`
`.
`
`Page 1 of 179
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`SYNGENTA EXHIBIT 1035 L.1j2
`
`i-SI
`
`SYNGENTA v. LJPL, PGR2023-00017
`
`

`

`_____
`
`APHDAVIT
`
`IT GiLsm .4pi’9cr1c’ Henl7or?&qiIdo Do O/heha, sclenri!y arlrrn and deciare as jider inni the Global
`Pcor;nn? Leiiii — Ssralecy & .?wo]t:or, rir LJPL &r:-inI Ltd.
`( am t3irO of !i;’c sub1&i matfoc £:iNi!.’;eø
`as b&?ia p:eJse’Rr/y amended, in wpr a if fluE lr:dian L/I.’hCit7lY1
`33&KCE 2O 3 ai air
`nanisct n; flu prosoit ej’takn’i
`
`1
`
`2
`
`I tid’df? hem rovidcd ‘uth the cpy of lidian Palieril Application No 1 336K0U2013 (reteried
`herein aer as
`‘133m,
`the ri:pe DI UPL LTD unlilied
`A METHOD FOR
`CONTROLLING RUST.
`
`fllJ in
`
`The presc:nt
`r.veflhion re?atUs :o a funqii:EaI t:i;nbindpon Comprising at east ens rnUItLs:te
`(unqirudo and al least two vsrernc 1tnqcides selected from a 11i19cflUO:JtsIcIe i1i1hior a
`qulnone nside i.q.iiibit.ar, a ciQrneLhyIalion nhibii>r art] a succraIe dehydrenatw I9nbilc
`1I!E preGent invCflhiofl also mobiles o a rnethcd ft]r treating soybn rs in a host legLirninoils
`r:lan by di,plng Iliese cor’it:.ratlDns AccordingEy Ihe peainL invent’on relates to a Iriple
`cumhinal:on of fungic;des essentially Ore ol The uses of Ihis r:nnibnatcl9 Is aqanst Rsiari
`soybean rust
`
`:3. &0 providing data thai esbihirshos tiattrna presoitly c’ainiet CD91LW1HIIOnS are syrergisic,
`I hereby explain L’lo¼’ the need for he present rwenhon
`
`Need for th& invention:
`
`4.
`
`Experiments weic concluded at the Eouncdiron t’M Rnndonopotis the Univursty ci Rio
`Verde arid instititions pal ticuatinq in the Cooperative I esorig f rungcdes (beqirirriny in
`?003é04) Thest xperinien1s proved 11w redut:tibn
`of
`control
`effectiveness y
`conlpariricj
`the oHrforinarce of aonazcje ftinqicides ri the 2och/’r season with the
`season 2012/13 l; the season 2005/06 tue avei ape rust control by ronazole lurgicides
`was 903%. After eight oacs. corcesponclig to the ?UI?f13 season ronr•l of conaznte
`rcing cicles was 520% wiTh a redurion in efficacy cii 42% labu 1).
`
`Table 1 Reducee scyhean rust coi-trcl by conan1e fur9cides
`
`S No.
`
`Fungtide
`
`I
`
`-
`
`..
`
`—.
`
`[3
`14
`
`.
`
`I.
`i-prxicoriazoIe
`fehucortazole
`Mean
`
`brops year
`]2005/O6
`95 0
`0
`5.U
`90.3
`
`I
`
`..
`
`-
`
`2012/13
`2.0
`4U U
`
`32.O
`
`Perrcentaqe
`fredisciion
`
`40.0
`326
`k2.D
`
`Page 2 of 179
`
`SYNGENTA EXHIBIT 1035
`SYNGENTA v. UPL, PGR2023-000l7
`
`

`

`0
`
`N.
`
`C0 V
`
`U
`
`Vt
`C,
`
`0 ‘
`
`-I-,
`
`C0
`
`C CC
`
`)
`
`2)a
`
`c
`
`,
`C
`
`4
`
`Sr
`
`x
`
`S.
`
`“I
`
`‘S1
`
`-‘S
`
`1;
`
`Vie—
`C,
`
`3
`
`Ciinrrole3.
`
`[C
`
`It— a
`
`C
`
`o
`
`C)
`
`U a
`
`=a
`r
`
`-n
`
`-J—
`
`Cl’
`
`CL
`C)
`
`a
`
`c03-
`
`-
`
`0
`
`2-
`
`003C
`
`,)
`
`C,
`
`) Sa C
`0 aC2
`
`(1
`
`C 2[
`
`ct
`
`C)
`-U
`
`r;
`
`0C
`
`-4
`
`)C a
`0 N
`
`Ca
`
`C)
`’)
`
`3 F
`
`3
`
`2 0a C
`
`D
`
`ci
`
`CD
`
`0
`
`N0
`
`CI)
`
`-.
`‘-E
`
`N)
`-4
`
`CDt
`ri
`
`<0
`II
`<9
`
`3‘
`
`—
`
`It
`
`C
`
`a2
`—C
`—ci
`5..
`
`3
`
`‘C
`3_
`‘.3
`to
`
`c
`
`(C
`
`Ct
`
`LI)
`It
`
`vp
`.)0
`N)
`I)
`
`—C
`N)
`-‘3
`
`C—,
`
`-J
`
`u
`
`‘3
`-0
`
`S
`
`0 (
`
`C V
`
`S
`
`CC
`C:
`
`2C
`
`CD
`-:
`
`C
`
`[C
`
`2
`
`‘C
`
`o
`
`it
`
`-J
`
`II
`
`C a2
`
`3
`
`C’,
`
`N
`)
`
`-
`
`—4
`
`o V
`
`u
`
`-U
`
`.t
`
`‘—..±?t
`
`—j..j!4—
`
`ee
`
`c
`
`Ciumirole1%
`
`I——.
`
`“I
`
`-—
`
`‘4
`
`I—a
`
`7—.
`
`—
`
`- -
`
`I,
`
`-
`
`•
`
`4
`
`I
`
`I—
`
`—
`
`L4
`
`0
`
`—C
`C,
`
`aa 3 U
`
`?
`
`C)
`
`-I
`
`U
`
`C-j
`C,
`[—3
`
`t
`Cf
`
`C‘
`
`Ce,
`Ct
`fl
`
`4,
`a.
`
`-I
`1)
`
`-4
`
`1’,
`3-
`—I
`
`3
`
`C,
`C,1
`Vu
`Cl,
`
`0)
`
`-‘3
`
`I 0 C
`
`D
`
`N)
`4.
`
`+ pc
`m
`
`c 0O
`0 -
`
`i C
`3c
`
`)
`
`[.0
`
`(0
`
`-Ic;’
`00 .aw
`0-a
`a-I
`‘3—
`
`W
`0M
`
`on
`.fl
`
`Co
`
`0S
`l>
`Cz0I
`0-
`z-
`
`ll
`
`C
`
`(0
`b14
`
`l
`C-
`
`3
`m‘
`
`(0
`.v
`
`

`

`the elfedjvsness of this n;Ixkjre has beeri
`2013114 seasnn on’y 4lYn conlro[
`
`eiciijced by 6.54% per year.
`
`ieiching [he
`
`10
`
`Figuie 3 depics :he rcUucHcl r;onlro’ ot soybean rust ty cyprooDnazoie + prcoxysrobin
`mixaice over sx sersons.
`
`v
`
`—Qx ÷ 14)4)
`= 0,5H!4)
`
`L)4
`
`SO
`74)
`
`41)
`
`20
`
`10
`
`I-fr
`
`-:
`
`-s
`
`I E
`
`C
`
`a
`
`S
`
`aCt
`
`4-
`
`•I’e Ii IpIU Is;
`
`11
`
`lisrnq the eqJatiori v = + lOOM 9.Ox II w;ls caicul.ated Ihal from 2008/Dc) the el[cc!iveriess
`of he rnxture cyprt)c:r]nazde
`picoxysirohin. nas been reduced b 9 0% per year
`ieachrng 37% curiicI r.rop in 2013/14
`
`12.
`
`Fiyiire 4 depicfs the rediced coritro) of soybean usi
`niixkjre over si sraaoris
`
`by epoxiconazole t pyracloslibbIn
`
`li.IIJ
`9)
`FI)
`74)
`(‘4,
`
`-‘I.’
`
`il)
`29
`III
`Ii
`
`-J
`
`I
`
`%$
`#
`
`.
`
`Itui A Iiriq
`
`$5.
`
`,#
`
`Page 4 of 179
`
`SYNGENTA EXHIBIT 1035
`SYNGENTA v. UPL, PGR2023-00017
`
`J i.
`
`

`

`13.
`
`14.
`
`The riix1ure ‘e:mx:conazo!e + pyracostrobii has been ‘used since LiUY/08 Witi fl:+
`the nercentoge at annual redLc:horI
`c.onirol (%) x
`÷ 99,0 -1 2,6x [w[wi oy
`eqLIhon y
`the effectiveness at
`t[i’s
`harvest
`of contoIj, h v/as atcu;atei hat from the
`nixtt” has been decreased by 126% per year. reacI-in lh last season 23%.
`
`Figure 5 dep,cts t[ average rediclion at Hoy’uc’an rust rontro by cyproconazole +
`azoxyIribin, epoxicuriacIe + pyrac.Iotrobin ind cyproccriainle ± preoxystrobin over six
`000soris.
`
`I’ll
`
`“II
`
`‘II
`
`. Sri
`
`411
`
`ill
`
`Iii
`
`a
`
`4,/
`
`I
`
`4’
`
`“P
`
`,,‘
`
`•g
`
`,“.‘
`
`4.
`
`‘iii::, V
`
`15.
`
`16,
`
`17
`
`18.
`
`IU.
`
`Accomirij to the eqtidlicn y z-99x + ‘1000 from 2’DD/D9 the 3v0Fage eflecti’,eness at
`and
`picoxystrotNn’
`“cypft’conazoie
`azoxystrobin”,
`÷
`cyprocc)n3zo +
`flixtures
`9 Q’¾ i-
`opoxicanazoo • pyraciostrobin” nvei six crops lia Len rediit:,J
`icachina 3/% in the Ia& season
`
`Fgjure 3 depicts t reduced control .:1 soybean ‘ijsl for azcxytibin cner six seasons
`
`It was observed that froru the 2005/09 season, the’e was reduction ri the control o(/kSian
`soybean rtn using azoxystiohin and reached only’Ib% olconirni in the 2013)14 season
`
`tlsing the equation y = ± 928 13,S ii was determinud that from 20D9!10 the effEcacy at
`this tungicide has been teducea by ‘13.8% per year and endini by reaching the 2013,
`at only 1 ‘S’”..e1 ‘Don trot
`
`A study was conductecs In determine the oamtrhuliun of the addition of niancuzee to the
`known mixtures at ‘‘1icIyiurin ‘F triaiotes7 The experimeis were uonduc.ted in the field,
`in nine different Iccation where the contrihuunri of the. addiliori of mancon± to the
`t’iszclns” was obsnved.
`rM-n’centage control ohseved using irlixturos of “strobilulin ‘I
`
`Page 5 of 179
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`SYNGENTA EXHIBIT 1035
`SYNGENTA v. UPL, PGR2023-00017
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`

`

`______
`
`_______
`
`______
`
`_________
`__
`
`20
`
`Twa closes woe [€ed
`(1.5 arid 2 0 kg / lia with lJaiiciIjs numbers ci rnancozeb
`appl:r;3tions The uffent of macozdi fl 5kg / ha) inr,orpoiat€’
`Kito ‘Di) i’iiflerrI.j mxtu4
`as aiso tesled
`
`21 Mnccieh arirulation vas used /W1 WDG water disparsible granula, conirnercia ly
`a,a;13h1e
`for aili’ation as nirrczeh.
`
`22.
`
`Table 2 lists Un? prccentage canirn’ of soybean rust by mixing flNtulCs of ‘strobiluriri +
`Fr H/ole witn na wilhcu; auded r-nancozob anplied L[iree
`inies rn
`‘‘o gro ups of
`Pheninogica s’aces of soybean. evaluated v the ales L1nCCI the disease crc.inss
`curve IAUDPC
`
`S r’To
`
`A;xture
`
`1
`
`‘2
`
`3
`
`6
`
`Cyprocona2oe
`A.’nrjstrohir
`$yproconazole
`
`Picowystrohrn
`
`Thhuconazole
`
`Mean
`
`Mancozob
`Wthout
`42.8
`
`74.0
`
`[DiUerence in percentage
`DOfllfol
`31.2
`
`+
`
`I
`
`19
`
`131
`
`I
`
`Seventy in The coqirol = 10%
`
`CV
`
`4 6c):.
`
`23.
`
`1 able 3 ists the perce9taqe cririliol of soybean rust by riixttjres of ‘strobihirin
`triaales
`v’th or will’oul added niancozeb applied tflIeH times at d;lfererz gro’vlfl stages and
`assessed thc± seveniy in leaflet
`
`S No
`
`ixiure
`
`proconaole ± tax tnhw
`
`‘T
`I?
`
`IPycIoslrc
`3JThhticonazole + Pcnxystrobiii
`jMean
`Sevwily in the oonlw = 77 3%. CV
`
`64:3%
`
`rvla ncczeb
`/cahni4
`
`(58:
`40.5
`
`57.B
`
`I..
`
`75.2
`H
`31 3
`
`1 :‘itterenbc
`poir:enitage
`koonirol
`2
`347
`
`235
`
`24.
`
`25
`
`Prom the expet menial resulI, it ws thus tourd that
`the ic1dkion of the niaricazeh
`fungicide not uri’y enhances the prr:entg’2 control, but also reverts tie ohsenjed ctriLrol
`to the original
`levei of O%.
`
`1 hus. in view ci the above results, it was surpnsngly found hat the addiiori ci niancozeb
`nrjeased corilicI of ‘ust ‘sith the ;urI’Jert. anal ‘ii1[Jlc’iIe mixture Di mixLunez of ‘‘strobiluri,.
`
`Page 6 of 179
`
`SYNGENTA EXHIBIT 1035
`SYNGENTA v. UPL, PGR2023-00017
`
`_
`

`

`I
`
`triazoles
`
`26
`
`27
`
`28.
`
`The coriboalion of a deinethsrlation ntihitor and a qHinorr outside ririi)itc’r flas ucen
`known to be used or the control of Esian soybean rust, pwtoulnrly n Braz I. However,
`these cori;biiations has decayed by
`the emoacy (ii
`it has heen seen reeenU Uiat
`tire cancellation of tIies rEgis1rations by the 6razIir
`to
`!e;idu1cj
`rude chari 50%.
`itqulatoiy aulhoiity MAPA In tact. e&rna1y as 63 existing reqisiratiors for thu control i,P
`efficacy
`decay
`Lu
`due
`Airan soybean rust were usriceiled
`h?psJ’wwt’s errbrapa.br?eiibua-de-noticIa&/r.oticil19373761riia.suscende-ieislro-
`de63ftrnc.ccI2spara controle-da ferr:. q-rIti-da-soja
`
`ri
`
`in
`
`Vhs regulatory action was uIjh:hcd on the Brazilian Official Gazehe {Act
`71)
`n
`Decembet, 2016. The action was based on Ihe ovaIuann o ofFectivenew reports and
`ft.chnical opuniol’.s by tire Technrr:4I Comniissrc;ri of icgr:morrrIc Revaluation of Pesticides
`Fejrniulated Products for the Conrcl of Pskys.ic.it:-.ci;y;?i; on Sotean Cioc
`
`Some Df the prodt;cts ftu which th€-i cfxsiirq reqslratiofls were cancelled were knower
`combinations of de’nelhylation inhik;rors and quin:nie outside inh;b ters Scrc’ of these
`products lam which the ecoinniendalons were sIJspt2ilded are
`
`Con-nec cial Narire
`
`Composition
`
`MArA Req ster NC
`
`RCADA
`
`kresoxinimethyl ÷ tebijccna,u:u
`
`8511
`
`Sovcr?I tailed attenipts in the prior art to conirol soybean rust
`
`29
`
`3D.
`
`3 1
`
`Applicant ‘iAtcs that the method of :;ontiohinq soybean rust us also a technnrar feaLre vht:lu
`us the or curial ing pa nt For cDnfer’ I in uuvefty and j ‘ivoru ie sic r on the cia cried rnDthad I his
`is because Inure rave reDi’ nume ous fai cr1 alttirr;pts in Inc aie of th. mit
`Ci conlra!tiriq
`soybean r.ist. and that :ie present invention ac;ovcs success nhere such n’Jrnerous prior
`kitlen’pts in ilic state of thu It have Iai[e.
`
`ri ornertn describe Lbe slate &tlie an aithetirne o’1ling efihe above or :a:cr. and a Icing
`fL need for a fungionda! combination as disclosed in Iheaoplr;atiun and recuhd n the cu’rentl
`punding claims, we p’ovudo flue foiky’ni;
`
`li’e applir;cliori as ciruqiriaUv filed, discioses triple Eombinati Dii or a least heo Iungirin1es
`
`Page 7 of 179
`
`SYNGEPITA EXHIBIT 1035
`SYNGENTA v. UPL, PGR2023-00017
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`

`

`cnlrprislriq at least are rnittAsite furigic:d such ris ditiiwcarbamatu (tingk.ide, at lcst one
`sdccnate nehydmgorias inhibitor furcide ancUcr at ‘es 311€ Quin::•re outside nhititor
`fL;ngicid andfor at
`leasl one demel’rylat’on inhibitor
`fungicide,
`arid
`the use of
`sUch
`•ooinbinatinn in lieairiq soybean rust Ax such,
`the application is directed to a furiqrdal
`cOn’biiiIion cornprisiri a nijlti.sjtc• coilacI ¶un•icide ccJ[9Ocarbar11aei and two sys[emi’c
`Iunqirirjes ‘:succinate dehydrcenase ntiihitor Quiriole CLitsida nhibitor fungicide, andör
`derriath ylation ir•l’ibilc’r: The oidini claIms aiD dwuted to the Iipe coinbiqaticjn of ‘jnqic dcc
`and [he use of such crnhinaon in treahng .soyxi’i rust
`
`Sot,ean rus also elerreuto as Asian soybean iul ‘s caused by P,awooso,a wich’,’thizi and
`is +n agjresstve lnJlho9en that as
`detected n Ihe U.S. n Lhe fall of 2004 Since then to
`Ike Inc .yf f’lirs of ne nMant applica’uon,
`it had sp’ead from
`:4ia to. atleasl, A’rmca, South
`America. and the U S Yield losses ‘ere estlinacd to be see& w’”i this ise
`api almost
`10-80% have ucen reported. Despite signiñcant ellorts to sustain soybean rust, it has ter a
`record crob:ouI (or soybean gIower in the sOLttw.sslern United S1aes.
`
`Ike control of styhean rust sa ma;or concern for soyeJfl puducers. For exflrnp;e. soybean
`r,;st-mediatod y.eld losses sciween 130% and 1(i[Y: were leixited n Brazil P;iraguay. aid
`Soun Africa diving the ear y 200Cs. Yo;iriofl, J,T, ci aL, Epic/emits of snyhean rust
`(Phzikc’osora eiitvr.bz.
`in Dme.rm and Para.Jjav horn 2001 to 2003 Plant Dis 2X)S, 3G. 675—
`
`ti 1
`
`Yilr] l0551J!; eshinated at 25% were first rec-orted troni conirncmc’I Iietds in t1ississippi in 21)00
`Aflen, T. W eta!., A contitttiinq saga: soybean rust in the continental United States, 2004
`to 2013. OutIoDks Pest ttThnag. 2014, 25, l1—174.
`
`‘Starling with me ?003/20r4 so?bean prc&cti’ season, economic losses du9 to the disease
`(including ccsts ::-t contrcl:l ha’se been esImated at rrore thai 5? bilion annually Schctrn ot
`a?., Crop Protection. 28(2009) 774-782
`
`rn 2012. cc ybean rust reduced y:eld by over 60% n ‘ 200 h in Alabama, Sikora, F,J. ci a!..
`Observations on soyh can rust
`rnannçscrnenl
`in Alabama in 2012.
`In Proceedings
`at the Southern Soybean Disease Workers 401k Armni& MeetirQ, Pensacola Beach, FL USA.
`13—14 March 2013
`
`Since from 2001200? crop season Ia 2011/2012 crop season, the a[nJLillt spent in c3ntR’11i4
`soybean iust Increased om USD 1 (I rnilln to L’SI) 1.73 bilNon Qodoy, CV. eta?., Asian
`soybean rust in Brazil: Past, presenW ann (orate. PesquisaAgropec4sAria Brasileira. 2016,
`
`32.
`
`33.
`
`31
`
`35.
`
`36.
`
`37
`
`Page 8 of 179
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`SYNGENTA EXHIBIT 1035
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`

`iic disease was slnhiti?d to cause ie d oSses ohip to
`51(?:407—42l. See Table I
`ri lIi industry. udgezt by Israpidepansion,
`lie irrlpDrlai’ce of soyteari rusi was ‘:ery evideni
`irulenc, aid amount ot osses. T9se are alsn [‘hI:htcd in Dr flodnys 5dy esinatinq
`fri
`qrain losses and coss due to Asian soyceon rust cjritm’j[
`
`f the Instant
`
`38. r-1 most commonly iJsE(l for soybean rList rnanaqc’iic il. until pihlk€jtii’j
`iiihibrois DMlm and
`rkirionyIatc’:i
`into :wa ciasss
`applicatr, v,’e typoally iln;I’:le(l
`4UflO9e ZR;tsrie iiiibiicrs (Qol) DM1 an Gd fungicides kite !oc-ally systemic, irbiinl Ma;
`thin the ea hut nUl neccosarily horn Iea Ic leaf
`they are laken up by the eases and i’iavo
`srobi1unns
`Several DM1 and Qol fuijcides, iiclidjqq 6 riazoles. 2 s;rohilurhs 5 triazoles
`use tcr 3obean rust contra. Since
`fits!
`trazoIe + hsrizridazole have hri
`aid I
`lurcicidos emer.janry recoiniended for ie 2002iC3 season (aza:qs:robin di1enocoriio
`and et1;conazoIe:i rnarw rUW’Q (flu ation: were
`flucsnazolo. pyraclosticibir • cpo;icon.aznl€,
`added to the arsen3i to contra! rust. Sensiliv.ly nioiitoring tests by vancts groups in the
`iiica’Wy over the
`industry rE-:iale’:l that the &f cacy of the kingicr3es has boon decrear.’nc Sc:
`
`:sears
`
`39.
`
`40.
`
`clear trer;d iowarcls decreasinqelficacy of funq.ciaes in cOrilr3ll iç so’cear
`Research shows
`rust severity Cr inceasing yield iii 2013. when corr’pared with 2006 o 200/
`Id.
`
`Stuthes roricluctod by Dr Cli:iia Viaira Goicy a:encwnocl and hichly puhisrcd scientst in
`:tau-.; . including spec lic;IIy soybean rust sont’oI
`abl:stied a
`the field ni kuigci’:la I co-nt
`iliiKtures towwds lIie .Ofltrol
`graduaL rtecay in thc &fcacy ni froblunns or c’jnazoles or Erci
`of soybsin rus with their use 9radLiaIIy o’Jer the years Claudia Weira Godey, Risk and
`Management Df Fungicide Resistance In the Asian Soybean Rust Fungus Phakospora
`pachyrhizi, Fungicide Resisfance in Ctop Protection: Risk and Management (ad. TS,
`Thind CAB International 2012 Coiutiinatior,s ct strcakiriris w lh lnazoles irnprovd dsaa
`tIuu+Juued1eiiom1ance:Thfiazolus
`arid yield loss cnm,lril concyed with eilhL?r class alone .
`ii asohed a level at wi:ri rust
`obsir’od 7 years after the inlrodimotion cit P pachyrh/zi in Hra,mI
`the se of straiqht s,nies has
`rj,’
`control with straighi azc.Ios became i:ns;iLisIacc’ry. Sine
`l)Rii- deceasing a-idh use of trmaole-- strcbilur’r n1xtires was intensified s tI’e niaOr
`statoqy to ‘educe the ii of resistnce. Id. Ilowever the cornbnaiOn of such Irizole ano
`slichilurin dd not piovido a consistent suyeai1 rust conVol ested from 2006J07 to ?0U91lD.
`the suidies show a decrease ri the eftacy at the combination of triaznle and
`lit PLrther
`frcbiIuin after use over a few years Id
`
`41
`
`A:.v cu aflce pen&rlinq a ineta-anelticai syntriesis ot the isuts of 71 ijr.ltorni fLn9icide
`trials Dontair ng R30 spc’c1k:: fungicide trek3tn’ents for the control of soytean rust and yet
`
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`

`42.
`
`43.
`
`concluded thai c.DiI;binalions of strcbilurrs with trjazoles was the Lest Ireatmert avajable iii
`he rdtslr. Scherrn. H. e( at. Quantitative review of fungicide efficacy ttlal-s for
`nianagbtg soybean rust in Brazil. Crop Proteclion. 2009, 28. 774-782. Latei. evidence
`showed that even the efficacy of this best -usihIe reatmen b\ c:jrnhinauons of slrobuurins
`c’iiTh 1riazclo was seen to be 3ecayiix eith jaot:al decay I:rQcI Il’s years Id Coir;biiialions
`of triatulus with a benz!nhidazDIa fiinqi:
`did not irnpf0i2
`:nrnn:ired witi Iria2OIes alcre
`
`Id.
`
`A newok cit
`InitOinl kingciot iials (LII- I s}, involved in ani,ually e’.a1uatin luncicides since
`the 2C<2i(i season orovided uviiJenc. stigqes.tuig a deell:ie in sens livily wthirl the local f
`j:ai;?:yyz; populations to irult pl f.:,qudes, sinco elicar:v nas been roativel’9 ‘rA’/ arc
`appentl’j ecreasing in recent years rgrnnnred to pre’iimis reports. Godoy eta)., 51(5):407-
`421
`
`II was reported that in ZODS?U6 season rust averajc CLHIITo. y DMls was [90.3% •Mler only
`eiuht seasons. corresponding to 201213, DM1 cenircil was 520%. sncwiiq 4?% control
`efficacy redi.iction Godoç C. V. et . Eüciáricia de fun gicidas pani a conEroio cia
`ferru gem- -asiãtico do soja, Phaknpsora pacliyrhizi,
`urn so fro 2012/13: resultaclos
`sumar&ados dos etwaios caoperativos. Londrina:2013 (Circular
`recnica, 9a) PR.
`Setenihro, 2011 7 p. The edtiolion in Pp sensiliv ly to the ftjnciicides Ivtniconazoe and
`cyproconazc!e. with only 42 and 38S control, rescc1;vety. was also establshed Gorfoy. C V:
`Palave;; I, Ensaio cuuperativo para avaliação do efici&icia dc fun gicido no control., do
`ferrugeni do soja. em Londrinji, PR, no sake 2010/11. In: Rcueiiáo do pesquisa cie sq/a
`cia reçjiio central do BrasH. 3Z, 2011, São Pedro. Resuoios. Sac Pedro, 2011,
`In tha
`same season, DM1 + Qul milL.res did no
`reduced effooncy ye:. cypoconazole +
`:l7oxyslrotiri had 72% orirr,l and pyraclostrobin t epoxyconazole, &B% control At this tinio
`the mean control for the mxtures was 80%.
`Id. It is likely that the otfec1iv&ness was ensurca
`by Qols. as th uuctnl uiein rr DM1 was only d0Y Sd DM1 and ‘:2o1 ILnoicides c+ct on only
`one speorfic sue of ihoiisii rcs of bin’:hemical reaclions in the tuiqal ce
`reretsre they are
`unerable to fLi’cial sIrdin sMection towards sensiti.’ty rec1i:1ion or loss The difficulty in
`coniroling ASR wiLl
`lunqicides is heccning ncneasingy evident. Lq the high ñjn[9al
`aaaptzoilky. Godoy et at, Londrina:2013 (Circzil.jr Tócrica.
`PR,Se(entbro. 2013;
`Schrnitz, H. K ef at, Pest Managevteexte Science, 2013. As an exinipfe tebuconazole
`&1cienc has becri uiNdiiaIIv redu:ed from 90% to 24% rn ten soascis (ci Sonic ac:ons
`shuId be taken In iroki AS •cheniraI control reach 80-90% eticioncy:qain as in 2002i03
`lo 2CCBt- grow rio seasons fri
`
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`

`44.
`
`4i,
`
`46.
`
`47.
`
`48.
`
`49.
`
`DiIa obtoinel from the studies corducted by ‘ubrapa Soy1ear, sI-o’ned a marked rrduciion
`ri Inc efficacy 0f soybean rust ron[rul. Claudia
`witi an increase in the reduction vory year,
`‘Ch3n yes in prfnmtance of SBR fun qicid’s over the years and new
`V. Cocky,
`nlanaqoflrent sfrategies adopted in Brazil, Enthrapa SoybeanS BR — slide presentation
`Ye, dudng those years &riost 0% of the soybi’i rust cont’oI 000sIrv was using nictures of
`systsr’ic turigicides despI.e oithe rE1ucfion in efficacy. Id
`
`repc’its of resislnce to [)M aim:I
`The poor fungicide pertonnces are ssiby linked it
`201.3 Schmitz, H. K. ot a?., Sensitivity of Phakopsoro
`Gel fi.i!icideS Schm,tz et al
`arid
`and demethylaUon-inli{bitors,
`towards qtsinnric-outsde-inIiibitors
`pachyrMzl
`coriesponding resistance inuchanisnis Pest N1naq. Sci. 2013, 70:372-388.
`
`As such, the industry was lw:ed with a prnbicrm ‘n the rc’sistait inaragenwrI DI furicida!
`corfliriatic:i’s and was in the need of a sniut,on to address s•jh pi ublem t reduc;n9 ercscy
`ur krcwr Fiiriqicides tawares soyuean rust
`
`11Th) efñcac of Lombinal’uns of varicLs systemic
`e decrease iii
`Rcognizinq the problem,
`ii&s were
`the effic;icy of be systemic fur
`liinqicides differert auproaches to nanI-iiri
`undertaken
`
`rarbencla:irn + Ihram or
`liealej wh comtnrIat(Jr’ of
`Soyoaar seed was
`epoxicorrazotc
`arid
`pyr:lcstrohin
`treatrient with
`toinwed
`by
`flllquiricofla7ritt
`:rifloxisrohin + tebtcc,rls2oie. Godoy and Henning, Pesq. agvopec. bras,1 Braslila, v43,
`n.1O, p1297-13OZ out 2003
`
`fungicdes
`
`+
`
`A prelilix at s’jtonik ‘ii:igi: Des aLOxystrobn and Cyprtro:i2ole) was appl!e1 IC- differen
`growh shoes o cortrrl s.cijbean rniiI. Godoy, (DiV. ef aL, Eticiènci a do centrole cia ferfugeni
`asiatkca da soja em tunçao do memento de apllaaflo sob condiçós de epideinia em
`Londrqua, PR. Tropical Plant Pathology 34 (1) Jamwry - Filbruary 2009.
`
`51)
`
`“.3jtei 2007P00tS the dmrLase in e1fcacy becaiiic a genera] trend for DM1 ung.c des.
`
`it had been
`ihe only oxceptiar was prnlhicconaiule, which vta launciwd ni 2010, •Jthougi
`assessed rce 20052006. Beciisu of Ire redLjc’ad sFfic.c:y of OMIa. prethicuonazolc was
`Ia’jnthed as a mixture wfth Uifloxystrobn.” Got-Joy, C. V. et at,. Pesq. aqropec. bras., Brasitia,
`v51, n. p407-421, male 2016
`
`51,
`
`,age Ivhib tors iSDIis
`Ccmhin1aor.s ccrflpr.sr-o iIQ\, broad-spectruni Sicc.pate I)&-wdro
`(Qols). aqan both .ysten’ic fungicides,
`fungcides rriixed with quinone nUtsde inht:i!c>i
`
`Page 11 of 179
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`

`‘/ere iauncIiri onto [ne market
`ii ?D13. Goday, CV ef aL, BraziU,9n sojibean pest
`management and threats to its susMinabliitv. Outlooks on Pest Management — June
`2015. Trijle conthiniions, conipr’sng a:l systemic kiriqi::ides. were also tested for
`irflCrcrt±Iieflt in th ellicacy comLuiiations in cenlroihnq soybean ii Godoy, C. V. ef 31.,
`Eficiéacia tie fun gicidas pars a controle da fcrrugern-asiátic da soja, Phkopsors
`pachyrhiii, na salts 2014/15: ress.illados sumarizadus tins ensaios coopenativos, p:1-6
`
`52.
`
`Tna offorts hgn,iqhtezt aba/c ri addition Ii> varioua utlw:
`to overconie [lie
`pobteins RssaoiaW:I with cecreas in efñcac •:it tunoi•oici& combinations in treating soybesn
`rt..st
`did
`rot
`esijll
`a
`in
`i’joraHe
`result
`Fur examp,
`seed treatment
`fluqurmonazol de;ayd neftnei he appearance of (ist syrnptoiri nor the ovolutor or
`tie
`jsaa in adiur to uickinq any benefit in the maiaqnlent of List Godoy and Hemiing,
`v.43. nW, p.129?-1302, 2008 rhese i:jdies asu :.nnr.Iuded [Hat rhe addition of a Icliar
`ILnqlcjde reatrtient rerun cii did not [iavi a avorahIe , rfj•jonce on the stRrdari known
`¶uatmenl legilne of slioc Li + ccazol fungiotes for the control of sc’vb4!an rust. d rhis
`Wds a clear teaching away from he scoud mf the preerit rQerIion
`
`V,Ilfl
`
`e(cacy of
`
`Eullnwng the wread ot sovbtan rust a Afitca and South America in the last decc,de the high
`tiazoles in i:ieiwisuwilh a few eceplinns sjch as triadcreronl 4ias been
`ccnrrne n ;‘ILF[l-yeaf Lr.al
`tnes& tEiafs showort that the st1ei:Jiirins, The newest class of
`f:iirjirdes ovkiated !oe Iho iianagemeil of soybean rust, we ulfecli’de in reducing disease
`i:ltersty and associated yield loss.
`
`The mca cfrecti:e strate’j avaiable to. arid unriorstood n,
`the industry — unit diSCc’sej
`in the instant application — was the use of doubt’:’ .s ud ti—plo corliorattens of deniethylation
`inhibitors, quinone inhibitors
`and succinate daiydrrqenasc inhibitors
`at of which are
`s’?stem;ofurigcides—forlhe cnrilra of soybean rust. Howe’ier. siriceeffecthc tirgicidos with a
`new niode ii acton aro not eai:lil uyailahe Ite prnhtems associalcu ‘vth Oecrease in
`tiingicidal efficacy over thr yers nersisld due to tiOsLicCeSSfUt illempts The need to reverse
`si:cb probler-ca v.’itn the elficacy of snternic Jniq.cies was ‘ketl recognized in Pie
`eld of
`‘ringitidal con-l:tnalons.
`
`tie inventors u’tlis appicatiori c9(iLCtOd strides sot Iorth in the lisrani applir;aicn to ornide
`a oiiq-o’naired Rokction for tIn? dre&ful piotern :c’ [ha industry :f li;r9icciai iriihinatci-s icr
`soybean aisi cirtrol
`
`As ;nen1ioad above [in paraqraph I most cc•mniont used fLriglcides w soytean iit
`inariaqemenl unhi puo1ication L)t the insla iii application heonged to dei’iehylaion inhibitors
`
`j4.
`
`55.
`
`56.
`
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`

`57.
`
`58.
`
`bY.
`
`60
`
`an’i
`
`ol which are ysemic :iinrri.s
`imntIt
`‘nrbilais Qc•I),
`-j.r,oie outside
`(DM1)
`and triple) nn’iibiriaioiis of systenic fur9icides wee Icsted for aiiIio.
`AIthouh ;:urlaii [clotjh
`such as
`a ccnibn alien ci systemic fungicides wilfl nijtisjte tunqcides
`of soybean r jst
`ci .tliocarbacHstLs was ItJ tested prior to the fil nq ol 11w riiflant appli catia
`
`Mull ste fiinycides such as Jithecarhan1 a are interim: in ensure ie çiroleclion 01 Clant:4
`before caIropii attack. They iriList be appliuu bofore the czlhoqens infect 11w plant, torn]ir[
`a protective h,rrer toxic for furiçj and hactera n ptants, Vdhen app1 CD to the surface of plant
`inhhit r. Inc spores
`iincji
`rc. ie iu:Cl, ation of
`tyj
`exert 1;x!C barrie’ pr€ccnt
`nerrn,nat’oD pracess. Synqcnta. B&ethn Ténicc, Pzio,i Xtra.SAo Paufu: Sec:orflqro; 2004,
`
`p. 31
`
`let
`
`the first
`
`lime. describes a funçjicidal ctiib:riaiion ccmmpr’sncj a
`The nitant apc.icslic:i,
`a Ioiq-awa’ted solution to the protlem
`tinq.c:ec- ann lw SySiCifliC ‘unqi’;itlet€,
`miultisne contarl
`Df rnairtairlincj etficac of the combHations tovtards m:ontrot;ing soybean I ust Specification
`as orignafly fled. pige 6.
`
`cr1 p115 P (lOt Ie sI uric flu Iti she :onl aut
`The anpl cation ci is Dlnsis a funqic.icla i 1:0 Ollal ‘‘31
`fui’gicide sucb as ii dithlccarbarnai4 4l.l:i[clde. at least one firsi systemic fungicide (sich as
`ci qicdDi, aid at least one second sjslernic. tcircIcIcJ.2
`a sui:.clnalo dci’ydrciqeriao nmbro’
`i’qi ce’: or a ernethyIatior inhbiar urig.cidei for trs
`(such as a qu i:or,e ouside rihiblto fi
`LcIlrol Asia sojbean rust, fri
`
`Studies rnrtfuctcd by the iwenlors ot the nislant appiication showed that sysleinic furcicid+
`‘ift,tted ecti.iniinoLs ont A’h;le
`cifi:ctiely penetrate We dense canopy ami’ier of Fhe
`il’r— contaci
`ii’:ulIarec.tsv rot alowinq [ho ?lJst paihogon to move mip t!io plan: foliaqt.
`potectiwe ci ti’,IuLaItnate (unqicide component .jf the coiribination efecIil’ penetrated
`l” dense plant folaoe. whPe the systeniicfiingicido comnponerll effcctivey priwented the rust
`the
`educinq
`the plant cffectivey
`Ierila:niig portion of
`;i’fectn9 1im+
`Imon I
`p;4thog’Dl
`Iowa, Js rie riecticr This synerq’slic coniplenmrlaliur’, was nol
`the clart
`susceclIhilly ot
`seen ‘.iben cithe the folar prc:i+ctive fungicide or the Systemic Iui’icicle was indi’dually used
`n isolation bit was obserjed when [he wo tiinr,cIdes i’,ere ‘.isen ri conjur-oton
`
`61
`
`In ±11 hon o a:t1iissncj the Ionq-s:ardng reed [of contro:I’r.i soybean rush in the industry
`the syneristir cornplementation between the contact preventi’edithiocarbin-.ate fuicicide and
`the treatnem;[ amid contro of Phakopsora
`tie cormior,at:on of [we systemic fuigeides for
`species of Linqcdes was toti’i:l to i:’e unexpeclecar:]strD-Isirv
`
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`1 tie understandinq in 9e industi w9s that since systemic funfilcides
`iDMl, Qol, ur
`:ornhiiiaion lt’i
`i:’I were ii’izated It, he ih e besi a’ t;4t)le (or the cont.oi cit soybean riis!,
`there woLia nd be:’iy 9eed ñjr a multisile !cirgicido Svsterric funo:cides such os DM1 and
`Gol, is taker up by i prt and is then Ii ansbcated, wil[iiri the plan systL?Ifl thus proteci4 tti
`plant from: the allac of pathoaenic fungi cr lirritinci api aiready established nfector.. Mwreas
`mullisite fungicide musf be appii’d betore the pathaqens r:fe:l the plant. forming a pi<tc:I ce
`oarrie[ ftxic for fungi and bacicr n plarus. Accodinqly. die t
`tie ci4’€-tern modes of actions
`of system L irid rn.j.115 C kinj:t[uj.s They were nine: ccristcierad ft ta oi-nbiricd unlil after
`the pubtca1 ni of the rsant au plic&icn
`
`is the ;;alt!::cn for toytea” rust is locahy sswrutr There was in Rxr,eo[ed advanlarie to be
`accfucc by Ihe adcition o a iiiu$lste fi:rgicide to d ccimhination of systemic tunciedes in use
`
`The ftseaich ccrmucrei:l oy the inventors, arid the sihecI mdltPr disclosed and rljned,
`in me irllnt appical co found thai the adciticri of a multiste luriqicicie e.g. iancoea to
`of 5cLinate
`C42TiibIfl.t!Ofl
`nehy’jroqc uise
`the
`nhjbiici
`dernef-ii,lalian
`iti”:;cide
`inhib.’tor or qunore oue-idu iiit’ibtor re’erses the daray of efficacy olihe known combination
`and evei Is it to the oriciiriai Ic’i:.,n efficacy or nidler efficacy.
`
`Tria were cnnci.red to aluate the inipoiftint;e of n;anc.ooh in associalion ‘At!; ome
`f1inqicides in r’hokcpsom 93’Jr’.rhizi cortici
`in oyheai- usiriq ‘uanccizeb ii c:wiihinaton
`wili rütures cit strchiluitus, or Iriazotes wth succinale deliydm uLer1ase inhibitai ILinqIEtnas
`
`62.
`
`6:3
`
`64.
`
`GF3.
`
`66.
`
`isolation,
`
`SLu’:Ins lwwed ha: the i,.trtticn of mancoieb.
`to -n 60k
`fungicide ando a srohiIurin
`funQicide ar1dD LI caqazole fLifKJ ride conibitialiun wSEa sLirpi sr;qtv ceae ilnii; what was
`expected Iron, a knowled
`of
`the ncoveinent accrJLm to Pie e1icacy iI
`si.JcDinaie
`dohydrc’genase inhibitci
`lurigickles with either The s?:ohi:Lrin fiingici’:Ie or
`the ronazole
`I! was corstenily rt*der than al east 20% :i.e. double the
`ir’Jmoverrent in the ‘soated s.iccrate dehycreqenase rI’tiIor tun’gicides wilK srobiiurin or
`tfle LYI iaole fungiDldc’)
`
`Funcji::ide
`
`fl
`
`67.
`
`Surputsirig!y,
`in the aoserce of maricozeb.
`the (Lingicidal efficacy of these tLingicdes was
`known it rrauai’.y decay wilt Ii’oi’ usage oyet the years See figure below.
`
`Page 14 of 179
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`

`Technical Circular5 EMBRAPA
`
`rn,
`
`,
`
`ii?
`
`7 I. tfln ran :-,‘
`
`I
`
`pp 21 1 7;
`
`, ri ‘met
`
`5pvtiii pti2 i.(iiiteIlPl p,,tti 17pri1 IIpiITh:P i1iie ;Phy dte kQ t.i.tlt.pv,I..,ii .+it’i t,up.p,ipp. Li’,’ 1’’’ace
`il hi.,pti I,, i’ tiw p.),, r,lni
`
`L’—_,_
`
`——‘I————F--- —z
`- -, —
`
`—
`
`--
`
`‘J.
`
`;).Z____
`
`4T
`
`.,,*..,.m-.a -
`
`V
`3
`
`4”
`
`0
`
`JrMHI,
`
`i’,iuii I
`
`/ii
`
`)[1fl1)
`
`Jütv I
`
`.‘,-,fl,
`
`t:ic(,.
`
`tI1f1r
`
`JUItiiI
`
`63
`
`69
`
`Tie rrorpoiation ot niaricozeb to io cornnaon reversed he decrease in the elticaoy
`‘ias surorising arfli 000xr3ecIe:
`nt ‘::mtic:I rc, soyhe;in ust by he coiiiuflaters. wr’ic
`
`in Ihe state o the art rot ftingcdes that can
`there tas been 3 diii? roeci
`Accc-rziirq]y,
`eflicaciciusly control mt A&iOr soyberi rust in Rr:lfi and other co:iiilries
`
`ioijjreserited by the InvontlOn:
`
`/0.
`
`71
`
`the Hratiliaii AgriculturaL
`Acccrlil9iy, a study was conirnissk:’nod by EMBRAPA i.e
`Research .cipo-ritimii, ‘Mitch is a stale LwilOil resear[;Ii auncy afliliated wv[th the Brazilidi’.
`r rstry of A.ricuhure Tlu research paper published by G000Y. Ctidia as a res’.ilt
`of this sliidy is annexed hereto arid also offered as posI publishei evidence in suppo’
`of the inventive step 31 Ihu oresert n’€’rilicr.
`
`[his research corrohora1c whal the present invention Eci2ld ai its priortty diLe (2012) Ic
`the additorn of a mu’tiMe fungicide e9 inaiicozeb to the c;ciitinit;rjri o( deiiethyialici;
`the kno’sn
`ci
`i evwsos the lecay of
`effir:;3r:v
`liihiihitor + (1[uJ;CnIe Ot:tSJdU inhibitor
`inhibitor • quinc’ie n itsidu inihi btor and everts ito ihs
`con,biraliun’ o[ deriielhyliLiori
`original krmwi efficacy or helter efia:;i
`
`72.
`
`Fle relevant dala [rem the table 5 ac•pearii1’ in thi. table is reproduced hiuruinbelow
`
`iTrertrr rid
`Thflexysli:iini
`
`* Prmhiocrn’azole
`
`Dosre ( a I Ha’
`60 + 3D
`
`.-e niyi)
`
`Page 15 of 179
`
`SYNGENTA EXHIBIT 1035
`SYNGENTA v. UPL, PGR2023-00017
`
`

`

`Itriloxystrobin
`rnanebzeb
`Tcittox’ptrohin
`nianccizeb
`[1i:1loxyscrohn
`
`T1if1oysi;nhin
`n,ancozcb
`
`+
`
`Prothioconazale
`
`andSO i 30
`
`220
`
`Prothoconzoe
`
`I
`
`•
`
`PieThunconazole
`
`Prothiconazole
`
`ani3O 1 30 + i%)D
`I
`aridQ 30 + 2210
`
`and6o t 30 • 2240
`[
`
`89
`
`121.2
`
`20. I
`
`I
`
`73.
`
`7&
`
`Acr:ording!y,
`it v
`observed that
`ri he presence ol rnancozeb,
`reduction in to peiccnaqe ocidence of soybean rust
`iii erent in the ri
`I t On clai Died 0 he pr esenc invenilorl
`
`there was 15 tO 30%
`
`rhis confirms Ihe inventive step
`
`rnpnrtanlly, these combinalions comprising niancozeb in addition In
`derrie1[iyrtion
`uth:hitor and a quirione outside irihibior were coisidered by EM BRAPA for
`the coriIrnI
`of -chean [List
`1h15 combination was :(und t’asUcceeo where I3 o1he exislt
`pLpciitQtJv 3uccessIulIy_conliol Asian soypeanmst.
`
`The enibinaUons ale yp@rqistic:
`
`75.
`
`1€3
`
`Not only The pesriiy claimed coriibinaions re.iert the ef1cacy of ilie systemic lunqicides
`ID the pro cocay Iceir2. the esuIt;riçj Lrirle coribinabori Of a IfluitIIiH contact fnqrides
`3Rd at cast Wc) FAStenhiC funjticies 3r0 also synergistic This ynerg:stIc colielation
`heM’een these conponents of the c:ci!nhinr4t+cns ‘31 lI