i
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`•
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`10 /5~0 '!~CT /JP 0 3/10490
`20008.03
`
`UNITED STATES DEPARTMENT OF CO:M:MERCE
`
`United States Patent and Trademark Office
`
`July 31, 2003
`
`THIS IS TO CERTIFY THAT ANNEXED HERETO IS A TRUE COPY FROM
`THE RECORDS OF THE UNITED STATES PATENT AND TRADEMARK
`OFFICEOFTHOSEPAPERSOFTHEBELOWIDENTIFIEDPATENT
`APPLICATION TBA T lVIET THE REQUIRElVIENTS TO BE GRANTED A ·
`FILING DATE UNDER 35 USC 111.
`
`APPLICATION NUMBER: 60/404,927
`FILING DATE: August 22, 2002
`
`.=
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`'=
`((j)
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`
`PRIORITY DOCUMENT
`SUBMITTED OR TRANSMITTED IN
`COMPLIANCE WITH
`RULE 17.l{a) OR (b)
`
`· :~ ~ By Authority of the
`-., .... , .... ·:s
`.
`\ 2, COMMISSIONER OF PATENTS AND TRADEMARKS
`..,.~~'"''·~}-,;..~-~~ .-....
`(~'\~}2&·~~.-:~l!;~/ ·.~: f
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`Jl'
`
`P.R. GRANT
`Certifying Officer
`
`Page 1 of 46
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`•
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`Box ProvisloDill Applialfon
`PTOISBII6(8-0D)
`
`PROVISIONAL APPliCATION FOR PATENT COVER SHEET
`This is a request for filing a PROVISIONAL APPliCATION FOR PATENT under 37 C.F.R. § 1.53 {c).
`
`:
`
`\I
`c
`~
`
`'U
`
`Filing Date
`
`CIM:nNm=(fins...S=Idlc[ol'""11)
`
`August 22, 2002
`
`...... _
`
`Jt1itsutak.a
`Shunsuke
`Masaaki
`
`HAKAMtJRA
`SAm
`OGASA
`
`INVENTOR(s)IAPPUCANT(s)
`
`I Docket No. I
`
`0020-5041P
`
`RESIDENCI!{aTY -"MD I!JTtiJ!ll
`STATE OR. FORI!IGN CDUNTR.Y)
`Osaka, Japan
`Osaka, Japan
`Osaka, Japan
`
`-
`
`D Addtbonal mventors are bemg llllltllld on the
`
`separately numbered sheets attaclled hereto
`
`11TLE OF 1liE INVENTION (280 characters max)
`
`AN AGENT FOR TREATMENT OF SCHJ:ZOPHRENZA
`
`CORRESPONDENCE ADDRESS
`Birch, Stewart, Kolasch & Birch, LLP or customer No. 2292
`P.O. Box 747
`Falls Church
`
`STATE
`
`I
`
`VA
`
`ZIP CODE
`
`I 22040-0747
`
`I COUNTRY
`
`U.S.A.
`
`181 Specification
`181 Drawmg(s)
`
`ENCI.DSED APPLICATION PARTS (clteck all thai apply)
`0 Appbcation Data Sheet. See 37 CFR I 76.
`0 Other (specify). __
`
`!§.
`·1,
`
`Number of Pages.
`Number ofSheels.
`
`METHOD OF PAYMENT (clzeck one)
`0 Appbcant clam1S small entity status See 37 CFR I :1.7.
`181 A check or money order is enclosed to cover lhe Provtstonal fihng fees.
`D The Comrrusstoner ts heteby authonzed to charge fibng fees and credit Depostt Account Number
`02-2448, tfnecessary.
`
`PROVISIONAL FILING FEE
`0 Small Entity ($80 00)
`181 Large Ennty ($160 00)
`
`The invention was made by an agency of the United States Government or under a contract with an agency of the
`United States Government.
`181 No.
`D Yes, the name of the U.S. Government agency and the Government contract number are:
`
`Respectfully submitted,
`
`Date: August 22, 2002
`
`swil!;d
`
`0020..5041P
`
`~~~~~~~~~~~~
`-Ia.;
`P.O.Box747
`Falls Church. VA 22040-0747
`(703) 205-8000
`
`I Rev. 0811&'02)
`
`Page 2 of 46
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`PROVISIONAL APPUCATION COVER SHEET
`Additional Page
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`PTO/SB/16 (8-00)
`
`Docket Number
`
`0020-5041P
`
`INVENTOR(S)/APPUCANT(S)
`
`Given Name (fust and
`middle [if any])
`
`Family or Surname
`
`Residence
`(City and either State or Foreign Country)
`
`Mitsutaka
`
`NAKAMURA
`
`2-8, Dosho-macbi-2-chome, Chuo-k.u, Osaka-shi, Osaka-
`
`fu. Japan
`
`Shunsuke
`
`SAMI
`
`2-8, Dosho-macbi-2-chome, Chuo-ku, Osaka-shi, Osaka-
`
`fu, Japan
`
`Masaaki
`
`OGASA
`
`2-8, Oosho-machi-2-chome, Chuo-ku, Osaka-sbi, Osaka-
`
`fu.Japan
`
`Number2of2
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`Page 3 of 46
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`SLAYBACK EXHIBIT 1005
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`FROM AOYAMA&PARTNERS •
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`Page 4 of 46
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`SLAYBACK EXHIBIT 1005
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`FROM AOYAMA&PARTNERS •
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`2
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`Page 5 of 46
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`SLAYBACK EXHIBIT 1005
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`FROM AOYAMA&PARTNERS •
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`dicarboximide ~ ft.f~-{:'<Dttliit&~ ~O)i!t • .l:l~~ ~ tL'!>til~t, ~~!R-RfiEG~~
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`methyl]-l-cyclohexylmethyl]-2,3-bicyclo[2.2.1]heptanedicarboximide
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`~~~~~~?t~~~·~~t..."'(Wf~:li~ 1 a ImJ6jfirp,~.lft.,t.:~ ::::.-? .. ~lA"'
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`25
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`Page 6 of 46
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`SLAYBACK EXHIBIT 1005
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`FROM AOYAMA&PARTNERS •
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`4
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`25
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`Page 7 of 46
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`SLAYBACK EXHIBIT 1005
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`

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`FROM AO~AMA&PARTNERS •
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`2002~ 8~228($) 9·04~ S4/X88~5300368777 P
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`Page 8 of 46
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`SLAYBACK EXHIBIT 1005
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`FROM AOYAMAQPARTNERS •
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`•
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`2002~ 9~22B<*> 9.05/Vm 8.54/X8S~S300368777 P 10
`
`~ !!"'!111:!!-o ll..Q . .-q ~ 7 _ n n ;? i::ll n.~
`
`6
`
`BAS:
`
`SAS:
`
`PANSS:
`
`Barnes Akathisia Scale
`(T7J~~THR.!e>
`Simpson-Angust ·Rating Scale
`(flf*M-M~I!lft:.fflWMfiR!Jf)
`Positive and Negative Syndrome Scale
`(~. ~~!iE~jif(pfiR.Yf)
`
`~-fiJl
`tmVJmntnta.*iita
`(1)~~
`
`s
`
`t~ 1 'C~T~f!r:II~J: I:J, *mil 5 Df!iii5N~:t:ut ."5 1 4 9 9iJOJ'":flll~~8#
`~~~ t,-c, ~t§:!t1Ul~~o7"7-t!~MW.t=.11m:f1(~f*~~&t,t.:.b 7"7
`--e~~-9-l;:J: 'Jwashoutfi .. SM-1 3 4 9 6 4 OmgJU;tl 2 Omg, ~\.,< t:t:1'
`
`7~~~1al~6~00~~\.,~~~~~&a~~~~~t,~o
`
`~1
`
`fh~
`
`1§1~
`
`)tf"fA
`
`A double-blind. randomized. fixed dose, placebo-controlled,
`parallel-groUp. 6-week, .efficacy • .safety, and tolerability study
`of two dose levels of SM-13496 in patients with scchizophrenia
`by DSM-IV criteria who are experiencing an acute exacerbation of
`symptoms
`~M;~Q(f)~~~~(DSM-~If~) t.:)Ct-j-.Q~'(}t~
`M:li::-?l-''"C .. :7'7~,ff~~~~~ t..t::. --li-~fti¥8111:1:;-~~J: 9~1M
`Too
`iiltR.£itfl
`1) DSM-~[filliif&li:: J:. .QM¥ft~~m,1f~WftilMJQ) b Q)
`2) Extracted-BPRSA ::J 7 4 2 Sl.J:n~--=>C G I - SA ::J 7 41:J.J:.
`3) Simpson-Angus_:;!;. :::z 7 2 *•»~~A I M S _:;~;. ::z 7 3 *t6tf
`4) mm1&FJ;J...C
`5) 1 8--6 4file1)'-Jtc
`I*M-£if@
`1) fafjflf:tfjt~(f)f'Rftt~li!!#
`2) 7,f-1iiJ&~-=PtT.>IAf.#-etfhJMPi!M*iff'z::~.om#
`3) ~lf$40)j\\rjt, '$#
`4) .r~-=\"-!/Y:YJW,. Alzheimerlif~ -sfl$ .. P1Kfftl:~.l\ ..
`tEEtlllJkotd t.. "'C'lt' o iif~M:O)~ o 'b QJ .. B!$LI:PQ)fA1=tf
`6)
`6) ~~-ii£~~-t'!Mt
`7) tb8Jt1£1!llifj:Dt~ ~ t.. -c~i8¥f ~ *UIW L tt$#
`mlfir"if-1~ 77Y~~OO··~~~·~ff~~~·-mD~
`
`•
`
`'"Civ'IJ'"'Iv$
`
`Page 9 of 46
`
`SLAYBACK EXHIBIT 1005
`
`

`

`FROM AQVAMA&PARTNERS •
`
`1
`
`1*JfJ.&UC
`fn:JJUiili
`
`'j)tJj.jj.~lj.jy 40mg/day, 1 20mgJday.J(t.t:1'7-e~~l a llm611!ltm~4 ..
`IJilfHHI'Rfft: 3 t:J) 0'):1'7 -e ~8t4f~ J: ~washout..
`1!:
`WashoutMIIIJJk. tm•Ui 2 iafiJU:l:)...~
`1) (l!le1)~gpf-~JF.It.t'rrb~li'o MIM~f:fafll(dfi~i£m L--c
`v' -5~J':t~~ < !: ~ 3 I=! IL, ~R1iiJ) JU";tl~W) ( 7~D C1J
`washoutJ9)1HJ~I9:~ 0 0
`2) tlf*M-MfiEtt~J!m L-tt.~Jo:.t.tmr~-=\'-;.; Y ::.--.-OXSI!m 'kAT~ -r
`Oo
`3) :lf:IJ.&t.~mm L.tdl-a-~t.t l:l 7 -tt .r~ A ~.f£1DT oo
`iti!iilft: : 1 3 2 f§ij (::f7~,ff.. 40mg, 120mg 45-~4$ 4 4 jlj)
`~~7~: 1 4 9t11(:7"7~~~4J¥5 Oflj., 40mg~..!J.IJ5 Ofl,
`120mg~..!J.I¥ 4 9 &lD
`U~ : PANSS, Hxtracted-BPRS, CGI-S/I
`~~~ : EPS Rating scale (Simpson-Angus. Barnes, AIMS), /'<-'( ~ Jv
`iJ"-'( :..-- (1$if!, .lfu./£, JlliUtllt>, 1 2 iM-·C..fiiSJ, lfiiD*.ffU!E
`cm~~~~ .. m~~~~~~~ .. :1'P7~~:; .. ~~
`.l .. M*#~~~ .. ~--~~-~~ .. fl~~
`
`~~-
`
`jijt{ilfilJi~
`
`(2)~~-
`
`1)~-fftO)~
`
`( i) B P R S, CG I- I &'CFCG I- SiWfiBiKtdv'"'C, Witltt~Tiitff;:,,fdtjQB
`P R S :to J: t)t PAN S S ;t.. :::t 7 ( L 0 C F) f~ IE> Ol~ C G I - S :IS J: 'CFC G I -
`I
`;t..::r7 (LOC F) .g, --t:n"'C~ 2~-tU~ 3lC~To ~2:toJ:~ 3~:l~f!}J e:,
`ir,.f~J:? ~~ .. SM-1 3 4 9 6 4 Omg]k'()t 1 2 OmgjStlj.J¥(1)~M-71Af(ji~
`6 ill> f~tolt ;ct,tl;}iiii;t}:.€> (/),A ::z Y~1>Dtt.t7"71!"'t9:.lj.!JO)..:Cn ~ ltf!f t.. -c'ff
`~~.t~n~ ... "j:f~PAN S SI¥{)Bj""t:~ ... ~T~l~t3&t-'5 SM-1 3 4 9 6 1
`2 OmgiSt.f!i.$(J).A ::z 7~1>:itf';t:1'7-e~&41¥(f).f:h~~~~J!~Ds;te:,tf,, SM
`- 1 3 4: 9 6 ·~ J: .QfiJ~JjE~O')Qfc~~;~af; ~tLt~ ..
`a5C2
`
`5
`
`10
`
`:7"7-e~
`(45)
`
`!t-9-:it
`SM-13496 40 mg
`(fka#lt)
`(47)
`lJZ.UJ (SD)
`lJZUJ (SD)
`1¥fllliRIJf.
`BPRS
`-4.0
`-10.0
`( 8.46)
`(12. 79)
`~lt.A::rY
`-5.8
`PANSS
`-14.1
`-8-ift.A::r7
`(23. 10)
`(14. 06)
`0.063
`n: jifijiJtil Dunnett's t--:Q:(~JU:Ii~F~ :1'7-t!~W~ 0)~)
`~ .. R~~mT,~~~~~~A~L~~~~~
`
`p{iil
`
`0.014
`
`SY-13496 120 mg
`(44)
`
`31Z1$ (SD)
`-11.3
`( 8. 89)
`-17.4
`(15. 70)
`
`p ••
`
`0.003
`
`0.010
`
`Page 10 of 46
`
`SLAYBACK EXHIBIT 1005
`
`

`

`FROM AOYAMA&PARTNERS
`
`•
`
`•
`
`2002~ 8~22B<*> 9.07/VS 8:54/~&~5300368777 P 12
`
`E"~ n 141-n ll.g..~ ~·7 .. .n n ;tP Dfl' n;?
`
`6
`
`~Jj.jj
`
`::1'7-kllf
`
`SM-13496 40 mg
`
`SM-13496 120 mg
`
`IWfdfi/Uf
`
`CGI-S
`
`p{jl' ~ (SD)
`(n=40)
`-o. 8 (1. 03)
`(n=42)
`3. 0 (1. 29)
`
`0.004
`
`pfl«'
`
`0.002
`
`0.005
`
`.j$ (SD)
`liZ~ (SD)
`(n=41)
`(n=41)
`-o. 7 (1. 12)
`0.0 (0. 77)
`(n=46)
`(n=47)
`CGI-I
`4. 0 (1. 41)
`0.013
`3. 2 (1. 66)
`. It: jif;j{l{JJ Dunnett's t-~i:i::(4}JD:fi1Je:1'7-k~i¥~ Q)J.tW
`~~~4-~~f~~4M·~~~~~~~~~-~fi
`i )~tt .. B P R S-€i"-if-.A::z7 (LOC F)<T.>ff£3~1/77·~~1"'~ ..
`( i
`
`1 ~~~-t" kto t) '"('-a,o~ 1M l·r:.~ t k td" .. SM- 1 3 4 9 6 *~41F•~j01t Q
`B P R S .A=::~ 7(7)~lj.ftfi]}=-~<1.>~9-.Itl'i .. 7'7~~~1j.-c lt~ L. -c 13l!t ~ TJ.,.b
`fi"~f,tj~~~~~t)b ~tJ,t~ (p<O. 05) a
`
`IS#<T.>(M
`
`6
`
`( i
`
`i i) ~ ~~~~ lit~7ilt"IO:::td~t~ B P R S(7)~~7Jt 2 0 %~~t..< I~CG
`I ;Ot 1 JUi 2 ~~ L.t~$# ( v .A~!.-'!/-) (l)llJ~~~ 4l~ff.;'"f* o ~ 4 'IJ>-o PR
`bt.~t~J:? l;::, SM- 1 3 4 9 6 4 Omg&Q 1 2 Omg~lj..IJc 7'7-e~~lj.fl.¥
`
`I -
`
`~'frilt.t~1J\a:B.bb ~nt~a
`
`10
`
`.4
`
`ti-4it
`(~#It>
`
`::1'7-e~
`(46)
`ff.lt
`
`SM-13496 40 mg
`(47)
`
`&l.llt
`
`pM"
`
`SM-13496 120 mg
`(44)
`
`&lJit
`
`pSi'
`
`VA~~~-
`
`26
`
`0.002
`
`22
`
`0.007
`10
`#: -~~{...~ Cochran-Mantel-Haenszel f*#E'(4i-JI'Hi:UJ~ :7"7-e~$~QJJ;t
`i!!rt)
`2):tc~d)~
`{ 1) 1 0 %P.J.J:.(l)l.ft.~IC·~~nt.:.l[" .. ~riia~ 5 fC~To
`
`~5
`
`:7'7~iff
`
`'UIC;."="t"a!ll:l'.
`
`60
`-lf~ammfiJtt<%> 36 (72)
`3 (6)
`
`Oo:>:ff~••JBm&lJ~t <9&>
`
`40 mg
`60
`
`40 (80)
`
`3 (6)
`
`120 mg
`49
`
`38 (78)
`
`3 (6)
`
`Page 11 of 46
`
`SLAYBACK EXHIBIT 1005
`
`

`

`FROM AOYAMA&PARTNERS •
`
`9
`
`~~~~~~~~~k~~~~~ 2 (4)
`(~)
`
`6 (12)
`
`6 (12)
`
`~~ftmmilllt<%>
`
`Wi-fr;:'f'J.\
`115~
`Jmli
`71Jf/:/7
`1'$!11tlt!:~~ "' (1§1~-~1*<)
`
`...
`
`4 (8)
`5 (10)
`8 (16)
`4 (8)
`6 (12)
`9 (18)
`4 (8)
`2 (4)
`
`2 (4)
`
`11 (22)
`3 (6)
`7 (14)
`6 (10)
`7 (14)
`5 (10)
`1 (2)
`
`6 (12)
`2 (4)
`5 (10)
`0 (0)
`3 (6)
`6 (10)
`2 (4)
`~
`5 (10)
`Mfti~~JIRJ
`tll!c(!)~fii . . »s$bf.> E>tLtt.fJMtJal0lJ ~ » ., ~ t- L-t~
`2t 5 l~ffi ~ tt,.Q c!:: :I'd t) .. 1 4 9 01Jc:p 1 1 4 f?IH 7 7 %H;:~!f ... tlS3!¥J &tLt=.
`»~ ... l~l::lv~'IJ~@lt::Rt.ttJ:I~~~;l?"?t;::o :fr1!l*iid::J:oa:f:lJ.I:&iJ~SM-1 3 4
`9 6 t9:40)jifij~~7"7~~~.lj.lf¥~ ~ 'b~<·Z~ €ltL1to
`~~fl~-~~U~, Mfit, Ufi~, jj(Ji, 7'Jl~.::/7, fJifJ~bb*li'(leJ~~-
`. ~ltt<)~~..:,·t~o flmtt.t?'"71?:~, SM·- 1 3 4 9·6 4 Omg,· 1 2 OmgB~I¥
`--e.:cn.:ett. 1 o %.. 1 s %... 1 4 %l~i86b ~nt=.a D!i~l'i s M- 1 s 4 9 6 1
`&.
`2 Orng1i4B¥~fti!O)M•r.l:t""iflil1ilr\:N.>--:>t~'/JS, tilHfj1'&t.t7"7i!~~lj.WJ: tJ
`'.}1-IJ::/J'---::>f;::o flt1*7)-§mJtt~fj:SM- 1 3 4 9 6 4 Omg&O 1 2 OmgiSt-9-(cid:173)
`(4%.&tJt2 %)"r!7'7~~~J§..IJ( 1 0%) ~ ~ !Pf.ttf\--:>f=.o 7'JJY.::/7r.tSM-
`1 3 4 9 6 iSt4D"1:Q).;%J-3lJ.bb &it., 4 0 mg.& 01 2 0 mg~-9--\!'..C~tL 8 %.&
`~1 4%'1:~--::>t;::o SM- 1 3 4 9 6~.fi8¥QJfl"l!f•fi!O)~m••'1:1'7~~ji:lj:.
`
`-c~~~"?~o~m~m .. ~~~ ... ~~~~ .. ~~~~~~ .. ~-~~
`&tl,f.tiJ:.? f;::o
`
`( i i )J:.~mn~~~~Wbb~tt.t~lfdil~~i!J~~l'~6 •=~1-o
`
`•s
`
`~:l-Ife
`~Jt(%)
`--~~1§~!!001&00
`~Q)~jtf.
`
`7"7~~
`
`50
`4 (8)
`
`0 {0)
`
`40 mg
`
`60
`3 (6)
`
`1 {2)
`
`120 mg
`49
`2 (4)
`
`0 (0)
`
`5.
`
`10
`
`15
`
`Page 12 of 46
`
`SLAYBACK EXHIBIT 1005
`
`

`

`FROM AOYAMA&PARTNERS •
`
`10
`
`0 (0)
`
`1 (2)
`1 (2)
`0 (0)
`
`0 (O)
`
`1 (2)
`1 (2)
`
`M:Mt;ntlml
`4 {8)
`M*l'~~tlmi
`~ .. ~ 0 (0)
`;R6f~~t;tt.otto~, :1'71!~ .. SM-1 3 4 9 6 4 Omg .. 1 2 Omg~.l§.
`D~-=ttven4 fii, a~, 2f!Ji;::!f!fit.t~i!fl¥~:6~~iJ ~ttt.:t>~ ..
`'-''"ftL'bfhll
`JH: (1)f8JJ!ml~fii!Hl:~tl-ft:o
`
`< i i i > * t~.. atilfiliil~'litWn:m~ &tLtt.i'JtF.ffl ~"'f~ 7 •;::~To
`
`5
`
`*.7
`
`"7'7-e~
`
`60
`22 (44)
`
`0 (0)
`0 (0)
`0 (0)
`0 (0)
`0 (0)
`0 (0)
`0 (0)
`0 (0)
`
`1 (2)
`1 (2)
`
`1 (2)
`
`im:ft"lfc
`ll'.lfFJfJ~~&lllt (%)
`ttf~lfflJ
`fj:'f:,:f ~ (7.) t.;: e
`*"~*-
`~
`~*~-
`=f:~Jt)!j
`~IOOiE
`~lOOft-
`mA"ft
`~itt&vt~-1$8
`**~
`*tikM-iA
`mn't&'CJ!ll~
`..C?~Ci.
`~~!i\m!
`0 (0)
`J!tlll~-
`0 (0)
`M-Jl:~
`~ 1 (2)
`0 (0)
`~-~~
`.lfn.tg~
`Mf6t
`li."C ~
`~.ft,Ml*IS.li~~
`IQI~J¥Jii
`
`1 (2)
`
`0 (0)
`
`0 (0)
`
`40 mg
`
`50
`33 (66)
`
`120 mg
`49
`36 (71)
`
`1 (2)
`0 (0)
`0 (0)
`0 (0)
`1 (2)
`1 (2)
`0 (0)
`0 (0)
`
`1 (2)
`1 (2)
`
`0 (0)
`
`0 (0)
`1 (2)
`0 (0)
`1 (2)
`
`0 (0)
`
`0 (0)
`
`1 (2)
`
`1 (2)
`2 (4)
`1 (2)
`2 (4)
`
`0 (0)
`1 (2)
`1 (2)
`1 (2)
`
`0 (0)
`1 (2)
`
`0 (0)
`
`1 (2)
`0 (0)
`
`0 (0)
`0 (0)
`
`0 (0)
`1 (2)
`
`0 (0)
`
`Page 13 of 46
`
`SLAYBACK EXHIBIT 1005
`
`

`

`FROM AOYAMA&PARTNERS •
`
`~~~-
`(.'~
`
`Wi]~
`BmW
`"~
`~
`Dlll!f:
`iJ!&
`-rm
`*t!
`~11
`m-f~~a
`~
`r:tP'J~-
`~$
`IIIDM
`~~ ... &v&4m;m:.mm
`-~
`il~tiR
`~
`AJD!!
`:Mr&*ll$W
`
`..
`
`7;JJV'!J7
`fil!ID~ao *",
`(181~11£·~~<>
`ill~
`Jm
`trtf*M-lll~m.
`lili'
`7;bV~7jftlf!
`
`~;i'.r.:.-
`•al*i§
`~(l)M._
`jjQillJiii
`Bllol$~
`&1t.W§.*:&ifta'€i'~
`
`11
`
`0 (0)
`
`0 (0)
`
`0 (0)
`
`2 (4)
`0 (0)
`1 (2)
`3 (6)
`0 (0)
`Q (0)
`2 {4)
`0 (0)
`
`1 (2)
`1 {2)
`2 (4)
`
`3 (6)
`0 (0)
`
`1 {2)
`1 (2)
`
`3 (6)
`0 (0)
`
`0 (0)
`
`2 (4)
`3 (6)
`0 (0)
`0 (0)
`0 (0)
`0 (0)
`0 (0)
`1 (2)
`
`0 {0)
`
`0 (0)
`
`0 (0)
`
`0 (0)
`
`0 (0)
`
`4 (8}
`2 (4)
`2 (4)
`3 (6)
`0 (0)
`1 {2)
`3 (6)
`
`1 (2)
`0 (0)
`0 (0)
`0 (0)
`
`3 (6)
`1 (2)
`
`0 (0)
`1 (2)
`
`9 (18)
`4 (8)
`
`6 (10)
`
`4 (8)
`
`6 (12)
`1 (2)
`3 (6)
`1 (2)
`1 (2)
`0 (0)
`0 (0)
`
`0 {0)
`
`0 (0)
`
`1 (2)
`
`1 (2)
`1 (2)
`
`9 (18)
`3 (6)
`0 (0}
`0 (0)
`1 (2)
`0 (0)
`2 (4)
`0 (0)
`0 (0)
`
`0 (0)
`0 (0)
`
`l (2)
`
`0 (0)
`0 (0)
`2 (4)
`
`1 (14)
`7 (14)
`
`5 (10)
`
`5 (10)
`1 (2)
`3 (6)
`3 (6)
`0 (0)
`0 (0)
`1 (2)
`0 (0)
`1 (2)
`1 (2)
`
`Page 14 of 46
`
`SLAYBACK EXHIBIT 1005
`
`

`

`..
`
`FROM AOVAMA&PARTNERS
`
`•
`
`&liJ!nt
`
`"
`-~
`OOMiJJ!ill
`I!!Jiitfll
`"
`
`~Wi~
`Jfn.tp~rz 7 ~ '1-::..--JihP
`lfn.tfl~v7':f"~·m.A
`$~7"--ttJIJJu
`,r,,mm~Jt'M'
`f*mt!l>
`•mtailhP
`lff•tmbB41it
`'M&.Vi!M~
`~1*
`8JUR
`~
`~
`
`12
`
`1 (2)
`0 (0)
`0 (0)
`
`0. (O)
`0 (0)
`·o (o)
`
`0 (0)
`
`0 (0)
`
`1 (2)
`1 (2)
`0 (0)
`0 (0)
`
`1 (2)
`1 (2)
`
`0 (0)
`1 (2)
`
`5
`
`10
`
`2 (4)
`0 (0)
`1 (2)
`1 (2)
`0 (0)
`1 (2)
`
`1 (2)
`
`1 (2)
`
`0 (0)
`1 (2)
`1 (2)
`0 (0)
`
`0 (0)
`0 (0)
`
`1 (2) .
`
`0 (0)
`
`1 (2)
`1 (2)
`0 (0)
`0 (0)
`
`1 (2)
`0 (O)
`
`1(2)
`
`0 (0)
`
`0 (0)
`2 (4)
`0 (O)
`1 (2)
`
`0 (0)
`0 (0)
`
`1 (2)
`0 (0)
`
`-~-
`it7l:.7F~ttol:to~ .. ~!f$~0)?-t:,, SM-13 4 9 6~~l:<DI~U~tll~
`~1§~~~v'::Ef.t't>(J)(jiJfFffl}J~ .. ~ .. llfi~ .. 7;JJ~V7 .. i!!JtbM:~*v'
`((§)~J~Xit~~< ), ftllill, SJJrnti~6?-':)f~o SM-1 3 4 9 6 {St-'!J-JF"e~A r .:=.
`-Q)~!Jl$t.t~tr!>-=>fc ( 4 %*TI!l>o 1 2 ~t~~t. .. f!IM•~:Jav'-c~I¥.JI~ftilO)i?o
`~{~l'ilm~ E>tLf,ttJ:.-?t~o 18..t*~{ll1)SJ\1it~lb~~ L-t.:.~#<D~J-&-~~4HI¥00-e
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`Page 15 of 46
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`

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`FROM AOYAMA&PARTNERS
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`13
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`methyl]-l-cyclohexylmethyl]-2,3-bicyclo[2.2.1]heptanedicarboximide ~t~
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`
`Page 16 of 46
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`

`

`FROM AOVAMA&PARTNERS
`
`•
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`•
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`2002$ 8ft22B<*> 9:12/VB 8"54~·~5S00S68777 p 18
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`~ff.:~tl,.Q (lR, 2S, 3R, 4S)-N-[ (lR, 2R)-2-(4-(l, 2-benziso1:hiazol-3-yl)-l(cid:173)
`
`piperazinylmethyl]-l-cyclohexylmethyl]-2,3-bicyclo[2.2. l]heptane(cid:173)
`
`dicarboximide *t::l':l:.:t'O)~~l:f-f~c;no:lji~ 1 a~4- 5 m g-1 20m g
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`yl)-l-piperazinylmethyl)-l-cyclob~xylmethyl]-2,3-bicyclo[2.2. l]heptane(cid:173)
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`dicarboximide hydrochloride -e~omYJitlJllJ;:ie.Q)fttti~o
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`3 • flt*:R:fiJl41£0)~~~~Q{(lf"toR'Jitli£ 1 *f::J':l; 2 ·~j'Clfit(f)J'hJlt.::JJ~o
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`5. fiS~it~~O,){lR,2S,3R,4S)-N-({1R,2R}-2-[4-(l,Z-benzisothiazol-3-yl)­
`l-piperazinylmethyl]-1-cyclobexylmethyl)-2,3-bicyclo[2.2.1]heptane(cid:173)
`dicarboximide hydrochloride~ l 13 &4-Bt 2 0 m g- 8 0 m g -e 1 13 liHJ~lj.
`"t" Q !mlltlJl 1 * tdj: 2 1~\ia-Q)f~::li'~
`6. rc~~JJEO)~~~~at~-t Q •*Jji 5 f~iajfl(f.):jj'~o
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`[(lR,2R}-2-[4-(1,2-benzisothiazol-3-yl)-l-piperazinylmethyl]-1-cyclo(cid:173)
`
`hexylmethyl]-2,3-bicyclo[2.2. l)heptanedicarboximide hydrochloride ~1 13
`~4it s mg-.. a om g-,:; 1 a 1 !e1~4T ."!>;:: ~ l=: J:-=> -c, t!f*M-H:3~1JfFJ¥1QJ
`~~I*;.:: l:. t.l <, lte~~!WIJE~afrYiT.OIDl*lll ~ t:.rt. 2 l~JiB$lt0)$1Jt~ ..
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`20
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`25
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`Page 17 of 46
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`

`

`FROM AOYAMA&PARTNERS •
`
`15
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`5
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`9. rtif~~fiE(1)~¥.EliEtftt:ilfc~'"J"" Q ft~ 8 lO:iatt(f.)fft./Jtha
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`yl)-l-piperazinylmethyl)-l-cyclobexylmethyl]-~,3-bicyclo(2.2. l]heptane(cid:173)
`dicarboximide hydrochloride -a: 1 a &-9-:lt t 0 m g ~ 4 0 m g ~ 1 a 1 @Mt-9-
`T o II*Jl 8 l;: fOit(T.)faUt1.7tho
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`3-yl)-l-piperazinylmethyl)-l-cyclohexylmethyl]-2,3-bicyclo[2.2.1](cid:173)
`heptanedicarboximide '3: t.:.f'i.:t."'(T.)(ii~.l:'ff~ ~tL.Qtiit: 1 a 1 fi!J~4:St~ L, -c
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`16
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`Page 18 of 46
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`FROM AOYAM~QPARTNERS
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`•
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`•
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`2002U 8A22B(*) 9.14/Vm 8 64/~~5300368777 P 20
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`methyl)-1-cyclohexylmethyl]-2.3-bicY.clo[2.2~l]heptanedicarboximide ~f;:
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`Page 19 of 46
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`

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`FROM AOYAMA&PARTNERS •
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`...
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`1/1
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`
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`
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`
`Page 20 of 46
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`

`

`•
`
`•
`
`United States Patent & Trademark Office
`Office of Initial Patent Examination
`
`·.
`
`'
`
`...
`
`.
`
`.
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`. ,
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`0
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`Application papers not suitable for publication
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`SN<604D492j
`· MaiiDate Oo·-22- cQ_
`~ N~n-English Specification
`_ 0
`Specification contains drawing(s) on page(s)
`. or table(s) _ _ _ _ _
`0 Claims D Abstract
`0
`Landscape orientation of text 0 Specification
`0 Abstract
`0 Handwritten
`0 Speeification
`· 0 Claims
`0 More than one colunm 0 Specification
`0 Claims
`0 Abstract
`0 Claims
`0
`Improper line spacing
`. 0 Specification
`0 Abstract
`0 Claims not on separate page(s)
`0 Abstract not on separate page(s)
`0
`Improper paper size-- Must be either A4 (21 em x 29.7 em) or 8-112"x 11"
`0 Specification page(s)
`D Abstract
`0 Drawing page(s)
`0 Claim(s)
`Improper margins
`0 Specification page(s) ____ _
`0 Drawing page(s) __ __ _ _
`0 Not reproducible
`Reason
`0 Paper too thin
`0 Glossy pages
`0 Non-white background
`0 Drawing objection(s)·
`0 Missing lead lines, drawing(s) ______ _
`
`0 Abstract
`0 Claim(s}
`
`Section
`0 Specification page(s). __ __ _
`0- Drawing page(s) _____ _
`
`0 Abstract
`D Claim{s)
`
`0 Line quality is too light. d_rawing(s) ____ __ _
`0 More than I drawing and not numbered c~rrectly
`0 Non-English text. drawing(s) _ __ __ _
`0 Excessive text, drawing(s) _____ _
`
`0 Photographs capable of.illustration, drawing(s) __ __ __ _
`
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`This Page is Inserted by IFW Indexing and Scanning
`Operations and is not part of the Official Record
`
`BEST AVAILABLE IMAGES
`
`Defective images within this document are accurate representations of the original
`-documents submitted by the applicant.
`
`Defects in the images include but are not limited to the items checked:
`
`0 BLACK BORDERS
`
`0 IMAGE CUT OFF AT TOP, BOTTOM OR SIDES
`
`0 FADED TEXT OR DRAWING
`
`0 BLURRED OR ILLEGIBLE TEXT OR DRAWING
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`0 SKEWED/SLANTED IMAGES
`
`0 COLOR OR BLACK AND WHITE PHOTOGRAPHS
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`0 GRAY SCALE DOCUMENTS
`
`~LINES OR MARKS ON ORIGINAL DOCUMENT
`
`0 REFERENCE(S) OR EXHIBIT(S) SUBMITTED ARE POOR QUALITY
`D OTHER: -------------------------------------------
`IMAGES ARE BEST AVAILABLE COPY.
`As rescanning these documents will not correct the image
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`Page 22 of 46
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`•
`
`*BIBDATASHEET*
`Bib Data Sheet
`
`SERIAL NUMBER
`10/525,021
`
`FILING OR 371(c)
`DATE
`02/1812005
`RULE
`
`•
`
`Page 1 of 1
`
`UI\ITED STATES DEPARTME.'IIT OF COMMERCE
`Unitoo l'lwt"" Puto<nt und 'l'rud01mur" om.,.,
`Addn:to: COMMISSIO>JER FOR PATENTS
`P.O. llo• 1•50
`Al<JUIII<hil1. Vugi:W. Z23U· WO
`ww"·WIVbJ.g\IY
`
`CONFIRMATION NO. 3141
`
`CLASS
`514
`
`GROUP ART UNIT
`1615
`
`ATTORNEY
`DOCKET NO.
`0020-5041 PUS2
`
`~PPLICANTS
`
`. Mitsutaka Nakamura, Osaka, JAPAN;
`
`Masaaki Ogasa, Osaka-shi, JAPAN;
`Shunsuke Sami, Osaka-shi, JAPAN;
`
`**CONTINUING DATA **"******u"*******"'***u
`This application is a 371 of PCT/JP03/1 0490 0812012003
`which claims benefit of 60/404,927 0812212002
`
`** FOREIGN APPLICATIONS ***************"'****
`
`I:J yes I:J no
`Foreign Priority claimed
`ps USC 119 (a-d) conditions I:J yes I:J no I:J Met after
`met
`Allowance
`Verified and
`AcknowledQed
`ADDRESS
`02292
`
`Examiner's Si!Jnature
`
`Initials
`
`STATE OR
`COUNTRY
`JAPAN
`
`SHEETS
`DRAWING
`
`TOTAL
`CLAIMS
`19
`
`INDEPENDENT
`CLAIMS
`3
`
`TITLE
`
`Remedy for integration dysfunction syndrome
`
`FILING FEE FEES: Authority has been given in Paper
`to charge/credit DEPOSIT ACCOUNT
`RECEIVED No.
`for following:
`No.
`1860
`
`ll:l All Fees
`
`ll:l1.16 Fees (Filing)
`
`l:l 1.17 Fees ( Processing Ext. of
`time)
`
`ll:l1.18 Fees (Issue)
`
`ll:l Other
`
`ll:l Credit
`
`I
`I
`
`I
`I
`I
`
`Page 23 of 46
`
`SLAYBACK EXHIBIT 1005
`
`

`

`MULTIPLE
`CLAIM
`FEE CALCULATION SHEET
`(FOR USE WITH FORM PT0-875)
`
`AS FILED
`
`AFTER
`I~ AMENDMENT
`
`AFrER
`z ..
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`~ERIALI"O.
`
`A A"'L A .,- ,.. .,- n ")) 4
`
`·--· _ L:JU L.. .L
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`CLAIM s
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`!FILING DATE
`
`IND. DEP.
`I
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`TOTAL •''1__(7
`ClAIMS
`'-"""
`rJO -l.l60_ (REV. 1110•)
`
`IND. DEP.
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`IND. DEP.
`
`-
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`.
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`.....
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`c
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`!TOTAl INn
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`TOTAL
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`
`AS FILED
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`_!ND. DEP.
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`AFTER
`AFrER
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`! .. AMENDMENT
`IND. DEP. _!_ND. DEP.
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`...
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`US "'MOTh'<~·='""'~,, 'P>t ~
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`P.ac~nc and Tnd~n,•ri. Ofrt<~
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`Page 24 of 46
`
`SLAYBACK EXHIBIT 1005
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`

`

`r. )
`
`•
`
`10/525021
`•
`D Rec'! PCT!PTO 1 8 FEB 2005
`
`IN THE UNITED STATES PATENT AND TRADEMARK OFFICE
`
`In re application of:
`
`Mitsutaka NAKAMURA et al.
`
`Serial No. 60/404,927
`
`Filed: August 22, 2002
`
`Docket No. 0020-5041P
`
`Attn: BOX MISSING PARTS
`
`AGE