throbber
esp@cenet document view
`
`Page I of I
`
`REMEDIAL AGENT FOR FATTY LIVER
`
`Publication number: JP2002220345
`2002-08-09
`Publication date:
`NOGUCHI TAKESHI; HIROTA KOTARO; TANAKA
`MASASHI
`SUMITOMO PHARMA
`
`Inventor:
`
`Applicant:
`Classification:
`- international:
`
`A61K45/00; A61K31/192; A61K31/216; A61K311437;
`A61K3114468; A61K311496; A61K311513; A61K45/06;
`A61P1116; A61P3/06; A61K45/00; A61K31/185;
`A61K31/21; A61K31/4353; A61K31/4468; A61K31/496;
`A61K31/513; A61P1/00; A61P3/00; {IPC1-7):
`A61K45/00; A61K31/192; A61K31/216; A61K31/437;
`A61K31/4468; A61K31/496; A61K31/513; A61K45/06;
`A61P1/16; A61P3/06
`
`- European:
`Application number: JP20010015602 20010124
`Priority number(s): JP20010015602 20010124
`
`Report a data error here
`
`Abstract of JP2002220345
`PROBLEM TO BE SOLVED: To provide a medicine for preventing and/or treating fatty liver that can
`prevent or cure fat accumulation in liver, decrease blood lipid, and can be used for a patient to whom a
`MTP inhibitor is administered, and also to provide a medicine for treating hyperlipidemia. SOLUTION:
`This invention relates to a medicine for preventing and/or treating fatty liver containing a PPAR&alpha
`activator as an active ingredient for a patient to whom a MTP inhibitor is administered, and also a
`medicine for treating hyperlipidemia containing a MTP inhibitor and PPAR&alpha activator as its active
`ingredients.
`
`Data supplied from the esp@cenet database - Worldwide
`
`http://v3.espacenet.com/textdoc?DB=EPODOC&IDX =JP200222034S&F=O
`
`I 0/12/2007
`
`
`1 of 11
`
`PENN EX. 2170
`CFAD V. UPENN
`IPR2015-01836
`
`

`
`(12) ~ lffl ~ff~. (A)
`
`(11)4ftfWli~BB3~
`4f ml2002-220345
`( P2002-220345A)
`(43)~11f B lfll111~8 /J 9 B (2002.8. 9)
`
`FI
`A 6 1 K 45/00
`31/192
`31/216
`31/437
`31/4468
`ftM~ *lit~ fflJiO)lt9 OL <~ 10 JO
`
`4 C 0 8 4
`4 c 0 8 6
`4 c 2 0 6
`
`fiUUH=R<
`
`(Sl)lntQ.1
`A6 1 K 45/00
`31/192
`31/216
`31/437
`31/4468
`
`(2l)tH8*~
`
`Molli2001- I5602( P'lOOl -15602)
`
`(22)ffillB
`
`lfll11134F 1 JJ 24 B (2001. 1. 24)
`
`(72)§!1Jnf
`
`(71)tH~ 000183370
`ttA . . Jt;Mj:
`*fiJtfXlifff~!J&l!G-2T~2&8~
`!1110 •
`*Em~g#BW~3-1-~ ~
`~~
`(72)J!tmf ftm ~XS
`*E*~gwaw~a-1-~ ~
`JUk~~
`(74)~ 100095832
`:11'111!± am :nm
`
`(54) C§!IJ!O)fi#l Ba&ft;;M
`
`(57) (~f.Jl
`r ~m 1 lJf IH:t.> it¢ JFaJVfiHft a-.:rlffj t t., < tl:mti-t ¢
`.: ):; 1iT:~, tP"?Jfni:pJFaf(a-fll;r~-t!-¢.:):; 1;\'(·~ ti,
`MT P 1i11.ff1'1>fj!; lj-:lttti:JJJ \.' t:>tl.¢ , !FalJ1ilJf'1>.:Y..lffjt.>
`J: tf / i t.:tl:iati1fll ; ~ t:> if i:~JFalfnnE a-ia1.!-t Q .: t
`ti~-c·t: Q. ~JFa.1mJ.1E~1a-m~-t¢.: t.
`rw-¥fil MT Plill.W1f!J'1)~lj-,m,=m:m\. ,t:>tl.¢, P
`PAR a Ritt1t1f!J a-Unt:fr):; l, "(*fl" t., "( ~ ¢ , JFaJVj
`)Jf0:>.:Y,.lffjt:; J: tf / i t.:,.;J:ifl1.!1f!J ; ~ f::,tf~:M T Plill. 91
`t P P A R a Rif:Ht1fll t a-:ff!QJnt:fr t l, "( *1r l, "( ~ Q
`~!Fa.lfnnEiati1fll.
`
`
`2 of 11
`
`PENN EX. 2170
`CFAD V. UPENN
`IPR2015-01836
`
`

`
`
`3 of 11
`
`PENN EX. 2170
`CFAD V. UPENN
`IPR2015-01836
`
`

`
`! ( 3) 0 0 2- 2 2 0 3 4 5 ( p 2 0 0 2-tfitii
`
`7-~ (Ciprofibrate)t?J:V'7/717
`D0v(Gemf ibrozi l)~~~QfiJ:9~~
`nt.:1t~-c·1>Q, iN~c c 1 J t l < 'j: c 2 J ~el\\O)f'
`llJii:lJ:V'/it.:U~L ( 4 J PP ARaffi111~J
`ii, 1 1J .J7177-t-"'C'l>Q, file c 1 J --- c 3 J ~'
`JIJ
`i'tliP,:liel\\O)f'llJit:>J:U/it.:'j:~1ftL ( 5 J
`JlblffiJ\ , MT Pm HJO)if JfF mt L- -c:i~ ~ n. Q m Jlblff
`-c· 1> Q , file c 1 J ---- c 4 J ~ ,i'tliJ,,:~Cl\\O)f'IIJi t:> J:
`tf/it.:Uibit1ftL (6J MTPllll.W1f!JtPPARa
`ffitt1t1f!Jt ~Unt;tt l-C%1fl -c~Qf.tiJIJilllnE~·
`1f!L ( 7 J MT P llll. HJfJ\, B M S - 2 0 1 0 3 8 ,
`BAY13-9952, CP-10447, R 103
`7 5 7 t:>J:UWM-1 1 5 9 iJ>~~QllfJ: 9~tR~tt.t.:
`1t~-c·1> Q, iiii~e c 6 J ~el\\O)~JIJJttln[~L
`( 8 J P PA R a ffitt1~JiJ!, 7 ~ .J 7 1 7 7- ~ ,
`WY-14643,~f7177-~, ?D7177-
`~, ?IJ.J7177-~, 8(S)-HETE,~/D
`7 1 77- ~i:IJ:tf7)7 1 7DY)viJ>~~QllfJ: t)~
`'!nt.:1t~®J-c·1>Q. file c 6 J t l< 'j: c 7 J ~el\\O)
`~D'fiJttln[~1ftL ~~u': ( 9 J pp ARaffi1H~J
`iJ>, 1 1J.J7177-~-c-1>Q, fileCGJ----caJ~'
`i'tliJ,,:~el\\O)raiJIJtt~1ftJ, t:OO-t Q •
`[0007]
`[~llJJO)~DmO)m~l *~llJJ:lj~li. lh®Jt?J:U A':t?
`~ '"'C, JttllfiJIJJi~fltT~-ttQfi, Jff~O)Dli.IJ1iiffil~:i
`~T Q.: t iJ~tiE~H'O~tt.-C i.. \Q MT Pllll.ffJ-C·;bQ :'ft"
`VIJ/~~f*t, 7177-~*?.i1f!Jt~~~-tQ.:t
`t:J: 9, f'~H: t, Jlffil!t:t?it QJIJ.IJ1iiffil~1flli61J l,
`iJ>-:>.ItllifiJIJfl~fltT~itQ.: b';'"'C'~ Qt.,.,?~< K..~
`i=OJit:~-:J <.
`[ 0 0 0 8 l T~b1?, *~BJIO)DliJlbJffO)T-IIJit?J:U/
`it.:'j:~1ftJ(JIJ.IJ1iJJf~tt!f1ftJ) Ii, ~ 1 D'/-A ~ lJ ?'
`1)~71 F~J.!::$1/1'\?fl (MTP (micros om
`altriglyceride transfer p
`
`r o t e i n ) ) llll.W1f!JO)f~..!H!~:lj':ffl~' ~h. P PA
`Ra(Peroxisome proliferato
`r-activated receptor a)ffitt
`1t1f!H:: ~1f~nt1t t l l" %1fT Q.: t t: 1 -:>O)j;:~ ~~
`t'jiJ>;bQ 0 :;$:~BJIO)f'IIJ.ji:)J:lj'/£t.:lj:~1f!Jlj:, file
`Unt1t~fl"T Q t.:ll>, MT P llll.W1f!Jf~~.[l:lji:t?~ 'l"
`i'JfFJfl t l l" ~T Q JffJJit:t?lt Q JIJJJbD < JIJJJb~
`nE ) ~ 1!P$1J l , iJ>-:> Jttl ifiJIJfl~ flt T ~ 1t Q .: t fJ\-c· ~ Q
`t ... ) ? iftlt.:tttt~~JJl l? Q.
`[ o o o 9 l JIJ.111ilfft ,i, JffBl*H:JIJJi, ±.i:, ~ U ?'
`l)~LJ F (j,j"'f, TGc~Q%;/J{;bQ) ~cO)ifi
`'fimlJjjiJ~tiH:O lt.::ttt;J, T~:b1?, Jff*HJJmO)'i'I
`~:'lH:JIJJJjj~JmiJ>~~tLQ:tt~~~'?. JIJJJjjlff
`Ii, JJfJlit:t? It Q ~ l) ?' lJ ~ IJ F ~.1£&.tf V L D L (@
`fltWJ.l 1J*:5'/J'\?fl) ~nt. 1tiM.>l-\i'tlfJ>O)~"'(·
`llfWiJ1!:Ett.:~i:u-tQc~i.. ~n.-ci..,Q.
`[ 0 0 1 0] MTPfillOc l l"ti, BMS 2 0 103
`8, BMS212122, BMS197636, BMS
`200150, BMS19295L GR32871
`3,CP-10447,WN-1159, BAY-13
`-9952, R-103757, JTT-722, ;bQ
`1,.\lj:OO~~lmM2 0 0 0 - 0 5 2 0 1 {j-J'\/7 v "I ~t:
`~Cl\\O)N-~/'f~?D7~ F~~f*- OO~~lmM99
`-31os5{j-H/7v·y H:~clt0)3-t"""lJY1v-
`4-~:'fY:'ft-V1J/~~1*- 00~~imm9a-541
`3 5{j-/'\/7v·y ~t:~Cl\\O)Ap o B;ti!f.llll.HL ~Im
`.!f-11- 3 5 5 5 5~1'.'11H:~Cl\\0)7 ~ .J .X1-JvUI.i
`#:7 ~ /~ ciJ'*tf ~h, ~f*£J{Jt:lj:, BM S - 2 0 1
`038, BAY13-9952, CP-10447,R
`103757, WM-1159, JTT-722, G
`R- 3 2 8 7 1 3~ciJ>*ff ~tt.Q. ~ip"'(·{,, fFJfl~
`~O)il&J> ~, Tlie~ < 1 > --- < 5 >
`[0011]
`[-ftl l
`
`r3
`
`NH
`
`0
`
`(1)
`
`{0012]
`
`[1t2 l
`
`(BMS-201038)
`
`
`4 of 11
`
`PENN EX. 2170
`CFAD V. UPENN
`IPR2015-01836
`
`

`
`
`5 of 11
`
`PENN EX. 2170
`CFAD V. UPENN
`IPR2015-01836
`
`

`
`
`6 of 11
`
`PENN EX. 2170
`CFAD V. UPENN
`IPR2015-01836
`
`

`
`
`7 of 11
`
`PENN EX. 2170
`CFAD V. UPENN
`IPR2015-01836
`
`

`
`! ( 7 ) 0 0 2 - 2 2 0 3 4 5 ( p 2 0 0 2 -035l•J)(lj
`
`< 1 9 7 9 > t~m!T .Q.: c fJ\-c·~ '.>.
`[0045]
`[~1iif91.ll J..J.""f. *~aJia-~:&&f§l.lt;:J: 1)§1,fllt~t;:~aJI-t
`.QfJ). *~aJitl:iJ)iJ).Q~f§l.lt;:J: IJfiiJ f:>IDUi:'.~h..Q tCT>
`-c·Cj:~\. '·
`[0046]~1iif§l.ll MTPmttfill.WWffl$J:UPP
`AR a mtt1tWJflCT>fl!{Dfi
`( 1) MTPmttl!.lii!ff1=JflCT>fi!filli
`MT Pmttl!.llWWJflt;:~-? < V L D L7tif:f!PftilJWJfl a-,
`Triton~~~ t- •J?'IJ-t•J ~.11IIJ.fE::C-TJv7·y l-!(cid:173)
`JflW(~filli lt.:. IN~C!::C-f Jv7 .,, H;:ll! Ve ( 1' ~/]
`?(Ishikawa)h, J. Lipid Res.
`20. 254-264, ( 1979)) t~m!lt.:. A
`fllt~t;:U, J..J.T CT>iM IJ-C''i> .Q.
`[0047lmtt, 5W~CT>Spraque-Dawl
`ey*77l-(CrJ:CD(SD). B*~~-~.A
`IJJ'\-1UU t 1 WFs:FfbifiiJ"ff lt.:. fiiJOmlifl. file!
`7 .,, H;:. C E - 2 l~Hg~fl ( B *? J./Ttf:r!) ~ eHb
`Hfjt~1tt.:.
`[ 0 0 4 8] "?\. \"(', 7bifiiJfffitCT>7 "I H;:"?W(, 1
`8~rn!J..::ll:Jf!jt~1t, "?\. Y'(\ ~1tfi~ c l "(MT P
`l!.liW1ilJ(BMS-201038, BAY13-995
`2,CP-10447,R 103757~J:UWM-
`1 1 5 9 ) a-t!Df9;1j-'t .Q. f9:1j-JM~ ( Wlli.Cf 1 ~ml
`•>~-*77l-~Triton WR-1339(~
`/J71'7.A?tf:~)300mg/kg!-~ff~~ttlj­
`l, ff~~t:llli\i!jff~fiJ: IJ f*Jfn.T .Q. ~$, *'!!'!« c l
`"C, ct? 1v1i!Ml a-ttlj-'t .Q.
`[ 0 0 4 9] .fCT>fl, f*Jfn.~h.t.:Jfn.?llt;:"?\.)"(. :11.C.v;f
`Ml, Ifn.ffl a-7tll!t't .Q. ~~ f:>h.t.:Ifn.fflt;:"?\. '"C, 00151::~
`.,, l- (ifliifb~: l- 1) ?' 1J-t71' ~ E-f" .Al-' f{]~
`!i <~>ti:~) a-Jfl\.\"(Ifn.ffll- 1J?' 1J-t~ ~fiia-00151::-t
`.Q.
`[ 0 0 5 0 ] -fCl)fili~. :M!mt;:.ftl'("(. fl!l19!1t~f9:1j­
`~';:$'t .Qifn.ffl l- I}?' I} -t I} ~fjiiJ-tm;-r l "C \. \.Q.: ct;:
`J: I), ~~fl!lf;t1tti~iJ~, MT Pmttl!.llWft:Jflt;:~-? < V
`LD L7tiMPftilJWJfl!-:ffT o.: c fJ{biJ).Q.
`[ 0 0 5 1] ( 2) p PARamtt1tWJflCl)~fillj
`cos- Ullll!t _ 2411 .:i:.1v7"v- H: 1. 2 5 x 1
`0 4 jJlll!/5 O o J.J. 1 /17 .:i:.Jv ( =---3 x 1 0° jJlll!/
`7"v- l- > "C11~. ~B •J ;}'f7 .:i:? ~ 3 ;r?t;;t;:J: IJ)lfi1
`-T~JdJ.:. Jlt1~-T~J-ii. Trans IT OftHiHt
`ii> -LT 1 ( PANVERA) !-Jfl\.', ~Cl)~#
`Cl)/O r ::1-Jvt;:f)E"'.>t.:. lff!t!!c l "C' ~.Ifnfff R p MI
`
`1 6 4 ot.g!fl!t Jfl\. 't.:.
`[0052l~filli*CT>lllfi1-=f~A~fll¥07"7.A~~~
`1Ja:~:U, 1 17 .:i:.Jv'i>t.: I) GAL 4 - Lu c ( 7•7 A~ ~
`p G L 3- bas i c Eil*; ;t;~ JvJv~7 .:i: 7--lt, :1
`/'-t >'--it AG AL 4 filitinc~IL 17--tt:¥ .B ?'o c/'/O::C
`-~-t:ffi"o; o. 05J,.Lg)' hPPARaLBD
`/pM(tl-PPARaLBD. GAL4filiti-M~!-:ff
`i" o ; 0 . 0 0 5 J.J. g ) , p R L - C MW ( 0 . 0 0 2
`5J.J.g), pBluescript (0. 4425J.J.
`g) t lt.:.
`( 0 0 5 3] lll1ii~~Jl4!R¥rnlfitt;:jJlllJ.!-8titl.
`5~%m~~17~Jfn.ffl-10-8M 1'/'.AIJ/'
`~:ffDMEM ( 7.:i:..1-Jvv·y }'~[.,) t:~~lt.:. ~
`f:>t;:, ft1t~: ? I}./ 7 .-f 77- l-, WY- 1 4 6
`43(Caymantf:~).~~7.-f77-l-(SIG
`MAtf:if!),7.:i:./7.-f/'7-l-(SIGMAti:~,/]
`1vif-/'Ht;:7tMf~Jfl) t l< li?o7 .-f 77-l-
`(ALDR I CHtf:if!) ~?WMlt.:DMSO?i?ll£t.:Ci
`8(S)-HETE(Caymantf:if!)!-?1JMl~I
`~ .1-1v?W?llt*8ll!';:w.:1Jnl, 2 41R¥mlttfi!ta-tr~"'.>
`
`C 0 0 5 4 ] J..J.r, D u a 1 - L u c i f e r a s e
`Reporter Assay System(7"0~
`ljtf:~) Cl)~if!7"0 l- :1-Jvt:t'l\.\, 1 0 0 J.J. I o:>*8JJI?l
`~-c-~J1lt.:flt:1v~7 .:i: 7--ttmttt$.15i:'.lt.:.
`*~ 1v1v~7 .:i: 7--ttmtt/17 E: ~1' ~7 JvY7 .:i: 7
`--ttmtt t •m l, ~itt1t~*~li'.jJllJ1?1Cl)@J;::MT Q
`ffl*t•lli lt.: 0
`[ 0 0 5 5] p PARamtt1tWJflfl!filljCl)lfj}1tlf!filc l
`. "(, fl/.lCl)7-{/'7-l-*1t~Cl)fl!!, 1::flltl*J9ff>'l'
`Cl)-"? c ~ i. f:> h. "( \. > .Q Jrnf(-C· 'i> .Q 8 ( S ) - H E TE
`!- ffl\. >"(. PP AR a mtt1tWJflCT>~filli*Cl)~~1!-rr~
`"'.>t.:. ~i:>. 1t~CT>P PARamtt1tWJflli, ~
`m!c l, "( Jfl\. )f.:WY- 14 6 4 3 Cl)3 0 }..L M~~~Jv
`~7.:i:7--ttm1tl:.~~a-1oocl.~tti~m~
`CT>m1ti:~7ta-lfdtHtlt.:. ? 9 ./7 .-f 77-l-. WY
`-14643(Caymantf:~).~~7{/'7-l-
`(SIGMAtf:~). 7.:i:./7.-f77-~(SIGM
`A, tJ1vif->'M~t;:7tMf&flffl> $J:rf?o7 -{ 77-
`l- (ALDRICH) Cl)p PARamtt1tWmt:"?\.•
`-C, 1"1UH:lkf§1tlt.:~~t~ 1 i:>J:U~2 t;:~
`T.
`[0056]
`[~1]
`
`
`8 of 11
`
`PENN EX. 2170
`CFAD V. UPENN
`IPR2015-01836
`
`

`
`! ( 8) 0 0 2- 2 2 0 3 4 5 ( P 2 0 0 2-9v4 5
`
`lO)IM
`
`30)1M
`
`WY-14643
`11•1m11-•
`'JD7.t1'H
`.... ·1·141;-•
`7J.JU1;-•
`
`21
`0
`3
`9
`32
`
`100
`1
`16
`31
`161
`
`100)1M
`
`-
`
`20
`S3
`70
`ND
`
`[0057]
`[~2 l
`
`£:"(. 1 i!M~f.ftif Ct.:. ~ f:>tLt.: 7 'Y ... a-JEJFe.I1o. 7 'Y ...
`1=-T1vc c 'tffl~'t.:.
`[0063]BMS-201038$J:YBAY13-
`9 9 5 2 ct£:. ?.i~~f!lli1=-T1v't·0?.i~~JJlffllit0:> i
`Offlffliit1J)f:>~5£Ct.:. ?3Btl:, O. 5ll%;i<1-1v-e
`JvO-.Ac L. 5 m I /k g"(~lj-Ct.:.
`[ 0 0 6 4] M~ffiliJ1o.7 'Y J-1::-T'Jva-, ~fi4~"(·J1o.
`?Wt- IJ ?' 1J-e IJ ~t:J\7'/~0:>~~ 'J:? t:lf;Ht C. t~
`-9-~ifiltfifl;IJ{-tt .Q ~#-r't·. B M S - 2 0 1 0 3 8 i
`t.:li BAY 1 3 - 9 9 5 2 a- 1 8 1 @I. EIJlWJ ( 8 : 0 0
`----2 O : O O) f~*':~:BIJffDt9:-9-Ct.:. t9:-9-fmtti~4
`B El. 7 8 EIO:>EIJlMOtr*t:lll~IJUJ: t)f*J1o.L,. J1o.?1f
`1~7 ;i<-:$'-a-00~ L,t.:. it.:. MB 7 8 E1t:JJfllia(cid:173)
`Mlf1L,. JFe1ta-tlblli l, 'tJJflliq:iJFe1fa-il{IJ5£L,t.:.
`C o o 6 5 l R.I1D. 7 .. , 1' =t::-T 1v't'0.I1D.?1fJFe!Jtf.!.tT t'Fffl
`c JJf JFelJ1jfifl .!:: O)llJ~ a-~ 3 $ J: y~ 4 i:~-t. ~ f:>
`£: • .A?a-.AAM7'Y1'1::fJv"(•0)7 -177- J-*?.i
`1f!J .!:: O:>Htffl~~t:--::> ~ ''t , lillt~H:~ 5 t:; J: rf ~ 6 t:~
`-t. ~3$J:Y~5£:1i, fi4it0:>.I1o.li!Jt- 1J?'1J-e71 ~
`@:$J:U:i v .A-Ta-1Viit. Xmttft:X-t l>t!P:BIJ$c
`a-, ~4$J:rf~6t:t:l:tf4if'7)1ff}- 1J:7" 1J-e71 ~~·
`$ J: Y:i v .A -ra-1v~.it c. Xmttft:x-9 .Q .fO:>ffl$
`c a-~-t. ;>j:-$. ~q:i, r ct? 1v~J I±, .ftL-f:'tL
`ct :7 1vllt~!k't19:-9-L,t.:=cf1va-~ c, n'n'l> :c-r1va(cid:173)
`Xmtfic Ct.:. it.: r TGJPffi!J$ J l.;t_
`... lJ ?'I) -e 1) ~
`JPmrJ$a-~c, rTcJP1&1J$J 1;;1:, :iv.A-Y-a-1vJPllil.I
`$a-~-t.
`[0066]
`[~3 l
`
`[ 0 0 5 8] ~ 1 j:;J:rf~ 2 O)l'Jj~;l))f:>. ;1)>1J>l> ~fiffi*
`t: J: t) P P A R a ffitt1t t'F ffl a- ~f!Hi"(• ~ l> .: .!:: ;I){ .b fp
`l>.
`[0059]~~f§IJ2
`!fttt. 5l!J!f*O:>S pr a q u e -Daw I e y*7 "' }(cid:173)
`(Cr j : CD (SD) • B*+~-Jv.A iJ1\-:ff:M)
`a-~2l!J~~.A?a-.A~(HIGH SUCROSE
`AIN-76A DIET. PURINA MILL
`
`s . I N c . ( 8 * s L c JN t) VH)) J El mm~~#-t:
`
`'tMAMC~.~f:>h~77t-a-~.A?a-.AAM77
`t-1=-TJvc vcm~'t.:.
`[ 0 0 6 0 l .A? a-.AAM7'Y1'1=-T1va-. ~If 6~
`'t'J1o.?W t- IJ ?' 1J-e 1J ~iU:J\7'/~0:>~~ 'J:? t:lf;Ht
`Ct.:. BM S - 2 0 1 0 3 8 , BAY 1 3 - 9 9 5 2 i
`t.:U?IJ/7-17v-t-a-, ~5$J:Y~6£:~~h.Q
`f~-9-iit"'C 1 8 1 @IEIJJWJ ( 8 : 0 0----2 0 : 0 0) fi*t:
`~161JffDt9:-9-Ct.:. ;>j:-$, ?3~1.;L O. 5ltiit%.X1-Jv
`-e1va-.Ac C, 5m I /k g.!::;>j:-.QJ: ?£:~-9-Ct.:.
`[ O 0 6 1 l t~-9-m!Wi4 8 El, 7 8 EIO:>EIJlMM*t:lll
`~Wf.IJKfiJ: tJ f*J1o. C, J1o.?WJ~7 .X-:$'-a-005£ Ct.:. i
`t.:. ft~B 7 8 El t:JJfllia-Mm C, JFe1ta-tlbtl1C 't JJflli
`q:.Dli1t a-oo~ Ct.:.
`[ 0 0 6 2] -jJ_ Mttt, 6)!;ilfifJO)S pr a q u e -D
`awley*77}-(Crj :CD(SD).8*+~
`-1v .A •J} \-:ff:~ J a-iim~ < c E - 2 > El ram~~
`iEBIJfD...,':lt-t-'f 1a..1:~1t.QDtHE"'FftiM<DDfllfi {7a)
`
`~ft,-
`BAY13-99S2
`30mg/q
`100mo/br
`3mglq
`lOmglq
`
`BMS-201Q38
`
`n
`
`4
`4
`4
`3
`4
`
`Jfu.l'itr!J::riJ!1'1J-t!!li-l'(JZlll!dl) TGJIJll:f!('lf>)
`-
`
`178.S ± 8.0
`1103±'1:1.2
`26.3 ± 93
`78.7± 8.8
`54.3 ± 4.1
`
`38
`85
`S6
`70
`
`[0067]
`
`[~4]
`
`Jfu.IJ::ii.-.A7'"12-11{mgldl) TOll!IU_.1'>)
`-
`
`'133 ±6.4
`60.S ±4.3
`313 ± 5.8
`S'J.1±5.9
`rl.S ± 3.S
`
`17
`51
`18
`62
`
`
`9 of 11
`
`PENN EX. 2170
`CFAD V. UPENN
`IPR2015-01836
`
`

`
`!(9) 002-220345 (P2002-
`
`1ii
`
`n
`
`Jlf)JJ~!l1!:!1J:fm<>J11\
`
`(ff)
`
`~~A-ft 4
`4
`BAYD-99S2
`30mgltg
`4
`lOOmolb>
`3aiwq
`3
`1oaiwq
`4
`
`BMS-201038
`
`13.2 ± 1.1
`32JI± 2.1
`49..6±9.!5
`55.0± lA
`69.5 ± 8.5
`
`[0068]
`
`-
`
`2.3
`3..8
`4.2
`S3
`
`[~5]
`
`lJf::iv ;ii,7a-A-(mg{g)
`-
`2.3 ± 0.1
`2.11±0.1
`3.0 ± D.2
`3.6± D.3
`3.4± 0.1
`
`(illfl}
`
`1.2
`L3
`15
`LS
`
`" dl.ffl-!1nl9"1J~!)J:(Dllrldl\ TGfllli!IJml''l(,) b.flt-:iv~'f'a-M""'1dl\ Tcilll!lllEt\i)
`.
`-
`lQS.3 ± 9.5
`~A-lllll! 6
`lmtlkg s
`!12.6 ± 9.2
`BAY13-9952
`l2
`·19
`10 - Ci
`57.3 ± 2.9
`49
`46
`jSjl±.5.5
`3Qmo/b 6
`71
`44
`~!J/7..,..7'7-I-
`90
`BA Yl~ 10msdbr+~Jn.f1"J-r3011111.11m 6
`32.8 ± 3.7
`6!I
`so
`64.7 ± 3.2
`BMS-201038
`Jmwq 6
`39
`
`221..8 ± '37.6
`264.D± 13.9
`112.8 ± 25.4
`64-' ± 4..8
`23.0± S.2
`llD.3 ± 14.8
`
`.
`
`[0069]
`
`[~6]
`
`·-·
`
`n
`
`Jlfl-!1?'1J~!W(11121R) .
`
`~/VQ 6
`1 malka
`BAY13-9952
`5
`6
`lOmallm
`?917.(7'7-t-
`30imrlb 6
`BA Y13-9!1S2 10 IDlllta + 19n 0'7-1-30 mJ!llc2
`6
`BMS-2011138
`lmglq
`6
`
`27.8 ± 6.0
`28.8 :I: 4.5
`8S.9 ± 9.4
`9.9± 1.1
`2A.6 ± 3.6
`14&9± J0.7
`
`{ft)
`.
`1.0
`3.1
`0.4
`0.9
`!1.4
`
`.ff::iv~1'P-N(~
`
`:z.s ± 0.1
`2.7 :I: D.l
`3.3 ± D.1
`2.4 ± 0.2
`3.4 ± 0.3
`4.2 ± D.1
`
`.
`
`(filt'I
`.
`
`1.1
`1.3
`1.0
`1.3
`1.7
`
`[ o o 7 o l ~313J:lf~4 t:~T J: '5 t:, llltll 7 ·:1
`t--:c-T1vt::t:n•-r, A.?o-A.itf.ii'7·:1 t--:c-T1vt:1:>'t
`oH1WlJlli:O':> 1 o fft.fi:(i')~1flJ~ m~ •t.:tM;, ltll7W t(cid:173)
`lJ ?' 1) -e 1) ~ jlJjfl.ff T Q 1J'' lfFBt:13 ~ Y'( ... l) ?' lJ {!
`1J ~tiRTo.:.ttibtPo.
`Coo 7 1 l -11, ~5:t:3J:lf~6t:~T J: -JJ:, lfFB
`t::t:3~•-C .B~ft~ill, iP"?P PAR a~ttftfl=ffl~
`fl'-t o t ~tt.o 7 1 /7- h*~JcO':>tJtffllj, ll!Mlt~
`-'t-t:Jtl'(-C J: IJ ~1J 'd:'IOI.m!Fafllfl.f'f fl=ffl ~~-t c c b
`t:, lfF !Fall1iimt ~ if~H:ft~ L, lfF t- 1J ?' 1J -e 1J ~ &: -::>
`~ •-C ljlEM'v~v c 'd:'...., -C ~' o o PP AR a ~ttftfl=ffl
`O':>J: '5 'd:', fl!lfiff{Jt:.8~ft~U-t of1=ffl~f1:1Jrrt o 1i
`lolttO':>UttiJ{~P1£ ~ tt.t..:.
`coo 7 2 l lEM'O':>ftafvJ'(11r-c-1:>01E!FaIOI.7 ·:1 t--:c-r
`Jvi:13~•-C b' :::Z? o-:::Zjtf,ij7 ·y J-.-:CrJv"C'O')~~~
`mffl.fi:O':> 1 0 ffifflJt;I;~ ~, 1:> o fm:~lj1:> o b O':>fTJ B
`A y' BM SiitiUi1flJ-c-~u I') 13.JWi'd:'.:atmMlol~~- 7
`·y J-- C.: ~ l -C ti:'.:!t''d:' < t b 1JfD§JJ1i'itfff~JJl t ~~~JJl t
`
`O':>~M:/J{ 1 O flll-.:lt-C' 1:> o c ~ i. ~tt.t.:. A.? a-A.it
`fiii'-:c -r 11rt:.1t 1'o c lfF !Fall1i~.-u:J..''d:' ~ • t (i')(i'), lff JmJJ1i
`ifflt(i') 1iJ!mttli=iS5E: l ~ tt. 'd:' ~ '.
`[0073]1-::tJ:J:IJ,MTPmmi'Jc, PPARam
`ttftfl=mi:~-?< .e~ftilfl=ffl~fl'-toc ~tt.o 71
`/v- t-~~1flJcO':>fltfflt:J: i'J, J: IJ~:h'd:'ltll?W!Fafll~
`iJ•-::>lfF.!Fall1if!ffftiJ"'=ififi£-t o.: b'J;~~:h.
`"ffl=ffl~~ L
`o.
`[0074]
`c ~13JJ(i')~* l *~13JJ (i') .JFall1ilfFO':>-TP.1i :t:3 J: lf / i t.:&jra
`8!1flH:J:tt.tf, JJfait::t:3't oJmJJ1iimt~T'Pli t l < tt.ra
`8!-to.: t;1;-r-r·~, ;1;~-::>ltlllfl.!Fafll~~"f~-tto.: ciJ{-r(cid:173)
`~ .Qt~' '5 ~.tl.t.:~* ~~To. it.:, *~BJ)O':>~!Faltll
`ni:~H: J: tt.lf, lfF Jli"-O':>!Fall1iO':>R ( !Fa Jl1ilff~ >
`~~~l-::>-::>,ltlllfl!FafllO':>ilJl'.~~"f~-tt.Q.:c#~
`~ , -t-tt.t: J: i'J ~Jm.r:fnni:~~-t o.:. c t;"'-C' ~ o c ~ • '5
`~tt.t.:~* ~~-to.
`
`
`10 of 11
`
`PENN EX. 2170
`CFAD V. UPENN
`IPR2015-01836
`
`

`
`(UO) >02-220345 (P2002-45
`
`(51) Int. Cl . 7
`A6 1 K 31/496
`31/513
`45/06
`1/16
`3/06
`
`A6 1 P
`
`(72)~1l.JJ~ BJi:j:I ~
`::klimiltir:IB:*Bttli:j:i3-1-98 fi~
`amA~t±l*J
`
`f-7:1-f (~)
`
`FI
`A61K 31/496
`31/513
`45/06
`1/16
`3/06
`
`A61P
`
`F:7'-A(~) 4C084 M17 M20 MA02 NA06 NA14
`ZA751 ZA752 ZC331 ZC332
`ZC751
`4C086 MOl M02 BC21 BC42 BC60
`CB05 GA02 GA07 GA12 MAOl
`MA02 MA04 MA09 NA06 NA07
`NA14 ZA75 ZC33 ZC75
`4C206 MOl M02 DA28 DB25 DB43
`GA09 GA28 KAOl MAOl MA02
`MA04 NA06 NA07 ZA75 ZC33
`ZC75
`
`
`11 of 11
`
`PENN EX. 2170
`CFAD V. UPENN
`IPR2015-01836

This document is available on Docket Alarm but you must sign up to view it.


Or .

Accessing this document will incur an additional charge of $.

After purchase, you can access this document again without charge.

Accept $ Charge
throbber

Still Working On It

This document is taking longer than usual to download. This can happen if we need to contact the court directly to obtain the document and their servers are running slowly.

Give it another minute or two to complete, and then try the refresh button.

throbber

A few More Minutes ... Still Working

It can take up to 5 minutes for us to download a document if the court servers are running slowly.

Thank you for your continued patience.

This document could not be displayed.

We could not find this document within its docket. Please go back to the docket page and check the link. If that does not work, go back to the docket and refresh it to pull the newest information.

Your account does not support viewing this document.

You need a Paid Account to view this document. Click here to change your account type.

Your account does not support viewing this document.

Set your membership status to view this document.

With a Docket Alarm membership, you'll get a whole lot more, including:

  • Up-to-date information for this case.
  • Email alerts whenever there is an update.
  • Full text search for other cases.
  • Get email alerts whenever a new case matches your search.

Become a Member

One Moment Please

The filing “” is large (MB) and is being downloaded.

Please refresh this page in a few minutes to see if the filing has been downloaded. The filing will also be emailed to you when the download completes.

Your document is on its way!

If you do not receive the document in five minutes, contact support at support@docketalarm.com.

Sealed Document

We are unable to display this document, it may be under a court ordered seal.

If you have proper credentials to access the file, you may proceed directly to the court's system using your government issued username and password.


Access Government Site

We are redirecting you
to a mobile optimized page.





Document Unreadable or Corrupt

Refresh this Document
Go to the Docket

We are unable to display this document.

Refresh this Document
Go to the Docket