`
`• C' v X • •••
`2 7 5 0 . • ? !
`. 4 9 3 . 5 9 ? . 9 0 i . S S 5 ^ 5 .
`
`»' •
`
`4.
`
`**1
`
`^
`
`*'
`. 0 :>
`
`j .CO
`
`1 0C > U
`
`— V
`
`S*
`
`J.i
`
`• 6
`
`•L* « *..• "J
`j . . ; . . o
`o '3 -? -i 9 . • J
`1^,00 in-'SGir;:,-'
`5 9 9 9 5 . . ^
`is.ee 1*7 3.;. ?
`6 0 7 v 5. . o
`1 3 3 - ^ . . y j
`
`47
`
`4S
`
`* 9
`i'O . SO ' lis359 . «:•
`5S21.5 . ^
`56 10 . 00
`icJ 0 ifS. 4
`? " .'•' •:'• 0 . i"
`
`5.®
`
`ia
`
`X u
`
`2 ^ «l :?• . •; 0
`
`i
`
`. <??:
`. 4 9 1 6 2 - : . J O 1 . 5 ? 5 - ; ? . - .
`^ .<:.:2
`2v.-':-c . •;•?
`.51 i^7i . 1 0 i.o'i
`. -*i .' f,'
`-V
`. ; : : • f e / j
`. 5 0 1 5 7 7 . 3 0
`(iLf?\3oH$s
`:v:is.46
`,51 1 2 1 3.30 'l.Sl-.
`2 0 0 0 . 2 3
`
`-2dll
`TvTT
`v . l ' '
`
`1 •
`
`51
`
`1 0 . 0 0 1 5 5 - ; 9 . 0
`5 c . S 7 S . 9
`
`. 5 1
`
`1 9 9 . P.0 J . 3 7 S A C .
`2 8 9 . 4 ?
`
`• 1
`
`. 0 1 3
`JV
`r t " . 0 0 5
`
`^34
`
`•< v 'V
`•r j.
`
`.S ^
`
`fc*. •
`
`J-vC
`
`•' ,^8
`
`t e ^ C -
`
`. * a
`
`. <57
`
`S #
`
`10
`
`1
`
`i a
`
`18
`
`5 9
`
`6 0
`
`T I M E C P M f l / K M O E V
`C'PMl/ K
`5 2 1 0 . 0 0 1 5 3 1 6 . 7
`5 7 8 3 7 . 6
`5 3 1 0 . 0 0 1 5 1 8 ' © . 4
`5 4 0 8 2 , 5
`5 4 1 0 . 0 0 1 5 7 7 4 . 1
`5 7 1 2 3 . 9
`5 5 1 6 . 0 0 1 5 9 0 0 . 1
`5 7 5 6 7 . 7
`5 6 1 8 , 0 0 1 6 5 0 2 , Si
`5 9 9 4 6 , 6
`1 0 . 5 7 1 0 , 0 0 1 6 3 8 7 , 2
`=•: Q 7 o , R
`5 3 1 0 , 0 0 1 6 2 0 0 . 5
`58151 , 9
`l O . O O 1 5 8 4 3 . 5
`5 7 2 8 3 . 5
`l O . O O 1 6 0 3 3 . 5
`5 7 7 0 7 . 8
`
`5 1
`
`C P M B / K 5SDEV Q I P F L R G 5
`D P f ' 1 2 / K
`0 3 * 5 6 7 „
`. 5 0 5 7 4 . 6 0 2 . 6 2 5 4 5 .
`.34-
`-3,016
`9 2 2 , 2 9
`5 7 8
`, 0 7 5
`1 1 4 5 , 3 0 1 . 8 6 5 4 7 ,
`.13
`1886•68
`- M . 8 3 4
`. 0 8 9 5 8 9
`. 5 0 1 4 0 1 . 0 0 1 . 6 8 5 4 5 .
`.0?
`- 5 * . © 4 1
`. 2 3 1 8 . 8 0
`, 0 9 5
`6 0 0
`. 5 8 1 5 0 9 . 0 0 1 . 6 2 5 4 5 .
`-V, 0 4 3
`2 5 0 1 , 4 4
`n ^
`6 1 : 1
`0 9 5
`, 4 9 1 5 7 4 . 5 0 1 , 5 9 5 4 3 .
`IL
`. 9 5
`2 6 1 2 . 5 5
`( d t O S C W V S j
`• 0 4 4
`.49 15 7 5 , 3 0 1 , 5 9 5 4 5 ,
`1 )
`. $ , 0 3 6 6 2 2
`gjiMB : ^->31, Z/lAi •04<l
`.^S"
`3?
`5 0 1 5 1 0 . 5 0 1 , 6 2 5 4 8 .
`. 0 3 3
`* i v >
`" 7 . 9 4 3
`. ^ 3
`2 4 9 7 , 3 6
`, 5 0 1 5 1 2 . 8 0
`. 0 9 5 6 ^ 3
`
`* WM 8 1 . 6 2 5 4 5 . - 1
`.<?$"
`2 5 0 7 . 2 1
`. 6 4 4
`. 5 0 1 5 1 4 . 7 0 1 . 6 2 5 4 7 .
`. 0 9 4 6 5 4
`fe . \ . 0 4 3
`2 5 0 6 . 3 1
`
`S C R
`
`M I N
`
`1
`
`1
`
`(i(«X
`
`£ 1 X
`
`4 r
`J O / C
`i o a e.
`
`l O ^ d ,
`
`Itfld-
`i o t (L/
`
`6 1 1 0 , 0 0 1 6 9 1 2 , 0
`6 1 0 6 9 , 5
`
`, 4 9 1 3 8 8 , 7 0 1 , 6 9 5 4 7 .
`2 2 9 2 , 1 9 •,
`
`. 0 8 ^ 6 o 5
`. 6 3 8
`
`" "
`
`''V-
`
`[a..
`
`/ li;r,''i>'—(V I. rki.Vi •!
`
`• — >•*•••• ' ^ ' "• ••
`
`TT"'"
`v'vi
`
`'
`
`.
`
`••
`
`. v."
`
`• ..- ,
`
`f -If*-
`
`•.. .j.
`
`-L..
`
`•, ,•
`
`-• I .iV-lU"'1'-" 'Vr1" •h—•-••••
`
`LCvj'.-?k-::-'4An>n,
`
`'.:•.- . .<•• -
`
`'V|'.-f.ii - •• VI T'^i-r'-
`
`.A**.,.,,
`
`v V.
`
`•
`
`"
`
`
`
`'
`
` :
`
`•
`
`'
`
`
`
`.
`
`A
`
`-
`
`.
`
` •
`
`'
`
`•
`
`.
`
`•
`
`:
`
`•
`
`
`
` .
`
`•
`
`?
`
`•
`
`
`
`
`
`•
`V.,i;
`
`- j • . . ' / £ ! ' . •-
`
`': .• •;'
`
`.'•>
`
`'
`
`• - ' ' • • • • -
`
`v
`
`' • • ' • i
`
`V;*:"
`
`;v
`
`• '*1 a
`
`••' • •'•' v
`• . V ,
`
`>»en.
`
`~:^£r :
`
`• *
`
`•
`
`r ; : - V : - •
`
`• - • '
`•#"» -
`
`• • '
`
`Sawai Ex 1005
`Page 782 of 4322
`
`
`
`
`
`5
`
`' >K."
`
`Sawai Ex 1005
`
`Page 783 of 4322
`
`Sawai Ex 1005
`Page 783 of 4322
`
`
`
`'
`^hr'
`B lifter A,-and DMA?0OHSO;:O.lM:NaOH ^;:T ^f?S-
`•^v
`
`-inih-: -
`
`.nfi©;"-
`
`^ /DHfi?M^ar;iousscon »ivtfat1on$
`
`'
`
`•
`
`?:
`
`•
`
`•v. •
`
`••
`' k*
`
`^
`4)
`M
`
`IS,Kill: f
`S'J
`
`"V
`• CAJ
`
`:
`
`-
`
`i '.v
`
`..:
`
`
`i;
`
`- : .. ..
`
`.. .-r-: • .•.y.-.fvi ?.
`
`.;;
`
`-
`
`Jul:
`SJCSlSiU.u fa
`' /
`ra DEC 5 01984 .
`
`yt>
`
`^ '•S r; f
`rH'^-
`
`!:M
`
`•:
`
`••
`.-i •
`
`• -' '
`
`•'•
`
`•
`
`•
`
`'
`
`1
`
`'''
`
`(SAE)! was saponifiedj)n a^50o waterbathlfdrvzifif. :•
`
`':•
`:
`
`:^4&: .••• •
`
`V }
`"
`
`;.; 'tr ' •
`
`• . '•'
`
`,'
`
`• j "'"{'ji1-''"•:'• • ''.
`
`4) ;S3;|.i6
`
`.
`
`i
`
`. :'• '.y.ii
`
`5:^
`v:! '& '
`
`. >•:'
`
`ii- x! f Vr
`
`•..•••
`
`* ^
`
`MX
`
`4 /• ^
`
`i.;'-;;
`
`of each to
`
`nildrbsomdl^sUS^nSlbn^and^;heyj:showed 'ntftiitjnlflfcant-lnhlbi^on^"^- &\*£" fa
`
`v-;
`d1VUt1on;weFfe :ass lyed'vfor HMG-CeA^reductase activity• - M v
`
`; :; '
`
`«vj
`
`i^0ft.«d:ttl-;.;ie:Sprag»«-n^8^^S»O5 '®
`
`'>• -
`
`Ifroiri ;$1<jiTia) • iand/Buffer^.A.'and DMSO: ).l M NaOH.
`
`.
`
`|: ;^v •;
`
`^3
`
`Sawai Ex 1005
`Page 784 of 4322
`
`
`
`<
`31
`LU
`d
`
`o
`
`C2
`U_ >—i
`
`T**
`
`vj '-o
`
`T—K
`V
`*
`
`o C£
`o 2:
`o
`>« o
`
`}• -J
`
`I
`
`<
`to,
`
`O O CM O CNJ
`cn cn <n cn
`
`I I I I
`
`o CNJ o \0 l l I
`en <71 co o
`
`CO
`
`1
`
`1
`
`1
`
`1
`
`1
`
`1
`
`1
`
`1
`
`1
`
`1
`
`1
`
`j>o
`
`O
`o
`
`\
`
`A-
`
`o
`
`As
`
`^5- O O CNJ O
`vD <Ti
`
`CNJ
`» O
`I
`
`O O
`CSJ CO O
`
`<• O
`
`co
`cn vo vo
`cn O O O
`
`o
`
`O CM fcO
`cn <M fM
`
`CM \D <\»
`o
`
`CO CM Ci CO r— CO
`O O O CO U") U") <X>
`
`CO
`m
`
`I
`
`co o 00 *>3- on r-
`LD in in
`o o
`
`m
`co ui co r-
`vO CO CT» CT»
`
`o co u"> on n o co
`U") <X> O U1 LT) o LT)
`
`zz
`o
`to
`z
`sc
`
`o
`o
`00
`a:
`CD
`
`CO
`I
`
`I
`CO
`
`C-<
`to
`
`LD
`
`LO
`CO
`
`•iA
`
`)
`
`&
`
`O
`
`\
`0/-
`\
`\
`0/
`
`<
`a:
`O
`
`CO
`
`CM
`
`O
`
`LD
`CO
`
`co C M n *r m \o r— co
`I I I I
`I
`1
`t
`r o o o o o o o o
`o
`
`vD
`co C M co ^ i/n vo r— o
`1 1 1
`j I J
`1
`1
`c o o o o o o o o
`o
`
`<
`o
`
`CO
`
`CO
`
`I
`
`rs
`rs
`c<
`
`I
`ro
`Z
`o
`CM
`co CM ro
`LTl <X) r~- co
`1
`1
`1
`I
`I
`I
`i
`C M O O O O O O O
`o
`
`t
`
`CM
`
`CO
`
`I • I
`>
`<
`X
`o o
`00
`
`o
`
`CM
`
`cn
`Co
`Co
`
`C
`
`o
`fO
`CM n *«• ^ r~ co
`E 5 I
`1
`1
`1
`1
`1
`1
`1
`o c O O O O O O O O
`{_>
`
`LU
`<
`Q
`
`o
`->-
`3
`c
`x
`o
`C_J
`
`Sawai Ex 1005
`Page 785 of 4322
`
`
`
`>
`m
`73
`
`J
`
`o
`—I
`
`C3
`
`Z
`^ r*
`
`o
`72
`
`=r o
`o
`o j-i
`
`:>
`(SI
`
`n
`<
`o
`(Si
`
`m
`
`O >
`
`o
`C
`C
`
`C
`t )
`
`•e-
`
`lit
`
`I
`
`1 CO I
`
`I
`
`ro ro o
`cn o
`
`t
`
`t
`
`o ro ro
`^ l-O
`
`I I
`
`I
`
`1
`
`[ I A ^ CD -£»• CO
`ro —J CD ^ >-0
`
`v
`
`o r-\
`
`LD
`—J
`co
`o o o o o a
`
`O CD CD CD O
`o IO
`
`ro
`
`ro o o o co cs
`o UD CJ
`
`ro ci cr* oi ro cr» ro
`O -J ro
`
`ro o —J O ro ro
`o o o vo o o C3
`
`cn o —J 0">
`cn cn
`a a cn-cn cn ro o
`
`o -J vo o*> o> o
`cn cn cn cn ^ ro o
`
`C3 cn vo co o CO
`o o o
`cn ci co
`
`f
`
`>
`Si
`o
`r~~>
`\
`
`y
`/
`A {
`\
`0
`\ /
`/o^i
`
`>
`
`o
`
`c
`CD
`
`CD
`
`ro
`
`CD
`
`cn
`no
`
`CJ
`2
`
`O"! U1 A CJ f\3C*>
`a
`I I I I I I I 1
`OOOOOOOCO
`
`r
`>
`r-
`ri
`(
`V
`
`Ci
`
`/j
`
`\
`
`\
`
`>
`2
`O
`
`CD
`
`ro
`
`cn
`
`tn
`ro
`
`CJ
`z
`ro
`en
`CJ rsjco
`Q -J cn ui
`I I I I I I I t
`OOOOOOOCJ
`cn
`
`>
`2
`O
`
`C9
`
`no •
`
`cr-
`
`cn
`ro
`
`<~h
`
`CN
`
`^ /;
`r
`J
`V/
`/ n\
`
`>
`3
`o
`
`o
`
`no
`
`CD
`O
`
`cn
`ro
`
`o
`
`/
`
`£
`
`/A
`
`/
`X-^ ^
`v
`
`w
`/h\
`
`CO
`en
`u rsjco
`CD -J 0> <-n
`t I I I I I
`I I
`OOOOOOOCO
`<T>
`
`CO
`Ln
`o>
`a -J o> ui A w roro
`I I I I I I I
`o o o o o o o
`<Jr<^
`
`i_n
`
`•Zf
`
`cr<
`
`<r
`
`LU
`
`Sawai Ex 1005
`Page 786 of 4322
`
`
`
`w
`
`d
`<
`21
`LkJ
`c:
`
`o
`
`=3
`
`O —
`ht >-
`
`o
`GZ
`u. h-
`o 2;
`o
`o
`
`i
`
`<
`
`to
`
`o o f — o
`o
`cn in
`
`r- 1 co
`
`o r- VTJ \£>
`o cn co
`
`1 in in
`
`o co CM o cn r—
`o ci r- m
`
`O
`CNI vO TOO
`o cn <n r-
`
`V
`
`r O
`
`o
`
`r*^
`
`u
`
`O
`
`O
`
`o o co co co r- vo
`m co cr> O
`a>
`
`1
`
`I co vn *r l in m
`co
`01 o">
`
`CO T
`1 r- 03 o
`CNJ LO cn cn cn
`
`1
`
`CO "C" o o
`CSJ o at
`
`o o vn o
`u-> Cn O
`o o
`
`c\> \n-
`o o
`
`1 ro co
`p-
`o ««r
`O O <— CO 00
`
`CM
`•«5- CO o o
`O P-
`O O fO in cn
`
`co ^3 *?- r- cn
`o o o <NJ cn cn o
`
`<
`a:
`o
`
`5S
`1 1
`>
`
`o
`to
`
`LU
`<
`Q
`
`CO
`fM
`
`00
`
`CM
`fM
`
`c
`
`a:
`o
`
`CO
`
`c\»
`
`' CM
`
`CO
`m
`00
`
`ra
`z
`
`<
`a:
`o
`
`CO
`
`c\»
`
`CM
`
`ro
`uo
`CM
`
`I
`f3
`2^
`o
`CM
`CO CM CO •«" W vO f— CO
`I I I I I I I I
`C M O O O O O O O
`o
`
`J <0
`A
`3
`/
`\
`
`>
`V /
`
`^'Z
`
`<
`a:
`o
`
`CO
`
`00
`
`CNJ
`
`CO
`o
`cn
`
`00
`
`N^VI
`
`^ // \
`~w
`/ ~ A
`V\!.<
`
`O
`w> vo r- co
`co CM co
`1
`1 1
`1
`1
`1
`1
`1
`co o o o 0 0 o o
`O
`
`ra
`z
`CM
`incM co m UD r~~ co
`1 i 1
`1
`i i 1
`1
`C M O O O O O O O
`vO
`
`vO
`
`o i c
`
`0
`rO
`
`o
`o
`
`CM co
`ir> vO r— co
`i 1
`1
`1
`1
`1
`1
`1
`0 0 0 0 0 0 0 0
`
`T**
`
`01
`y v . |
`2;
`oi
`
`cn
`
`5^
`
`>
`
`CM
`
`• ' . :*VJ.
`
`Sawai Ex 1005
`Page 787 of 4322
`
`
`
`11
`11
`22
`79
`90
`90
`100
`
`9
`11
`15
`60
`76
`95
`100
`
`9
`6
`7
`10
`14
`
`o.oo ^
`
`OJ) 0<|
`
`U V*
`
`09
`09
`70
`21
`10
`2
`
`91
`09
`05
`40
`24
`5
`
`91
`94
`93
`90
`06
`
`.96
`.96
`.04
`.22
`.11
`.02
`.00
`
`.90
`.96
`.92
`.44
`.26
`.05
`.00
`
`.99
`1 .02
`1 .01
`.97
`.94
`
`Is
`
`Q\{ Oil
`
`\
`
`I
`
`:-/
`/
`
`DHA
`
`OH w
`
`©
`
`/
`
`OHA
`
`0
`
`15) 63-356 (25400) 12/12/04
`
`ot-l
`
`\
`
`I
`
`TO"0
`TO"7
`TO"6
`lO"5
`
`Y
`
`12/12/04
`
`16) 62-265/3 (25400)
`
`10-°
`io-7
`io-6
`io-5
`io-4
`TO-3
`TO-2
`
`V
`
`10-°
`IO"7
`TO-6
`io-5 •
`So TO-J
`10-3
`lO'2
`
`7
`
`jj •
`i*.
`
`Sawai Ex 1005
`Page 788 of 4322
`
`
`
`V
`
`0
`10
`11
`30
`03
`92
`90
`
`13
`9
`n
`4
`5
`9
`24
`
`4
`2
`10
`73
`06
`96
`99
`
`0.1517
`
`> 10
`
`O.DO-]
`
`92
`90
`09
`62
`17
`0
`2
`
`07
`91
`09
`96
`95
`91
`76
`
`90
`90
`90
`27
`14
`4
`
`.87
`
`• .05 •
`
`.04
`.50
`.16
`.00
`.02
`
`.02
`.06
`.04
`.90
`.09
`.06
`.71
`
`.90
`.92
`.04
`.25
`.13
`.04
`.01
`
`iflA.
`
`/
`
`o
`if
`I
`
`U'
`X
`
`L {
`
`10-°
`10-7
`lO"6
`10-5
`lO"*
`10-3
`lO"2
`
`Jo
`
`12/13/04
`
`20) 63-365 (25490)
`
`OMA
`
`12/13/84
`
`19) 63-364 (24409)
`
`DMA
`
`10) 62-320/Na-4(-2jt2gT) 12/13/84
`
`10-0
`10~7
`10-6
`10-5
`•) 0-4
`lO"3
`10-2
`
`>0
`
`OHA
`£// wt 0
`//
`
`I
`
`rt
`
`•
`
`10-°
`10-7
`10-6
`10-5
`10-4
`TO"3
`10-2
`
`Sawai Ex 1005
`Page 789 of 4322
`
`
`
`16
`18
`24
`70
`91
`95
`99
`
`17
`14
`3
`80
`89
`98
`99
`
`6
`8
`23
`34
`54
`85
`98
`
`0. Oo ^
`
`fro 07
`
`0:0
`
`84
`82
`76
`30
`9
`5
`1
`
`83
`86
`97
`20
`11
`2
`1
`
`94
`92
`77
`66
`46
`. 15
`2
`
`.79
`.77
`.71
`.28
`.09
`.05
`.01
`
`.78
`.81
`.65
`.19
`.11
`.02
`.01
`
`.88
`.87
`.72
`.62
`.44
`.14
`.02
`
`Alt
`
`(j
`'.
`
`o OA c/vf
`
`vC
`(
`
`/"•
`
`(
`
`DMA
`
`b'
`(At
`
`12/13/84
`
`-/
`£
`
`£
`
`DMA
`
`12/13/84
`
`24) 63-270/2
`
`10-8
`IO"7
`IO"6
`10-5
`IO"4
`IO"3
`10-2
`
`x>
`
`23) 63-162/3 (25500)
`
`IO"8
`IO"7
`IO"6
`10-5
`IO"4
`IO"3
`IO"2
`
`>s
`
`i O \ o
`
`o H OH
`
`IO"8
`io-7
`yp 10-6
`IO"5
`IO"4
`10-3
`IO"2
`
`Sawai Ex 1005
`Page 790 of 4322
`
`
`
`--cr
`KJ
`
`r
`
`18
`
`3
`7
`1
`5
`1
`
`31
`
`4
`
`7
`75
`90
`100
`100
`
`> 10
`
`>10
`
`0.0^7
`
`103
`100
`. 105
`109
`105
`105
`82
`
`97
`93
`99
`.95
`99
`104
`89
`
`96
`106
`93
`25
`10
`
`'
`
`.96
`.94
`.97
`1.02
`.97
`.97 •
`.76
`
`.83
`.80
`85
`.81
`.85
`.89
`.59
`
`.80
`.88
`.78
`.21
`.08
`.00
`.00
`
`V U* //<«_
`
`/
`
`(M 0-1
`
`DMA
`
`r
`
`12/14/84
`
`(
`
`Lq,bl'
`
`V^jL.
`(Al
`Uvf-
`
`0H$0:0.1H NaOH
`
`12/14/84
`
`DMA
`
`12/14/84
`
`28) 63-347 (25468)
`
`io-0
`10-7
`10-6
`' IO"5
`V 10-4
`10-3
`10~2
`
`10-°
`TO-"?
`10-6
`io-5
`io-4
`10-3
`10-2
`
`>•
`
`27) 63-346 (25467)
`
`26) 62-320/Na-4
`
`10-8
`10-7
`10-6
`10-5
`10-4
`^ 10-3
`10-2
`
`Sawai Ex 1005
`Page 791 of 4322
`
`
`
`M
`
`UJ
`ct
`
`zn
`o
`
`C3
`
`U.
`
`o
`cs:
`LL. t—
`O 2
`O
`^ o
`
`<
`CO
`
`O if) CM
`cn uD
`
`l
`
`*r l
`
`r— r— un o CM
`cn en CD *s-
`
`I
`
`1
`
`I
`
`cn m co co
`cn cn CO U")
`
`I I i
`
`c> VD CNJ CO CNJ If) m
`Oi C
`r—
`
`rv^
`
`f
`r-
`9 o
`
`\
`
`s
`
`O
`o
`
`OLT) CO O T >-0 r—
`CO CO O cn cn O
`
`co co u">2 co cn m o
`m1-" cn O O
`
`in r— CM CM *r uo
`*s- o o o
`
`^s- co CM co m m
`CM CO
`cn
`
`CO Cn CO CO cn O Cn
`o CM r- co r- co co
`
`co *?-• o cn CM CD co
`vO O O CM
`CM
`• o o
`
`u-> co r- CO CM CD
`o o
`T
`
`ID CD vO vO
`O O O CM cn O O
`
`)
`
`~5
`
`<
`Z
`o
`
`/-t
`
`v.
`
`/
`
`CO
`r—
`
`CM
`
`J
`V
`
`<
`
`CO
`r-cp
`
`CM
`
`<
`ac
`o
`
`co
`
`CM
`
`Jk
`
`C5
`r*«5
`/
`/
`.^N
`/
`\
`
`V
`
`.•v
`
`CP
`
`f4 CM
`
`cn
`CM
`CM
`c
`-M
`u
`^3
`CL
`co
`C M co m LO
`E s: i i i i i i i i
`o E o o o o o o o o
`<_>
`
`co
`co
`in
`CM
`CM
`I
`I
`ro
`re
`z u>
`z
`s
`o
`xS
`CM
`rJificM co •j'm ID r* O
`CO CM CO ^ m vD f-~ CO
`I J
`I I I I I I
`«
`l
`i i i i
`l I
`C M O O O O O O O
`C M O O O O O O O
`«x>
`vtf
`
`<
`ac
`o
`
`2
`UJ
`>
`o
`IS)
`
`<-
`
`CO
`
`CM
`
`in
`
`in
`CM
`
`i
`
`LU
`
`O
`
`o
`
`ZD
`o
`ar
`o
`<_>
`
`CM
`m
`co C M co T m uo r— co
`i i i l i i i i
`n o o o o o o o
`o
`
`cn
`CM
`
`o
`CO
`
`CO
`
`£
`
`C M
`CO
`
`Sawai Ex 1005
`Page 792 of 4322
`
`
`
`w
`
`J
`
`I
`(
`
`7- c
`<• J c.
`
`u-
`
`co cn ro co uD
`{J1 -«J
`
`I
`
`CO —J O ^
`-J CD
`U3
`
`U3 CO
`
`CT1 CT> CO 03 "-O -£» CD
`cn C3 U3 UD
`
`O CO ^ UD lO
`LTI CD UD UD UD
`
`UD
`
`\
`O •
`o
`
`o
`
`OQ
`
`o
`
`o
`o
`
`LH CD -J
`ro
`
`O UD
`
`o ^ to
`
`ro en ro co -i» —•
`vo co ro
`
`ro
`
`j* —J ro
`(A (A CO J*
`
`l£> o -J o*i
`UD ca cn
`
`o
`o
`C3
`o in co o o
`
`-»•
`o o
`
`ro a"> cn
`o o vo ro
`
`—J —J ro —J ro
`o o vo
`o o
`
`vo LTI CO —J
`o o o
`
`o vo LTI
`
`\
`
`[
`
`c
`r-
`
`0
`
`)
`/
`_/
`
`/'A
`
`>
`IE
`a
`
`CD
`
`ro
`
`o
`en
`cn
`ro
`
`£
`(S
`\
`/
`\
`/
`
`S
`
`t
`v" -'
`/
`
`FA
`
`ro
`o
`a> cn -£»• CJ [\jr\ji
`CD
`i
`i
`t
`i
`i
`i
`i
`i
`OOOOOOOOJ
`a>
`
`<S>-
`
`5^
`>
`
`\\
`
`/l^
`\
`\
`/
`\ .n
`/IN
`
`>
`zc
`o
`
`CO
`-j
`
`ro
`
`CO
`CO
`-u
`cn
`rsj
`
`CO
`
`o>
`CD —I
`OJ M (\J
`cn
`!
`I
`I
`I
`t
`I
`I
`I
`OOOOOOOfVJ
`o
`
`>
`Z
`a
`
`m
`<
`a
`00
`
`CO
`
`ISJ m
`>
`a
`
`en
`C3
`cn
`(NJ
`
`r
`
`-i4
`
`r
`\
`/ISN
`
`>
`3:
`o
`
`CD
`
`ro
`
`o
`o
`cn
`cn
`rsj
`
`CO
`
`cr
`
`—
`
`o
`
`a>
`CD ~-J o> cn -t"" Co fs)OJ
`i
`i
`t
`i
`i
`i
`i '
`OOOO.OOOOJ
`CP
`
`(NJ
`a>
`co -J
`cn ->• co M—'
`I
`t
`I (
`t
`I
`I
`I
`oooooooto
`cr>
`
`CO
`CO
`
`u>
`
`r
`
`T-V ' . .
`
`on
`CJ
`
`<*
`
`•CTV
`CO
`
`Y
`
`Sawai Ex 1005
`Page 793 of 4322
`
`
`
`V
`
`DFfr?
`
`S—'
`tnn^iy
`
`XS&
`JUN 2 8 19*r
`
`of HMG-CoA reductase.
`200 yl of microsomal suspension and they showed no significant.inhibition
`
`inhibition also and is indicated in the results. Buffer A, and DMA
`
`Compactin in DMA at various concentrations was assayed for
`
`were also assayed by adding 10 yl of each to
`
`reductase activity.
`
`plus 10 yl of drug dilution were assayed for HMG-CoA
`experiment. 200 yl Aliquots of microsomal suspension ( .97 - l.llmg/ml)
`in Buffer A with 10 mM DTT and frozen at -80"C until thawed and used for
`
`Microsomes were prepared from male Spraque-Dawley rats (l63 q
`
`)
`
`results.
`Dilution of each compound gave the concentrations indicated in the
`
`Sawai Ex 1005
`Page 794 of 4322
`
`
`
`4
`16
`32
`00
`96
`
`4
`
`4
`20
`
`4
`32
`60
`00
`96
`100
`
`0
`
`o.
`
`>10
`
`D.ooVi
`
`100
`100
`96.
`04
`60
`20
`4
`
`104
`104
`100
`96
`104
`96
`00
`
`100
`96
`60
`32
`20
`4
`
`104 •
`92
`100
`
`.47
`.47
`.45
`.39
`.32
`.09
`.02
`
`.49
`.49
`.51
`.45
`.49
`.45
`.37
`
`.47
`.45
`.32
`.15
`.09
`.02
`.00
`
`.49
`.43
`.47
`
`Ij1!/
`
`OMA
`
`If
`
`Cfybl
`
`DMA
`
`'•
`
`10-8
`io-7
`IO"5
`10-5
`10-4 •
`. IO"3
`10-2
`
`DMA
`
`2) 62-320/Na-4(23531) 6/13/05
`
`IO"8
`"IO"7
`TO"5
`
`/
`
`Oil
`
`10-0
`io-7
`10-6
`io-5
`IO"4
`io-3
`IO"2
`63-537/Na(RN 26039) 6/13/05
`
`TO-8
`IO"7
`IO"6
`IO"5
`lo-^
`IO"3
`IO"2
`63-51G/2(RN 26020) 6/13/05
`
`(.
`
`n
`
`0^7
`
`4)
`
`3)
`
`Sawai Ex 1005
`Page 795 of 4322
`
`
`
`CS
`
`X2582A
`
`12
`40 -
`84
`
`^t.R
`
`12
`56
`
`4
`
`4,
`
`20
`72
`
`IM
`
`100
`100
`100
`100
`88
`60
`16
`
`100
`96
`100
`100
`100
`88
`44
`
`96
`100
`96
`100
`100
`80
`28
`
`.47
`.47
`.47
`.47
`.41
`.28
`.07
`
`.47
`.45
`.47
`.47
`.47
`.41
`.21
`
`.45
`.47
`.45
`.47
`.47
`.37
`.13
`
`I
`ci-i
`
`O
`
`\_/
`0
`
`DMA
`
`•1
`
`6/13/85
`
`l o i
`
`KO
`
`DMA
`
`6/13/85
`
`8) 63-550(RN 26083)
`
`7) 63-549(RN 26082)
`
`10-8
`IO"7
`10-6
`10-5
`10-4
`10-3
`10-2
`
`IO"8
`IO"7
`IO"6
`IO"5
`IO"4
`10-3
`IO"2
`
`(A-l cv)
`
`. o
`
`ro^,
`
`DMA
`
`/^/13/85
`
`10-8
`10-7
`10-6
`. 10-5
`io-4
`10-3
`10-2
`63-548(RN 26080)
`
`6)
`
`Sawai Ex 1005
`Page 796 of 4322
`
`
`
`oo
`VJ
`
`5
`1
`
`3
`3
`
`20
`
`3
`
`1
`
`7
`24
`
`5
`3
`13
`63
`04
`96
`90 •
`
`5
`
`'> ( 0
`
`•
`
`>10
`
`o>on\.
`
`95.
`99
`95
`97
`97
`101
`00
`
`97
`-95
`99
`101
`97
`93
`76
`
`95
`97
`87
`37
`16
`4
`2
`
`107
`101
`95
`
`.90
`1 .02
`.90
`1 .00
`1.00-
`1.04
`.02
`
`•
`
`1 .00
`.90
`1.02
`1.04
`1.00
`.96
`.70
`
`.90
`1.00
`.90
`.30
`.16
`.04
`.02
`
`1.10
`1.04
`.90
`
`DMA
`
`6/10/05
`
`DMA
`
`10) 62-320/Na-4(23531) 6/10/05
`
`10-0
`lO"7
`10-6
`10-5
`.10-4
`10-3
`10-2
`
`10-0
`1G~7
`TO"6
`
`11) 63-551(RN 26004)
`
`10-°
`10-7
`10-6
`10-5
`10-4
`io-3
`lO"2
`
`DMA
`
`D
`
`6/10/05..
`t'M
`
`i
`Kr
`
`o
`
`0(1
`
`^
`
`e
`
`0
`
`/
`
`Co"\
`
`12) 63-552/Na(RN 26005)
`
`10-°
`IO"7
`10-6
`1.0" 5
`10-4
`IO"3
`IO"2
`
`Sawai Ex 1005
`Page 797 of 4322
`
`
`
`C/^
`
`33
`54
`79
`92
`96
`
`7
`47
`05
`. 96
`96
`
`5
`1
`1
`3
`11
`38
`03
`
`3
`
`,00^
`
`I
`
`C
`
`107
`105
`67
`46
`21
`0
`4
`
`103
`109
`103
`101
`93
`53
`15
`4
`4
`
`95
`99
`99
`97
`09
`62
`17
`
`97
`
`1.04
`1.02
`.65
`.45
`.20
`.00
`.04
`
`1.00
`1.06
`1 .00
`.90
`.90
`.51
`.14
`.04'
`.04
`
`.98
`1 .02
`1 .02
`1.00
`.92
`.64
`.18
`
`1 .00
`
`DMA
`
`DMA
`
`0
`
`/Jo-
`
`DMA
`
`a; I
`GJ*
`
`O
`
`10-0
`io-7
`10-6
`IO"5
`1 o-^
`IO"3
`10-2
`
`11) 63-554/Na{RN 26007) 6/18/05
`
`16) 62-320/Na-4(23531) 6/19/05
`
`10-0
`IO"7
`IO"6
`10-5
`IO"4
`IO"3
`10-2
`
`15) Compactln (24291) 6/19/05
`
`'
`
`10-0
`IO"7
`10-6
`10-5
`10-4'
`IO"3
`10-2
`IO"1
`ImM
`
`Sawai Ex 1005
`Page 798 of 4322
`
`
`
`1
`10
`/ 60
`
`•4^
`
`3
`45
`07
`
`5
`
`•
`
`7
`49
`07
`
`MM
`
`105
`103
`103
`99
`02
`32
`
`107
`105
`105
`103
`97
`55
`13
`
`95
`103
`103
`101
`93
`51
`13
`
`1 .02
`1 .00
`1.00
`.96
`.00
`.31
`
`1.04
`1.02
`. 1.00
`1.00
`.94
`- .53
`.12
`
`.92
`1.00
`1.00
`.90
`.90
`.49
`.12
`
`0
`/
`
`U/
`
`r\
`
`C^C
`
`DMA
`
`6/19/05
`
`20) 63-563(RN 26127)
`
`10-7
`io-6
`10-5.
`10-4
`. 10-3
`lO"2
`
`CA hO
`
`M [M
`
`DMA
`
`6/19/05
`
`j#
`
`.
`
`C'J.
`f
`19) 63-550/2 Na(RN 26100)
`
`10-0
`lO"7
`TO"6
`10-5
`10-^
`10-3
`10-2
`
`U\M
`
`'{
`
`o ^
`
`O
`
`DMA
`
`6/19/05
`
`10) 63-559(RN 26106)
`
`10-0
`10-7
`10-6
`-10-5
`10-4
`TO"3
`. TO"2
`
`•
`
`Sawai Ex 1005
`Page 799 of 4322
`
`
`
`Ko
`
`6
`61
`02
`94
`100
`
`3
`39
`• 85
`97
`97
`
`1
`
`1
`20
`66
`09
`
`0 .01
`
`1
`
`ChS'O
`
`106
`103
`94
`39
`10
`* 0
`
`106
`109
`115
`109
`97
`61
`15
`3
`
`101
`99
`103
`99
`80
`34
`11
`
`107
`
`.00
`.86
`.70
`.33
`.15
`.05
`.00
`
`.08
`.91
`.96
`.91
`.81
`.50
`.13 -
`.03
`.03
`
`.98
`.96
`1.00
`.96
`.70 •
`.33
`.10
`
`1.04
`
`DMA
`
`DMA
`
`24) 62-320/Na-4(23531) 6/24/85
`
`10-8
`
`io-7
`10-6
`IO"5
`10-4
`IO"3
`IO*"2
`
`23) Compactln (24291) 6/24/85
`
`"
`
`IO"8
`IO"7
`10-6
`IO"5
`IO"4
`io-3
`IO"2
`IO"1
`ImM
`
`&'[ ^
`
`DMA
`
`6/19/85
`
`22) 63-565(RN 26128)
`
`io-5
`io-4
`IO'3
`IO"2
`
`IO"0
`10"7
`10-6
`
`"
`
`/
`
`P
`
`10-0
`
`Sawai Ex 1005
`Page 800 of 4322
`
`
`
`-C
`NJ
`
`3
`3
`12
`48
`91
`
`6
`6
`6
`67
`85
`97
`
`9
`6
`6
`9
`15
`24
`73
`
`7
`
`103
`106
`97
`97
`88
`52 -
`9
`
`94
`94
`97
`94
`33
`15
`3
`
`91
`94
`94
`91
`85
`76
`27
`
`109
`
`'
`
`.86
`.08
`.81
`.01
`.73
`.43
`.00
`
`.78
`.78
`.81
`.78
`.20
`.13
`.03
`
`.76
`.70
`.78
`.76
`.70
`.63
`.23
`
`.91
`
`X
`
`1
`
`A O
`
`Buffer A
`
`6/24/05
`
`/
`
`0
`
`DMA
`
`I
`ov(
`
`&J.
`
`6/24/85
`
`10"°
`10-'
`10-6
`lO"5
`10-4
`lO"3
`10-2
`
`28) 63-560(RN 26107)
`
`10-0
`lO"7
`lO"6
`lO"5
`-10-4
`10"3
`lO""2
`
`•
`
`27) 63-568(RN 2615X)
`
`DMA
`
`V
`
`O .—i
`
`' otl Oi-t
`
`0
`
`10"°
`lO"7
`10-6
`lO"5
`10-4
`10"3
`10-2
`
`.
`
`6/24/85
`
`26) 63-567(RN 26149)
`
`Sawai Ex 1005
`Page 801 of 4322
`
`
`
`"H or*
`
`1
`6
`23
`51
`88
`
`4
`9
`68
`85
`95
`100
`
`1
`6
`
`16
`51
`08
`90
`100
`
`6
`
`0 <7 ^ ^
`
`D .00 ^
`
`96
`101
`99
`94
`77
`49
`12
`
`101
`96
`91
`32
`15
`5
`
`99
`94
`
`101 '
`
`99
`84
`49
`12
`2
`
`94
`
`.85
`.90
`.87
`.83
`.68
`.44
`.11
`
`.90
`.85
`.81
`.28
`.13
`.04
`.00
`
`.07
`.03
`.90
`.07
`.74
`.44
`.11
`.02
`.00
`
`.70
`
`f/l i;"l
`
`<!/
`
`(M
`
`UM
`
`(f
`
`10-°
`io-7
`io-6
`IO-5
`10-4
`IO"3
`TO"2
`
`DMA
`
`32) 63-556.(RN 26093) 6/26/05
`
`DMA
`
`DMA
`
`31) 62-320/Na-4(23531) 6/26/05
`
`10-0
`io-7
`10-6
`TO"5
`10"4
`10-3
`IO"2
`
`10-°
`io-7
`10-6
`IO"5
`• 10-^
`IO"3
`TO"2
`IO"1
`ImM
`
`30) Compactln (24291)/ir6/26/05
`
`GV Ct-f
`
`Q-f '
`
`•j o-o
`
`Sawai Ex 1005
`Page 802 of 4322
`
`
`
`(J-v
`fc
`
`"\
`
`091 2 01987
`
`D!
`
`of IIMG-CoA reductase.
`200 pi of microsomal suspension and they showed no significant inhibition
`
`inhibition also and is Indicated in the results. Buffer A, and DMA
`
`Compactin in DMA at various concentrations was assayed for
`
`were also assayed by adding 10 pi of each to
`
`reductase activity.
`
`plus 10 pi of drug dilution were assayed for IIMG-CoA
`experiment. 200 pi Aliquots of microsomal suspension ( o.9l
`mg/ml)
`1n Buffer A with 10 mM OTT and frozen at -80- C until thawed and used for
`
`)
`
`Microsomes were prepared from male Spraaue-Dawley rats ( 150 q
`
`Sawai Ex 1005
`Page 803 of 4322
`
`
`
`2
`
`2
`32
`80
`
`46
`74
`90
`99
`99
`
`18
`64'
`80
`94
`99
`
`20 ^7
`
`.98
`102
`98
`102
`98
`68
`
`O.OOIL
`
`o.o07
`
`100
`100
`54
`26
`10
`1
`1
`
`100
`100
`82
`36
`20
`6
`1
`
`.99
`1.04
`.99
`1.04
`.99
`.69
`.20
`
`1.02
`1.02
`.55
`.27
`.11
`.01
`.01
`
`1.02
`1.02
`.83
`.36
`.20
`.06
`.01
`
`i
`
`I \
`(M
`iM
`
`V"
`e-r
`
`<:(•
`
`DHA
`
`10-8-87
`
`0 64-933 (RN 30441)
`
`» io-8
`io-7
`10-6
`10-5
`io-4
`MO"3
`i 10-2
`I
`io-0
`IO"7
`IO"6 ft
`IO"5
`io-4
`io-3
`10-2
`
`DHA
`
`/4
`
`UV
`
`p
`
`C'-
`
`10-8-87
`
`i) 64-906 (RN 30393)
`
`DHA
`
`10/8/87
`
`!) 62-320 (24135)
`
`10-8
`IO"7
`10-6
`10-5
`10-4
`IO"3
`10-2
`
`Sawai Ex 1005
`Page 804 of 4322
`
`
`
`oo
`VJ
`
`2
`2
`
`11
`62
`94
`
`- vial.
`- and made directly In
`- dilution calculated
`5 sent frpm Sandoz,
`2 exactly 0.6mg in via
`2 compound-assuming
`30 Unable to weigh out
`
`0.73
`
`> to
`
`'J
`71}
`f.l
`i I
`
`cm
`
`98
`98
`105
`100
`89
`38
`6
`
`100
`100
`100
`95
`98
`98
`70
`
`100
`95
`93
`91
`72
`31
`13
`
`.99
`.99
`1.06
`1.02
`.90
`.39
`.06
`
`1.02
`1.02
`1.02
`.97
`.99
`.99
`.71
`
`1.02
`.97
`. .95
`.92
`.74
`.32
`.13
`
`DHA
`
`DHA
`
`r\
`
`frfa
`
`0
`
`lO"6
`10-5
`10-4
`10-3
`lO"2
`10-1
`1 mH
`
`B) 64-727/Na(RN 30024) 10/8/87
`
`O/
`
`lfz>
`
`0
`
`7) 64-942/Na(RN 30461) 10/8/87
`
`lO"8
`lO'7
`lO"6
`10-5
`10-4
`lO"3
`lO-2
`
`<M
`
`CM
`
`10-8
`10-7
`10-6
`10-5
`10-^
`10-3
`10-2
`
`Sawai Ex 1005
`Page 805 of 4322
`
`
`
`0257
`
`.222:25:35:8
`
`_59.55H
`
`H=m>4om.
`
`uhca
`
`.|\|
`
`ozpomzow.
`
`I.
`
`NW
`
`ILHNNF"
`
`.S:m:A2..
`
`mm
`
`mm
`
`mm
`
`2..
`
`2..
`
`mm.
`
`mm.
`
`mo.r
`
`hm.
`
`mm.
`
`mm.
`
`mm.
`
`<59
`
`
`
`.5:3:seen252:?
`
`muor
`
`leF
`
`mics
`
`claw
`
`blow
`
`clap
`
`much
`
`mace
`A
`
`Sawai Ex 1005
`
`Page 806 of 4322
`
`i
`
`i
`
`i
`
`f
`
`Sawai Ex 1005
`Page 806 of 4322
`
`
`
`u falu
`
`Y( OCT 2 (j 193r
`[pf&EtlMEr1 In
`
`of HMG-CoA reductase.
`200 yl of microsomal suspension and they showed no significant inhibition
`
`were also assayed by adding 10 yl'of each to
`
`Inhibition also and is Indicated in the results. Buffer A, and DMA
`
`Compactln 1n DMA at various concentrations was assayed for
`
`reductase activity.
`
`plus 10 pi of drug dilution were assayed for HMG-CpA
`experiment. 200 vil AHquots of microsomal suspension ( 0.96
`mg/ml)
`1n Buffer A with 10 mM DTT and frozen at -80flC until thawed and used for
`
`Microsomes were prepared from rfiale Spraque-Dawley rats ( 150.g }
`
`Sawai Ex 1005
`Page 807 of 4322
`
`
`
`(S-s
`
`14
`50
`00
`90
`
`2
`
`21
`
`60
`00
`95
`90
`
`106
`106
`101
`06
`50
`12
`
`106
`100
`101
`90
`113
`103
`79
`
`103
`106
`93
`32
`20
`5
`2
`
`.90
`. .90
`.93
`.00
`.16
`.11
`.02
`
`.90
`1.00
`93
`.91
`1.05
`.95
`.73
`
`.95
`.90
`.06
`.30
`MO
`.05
`.02
`
`DMA
`
`10-13-07
`
`DMA
`
`10-1-3-07
`
`DMA
`
`10-13-07
`
`62-526/Na (29721)
`
`lO"0
`lO-7
`: lO"6
`lO"5
`io-4
`lO-3
`lO"2
`•1)
`
`IO-O
`lO"7
`lO"6
`lO"5
`10-4
`lO"3
`lO"2
`3) _M-942/Na (30461)
`
`lO"0
`lO"7
`10~6
`10-5
`10-4
`10-3
`lO"2
`Z) 62-320 (21135)
`
`£
`
`Sawai Ex 1005
`Page 808 of 4322
`
`
`
`1Q
`
`T—
`c
`
`T~*
`
`/
`
`J
`c:
`! ~
`j
`
`to
`
`LU
`>
`o
`v)
`
`I I
`
`c
`o
`
`c
`rs
`c
`t .
`o
`CJ
`
`Ln n c v i i
`cn 'S:
`
`t I
`
`I
`
`I
`
`en o
`en o CNI
`
`I i l
`
`r>
`n
`m r~- C2
`C 7 C 2 0 0 0 0 0 0
`
`r> o o o r> o
`o o o o o o
`
`P- <• G\ \C
`c-5 cn
`cn r~ cn o o o
`
`rsj o u-i CD n n m
`m
`o n c c c n c n c n c n c n c n
`
`LTl o Ln CD Ln CD
`CTl O CD CD CD CD
`
`r- (Ni n cn n U-I LI
`C O r o r — C D C D C D C D
`s:
`a
`
`r—
`CO
`I
`n
`rj-
`Q '
`
`CD
`
`o
`CO
`z ;
`C£
`
`n
`2:
`vO
`CO
`C D
`1
`
`VJD
`
`r~» o
`v.o
`CM o
`I I I I I I
`1
`o o o o o p o
`
`a
`
`p--
`C 5
`I
`o
`rj" .
`o
`
`a
`o
`o
`C
`c :
`a
`z
`o
`o
`I
`CM o -c- tn \o
`
`!
`I
`I
`I
`!
`!
`• O O O O O O
`
`\Z>
`
`r—
`C 3
`t
`n
`I
`o
`
`CM
`o
`o
`n
`
`fs.*
`I
`
`c?
`rv n •<• i.n o
`t
`t
`J I I
`1
`c r O O O O O O O O
`C^5 —•
`
`V
`
`Sawai Ex 1005
`Page 809 of 4322
`
`
`
`Exhi
`
`it F
`
`
`
`@wumvflaomcou.ZHmd249943
`
`
`
`hCOEHummH#HbMUHmmd
`
`
`
`3333new.
`
`q
`
`Sawai Ex 1005
`
`Page 810 of 4322
`
`
`
`mWMW%flanhm..NOH.ozwucmuomumncH.
`
`
`
`
`
`
`
`.QVQVwflWr.mvm.moa..ozmucwumuumucH
`
`er
`m x
`
`HHH.mEDQO>
`
`Sawai Ex 1005
`Page 810 of 4322
`
`
`
`
`1
`
`>u
`
`Sawai Ex 1005
`
`Page 811 of 4322
`
`Sawai Ex 1005
`Page 811 of 4322
`
`
`
`('£'
`
`'-30
`
`i^V.—
`
`Title-
`
`V " I
`
`- \ ^ )
`
`i.nr-2
`
`!.
`
`•
`
`! » -
`•
`• M , •
`:(.} • .
`}'& i
`
`9^-
`itr
`la-nC—
`
`.{U.J[-
`
`• Aipcrs/re. Wx-i.
`U >0 .
`.
`
`•15
`;H--ry I^-
`;.-f..-:6lo.?.
`
`cyr ......
`
`Date
`Cont'd Fc^m-
`
`Proj.
`
`:.i
`%
`
`'
`
`3i0r.4(i •
`
`•
`
`J (^'^^^o-rn'yU?.)
`
`-
`
`( o - o- p
`.
`
`
`
`- ^ 9 ^ ^ •
`
`.
`
`.
`
`•
`
`•
`
`•
`
`
`
`:':
`
`. - . i l l . : ! > "
`j | : ; ^ s
`•__:
`v o ' c r^
`x
`<?"V -S
`
`•
`
`• ' • • • -
`
`• " " " Y
`
`. cUr. .yk;.-.^^4 V
`
`: z.^0- .
`
`•
`
`' " "
`
`'
`
`•
`
`•
`
`i^r
`
`o - -
`•© ; /
`
`£_o>T>Nra(! , ;~Vx> .
`
`4^ -yen^
`
`or,
`
`.
`
`•
`
`v
`
`,•
`
`,
`
`.. ^yuvc{ s ^
`
`J^'VVV-
`
`'
`TK^ : '\.,i-
`
`1
`
`.Vv^ ^ ^ .»>^='7_0_ L ;y.r^ ^
`30.0
`• yy\
`V
`
`""
`
`ov^x^ri
`
`30
`
`36
`
`Performed by-
`
`(2ns (ki-e.(
`
`Witness-
`
`Cont'd to-
`
`•^j
`
`/i
`
`Sawai Ex 1005
`Page 812 of 4322
`
`
`
`aoNVsyossv
`in
`
`s
`
`b
`
`ii'
`I »
`
`i I r
`
`;r- ••
`p
`::!
`J:;. I i:
`jL
`
`i:i|
`i
`
`ili
`Uii
`jLiijii
`
`I
`
`:: :
`
`A^r
`
`&>
`
`§ r-
`
`p
`s
`I'll.
`,4 j-t H'il-l'l|-:i4MillrA-{4'."n"1 "I->
`.;L:
`::u is.d.^j
`.Li:;]!
`i 11!
`•IJj.
`liiiinM
`H tin \\\\ ww ww PIS iiii Hi: iiii
`lil
`iiiil;!!; :M i|!!
`ji jii! j
`i
`i
`iiiii im i^r,.
`,.,
`,
`u
`WMi
`•:i liliiili
`r rrr
`! n
`ill!
`; . . . i . i
`r^l^TqF7-5
`in
`w #1
`n:
`iiii
`
`p
`
`i
`
`I;: •
`; I .
`
`ilh
`:J:
`
`;•[
`
`-:::,r:T7 Trrr TTTT
`WW hi: .illiiiliJ
`iiiMq).;;:
`rt«!
`g
`i-;
`: r.;.f — }::i^ -.-i-;
`:::||rfnp"iiiTlli::
`... ..t. i.,. i^...,,
`i'lii-nTi'jrtl Hi:r
`.liii lilL
`^T-i-E
`:'Fii iij! "!:
`;:::
`:r-
`
`r
`
`< i
`
`8
`5
`
`I I
`sg
`sg
`
`a
`>
`S
`8
`§
`
`1^
`z
`2
`§ g ^
`•:O 3 I
`S IS 3
`o
`
`8
`
`S
`
`li-
`
`o
`s <
`•• 1 F
`m
`>53
`? » I
`o >
`£ o
`1 I 2
`2 to a
`c P 5
`
`• |::L;
`
`i-!: 1 i
`
`i
`:t frfi ri-rr:
`
`IT!
`
`:!;.
`: ri h i
`
`i:;
`
`i •3
`:<v
`
`; : j;
`
`:ST T::
`• c •
`m«
`
`I
`
`Vi
`*
`% o i
`i g >
`
`J-
`
`I
`
`I
`
`(
`
`<
`
`4
`
`i!:,
`« •
`<
`>
`
`r
`
`I • •
`
`• •
`
`ill.
`
`:
`
`rrrr
`
`;[1
`
`c
`
`' M :i; 8 O
`:: I:
`IT
`! :::C
`
`:: :
`
`• I'::.
`
`-trWr
`::: i
`
`•>;: :
`j
`
`•; I
`iixl
`
`frH
`1 »•» f
`u:;
`nil j.:! i ' i i
`
`JJ:.
`
`;:
`
`:S-!rg^§:!-gv
`
`i
`
`i
`
`1
`
`I
`
`»
`
`TT.r*
`
`I
`
`i
`
`J i.:.
`
`:
`
`I
`
`— - r^-
`
`!:fl
`
`• I • '•
`
`h
`•I.
`ipR
`I
`
`B
`
`r
`
`e
`
`c
`
`iiTi "n'l
`
`i'l:
`
`•:::
`n:.:
`:~L
`n;T~n'
`rl-l
`• • >i • g
`:4r: n:'
`: MTV
`ff:
`T^
`
`i^il!
`
`!:r. i J:
`iTlilil'lTi ill I: I:
`
`i:;;
`
`"•/rr
`
`ol .1" '
`
`CD
`ru
`
`=• 'i =
`
`•.<1
`•d
`
`if:'
`
`••I K
`
`5:
`''i Ui S/
`n s a « ^ (5
`
`•T>
`
`* i
`
`i
`
`.t. «• w
`i;
`^ s
`
`T!
`
`; h''
`
`!i
`r;
`U-iJ
`Liii.!;:1|;i
`
`i;
`
`I!: I
`
`i
`
`iiTi
`
`o
`8
`
`' :!<
`
`o
`
`iiliMiiiMii
`iillli
`•]:"
`i 11
`^ipifrp
`:! i'
`Ii Hii -IH ih!::::
`::ii
`:i:: —
`--HT :T"- "t !• :r::
`TTIT -.rf;
`.11.!:
`jH-iiiiitiJjiiiiiiiiii
`•iH ij! Sw
`S
`o £
`y
`
`-u .Jl
`
`4-
`
`3;)
`3 w
`"4, 'I
`ill:\
`
`•
`
`»•- k
`8
`TRANSMITTANCE (%)
`
`s
`
`.r
`
`t.
`C5
`
`ff
`
`5s
`
`j
`
`HR
`m
`*8 S -
`i—
`• * m
`_ ^
`^ S 5
`
`=e
`
`{
`
`—i
`
`VA
`
`S
`1 i
`
`f I"
`
`0 52 O
`
`i;i -x. -J •-o
`•D ^ fO ® •"
`.t O 0.. -il' »J J- i» -fc. •*) -U- 'J tfl O ^ ®
`
`i
`
`>
`
`VJ
`
`.7-
`
`ssasnssssRSSSSSfiif:
`iilii'iijllHkiiiliiirfsit
`:" i'v-r :'l h.:
`cn i
`s
`S
`s
`
`SHIM
`
`o
`•3
`
`c
`
`ll.l'IMBIHHUri
`
`rni" ••••inmH'rirTTniwiiiii"aaaiftiMii
`
`T'i
`
`Sawai Ex 1005
`Page 813 of 4322
`
`
`
`V"
`
`BTSSSSI (R«v. ff
`
`0
`
`X
`
`1
`
`' l
`
`I ' I
`
`i
`
`I
`
`I
`
`1 1 1 ! 1 1
`
`J
`
`50
`2
`• I 1 1 ' 1 | 1
`
`I—i—r
`
`3
`
`"n-r
`
`4
`T
`
`100
`1
`
`T
`
`I
`
`1 1 1
`
`5
`| 1
`
`X
`
`T~™r
`
`J.
`
`1
`
`6
`I | 1
`
`150
`
`7
`
`4
`
`I ' 1
`
`1
`
`T
`
`8
`
`{^k
`
`200
`
`«.
`
`I | i r
`
`I
`
`'H
`
`(
`
`i
`
`-UvTS 6-
`
`SPECTRUM NO.
`
`FX
`
`OPERATOR
`
`DATE
`
`SPECTRAL WIDTH
`
`DATA POINTS
`
`PUMOO m
`
`NO. of ACCUM.
`
`0
`/
`
`IRR. POWER
`
`IRMOO
`
`MENU NO. .1
`
`OBSERVE NUCLEUS
`
`mm
`
`TEMP. _0CTUBEiI_
`
`SOQ
`lb
`UsdM
`
`Sawai Ex 1005
`Page 814 of 4322
`
`
`
`-t; Date ^ if)
`Cont'd From-
`
`Proj.
`
`Title-
`
`187
`
`<;•)
`
`Cc^V-
`
`.
`.
`. . . L ^ V ;
`
`:
`
`' \
`
`^rw '
`
`' T^JL^
`
`: ^
`2.-7 -7- ^ ^
`Ca., W
`a i
`
`C & •' .^B ^ ^2. "J
`
`fyv-i (A^ ^
`
`10
`
`~
`
`•
`
` (
`
`0' * • *
`^ r ^ 5 S
`( 0 O^n^,
`
`i?
`
`—
`
`20
`
`'2o
`
`">^
`
`^0
`
`J
`
`I
`
`"i
`-S:
`
`-Ji
`?j
`E' s
`I"
`
`»:
`'Zi »:
`
`I
`
`.^i
`
`ij
`
`B ti
`I
`
`:•
`
`ei
`
`• .•
`
`c-
`
`• i
`
`S^r
`
`»
`
`kHf* (
`
`s*
`
`.
`
`•|.
`
`:®
`
`•}&$ s
`
`12,514-
`' . . LZ - H
`.
`fL^ ^ ^
`To . ^0(^—1^6-^-? ' V-TTN ci/T-Y
`C A".H - . (pcr^Wxt^-oo'c^.. / ,.
`.^V'Opr^-a. . 6a-
`. <hoC.
`
`CrJ
`Po
`OvAA^v^y
`I
`
`j
`
`^YV+t^ <U).*Lx^
`
`. . ..d
`
`»••; .
`
`^ • • **+
`
`• O '? <$
`
`»
`
`..
`
`' ""V*
`
`Pcvv^
`^ tAA^ .
`Vn+i^ erv^
`&-^K^
`r
`(A^sVlc,^ y-^^f
`r-
`,,' ihy-cj,
`C"\i-0i^.^7>'-3i')
`-VN'W- l x—- ^5
`y
`C
`
`- n > ^ • %
`
`• « ' / . )
`
`0 «•
`
`y^p Ceo
`• 4/yi^
`w,-V^ W o XSnr^f-Q
`^J-31
`f-i (s]- -
`
`Performed by-
`
`"0^
`
`Witness-
`
`^—
`
`.....Zl2"!^
`
`C o n t ' d t o -
`
`-
`
`Sawai Ex 1005
`Page 815 of 4322
`
`
`
`"P
`CTN
`
`V
`
`1
`
`a
`z
`03 >
`1.5 »
`O
`>
`
`.111
`
`H- - |
`""F
`
`t
`
`•h~
`
`:T1— T:
`
`I
`
`i
`
`1
`
`I
`
`rr:.;
`
`+
`
`i
`
`|;
`••!
`1
`
`0.0
`
`400
`
`0.5
`
`1.0
`
`SANDOZ
`
`SPAN
`
`SPAN
`
`>
`o
`
`HOR. ORIGIN
`
`VERT. ORIGIN
`
`J
`
`TRANS. { -^fABSORBANCE (
`
`> INTERLEAVED <
`
`800
`
`1200.
`
`1600
`
`2000
`
`T
`
`1..
`•r—
`
`;1 I
`
`:U
`
`I
`!
`
`TjT
`
`-jr-rr"IT:
`
`i
`
`•
`
`1
`
`1
`
`J :.. 1
`
`r
`1
`
`11
`
`•
`
`i
`
`I
`
`AUXILIARY DISPLAY
`NO. SCAN PAIRS ISAM/BKG) tW1/ >
`STORED (
`
`U
`ir-
`
`>-$Ca/a
`\^5>',irerli
`
`r-.p.^y
`
`let, WJ 7-3/
`
`NOT
`
`QAUP.E Jv^-07-3/
`
`THICKNESS
`
`2i2i
`
`OPERATOR
`
`PHASE
`
`SPECTRUM NO.
`
`2400
`
`2800
`
`3200
`
`3600
`
`WAVENUMBER (cm
`
`•
`
`1
`
`I
`
`rr
`
`I
`
`1
`
`?
`
`I
`
`1
`
`•i-
`
`•
`
`•-4
`
`1:: 1
`
`4000
`
`HEM.
`
`DATE
`
`4400
`0
`
`10
`
`20 tr
`
`fcjr
`
`x
`
`1
`
`J
`
`!
`x
`
`4-
`
`+
`
`jp:
`
`40
`
`4?.
`h':- • T J
`ti7. 7 ?
`43. «•>
`C
`ev.tc
`."4. 4
`
`•>9E:ADT
`?36£.7
`!.!..• suse.;
`.!"2?. 1
`n
`w:rc. ;
`1 -3?.?. ?
`1C3S. 'i
`: •iO j
`
`H 50
`<
`('2
`
`t 60
`<
`z
`UJ
`
`70
`
`j
`
`Sawai Ex 1005
`Page 816 of 4322
`
`
`
`j'V.'
`
`ON
`
`8736V9I (Riv. II
`
`0
`
`\
`
`' T
`
`1
`
`I
`
`I ' 1
`
`«
`
`j.
`
`1
`I
`
`T
`
`Tr
`
`50
`1
`2
`
`J.
`
`T T
`
`X
`
`3
`
`T—r
`
`T
`
`V
`
`SPECTRUM NO.
`
`OPERATOR gQQ
`
`FX
`
`DATE
`
`SPECTRAL WIDTH
`
`DATA POINTS
`
`NO. olACCUM.
`
`A
`
`PUMOO
`
`IRR. POWER
`
`IRMOD
`
`MENU NO.
`
`T
`
`T
`
`T
`
`T
`
`I
`
`I
`
`I
`
`T
`
`6
`
`100
`
`4
`
`X
`5
`
`X
`
`_L
`
`150
`1
`
`•
`
`200
`
`8
`
`13,
`
`T
`
`1
`
`I
`
`' '
`
`1
`
`| 1
`
`T
`
`T
`
`'H —l—I—[•
`
`(
`
`Sawai Ex 1005
`Page 817 of 4322
`
`
`
`j
`
`145
`
`m
`
`C H & . . . .
`
`•••( ..
`
`!C H
`i
`r l ? ?
`
`:
`
`:
`•
`
`5
`
`10
`
`15
`
`20
`
`Cb.c).. •^J.
`Wc> AloJ3.oV CA^tis .
`4^.1'v^w. '
`' NpA-W-^.. .-te. ...d^vvi^s./.
`; a.,»/.e C 1^.9.. c\.ftos-.\^:C-.2s;C) .;..i^v,.| :..!2; i-jias- ^T-rJ?f,
`sJl
`. 0%s C>~\AT.--..xf?) ... !>.^v.,.L \x
`l^>.- .V)^+-.Z9&
`
`•
`
`..„.
`
`5
`0
`
`;
`'VcArts VO
`
`.-V'
`
`CrJ-0
`
`. B O .-VN j $
`
`tvU^'cX^ 4vv-^<
`
`30
`
`••^-\' 'y-> Vi
`A 1 '^ov^d1;
`
`( p '
`
`'
`C--
`C?A;<U-H,.I
`
`T\ e c ^ : 7 - R I ^
`
`•Tc>b:-.l -y /fi-f <4
`
`<£• • <S
`
`- S Z' / . J
`t! v 4"
`
`A6 cT-
`cvioa-i^s-v,;
`
`I
`
`s.
`
`Cont'd to-
`
`" j\^i''"
`
`Performed by-
`
`Witness-
`
`ip >^8 m
`
`(i^.
`
`1®
`
`V Date 6-17-^
`Cont'd From-
`
`Proj.
`
`Title-
`
`: "
`
`•f.. , •
`
`»s^
`
`• r "•*
`
`r^P;
`
`Uc>k-:\39-^
`;
`^ . .
`
`•••
`
`•
`
`*2-'? '?' \
`
`-^'V
`l^L ^(jr" ^ ^7
`. ,
`P^on.^'X •
`•
`: . » . .
`
`- -
`
`-".S .:0.
`. 1 6 ' . 0 ; _
`.( Sb..:..r—
`c
`
`1
`
`^fo ^
`:^j2_G.\.bte'l ; ^ ^
`
`k>:
`'..'v^rv^^r- •-- G'-r1'-
`
`; C^/txs
`••;-•
`•:—•• •
`
`U. T' •
`
`* f y
`
`^ f- M -
`: O" O ' O : • ;
`^
`O- > •)
`• • O'
`
`•^4
`
`J),
`
`ii:
`—
`
`'J -I
`
`3;
`Jf
`i-Ar ~J?.
`
`k
`
`V-oS
`
`^r'T"'
`pi.' -
`
`-
`
`;V8v
`
`•': iS
`
`^BSi
`
`"•*%•
`
`t-rt"?®
`
`Sawai Ex 1005
`Page 818 of 4322
`
`
`
`9o
`
`6735981 (fltv. 1}
`
`0
`
`X
`
`1
`
`III "|"r T-T
`
`I
`
`T
`
`Jy •
`
`I
`
`1
`
`1 1
`
`M
`
`. AVJO
`
`SPECTRUM NO
`
`cr«
`
`•7
`
`1
`
`50
`1
`2
`I
`
`1
`
`-Job
`UHM
`
`FX
`
`OPERATOR
`
`DATE
`
`SPECTRAL WIDTH
`
`iQ-
`MENU NO. a
`OBSERVE NUCLEUS JL m
`9C TUBE J" m
`
`L
`
`TEMP.
`
`DATA POINTS
`
`NO.of ACCUM.
`
`PUMOO
`
`1RR. POWER
`
`IRMOD
`
`1
`
`' I ' 1
`
`1 1
`
`3
`I
`
`• 1 1
`
`1
`
`' ' I
`
`X
`
`4
`
`100
`1
`
`±
`
`5
`T T
`
`150
`1
`
`6
`
`I
`
`I
`
`T
`
`-L
`
`J.
`
`7
`
`T
`
`8
`T I T
`
`200
`1
`
`"C
`
`T-T
`
`1H
`
`[
`
`c«
`
`/
`
`}J\.
`
`Sawai Ex 1005
`Page 819 of 4322
`
`
`
`.inr/ ^
`
`FX
`
`DATE
`
`J>
`CV.
`
`Sr>
`v>
`
`873 SSfSI IR«v. 1)
`
`0.
`
`1
`
`l
`
`I
`
`l | I
`
`T
`
`T
`
`^-1 .
`
`•L
`
`TT
`
`50
`1
`2
`
`
`
`')'
`
`I11'
`
`X
`3
`T M
`
`4
`
`T
`
`100
`1
`
`JO^
`
`SPECTRUM NO
`
`SPECTRAL WIDTH
`
`DATA POINTS
`
`NO. o( ACCUM. JLO
`
`PUMOD
`
`IRR. POWER
`
`'Ji
`OBSERVE NUCLEUS
`TEMP. _0C TUBE jLmm
`
`MENU NO. 0
`L
`
`IRMOO
`
`OPERATOR 900
`HE
`fnhf/il
`
`5
`
`r'nv
`
`J
`
`I**
`
`150
`1
`
`6
`
`7
`
`r ' r T
`
`T
`
`T
`
`f-r-j-
`
`8
`
`200
`1
`
`"C
`
`I
`
`•
`
`' I
`
`I
`
`I
`
`'H —r
`
`/
`
`c
`
`(
`
`Sawai Ex 1005
`Page 820 of 4322
`
`
`
`• 7 . Date
`6-. g^Proi
`Cont'd From-
`
`Title-
`
`f
`
`'
`
`
`
`•
`
`,
`
`0
`,
`
`.
`
`.,... . ^
`
`.. • • ; -
`
`, h, »
`
`153
`a?2.
`
`"f-
`
`5
`
`Z-? Z
`
`C^o s;
`
`( ,\^oC-
`
`.
`
`, PfiaptZy—
`
`(\^4;
`
`G
`
`10
`! ^-554-
`•
`^ ^Co.-o^ A jcpf'toAi
`'
`i' 1
`\ L--^ ^ S-
`":
`:
`V^vJLMaV '^JL -
`- . ;
`'" •;
`.•g - 6 [Z 'S ^ 'cq- oa V pg^jv^oi^ (-izQ^a A-
`15
`
`*=
`
`:...
`
`1
`
`-I
`
`Re{ :
`
`6 ^
`
`- -i
`
`•
`
`A\3&O^
`
`0^€~pP CMJ>
`C N'e^ V v^W".
`'7^lS2
`«• f
`
`.'
`
`vyi.^'X--
`(r>Po^''M'!i^
`^
`
`'Y- '• £ ^
`..-^vU...\.i^2. io'V"'5--; ^Sin'TY^dl .:o4.V. 't\-
`
`20
`
`o
`^:. : :::%
`. o
`S'A
`•••••,?::•¥,;
`.•;:
`.
`. %
`^Vf-, 567. ^aP Lf?M ^Ttsj-y f,"
`'JLJl.> 9^
`T>v t wW cl
`CN ^Uc^A C-Vev ^ CIT^ VvC s $"
`g
`4^VcJ^
`* A
`op-f
`(^eo\-t . q&v-e
`OvvVt)
`^Tv, ^ v - V7 : v- 1 1 ^ ^
`^ : U C^-]^3