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`
`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
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`
`Sawai Ex 1005
`Page 789 of 4322
`
`

`

`16
`18
`24
`70
`91
`95
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`12/13/84
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`
`Sawai Ex 1005
`Page 790 of 4322
`
`

`

`--cr
`KJ
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`12/14/84
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`
`10-8
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`
`Sawai Ex 1005
`Page 791 of 4322
`
`

`

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`Sawai Ex 1005
`Page 792 of 4322
`
`

`

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`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
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`32
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`2) 62-320/Na-4(23531) 6/13/05
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`
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`
`Sawai Ex 1005
`Page 795 of 4322
`
`

`

`CS
`
`X2582A
`
`12
`40 -
`84
`
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`6/13/85
`
`8) 63-550(RN 26083)
`
`7) 63-549(RN 26082)
`
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`63-548(RN 26080)
`
`6)
`
`Sawai Ex 1005
`Page 796 of 4322
`
`

`

`oo
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`
`5
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`6/10/05
`
`DMA
`
`10) 62-320/Na-4(23531) 6/10/05
`
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`11) 63-551(RN 26004)
`
`10-°
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`
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`
`D
`
`6/10/05..
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`
`10-°
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`10-6
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`10-4
`IO"3
`IO"2
`
`Sawai Ex 1005
`Page 797 of 4322
`
`

`

`C/^
`
`33
`54
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`
`16) 62-320/Na-4(23531) 6/19/05
`
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`15) Compactln (24291) 6/19/05
`
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`
`Sawai Ex 1005
`Page 798 of 4322
`
`

`

`1
`10
`/ 60
`
`•4^
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`3
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`07
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`
`6/19/05
`
`20) 63-563(RN 26127)
`
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`
`6/19/05
`
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`19) 63-550/2 Na(RN 26100)
`
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`
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`
`6/19/05
`
`10) 63-559(RN 26106)
`
`10-0
`10-7
`10-6
`-10-5
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`TO"3
`. TO"2
`
`•
`
`Sawai Ex 1005
`Page 799 of 4322
`
`

`

`Ko
`
`6
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`94
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`
`3
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`.03
`
`.98
`.96
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`.70 •
`.33
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`
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`
`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
`
`"
`
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`IO"7
`10-6
`IO"5
`IO"4
`io-3
`IO"2
`IO"1
`ImM
`
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`DMA
`
`6/19/85
`
`22) 63-565(RN 26128)
`
`io-5
`io-4
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`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
`
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`6
`6
`9
`15
`24
`73
`
`7
`
`103
`106
`97
`97
`88
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`94
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`
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`76
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`
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`
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`.70
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`
`6/24/05
`
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`
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`6/24/85
`
`10"°
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`
`28) 63-560(RN 26107)
`
`10-0
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`lO"6
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`
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`
`27) 63-568(RN 2615X)
`
`DMA
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`10-2
`
`.
`
`6/24/85
`
`26) 63-567(RN 26149)
`
`Sawai Ex 1005
`Page 801 of 4322
`
`

`

`"H or*
`
`1
`6
`23
`51
`88
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`4
`9
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`32) 63-556.(RN 26093) 6/26/05
`
`DMA
`
`DMA
`
`31) 62-320/Na-4(23531) 6/26/05
`
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`30) Compactln (24291)/ir6/26/05
`
`GV Ct-f
`
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`
`Sawai Ex 1005
`Page 802 of 4322
`
`

`

`(J-v
`fc
`
`"\
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`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
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`80
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`10/8/87
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`10-2
`
`Sawai Ex 1005
`Page 804 of 4322
`
`

`

`oo
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`
`Sawai Ex 1005
`Page 805 of 4322
`
`

`

`0257
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`Sawai Ex 1005
`
`Page 806 of 4322
`
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`
`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
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`Z) 62-320 (21135)
`

`
`Sawai Ex 1005
`Page 808 of 4322
`
`

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`Sawai Ex 1005
`Page 809 of 4322
`
`

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`Sawai Ex 1005
`
`Page 810 of 4322
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`Sawai Ex 1005
`Page 810 of 4322
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`Page 811 of 4322
`
`Sawai Ex 1005
`Page 811 of 4322
`
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`Sawai Ex 1005
`Page 812 of 4322
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`Sawai Ex 1005
`Page 813 of 4322
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`

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`Sawai Ex 1005
`Page 814 of 4322
`
`

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`Sawai Ex 1005
`Page 815 of 4322
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`Sawai Ex 1005
`Page 816 of 4322
`
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`Sawai Ex 1005
`Page 817 of 4322
`
`

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`Sawai Ex 1005
`Page 818 of 4322
`
`

`

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`Sawai Ex 1005
`Page 819 of 4322
`
`

`

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`Sawai Ex 1005
`Page 820 of 4322
`
`

`

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