02;. United States Patent
`Davis et al.
`
`(10) Patent N0.:
`(45) Date of Patent:
`
`Us 7,053,080 B2
`May 30, 2006
`
`US007053080B2
`
`(54) METHODS AND TIIERAPEUTIC
`(I()MBINATIONS FOR TIIE TREA'l‘MlCN'l' 0|"
`OBESITY USING STEROL ABSORPTION
`]NI]IBI'[‘()RS
`
`(75)
`
`Inventors: Harry R. Davis. Berkeley lleighls, NJ
`(US): Rudyard J. Ross. Elemingtoil. NJ
`(US): John '1‘. Struny. Lebanon. NJ
`(US): Enrico P. Vcltri. Princeton, NJ
`(US)
`(73) Assignee: Scliering (fnrpnratitin. Kenilworlli. NJ
`(U5)
`‘
`‘
`_
`_
`‘
`Subject to any d1scla1n1er_. the term 0111118
`patent is extended or adjusted under 35
`U.S.C. l54(b) by 295 days.
`
`‘
`( * _| Nottce:
`
`(21) Appl. No.:
`
`l0a'247,397
`
`(223
`(65)
`
`Ffled;
`
`sep_ 19‘ 2002
`Prior Publication Data
`US 2[}()3fUl 19428 A1
`Jun. 26. 2003
`
`Related U.S. Application Data
`,
`_
`_
`‘
`_
`,
`\
`(63) Continuation-n1-part 01 application No. 101166.942.
`filed 01111111. 11, 2002-
`_
`I
`.
`.
`l2’1]'o\:*z1(:;3Jln(11 application No. 607323.840, filed on bep.
`’
`‘
`
`_
`(60)
`
`(51!
`
`1111- CL
`/161K 3I/00
`A6IK 3}/7028
`A6IK 31/397
`
`C07H 17/00
`(523 U.S. (II.
`
`(200601)
`(2006.01)
`(2006.01)
`
`(2006.01)
`514,210.02; 514723; 514125;
`5141449;
`
`5]-‘U25,
`(58) Field of Classification Search
`514723. 210.02, 449; 536."l7.4
`
`BF.
`
`4.260.743 A
`4.304.718 A
`4.375.475 A
`4.443.372 A
`4.444.784 A
`
`4-472-399 A
`4-479-999 A
`4'599'459 A
`
`.
`.
`4667195 A
`K
`4.576.753 A
`4.581.170 A
`4‘_;g_-3532 A
`4.502.003 A
`4.602.005 A
`4.614.614 A
`4.616.047 A
`4.620.867 A
`
`4.626.549 A
`4.633.017 A
`4-643-903 A
`4.654.362 A
`4.675.399 A
`
`4.680.289 A
`4.680.391 A
`4.687.777 A
`4_;r39.1m A
`4.778.883 A
`4.134.734 .4
`4_?94J08 A
`4.300.079 A
`4.303.266 A
`4.314.354 A
`4.334.846 .4
`4.871.752 A
`
`4.-" 981 Bose
`12.-" 981 Kamiya
`9533 Willard
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`7.-' 935 3»1,1|im,w
`7.-" 986 Nlalinow
`9.-" 986 Ernest
`10.-" 986 Lafon
`11:" 986 Ltlo
`
`12.-" 986 Nlollltluy
`12.-" 986 .\-"l1I¢ CI‘
`2-"' 987 Dam
`3.-" 987 Lommcn
`6.-" 987 .\4i11ci'
`
`987 Applczwcig
`7-" 987 l'II'cSt0nc
`8.-" 987 .\4cgl1i'o ct a1.
`4; 933 Bourgognc
`10.-' 988 Yoshioka
`II.-" 988 Torii
`12:, 988 Kishimoto
`1:" 989 Boyer
`2.-" 989 Knwashiimr
`3.-' 989 Ghcbrc-Scllassic
`95:9 Abrmnson
`10.-" 989 Zcrinalter
`
`[:(:Qntinued)
`‘
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`884722 A
`I2.-‘I980
`
`See application file for complete search history.
`
`((jm]1jmwd)
`
`(Sf?)
`
`References Cited
`
`OTIIER PU'Bl.lC/\Ti0NS
`
`U3 PA,I.].N.I.
`
`|)O(.UM|_.N.l.S
`
`The Merck Manual, 159' Edition. 1987. p. 9533*
`
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`
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`3-" 995 H¢I'|1h'|-US
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`9: 972 _\le1s0n
`2:" 973 _\lak;unuIa
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`4: 975 Phillips
`2.-".978
`.\'Iicvil1c
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`4-“.979 (jiudic-2111
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`13"-979 E"_9¢i_3
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`
`"(jm]1inm:d)
`‘
`1’rimari-‘ L:'.mi::iJ3er—.1z1n1es O. Wilson
`./Issisfaiit E.wm:'Jrer Ganapathy Krishnan
`(74)AHorrrct‘.Age.m'. 0rFirm—Mark W. Russel1:An11 Marie
`Canmni
`‘
`
`(57)
`
`.
`ABSTRACT
`
`The present invention provides methods for tl1e treatment of
`obesity using stern] or 51:.-slanol absorption inhibitors and
`compositions and therapeutic combinations including sterol
`or Su.-slanol absorption inhibitors and at least one obesity
`coulrolinedicatioii.
`
`I of 43
`
`35 Claims, No Drawings
`
`PENN EX. 2234
`
`CFAD V. UPENN
`IPR20l5-01836
`
`

`
`US 7,053,080 B2
`Page 2
`
`U_S, PATENT DOCUMENTS
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`IPR20l5-01836
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`

`
`US 7,053,080 B2
`Page 3
`
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`12.31997
`131998
`231998
`431998
`7.31998
`731998
`731998
`1031998
`1031998
`1231998
`2.31999
`2.31999
`2.31999
`3.31999
`331999
`3.31999
`4.31999
`4.31999
`431999
`431999
`4.31999
`431999
`5.31999
`631999
`831999
`8.31999
`831999
`931999
`9.31999
`931999
`12.31999
`12.31999
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`3.32000
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`432000
`4.32000
`432000
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`532000
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`
`US 7,053,080 B2
`Page 4
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