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`utility of 1h: ‘mvaution. Define any terms that may have a special meaning. 'Give examples 0r relcVam cimtinnéi, fiNhOIS, etc, if
`known. Home attach a copy of the newer shm pcxflngnt claims, and abstract.
`* T-itlc oflnvention: 1‘ M \DL :0 If RU/F'VTU/L S (3% E, (\ LT‘S T [.4 E, {A}: (347?”
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`CM1 mgrmveweammf‘“
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`SAWAIR 1015
`Page 534 of 1092 PTO_00000535
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`09/529096
`
`Page 1
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`w) fil reg; d fitat qua 18; iii capl; d qua n05 l9
`
`FILE 'REGISTRY‘IENTERED AT 15:59:09 ON 21 AUG 2000;}
`USE IS SUBJECT TO THE TERMS OF YOUR fiTN CUSTOMER AGREEMENT.
`PLEASE SEE "HELP USAGETERMS” FOR DETAILS.
`COPYRIGHT (C) 2000 Amexican Chemical Society (ABS)
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`STRUCTURE FILE UPDATEfi:
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`L6
`
`STE
`
`2
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`@c:
`
`@3
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`Na
`5
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`NODE ATTRIBUTES:
`DEFAULT MLEVEL IS ATOM
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`DEFAULT EChEVEL IS LIMITED
`
`GRAPH ATTRIBUTES:
`RXNG(3) ARE ISOLATED 0R EMBEDDED
`NUMBER OF NODES IS
`23
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`STEREO ATTRXBUTES: NONE
`L8
`172 SEA FILEMREGISTRY SSS FOL L6
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`100.0% PROCESSED 102627 ITERATIONS
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`PLEASE SEE "HELP USAGETERMS" FOR DETAfiLS.
`.
`Seaxched by Barb O'Bxyan, $TIC 308-4291
`
`SAWAI EX. 1015
`
`Page 536 of 1092
`
`PTO_00000537
`
`SAWAI EX. 1015
`Page 536 of 1092
`
`

`

`Panml
`
`09/529096
`
`Page 2
`
`COPYRIGHT (C) 2000 AMERICAN CHEMICAL QOCIETY (ACS)
`
`the artiwles to which records in this database refigr is
`Copyright mf
`hald by the publiahers liated in the PUBLISHER (PH) fiald (availabla
`fior xacordm publiahad an updated in Chemical Abstxacts aften Decamher
`26, 1996), unless atherwise indicatad in the original publicatiuns.
`
`F113 COVERS 1967 n 21 Aug 2000
`FILE LAST UPDATED: 20 Rug 2000
`
`VOL 133 158 9
`(20000820/30)
`
`Thifi filw contains CA3 Registry Numbara for @asy and accurate
`fiubstancfi id$fltifiicat10n,
`
`This file supports RmGlskRY for direct bxowslng and fiearching mf
`all substanme data from the REGISTRY Eile. Enter HwL? FIRST fiat
`mora information,
`
`Now yuu can axtemd your author, patent assignam, patent inflammation,
`and title searchas back to 1907.
`The records from 1907~1966 now have
`thia searmhablm data in GAOLD.
`You now have Electronic accasfi to all
`of CA: 1907 to 1966 in CAOLD and 1967 to the preaent in GAPLUS on STN.
`
`L6
`L8
`1,91
`
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`112 am FILEmREGISTRY sss FUL 1,6
`6 mm Ethwmpms mama»:
`1,3
`
`m} d ibib abs hitsur l9 l~6;ȣ11 cam; d qua nos 110
`
`ANSWER 1 OF 6
`L9
`ACCESfiION NUMBER:
`DOCUMENT NUMBER:
`TITLE:
`INVENTOR1S):
`
`PATENT ASSIGNEE(S):
`swam:
`DOCUMENT TYPE:
`LANGUAGE:
`FAMILX ACC. NUM. COUNT:
`PATENT INFORMATION:
`
`COPYRIGHT 2000 ACS
`CAPLUS
`1999:282201
`CAPLUS
`'
`‘ 1302311793
`preparatian of amidem a3 antidiabaticm
`Maruyama, Tatsuya; Suzuki, Takayuki; Onda, Kanichi;
`Hayakawa, Mafiahiko; Moritomo, Hiroyuki; Kimizuka,
`Watsuya; Matsui, Tetsua
`Yamanouchi Pharmaceuuimal 00,, Ltd.,
`PC’I‘ Int. AWL, 45 pp.
`CQDEN:
`?IXXU2
`Patent
`Japanese
`1
`
`flapan
`
`PATENT NO.
`
`K1ND DATE
`
`,APPLICATION NO.
`
`DATE
`
`19.981015
`wo 1998~~JP4671
`19990429
`A1
`1709920607
`cm,
`(310,
`1369, an, m, CA, CN, cu, <32, m1,
`w:
`AL, PM, AU, AZ, BA, BB,
`IS, JP, KE, KG, KR, KZ,
`11C, LK, LR, LS,
`1311, GM, HR,
`rm,
`1):),
`In,
`m, 1"], MD, MG, MK, MN, MW, pm, No, NZ, E’L, no, RU, 5m, 59:, 53:,
`SK, 81., TJ, TN, TR, TT, UA, us, us, uz, 1m, m, w, AM, AZ, BY,
`KG, KZ, MD, RU, TJ, m
`w: GH, GM, KE, LS, MW, so, 52, US, ZW, M, BE, CH, CY, DE, DK, ES,
`m, FR, GB,
`can,
`IE, 11‘, LU, MC, NL, PT, SE, BF, BJ, CF, CG,
`0:12,
`CM, GA, GN, GW, ML, MR, NE}, SN, TD, m
`AU 9889288
`A1
`19990506
`AU 1998—89288
`19981013
`AU‘9894621
`Al
`19990510
`AU 199$MB4621
`19981015
`1? 1023111
`A1
`30000816
`ER 199BM947894
`19981015
`R:
`AT, BE, CH, DE. DK, ES. FR, GB. GR, IT..LI. LU. NL. SE, PT,
`Saarched by Barb O'Bryen, STIC 308*4291
`
`IE,
`
`F1
`
`SAWAI EX. 1015
`
`Page 537 of 1092
`
`PTO_00000538
`
`SAWAI EX. 1015
`Page 537 of 1092
`
`

`

`Patel
`
`09/529096
`
`Page 3
`
`CN 1218045
`NO 2000001983
`INF01!
`PRIORITY APPLN.
`
`A
`A
`
`19990602
`20000414
`
`OTHER SOURCE(S):
`GI
`
`MARPAT 130:311793
`
`CN 1998~121375
`NO 3000w1983
`JP 1997w23§213M
`W0 1998wJP4671
`
`19981016
`20000414
`19971017
`1998101$
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`[ring 8 n
`The title aompds‘ I
`an optionally substitutad hetarmaryl
`a bond,
`lower alkylene at lmwar
`optionally fused with a bmnzana ring; X #
`alkenylene (optionally subltituted by hydroxy or lower alkyl), cathonyl,
`ox NH (fiuxthex detall$ related to X ara given); A m a lower alkylane or a
`grmup repremented by (lower alkylene)wo: Rla and Rlb % hydrogam an lowar
`I
`alkyl; R2 m hydxogen 0r halogano; and Z w nitrogan or CH] ara pxapd,
`are maeful as diabatas remediaa whiah mat iny function to accalexate the
`sacration of insulin and enhance inaulin Sensitivity but also have an
`antiwobesity action and an antihyperlipemia amtxan based an thair
`imidazole
`salactiva
`$timulativa actian on
`.bmta.3 receptor.
`For example,
`deriv.
`of this invention significantly decreased
`II was pxepdn
`Compds.
`blood sug&r in mica.
`223672«11—5?
`223672—DBWIP
`223672m10W4P
`22367ZM12-69
`223672—13*7P
`223672-14-99
`223612—15~99
`223672~16~0P
`223672W17H19
`223672“19“3P
`223672W20W6P
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`223672-24~OP
`223672~25~19
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`223672-27—3?
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`223672 77 3?
`22$672-75-1P
`223672-76-2?
`223672 -~BO--EE’
`223672~78de
`223672--79—5P
`Saarchad by Barb O'Bryan, SWIG 308— 4291
`
`SAWAI EX. 1015
`
`Page 538 of 1092
`
`PTO_00000539
`
`SAWAI EX. 1015
`Page 538 of 1092
`
`

`

`Patfil
`
`09/529096
`
`Page 4
`
`RZESVZMBZWOP
`223672“85U3P
`223672-88-69
`223672M91W1P
`22367ZMSKM4P
`223672-97-79
`223673’00DSP
`22367EWO3m8P
`223673‘06“1P
`223673w09w4?
`223673*12-BP
`223673~15"2P
`223673-18-"P
`223673‘ZIHOP
`223673W25W4fi
`2ZBSVEW2G~VP
`223673-31DZP
`223673~58fl3$
`223673—61—8?
`223673-64-19
`
`223672-83-1?
`223672-86~4P
`223672we9-7P
`223672”92*2P
`223672-95-5F
`22367ZAQBMEP
`223678WOIWGP
`223673-04-9?
`223673~07~2P
`223573m10va
`223673-13-0P
`223$73“1fiw3?
`223673-19-6P
`223673~22~19
`223673w26w5?
`223873-29wfiP
`223673“32*3P
`223673~59-4P
`223673-62-9?
`223673~65w2P
`
`223672mfilm99
`223672wfi4-2?
`223672W87~5P
`223672“BOMOP
`223672-93-BP
`223672—95-69
`223672-99-9P
`223673W02W7P
`223673~05*Ofi
`223673»08w39
`22367BWIIWBE
`22367BW14-IF
`223673~17~4fi
`223673-20*99
`223673W23w2fi
`'223673-27*BP
`223673“30“19
`223673~33~49
`223673-80-79
`223673-63-09
`223673M66W3?
`RL: BAG (Biolmgical activity or effector, exaept adverae); SPN (Synthatia
`preparation); THU (Therapeutic use); BIOL (Biological 5tudy); PREP
`(Praparanion); USES (U$&$J
`(prepn. Df amides as antidiabetics)
`223672m09m1
`CAPLUfi
`3-Pyridinecarboxamide, N—[a-[Z—[[(2R)—2-hydroxy»2w
`phanylathyIIumino}fithyllphenyllw, dihydrochloride (QCI)
`
`RN
`CN
`
`(CA XNDEX NAME)
`
`Absolute ataxaochamifltny,
`
`02 HCl
`
`RN
`CN
`
`CAPLUS
`223672m10w4
`8wQuinolinecarboxamida, Nw[4~«[2~[((2R)w2mhydroxyw2w
`phenylehhy13amino]ethlephenleW, dihydrochloride (9C1)
`
`(CA INDEX NAME)
`
`Absolutfl finaxaoahamifitxy.
`
`Smarchad by Barb O'BrYan, SiIC 308w429l
`
`SAWAI EX. 1015
`
`Page 539 of 1092
`
`PTO_00000540
`
`SAWAI EX. 1015
`Page 539 of 1092
`
`

`

`Best Available Copy
`
`Patel
`
`09/529096
`
`Paga 5
`
`H
`
`HORN}?
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`m
`
`H
`
`/// NT
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`
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`223672wllw5
`2~Propenamida, N-[4~[2—L[(2R)‘Z—hydroxym2~phenylethyl]amino]ethyl]phenyl]—
`3w¢2*pyzidinyl)~, dxhydrochloride,
`(ZE)W (961)
`(CA INDEX NAME)
`
`Absoluta atanamahamifitry,
`Doubla bond geomatxy as shown.
`
`23b
`5
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`
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`223672w12w6
`2wEanzothiazoleametamide, Nm[4w[2m[[(2R)m2~hydxoxyw2w
`phmnylathyllaminolathyljphenleW, dihydrochloride (901)
`
`(CR INDEX NAME)
`
`Absmlute finereochemiatry.
`
`a?“
`
`S
`
`/0
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`
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`
`223672w13—7
`
`CAPuUS
`
`‘
`-
`Searched by Barb O'Bryen, STIC 308~4291
`
`SAWAI EX. 1015
`
`Page 540 of 1092 PTO_00000541
`
`SAWAI EX. 1015
`Page 540 of 1092
`
`

`

`Patel
`
`09/529096
`
`Page 6
`
`CN
`
`Imidazo[2,1~b]bhiazolews—acetamida, NMI4w[Z~[I(2R)—2-hydraxy'2»
`phenylethyl]amino]ethyl]phenyl]~, dihydrochloxide (BCI)
`(CA INDEX NAME)
`
`Absolute fluexaachemistry.
`
`9h
`
`1, V NA
`II. J
`f 1 M ,
`
`,1
`
`[M
`
`
`
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`
`RN
`0N
`
`CAPLUS
`223672w14w8
`4~Thiazoleacatamidg, N—[A—[Z—[[(2R)-2mhydxoxy—2—
`phenylethyljamino]ethyllphenyl]m2wmethylw, dihydrochicride (QCI)
`INDEX NAME)
`
`(CA
`
`Abaolute svereochemistry.
`
`N
`we“? “7/“ \I/wo
`59ml
`H‘N\ ”I,
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`Kx /* “MAN 1/“ng”OH
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`223672»15~9
`1H~ImidazmlQWZflametamide; Nwl4"[2m[[(2R)w2whydroxy"2w
`phenylethyllanunolethyl]phenyl]w, dihydtochloxide (9C1)
`
`(CA INDEX NAME)
`
`Absolute stereochemistny.
`
`Searched by Barb O'Bryen, STIC 308w4291
`
`SAWAI EX. 1015
`
`Page 541 of 1092
`
`PTO_00000542
`
`SAWAI EX. 1015
`Page 541 of 1092
`
`

`

`Fatal
`
`09/529096
`
`Page 7
`
`Nx¢
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`CAPLUS
`223672w17~1
`1H—1,2,Amwriazolew3macetamide, 2,5wdihydrOMNME4w[2wf[(2R)w2mhydroxyw2w
`phanylmtbyl]amino]ethyl}phenyl]wfimthioxww, monmhydroahloride (SCI)
`(CA
`INDEX NAME)
`
`Absalute sterwoahemiutry.
`
`“NV/x“my/«\fyo
`)/ H
`
`
`
`3
`
`0 Hal
`
`Searched by Barb O'Bryen, STIC 308w4291
`
`SAWAI EX. 1015
`
`Page 542 of 1092
`
`PTO_00000543
`
`SAWAI EX. 1015
`Page 542 of 1092
`
`

`

`Fatal
`
`09/529096
`
`Page 8
`
`RN
`CN
`
`CAPLUS
`223672m18m2
`4~Thiazoleacatamide, Zwamino~N~Iqwt2M[[(2R)~2—hydrmxyw2m
`phenylethyl]aminolathyllphenyllm, dihydrmchloride (QCI)
`
`(CA INDEX NAME)
`
`Absolute stareochamiatry.
`
`H2N
`Nx\ w,/W\~T/,
`~-\N'
`
`
`
`O 2
`
`1163.1
`
`RN
`CN
`
`
`CADLU$
`223672“”9w3
`l,2,4»Thiadiazcle—3—acetamide, SwamiHOMNMEA-[2*I[(2R)~2—hydroxy~2—
`phanylmthy11aminm]ethyLJphmnyllw, dihydxochlorida (QCI)
`(CA INDEX NAME)
`
`Absoluta stereochemimtry.
`
`3\
`
`>311
`$le
`x111
`112“]? /:L ‘
`
`‘
`
`‘
`
`,1
`
`02 HCLL
`
`RN
`CN
`
`CAPLUS
`223672m20w6
`Carbamic acid,
`[3~[2w[[4m[2w[[(2K)w2~hydr¢xy«2w
`phenylathyllamino]ethyljphenleaminolmZ—oxoehhyl]«l,2,4wthiadia20lv5wyl]"y
`@thyi @5Lcr, monohydrotharida (QCI)
`(CA INDEX Nnmm)
`
`Absmluta atareochemiaury.
`
`seaxahed by Bach O'Bryan, 5%IC 308m4291
`
`SAWAI EX. 1015
`
`Page 543 of 1092 PTO_00000544
`
`SAWAI EX. 1015
`Page 543 of 1092
`
`

`

`Panel
`
`09/529096
`
`Page 9
`
`Eto
`
`N‘
`H
`
`’
`
`0 Mil
`
`RN
`CN
`
`CAPLUS
`223672—21—7
`AHThiazolaacatamida, 2m[(3Mfluormphmnyl)aminoijw[4w[2w[I(2R)m2mhydroxyw2w
`phenylathyl]aminoxethyllphenyljw, dihydrochloride (SCI)
`(CA INDEX NAMEY
`
`Absnlute steraochemi$tty.
`
`N
`
`Ex (KI/Rf :/7/\ /°
`Lwfi/Lx/Vw \xNMf‘VNW077!
`
`HNK /Ȣ%
`
`1
`
`[\N%
`
`s
`
`Ph
`
`.2 HC].
`
`RN
`CN
`
`CAPLUS
`223672m22w8
`2waxidineacetmmide, 6»chlor0»N~[4u(2~[[(2R)~2-hydroxyw2m
`phenylathyl]aminQJathyljphanleM, monohydrochloride (90X)
`
`(CA INDEX NAME)
`
`' Absaluta staraochemistny.
`
`Egh
`E
`
`H
`
`0 H63.
`
`Searched by Barb O'Bryen, STIC 308M4291
`
`SAWAI EX. 1015
`
`Page 544 of 1092
`
`PTO_00000545
`
`SAWAI EX. 1015
`Page 544 of 1092
`
`

`

`Patel
`
`09/529096
`
`Page 10
`
`RN
`CN
`
`CAPLUS
`223672w23m9
`Zwaridinaaaetamide, NMIQWIZWIE(2K)“2“hyd30XY“2“
`phenylehhyl]aminojethlephenyl]—6w(phenylmethoxy)fi, monohydroahloride
`(9C1)
`(CA INDEX NAME)
`
`Absolute stereochemistry.
`
`
`
`0 Hal
`
`RN
`CN
`
`CAPLUS
`223672w24~0
`lflmImidazolew2«acetamidm, N-[4w[2w[[(2R)m2~hydroxym2w
`phanylmthyljamino]ethyljphanyl]mlw(Zwmathylwzmprapanyl)w, dihydrochloride
`(90E)
`(CA INDEX NAME)
`
`Ahaolute staxenchemifitryu
`
`“MN 2&0
`\
`v *
`‘
`a
`_‘N
`
`KN.
`
`\
`
`/E\
`
`O 2 ml
`
`RN
`CN
`
`CARLUS
`223672~25w1
`lH—Imidazol&-4—acenamida, N~[4~[2w[[(2R)w2mhydrmxyw2w
`phenylethyl]amino]athyl]phenyl]~1~tphenylmethyl)~, dihydroahlorida (9C1)
`(CA INDEX NAME)
`
`Absuluta gteraochami$hxy.
`
`Saamhad by 13mm (smug/em,
`
`s'wxc 308«4291
`
`SAWAI EX. 1015
`Page 545 of 1092 PTO_00000546
`
`SAWAI EX. 1015
`Page 545 of 1092
`
`

`

`Panel
`
`09/529096
`
`Page 11
`
`“m/
`
`“mw’wm‘%b{”rN”MB’W0H
`H
`1
`25:3
`
`.2 H01
`
`RN
`CN
`
`CAPLUS
`223672-26—2
`1H*Xmidazolew4~acatamida, 1M[(2wahlar¢phanyl)mathyl]meE4m[2w[[(2R)w2~
`hydroxy—Z—phenylethyl]aminw]ethyl}phenyl]—, dihydrochloride (SCI)
`(CA
`INmEX NAME)
`
`Absolute sterecchemistry.
`
`//4:h %;7//Y
`[L123:»le«WNW
`HN%/mfi
`IWN,”‘xN/’“~\I}r
`
`13h
`
`02 1101
`
`RN
`CN
`
`CAFLUS
`223672w27~3
`lmfl(3~chlormphmny1)mfithyl]wN«[4-[2-[[(2R)—2—
`1H—Imidazole~4maaetamide,
`hydroxymzwphanylethyl}amino]ethyl]phenyl]—, dihydrochloride (9C1)
`(CA
`INDEX NAME)
`
`Abmolute atereochamiatry.
`
`N
`
`<%:;:7///~\
`[:/Tqm
`01/“ «5?;LNm//N
`
`//90
`HN‘
`l/flkx
`
`yr”? \M,/fl\‘\ {\g/ 0H
`H
`'h
`
`5 p
`
`02 HQ].
`Saarahad by Barb O'Bryfin, STIC 308m4291
`
`SAWAI EX. 1015
`
`Page 546 of 1092
`
`PTO_00000547
`
`SAWAI EX. 1015
`Page 546 of 1092
`
`

`

`Patel
`
`09/529096
`
`Page 12
`
`RN
`CN
`
`'
`CAPLUS
`223672~29m5
`1H~ImidazoLewdmacatamiflm 1—[(4—mhlomphanyl)mauhy1]—N~M~[2~{I(Em-2—
`hydroxyWZthenylethyl]aminolethyllphmnyllw, dihydromhlorida (9C1)
`(CA
`INDEX NAME)
`
`Abswluhfi sceneochemistry.
`
`N /kN~wfwg
`
`“N /”/l\»
`\[\ /" w ,/"\ y/“xxg/o"
`
`,
`
`.2 EC].
`
`RN
`CN
`
`CAPLUS
`223672w30~8
`lml(awfluoxophenyl)methyl]~N~[4w[zw[[(2R)w2w
`lfl—lmidazole~2~aaetam¢de,
`hyflroxy—E—phenylethyl]aminojethy11phenyl]-, dihydrochlorida (9C1)
`(CA
`INDEX NAME)
`
`Abfiolutfi stmxeochemxstxy.
`
`\lefip‘uxfl
`QkQ/M/Ngk]N
`i:/ NZrI/M»MNT¢;O
`HNTV/KKMM¢¢LN/flwaMm&/w
`
`g9
`
`h
`
`-_——N
`
`11
`
`0 2
`
`11101
`
`RN
`CN
`
`CAQLus
`223672w31w9
`lH—Imida2015—2—acetamide, 1—!(4—bromophenyl)methyl]‘N-[4—[2~[[(2R)w2w
`hydraxy~2~phenylathyllamin01athyllphanyl]w, dihydrochlorida (QCI)
`(CA
`INDEX NAME)
`
`Absolute shmxaochemistry.
`
`Searched by Barb O'Bri/en,
`
`S'i‘ICJ 308w4291
`
`SAWAI EX. 1015
`
`Page 547 of 1092
`
`PTO_00000548
`
`SAWAI EX. 1015
`Page 547 of 1092
`
`

`

`Patel
`
`09/529096
`
`Page 13
`
`
`
`.2 am
`
`RN
`CN
`
`CAPLUS
`223672—32~0
`lfl— ImidazoleWZMaamt amida, N [4 [2 [[(22)M2hydroxywzm
`phany&athyl]aminolfithyllphenyl]«l [(4 iodophmnyl)methyl] , dihyarachloria&
`(SCI)
`(CA INDEX NAME)
`
`Absolute stereochemistry.
`
`«NT “\Q\\;§;1\\ w“‘N\N//”“«\R/“DH
`
`3/
`
`W
`
`H
`
`25h
`
`02 HO].
`
`RN
`EN
`
`CAPLUfi
`223622w34~2
`leImidazalawzwacetamide. Nw[4w[2w[[(23)w2whydr¢xywzw
`phenylethyA3amino]ethyl]phenyLl—l-[[4-(trifilucxomathyl)phanyllmathyl]w,
`dihydrochloride (SCI)
`(CA INDEX NAME)
`
`fibsclute stexaochemistry.
`
`Seagched by Barb O'Bryen, STIC 308—4291
`
`SAWAI EX. 1015
`
`Page 548 of 1092 PTO_00000549
`
`SAWAI EX. 1015
`Page 548 of 1092
`
`

`

`Patal
`
`09/fi29096
`
`Pagm 14
`
`F3C
`
`MkffiflxwlL
`*‘v N1
`// N‘K.‘
`\\
`//
`N
`
`“/W‘K‘ / 0
`1
`RN»
`
`N
`
`11/1
`
`Raf/4,” Nl/IIN» M/xmg/M OH
`H
`
`gm
`
`d 2 m1
`
`RN
`CN
`
`(1211911113
`223672m36w4
`leImidazoleuz”acetamide, NM[4«[2w[[(2R)m2whydrcxyw2w
`phanylathy113mino]ethyl]phenyl]~1~(2—naphthalenyl)—, dihydxochlaridm (9C1)
`(CA INDEX NAME)
`
`Absolute Shereechemistry.
`
`13/“ \
`<;T\%m,/?bk‘yr \ ,c/N
`
`
`HNK~TWQEQ§~
`
`\%NV/»\me\g// OH
`H
`h
`
`I P
`
`02 11c;
`
`RN
`CN
`
`CAPLUS
`223672m38w6
`1m( (4»flu0xophenyl)mathyl‘l ~N— [4w [2% [ (2R) w"2m
`lHMImidazale-2mace‘camide,
`hydraxywzwphenylethyl]amino]athyllphanle—Smmethylw, dihydrochlaridm (SCI)
`(CA INDEX NAME)
`
`Absolute stereochemistry.
`
`Searched by Rank) O'Bryen,
`
`s'rxc 308m4291
`
`SAWAI EX. 1015
`Page 549 of 1092 PTO_00000550
`
`SAWAI EX. 1015
`Page 549 of 1092
`
`

`

`Patel
`
`09/529096
`
`Page 15
`
`1:]
`
`11m
`“aim“? 31:0/
`1
`\v/ Mar/"mfi/W
`15h
`
`OH
`
`.2 Hal
`
`RN
`CN
`
`,
`CAPLUS
`223672“40m0
`lm[(Amfluarophenyl)mathyl]~Nw{4m[2w[[(2R)w2m
`lH—mmmdazole—Zmacetamide,
`hydrbxy~2~ph¢nylathyl1amino}ethlephenyl1w4wmchylw, dxhnyocblmxida (Sax)
`(CA INDEX NAME)
`
`Abfiolute Stereoahemistry.
`
`fih
`
`.2 HO].
`
`RN
`CN
`
`CAPLUS
`223672w42~2
`IHMTetxazolew5«acetamide, 1*[(4*fluorophenyl)methyllwNwE4mI2m[[(2R)m2w
`hydroxym2~phenylethyljamino]éthyl]phenyl]—, monohydrochloride (BC!)
`(CA
`INDEX NAME )
`
`Abaoluta Etereochandstxy.
`
`fiaarahed by Baxb O'Brymn, STIC 308w4291
`
`SAWAI EX. 1015
`Page 550 of 1092 PTO_00000551
`
`SAWAI EX. 1015
`Page 550 of 1092
`
`

`

`Patel
`
`09/529096
`
`Page 16
`
`15h
`
`w;/ W//‘«M N/AM‘VR/ 0“
`3
`
`0 ml
`
`RN
`CN
`
`_
`CAPLUS
`223672—44~4
`lflmthrazwlamSmacatamida, 1w[(3,4—dichlorophenyl)mmuhyl]wNwIQ—[Z-[((2R)w2w
`hydrnxyw2wphenylethyl]aminolethlephenyl]«, monohydrochlarida (9C1)
`(CA
`INDEX NAME-1)
`
`Abflolute atar&mchemiatry.
`
`
`
`d HCl
`
`RN
`CN
`
`CAPLUS
`223672—46—6
`ZflmTetrazalemfiwaaatamida, 2«[(4—fluorophemy1)mehhyl}MN»{4w[Z-I[(2K)»2w
`hydroxymzmphenylethyl]amino]athyllphenleM, monahydrcchlorida (9C1)
`(CA
`INDEX NAME)
`
`Absolute mtereechemiatry.
`
`Searched by Barb O'Br§en, 8510 308~4291
`
`SAWAI EX. 1015
`Page 551 of 1092 PTO_00000552
`
`SAWAI EX. 1015
`Page 551 of 1092
`
`

`

`Patel
`
`09/529096
`
`Page 17
`
`”0
`
`/\N\/”Ny/Y
`
`NW“ N
`
`HN
`
`on
`
`M
`“mm" W”,
`H
`h
`
`3P
`
`\\A
`U/a.
`
`0 HO].
`
`
`
`RN
`CN
`
`CAPLUS
`223672m47m7
`1Hm1,2,4waiazalaw3wacatamida, Nw[4w[2w£((2R)w2whydroxyw2~
`phanylethyl]amino)ethyl]phenyl]-, dihydrochloride (SCI)
`(CA.INDEX NAME)
`
`Abfimluta atareochamistry*
`
`.2 Hal
`
`RN
`CN
`
`CAPLUS
`223672w48w8
`lfi—l,2,4—Triazwla-3—acetamide, N-[d—[Znii(2R)—2-hydroxy—2~
`phanylathyllamino]athlePhanyl]w$~[(phanylmwthyl)thi0]w, dihydrochloride
`(96E)
`(CA INDKX NAME)
`
`Absolute stereochemistry.
`
`N
`:C‘
`N/ h7//Akxffi
`/\ L N
`m:
`H
`1911’
`""
`
`OH
`
`«..//“\$9”
`:12
`
`£511
`
`.2 HCZL
`
`Searched by Barb O‘Bryen, STIC 308—4291
`
`SAWAI EX. 1015'
`
`Page 552 of 1092 PTo_ooooosss
`
`SAWAI EX. 1015
`Page 552 of 1092
`
`

`

`Fatal
`
`09/529096
`
`Faga 18
`
`CAPLUS
`223672~49~9
`RN
`CN mehiazmleacahamide, 2M(acetylamino)—Nw[4«[2w[f12R)w2mhydroxyw2w
`phmnylathyl]amina}mthyl]ph¢nyl]—, monohydrochloxida (BCI)
`(CA INDEX NAME)
`
`Absalute stfiraochemistry“
`
`‘AcmqwfNyf/xTri/x,0
`T;K;;]Mx\//’\mNfl/ngy/OH
`
`i9
`
`h
`
`H
`
`5-”
`
`ENNN M”&\
`
`I Will
`
`RN
`CN
`
`CAPLUS
`223672~50w2
`4—whiazaleaaetamida, N«[4m[2~[[{2R)w2mhydxoxyw2w
`phanylmthyl}amino]ethyl]phenyl]~2~[(methylfiulfonyl)amino]m,
`monohydrochloridfl
`(BCI)
`(CA INDEX NAME)
`
`Abscluta stareochamistxy.
`
`H
`
`5
`‘.
`Me\ V/WN.‘
`”AK /M/\ {/50
`//\\ X //
`T
`0
`0
`G”““““““““
`HN\
`
`x
`
`mm
`\N
`(/ “VWRNK/‘m‘kfi/
`I
`r“
`
`H
`
`i
`fin
`
`,0“
`
`Q HG].
`
`RN
`CN
`
`CAPLUS
`223672w51w3
`4~Thiazoleamatam¢de, 2~[(aminmiminomethyl)aminDJ’N~[4~[2-[[(ZR)m2whyfix0xy~
`2wphanylethyl}aminoJeLhyllphanyl]w, dmhydrochlwrida (901)
`(CA INDEX NAME)
`
`Abwolute atereochemiatry.
`
`Searched. by Barb O'Br§en, SlTIC 3084291
`
`SAWAI EX. 1015
`Page 553 of 1092 PTO_00000554
`
`SAWAI EX. 1015
`Page 553 of 1092
`
`

`

`Patel
`
`09/fi29096
`
`,
`
`Page 19
`
`“W““ Wm“
`H
`h
`
`:P
`
`"Til
`
`\R‘NW/
`
`.2 Hal
`
`RN
`CN
`
`CAPLUS
`223672w52w4
`4—Thiazoleacetamide, wadeZwEI(2R)~2~hydroxy~2~
`phenylethleamino]ethyllphenyl]m2m(phanylamin01m, monohydrochlaride (961)
`(CA INDEX NAME)
`
`Absoluta stereochemigtry.
`
`PhwmffiM
`
`I
`/
`
`/’“\f’0
`
`0 m3.
`
`RN
`CN
`
`CAFLUS
`223672v53w5
`lflwImidazolewzwacetamide, N*[4~[2w[[12R)«2whydnaxyw2~
`phenylethyllamino]ethlephenyl]—4—[(4—nitrophenyl)mathyl]—,
`monohydxochloride (BC!)
`(CA INDEX NAME)
`
`Abgalute stareochemistry.
`
`Searchad by Barb O'Bryem, $TIC 308w4291
`
`SAWAI EX. 1015
`
`Page 554 of 1092 PTo_ooooosss
`
`SAWAI EX. 1015
`Page 554 of 1092
`
`

`

`W
`
`
`
`Patel
`
`09/529096
`
`Page 20
`
`0 EC].
`
`RN
`CN
`
`CA?LUS
`223672~55w7
`4wThiazoleCarboxamidé, 2maminowwaa—[2~[[(2R)m2whydruxym2m
`phenylathyl]amino}etbyl]phanyllw, monohydrochloride (Sex)
`
`(CA INDEX NAME)
`
`Abaolute starflochamistry.
`
`I am
`
`RN
`CN
`
`CAPLUS
`223672-58-0
`4wThiazolaacetamide, 2wamino~N~[4w[2~[[(2R)m2whydroxyw2w
`pnenyianhyl}amino]ethyl]phanyl]mfiwmethyl—, dihydrochloride (9GI)
`INDEX NAME)
`
`(CA
`
`’
`
`Absolute staraachemiatry.
`
`Saarahed by Bath O'Eryen. STIC 308w4291
`
`SAWAI EX. 1015
`Page 555 of 1092 PTO_00000556
`
`SAWAI EX. 1015
`Page 555 of 1092
`
`

`

`Patel
`
`09/529096
`
`Page,2l
`
`Hgwar/MN mC-0
`S.m IfMN
`
`9h
`
`02 Hal
`
`RN
`CN
`
`CAPLUS
`223672-60w4
`4wwhiazolepropanamide, 2—amino-N~[4m[2~[[(2R)w2mhyflroxym2~
`phenylethyl]aminQJethyllphanyljm, monahydrochlarida (SCI)
`
`(CA INDEX NAME)
`
`Absolute steramahami$txy~
`
`Ph
`
`H
`
`(”1% /"“\~v~"”\ / RN OH
`1 ,J
`HN/ mmw/’
`H2wam<5fiwjyW/VANKM/z/Lh30
`
`SW”
`
`0 HCJL
`
`RN
`CN
`
`CAPLUS
`223672-63w7
`4~$enzothimzolmcmrhaxamide, 2~aminw—4,5,6,7-taurahydr0wN~[4~[2M[f(2R)~2w
`hydroxy-Q-phanylethyl]aminOJethlephenyll~, dihydrochloxide (9C1)
`(CA
`INDEX NAME)
`
`Absolute 5tereochemi3txy~
`
`
`
`Iacxfiflr'KWN/AKN A:
`Pb
`
`H
`
`x Nfi/NH
`J;
`
`.2 Hal.
`Searched by Barb O‘Bryen, $TIC 308 4291
`
`SAWAI EX. 1015
`
`Page 556 of 1092
`
`PTO_00000557
`
`SAWAI EX. 1015
`Page 556 of 1092
`
`

`

`Patel
`
`09/529096
`
`Page 22
`
`RN
`CN
`
`CAPLUS
`223672w6fiw9
`'
`Imidazm[a,1wb}nhiazolawzmammnamida, N~[4m[2~[((2R)~2mhydroxyw2w
`phenylathyl]amincjethyilphenyllw, manmhydxoahlorida (BCI)
`(CA INDEX NMME)
`
`Absolute stereochamistry.
`
`
`
`6 BC].
`
`RN
`CN
`
`CAPLUS
`223672w66m0
`le1,2,4mTriazolam3wacetamide, Nfl[4w[2~[[(2R)~2~hydroxym2w
`phenylauhyl]amxn016thyl1phanyl]“1w(phenylmethyl)* (SCI)
`(CA INDEX NAME)
`
`Absalutm starawcbami$txyy
`
`,QH
`
`‘
`xN
`NNXW «(N//”ng;r
`H
`h
`
`3P
`
`/
`
`3&0
`
`N
`i\
`,/“x\
`/
`“N/ \7/ \r
`\”“"N
`ENNNfl/mQQ
`I
`/‘
`
`_
`
`Ph
`
`RN
`cw
`
`QAPLUS
`223672m67m1
`4mThiazoleaa5tamida, 2,3mdihydewNw[4w[Zw[[(2R)w2whydxoxyw2~
`phanylethyl}aminOIethyllphenyll“3w(phenylmethyl)"2wthiox0w,
`monmhydrcchlorida (SCI)
`(CA INDEX NAME)
`
`Abfimlute fitermomhamistry.
`
`Saarchad by Haxb Q'Brymn, $TI¢ 308w4291
`
`SAWAI EX. 1015
`
`Page 557 of 1092 PTo_ooooosss
`
`SAWAI EX. 1015
`Page 557 of 1092
`
`

`

`Patel
`
`09/529096
`
`Page 23
`
`N
`
`Kw[’/t§5~wb‘xm 'MmM‘mg/xOH
`
`H
`
`5P
`
`h
`
`0 Hal.
`
`RN
`CN
`
`1
`CAE’LUB
`223672w68m~2
`Swguinolinecarbaxamide, 5,6,7,BMtatrahydKOMNw[4w[2w[t(2R)w2whydroxyw2w
`phanylathy11amino]athy11phenyl]—p dihydrmchlorifie (961)
`(CA INDEX NAME}
`Absalute stereochemistry~
`
`.2 H01.
`
`RN
`CN
`
`CAE’LU3
`223672w69~3
`lu—Imidazolé—Z"acetamide, Nw[4m{2“[I(2R)w2mhydroxym2«
`phenyletbyl]amino]ethyl]phenyl]mlmphenylw, dihydxochloride (BCI)
`INDEX NAME)
`.
`
`(CA
`
`Absoxuta staxaochmmistxy.
`
`fieaxchad by Barb O'Bryen,
`
`flTIC 308w4291
`
`SAWAI EX. 1015
`Page 558 of 1092 PTO_00000559
`
`SAWAI EX. 1015
`Page 558 of 1092
`
`

`

`Patel
`
`09/529096
`
`Page 24
`
`ah
`wNK' //\Nfl //0
`mm““““““ N
`
`HNN
`
`.2 Hal
`
`RN
`CN
`
`4
`CAPLUS
`223672w70w6
`lH-Imidazolane~acetamidm, Nu[4m[2m[[(2R)w2whydroxy~2w
`phenylethy11aminolethyl]phenyl]«1w[[4w(1wmethylethy11phenlemathyl]~,
`dihydrochlmridm (9C1)
`(CA INDEX NAME)
`
`Abscluta staramchamistry.
`
`”m¢&7\x
`
`1% k
`
`"1
`11’””77"'”“T/”0
`\U'Nxfij"wa"‘w\xNfi/Wxx’z/r“*1
`
`MN
`
`HM“
`
`//§%
`
`H
`
`;
`
`.2 HCl
`
`RN
`CN
`
`CAPLUS
`223672w71w7
`lw([1,1'mbiphanyl]m4mylmathyl)—Nn[AMEZWII(2R)—2*
`lflwimidazolam2macetamide,
`hydrmxywzmphanylathyl}aminojathyllphenleM, dihydrochlcrlde (9cm)
`(CA
`XNDEX NAME)
`
`Absoluta suerewahemistry,
`
`Searmhad by Barb O'Eryen, STIC 306w4291
`
`SAWAI EX. 1015
`
`Page 559 of 1092 PTo_ooooosso
`
`SAWAI EX. 1015
`Page 559 of 1092
`
`

`

`Fatal
`
`09/529096
`
`Page 25
`
`.2 H01
`
`RN
`CN
`
`CAPLUS
`223672m72w8
`lfiwlmidazolawzwacetamide, 1w[(2Mchlorophenyl)methyl]MN“[4~[2~[[(2R)w2m
`hydroxymzwphenylethyllaminm]ethlephenyl]—, dihydroahloride (SCI)
`(CA
`INDEX NAME )
`
`Ab$aluta stareaahamistry.
`
`“Nat?M i»
`
`m2
`
`w/WNNMEMVOH
`
`2311
`
`.2 Ha].
`
`RN
`ON
`
`CAPLUS
`223672w73~9
`l»[(Ewahlnxophany11mauhylj~N~K4w[2w[I(2R)~Z~
`lH»Imidazol&“2*aCatamid&,
`hydroxywzwphenylethyl]aminmlethyljphanyl)‘, dihydrochloride (9C1)
`(CA
`INDEX NAME)
`
`Absoluhm stereoghamifihry,
`
`$eax¢hed by Barb O‘Bryen, STIC 308—4291
`
`SAWAI EX. 1015
`Page 560 of 1092 PTO_00000561
`
`SAWAI EX. 1015
`Page 560 of 1092
`
`

`

`Patel
`
`09/529096
`
`Page 26
`
`w
`
`cl
`
`1 m?
`
`,2/1"»
`
`\
`
`7
`N
`
`/
`......MN
`
`H
`
`/”MNW&O
`I”
`BMW/ml“:
`\XKM55fll“xwfwyflw\u“/,x\\?//w
`
`vm
`
`;
`
`‘2 H01
`
`RN
`CN
`
`CAPLUS
`223672w74~0
`lelmidazolawzmacetamida, 1w((3,4wdichlor0phanyl)mathyl3WNW[4w[2w[[(2R)—2—
`hydroxywzmphenylechyl]amin019thy11phenyljw, dihydrochloride (SCI)
`(CA
`ENDEX NAME)
`
`Ahsmlute fihmraachemistxy.
`
`PAGE IMA
`
`Cl
`ClkfififJNN
`1Lia/mt
`/“
`“x "0
`\\ V f
`
`~—~N
`
`1m
`
`.2 Hal
`
`PAGH 2~A
`
`RN
`CN
`
`CAPLUS
`223672w75w1
`lflwimidazole 2acetamide, N-[4- [2- [[(2R)-2hydroxy 2m
`phanylethyl]aminclathyllphenyll—1—(2—pyridinylmathyl)m, dihydxaahlorida
`(901)
`(CA INDEX NAME)
`Searched by Barb O‘Bryan, STIC 308 4291
`
`SAWAI EX. 1015
`
`Page 561 of 1092 PTo_ooooossz
`
`SAWAI EX. 1015
`Page 561 of 1092
`
`

`

`Panel
`
`09/529096
`
`Page 27
`
`Abaoluté stereochemistry.
`
`
`
`\E/k«15*me”NVon
`
`a
`
`3 P
`
`h
`
`02 HCl 1
`
`RN
`CN
`
`CAPLUS
`223672~76w2
`QmThiazolaaafltamida, Zwaminow.alpha.mhydroxymww[4w[2wE[(2R)w2whydrmxyw2m
`phenylathleamino]ethyllphenyl]w, monohydromhlouide (901)
`(CA INDEX NAME)
`
`Absolute aflereochamistryw
`
`OH
`
`0 Hal
`
`RN
`CN
`
`CAPLUS
`223672w77~3
`leXmidazolewzwacatamide, waQwE2w[[(2R)~2whydraxy~2»
`phenylethyl]amin01ethyllphenyllwlw(2mmethylpropyl)w, dihydrochlwride (9C1)
`(CA INDEX NAME)
`
`Absolute stereochamistry.
`
`Saazched by Barb O'Bryan, STIC 308~4291
`
`‘
`
`SAWAI EX. 1015
`Page 562 of 1092 PTO_00000563
`
`SAWAI EX. 1015
`Page 562 of 1092
`
`

`

`Patel
`
`09/529096
`
`Page 28
`
`
`
`‘2 ml
`
`RN
`CN
`
`'CAPLUS
`223672m78v4
`mflwxmidazwlew2macetammde, 1w!(waluarapheny11methyllWNM[4w[2w[f(3R)~2~
`hydroxyn2~phemylemhy11amino]ethyl]phenyl]—, dihydnwahlnride (901)
`(CA
`INDEX NAME)
`
`Absalute atereochemiatry.
`
`‘2 mil
`
`RN
`EN
`
`CAPLUS
`223672w79w5
`lflmlmidaZolawzwacetamida, 1w[(Bmfluorophenyl)mehhy1]WNW[4w[2m[[(2K)w2~
`hydroxym2wphenylethyllaminmlethyllphanyljw, dihyarmchlorida (SCI)
`(CA
`iNDEX NAME)
`
`Absolute staraoahemistry.
`
`Searchad by Barb O'Bryen, STIC 308w4291
`
`SAWAI EX. 1015
`Page 563 of 1092 PTO_00000564
`
`SAWAI EX. 1015
`Page 563 of 1092
`
`

`

`Fatal
`
`09/529096
`
`Paga 29
`
`12"” / \I
`C277”
`
`HNN/// \
`
`Uk
`
`w MMMAN NMAM};/, {>11
`H
`§
`rah
`
`.2 H1211.
`
`RN
`CN
`
`CAPLUS
`223672m80m8
`1H~Imidazalaw2wacetamide, 1-[(2,4-difluorophenyl)méthyl]"N‘[4~[2w[[(2R1m2e
`hydroxy—2~phenylethyl]amino]ethyl]phwnyl]—, dihydra¢hloride (SCI)
`(CA
`INDEX NAME)
`
`Abfiolutm atmremmhemistry.
`
`79"
`
`rm
`
`\T/AQQ
`'
`.
`* ’“L
`
`
`m
`
`M\
`
`OH
`
` F..\W/,w:1
`
`1 \
`
`y’ k
`g
`F
`
`1
`/N«\
`§\
`//N
`
`.2 H01
`
`RN
`CN
`
`CAPLUS
`223672w81m9
`lw[(Z,6—difluarwpheny11methyl]«NM[4~[2M[[(2R)«2m
`lH—Imidazole~27a¢enamide,
`hydroxyw2wphmnylethyl]aminolethlephanyllw, dihydrochloride (9C1)
`(QR
`INDEX NAME)
`
`Absoluta staxaochemistry.
`
`Searched by Bath O'Bryan, STXC 308—4291
`
`SAWAI EX. 1015
`
`Page 564 of 1092
`
`PTO_00000565
`
`SAWAI EX. 1015
`Page 564 of 1092
`
`

`

`Patel
`
`09/529096
`
`Page 3 0
`
`
`
`’\/NW/«Nf/O
`REKx;5;L\xv/”AKMNx/mmxfix’0H
`
`“N
`
`“Nxv
`
`//§§
`
`H
`
`3
`Ph
`
`'
`
`62 HCl
`
`CAPLUS
`223672w82w0
`lH—Imidazolm~2~aceuamide, 1%(3, Sudiflumrophmnyl)methyl] MNM [4,. [2% [ (2R) "2”
`hydroxywbphenylethyl]amino] ethprhenyl] m, dihydrochlarida (QCI)
`(CA
`lNDEX NW)
`
`Absolute smmochémisztny ,
`
`I?
`
`mm: 1~A
`
`F’dfkfl‘mwfl/ M]
`(’Nx7Mr/m‘xTfifio
`N
`H
`
`//%«l
`
`NM” ~v»~.»/"“"~«NM“W$/ OH
`H
`%
`fin
`
`.2 ml
`
`mm 2%
`
`RN
`CN
`
`cmnug
`223672w83-1
`1H~Imdazole~2—acetamde, 1-{ (2, 5—dif1uoropheny1)met‘hyl] mm“ Mm [2w I 1 (2m ~2“
`hydroxywz—phanylethyl] amino] ethyl 1 phanyl] m , dihydrachlomde (9C1)
`(CA
`INDEX NAME)
`.
`.
`fiearmhad by Barb O'Bryan, STIC 308-4291
`
`SAWAI EX. 1015
`
`Page 565 of 1092
`
`PTO_00000566
`
`SAWAI EX. 1015
`Page 565 of 1092
`
`

`

`Patel
`
`09/329096
`
`Paga 31
`
`Abfiolute shereechemistry.
`
`”N.
`
`Mu¢7Nw//\”WANV/mm
`
`15b
`
`‘2 HCl
`
`RN
`0N
`
`CAPLUB
`223672m84~2
`le(3,4~difluwropheny11mathylj«Nm[4m[2w[[(2R)w2w
`lH~Imidazole~zwacetamida,
`hydroxywzmphenylethyl]amino]@thyl]pheny1]-, dihydxochloride (SCI)
`(CA
`XNDEX NAME)
`
`Absolute stereochemistry»
`
`was 1*};
`
`F
`
`”Tmh§9//LW1
`
`
`
`<~’{N‘7/NW\ /0
`/
`f
`L
`N
`11nyGI _/J
`
`,0};
`
`19h
`
`mm: 2m
`
`.2 Hcl
`
`RN
`CN
`
`CAPLUS
`223672w85w3
`luvlmidazclaWZWauatamide. Nw14w12mrf(2R3m2mhvdrovaaw
`Searched by Barb O'Bryen, STIC 308~429l
`
`SAWAI EX. 1015
`
`Page 566 of 1092 PTo_oooooss7
`
`SAWAI EX. 1015
`Page 566 of 1092
`
`

`

`Patél
`
`09/529096
`
`Page 32
`
`phenylehhyllamino1ethyllphanyl]~1—[(2,3,G-trifluorephmnyl)methyl]-,
`dihydrochloride (BCI)
`(CA INDEX NAME)
`
`Absclute stexaochemistry.
`
`/”~?;.\ /' F
`I
`
`13/, A? WF
`,N
`1 T"
`
`.2 Hal
`
`RN
`CN
`
`CAPLUS
`223672~86~4
`lH—Imidazole~Z—acetamide, Nm[4~[2w[[(2H)~2*hydx0xyw2w
`phanylathyllamino]ethlephenyljm1u[(2,4,5~trifluorophenyl)mathyl]m,
`dihydrvchloride (96X)
`(CA INDEX NAME)
`
`Absolute atar&oahamistry.
`
`PAGE 1MA
`
`
`
`l\
`
`\/ WWM/IOH
`H
`b
`
`EP
`
`PAGE 241
`
`.2 11m
`
`Searchad by Barb O'Bxyan,
`
`swxc 308M4291
`
`SAWAI EX. 1015
`
`Page 567 of 1092 PTo_ooooosss
`
`SAWAI EX. 1015
`Page 567 of 1092
`
`

`

`Patel
`
`09/529096
`
`Page 33
`
`RN
`CN
`
`CAPLUS
`223672w87w5
`leImidazolauz-acetamide, N~[4—[2—[[(2R)~2-hydroxy-2—
`phenylethyllamino]ethyl)phenyl]«l«[(3,4,Swtrifluorophenyl)methyl]m,
`dihydrochlorida (901)
`(CA INDflX NAME)
`
`Absolute stexaochamiatry.
`
`FAGE lwA
`
`F
`J.“4km
`
`F
`
`ij‘qwkk
`
`\
`
`ijr//w\
`4
`WM"
`
`[;
`
`;&§Q
`\1
`”Nwm //?m\
`
`¢:L\m//A\KN/¢«\¢p,on
`
`\x?
`
`m
`
`P11
`
`PAGE 2MA
`
`‘2 HCl
`
`RN
`CN
`
`CAPLUS
`223672m88w6
`lfiwmmidazole-Zwacetamide, N~£4~f2~£l(2R)w2mhydroxym2w
`phenylathleamino]ethyllphanyl3wlwl(pantafluarophanyl)methyl]w,
`dihydrachlorida (SCI)
`(CA INnEX NAME)
`
`flbmolute stfireochemistry.
`
`Saanched by Barb O'Bryen, STIC 308w4291
`
`SAWAI EX. 1015
`
`Page 568 of 1092 PTo_ooooosss
`
`SAWAI EX. 1015
`Page 568 of 1092
`
`

`

`Patal
`
`09/529096
`
`Page 34
`
`PAGE 141;
`
`E.
`‘//k //E'
`
`F
`
`ff/QQT/W«N{177Wmg
`\I:f//LNN$/\NM&/,OH
`
`:51»;
`
`9mm 2%
`
`.2 HQ],
`
`RN
`CN
`
`CAPLUS
`223672M89«7
`leImidazoléwzwacetammde, N»[4~[2»[[(2R)m2whydroxym2w
`phenylathyl]aminalathyllpheny11wlw[(3wiodcphanyl)mathyl]—, dihydrochloride
`(96$)
`(CA‘INDEX NAME)
`
`AbSaluta staraochemistry.
`
`/»/7b«
`
`1 1 M1
`
`/0
`
`1
`/i\I
`MM»
`~ /,
`,1
`«j
`1 7 \7
`.....N
`H
`
`//:\91
`
`\xflfig “NV/”’W‘WN/Mrk“x§//OH
`H
`2
`{in
`
`.2 full
`
`RN
`CN
`
`CAPLUS
`223672~90~0
`leImidazola 2acatamida, m[(2, 6dichlarophanyl)mmthyllmfl—[4»[2-[f(2R)m2*
`hydroxyHZphenylethyl]amino]ethyl]phenyl]~, monohydrochloride (BCI)
`(aA
`INDEX NAME)
`fiearchad by Bath 0' Bryan, STXC 303 4291
`
`SAWAI EX. 1015
`
`Page 569 of 1092
`
`PTO_00000570
`
`SAWAI EX. 1015
`Page 569 of 1092
`
`

`

`Patel
`
`09/329096
`
`'
`
`page 35
`
`Abscluta starmvmhemistry.
`
`n\\[:w
`
`iii: WWW“
`
`éh
`
`I HCLL
`
`RN
`CN
`
`CAPLUS
`223672m91~1
`leImidazol&M2~ametamide, 1w[(4wayanophanyl)matbyllmeI4m[QMI[(2R)~2m
`hydroxwa—phenylathyl]amino]ethyl]phenyl]w, dihydrochlorida (9C1)
`(CA
`INDEX NAME)
`
`Abguluta staranchemistry.
`
`MNEVI
`
`Q2 m1
`
`RN
`CN
`
`CAPLUS
`223672w92~2
`leImidazcleE-acatamida, NmeiZmH(2Rh2—hydroxyw—2w
`phanylethyl)amino)wthyllphanyllwlw(2wquinolinyl)w,
`trihydchhloxida (9CI)
`(CA INDEX NAME)
`
`Absoluta stereochamistxy.
`
`Searched by Barb O'Bryen, STIC 308-4291
`
`SAWAI EX. 1015
`Page 570 of 1092 PTO_00000571
`
`SAWAI EX. 1015
`Page 570 of 1092
`
`

`

`watel
`
`09/329096
`
`'Paga 36
`
`
`
`
`
`.3 m2),
`
`RN
`CN
`
`CAPLUS
`223672~93~3
`1m [ (2mchl¢raw6~flu0xophenyhmathyil] "N— [4- [2-
`lflmlm<iazmlamzwacet