16/461,512
`
`=> d his
`
`
`
`
`(EILL '{OMN' LN1LRND A1 11:57:01 ON 16 OCT 2019)
`
`
`
`
`
`
`
`
`
`
`
`fiNifiRfiD A1 11:57:14 ON 16 OCT 2019
`bILL 'RfiGISiRY'
`STRUCTUR? JPLOAD?D
`50 S L1
`1141 S L1 SSS FJL
`3 S
`(L3 AND SR/FA NOT CA/SR) OR (L3 NOT CAPLUS/LC)
`
`
`
`
`FIL? 'CAPLUS'
`fiNifiRfiD A1 11:58:05 ON 16 OCT 2019
`64 S L3
`
`ANALYZE L5 1- RN HIT :
`
`
`1138 TERMS
`
`
`
`
`
`
`
`
`bILL 'RfiGISiRY'
`fiNifiRfiD A1 12:00:17 ON 16 OCT 2019
`1 S 1616632—77—9/RN
`1140 S L3 NOT L7
`
`
`
`
`
`
`fiNifiRfiD A1 12:03:22 ON 16 OCT 2019
`FIL? 'CAPLUS'
`27 3 L8
`24 3 L9 NOT (2019/SO OR 2018/SO)
`
`L1
`L2
`L3
`L4
`
`L5
`L6
`
`L7
`L8
`
`L9
`L10
`
`=> d 11
`
`L1 HAS NO ANSWERS
`L1
`STR
`
`O
`
`
`
`N"
`
`N
`
`"G1
`
`/"N"
`a
`
`W
`
`N
`
`G1:C,N
`
`Structure attributes must be viewed using the Structure Drawing program.
`
`=> d ibib abs hitstr total
`
`Page 1
`
`

`

`16/461,512
`
`L10
`
`ANSWER 1 OF 24
`
`CAPLUS
`
`COPYRIGHT 2019 ACS on STN
`
`
`
`PatentPak PDF+ I PatentPak Interactive
`PatenIPak PDF
`
`ACCESSION NUWEER:
`2019:899802
`CAPLUS
`
`
`
`DOCJWENI NUME«R:
`170:594364
`
`TITLE:
`INVENTOR(S):
`
`
`
`
`
`PATENT ASSIGN««(S):
`SOURCE:
`
`
`
`Imipridones for gliomas
`
`Allen, Joshua E.; Stogniew, Martin; Prabhu, Varun
`Vijay
`Oncoceutics, Inc., USA
`PCT Int. Appl., 145pp.
`CODEN: PIXXD2
`Patent
`DOCJWENI TYPE.
`
`
`English
`LANGJAGE:
`4
`FAMILY ACC. NJM. COUNT:
`
`PATENTPAK PATENT INFORMATION:
`
`PATENT NO.
`KIND
`
`
`
`
`
`
`
`
`DATE
`
`
`LANGUAGE
`
`PatentPak
`
`20190509
`A1
`WO 2019090222
`WO 2018—US59209
`20181105
`
`W: A3, AG, AL, AM, AO, AT, AJ, AZ, 3A, 33, 3G, 3H, 3N, 3R,
`3W, 3Y,
`
`
`
`
`
`
`3Z, CA, CH, CL, CN, CO, CR, CU, CZ, 33, DJ, DK, DM, DO, DZ, 3C,
`
`
`
`««,
`«G, «S, bI, G3, G3, G3, GH, GM, GT,
`1N,
`1R,
`1U,
`ID,
`IL,
`IN,
`
`IR,
`IS,
`JO, JP, K3, KG, K1, KN, KP, KR, KW, KZ, LA, LC, LK, LR,
`
`LS, LJ, LY, MA, M3, M3, MG, MK, MN, MW, WX, MY, MZ, NA, NG, NI,
`
`No, NZ, OM, PA, P3, PG, P1, PL, PT, QA, Ro, RS, RU, RW, SA, SC,
`
`
`S3, S3, SG, SK, SL,
`SM, ST, SV, SY, 11, 1J,
`1M,
`1N,
`IR, 11, 1Z,
`
`JA,
`JG,
`JS,
`JZ, VC, VN, ZA, ZN,
`ZW
`
`
`
`1R,
`RW: AL, AT, 33, 3G, C1, CY, CZ, DE, DK, ««, «S, bI, bR, G3, GR,
`
`IT, LT, LJ, Lv, MC, MK, MT, NL, NO, PL, PT, RO, RS,
`iJ,
`I3,
`IS,
`
`IR, 3P, RJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM,
`SE, SI, SK,
`SW,
`
`
`3W, GI, GM, K3, LR, LS, MW, MZ, NA, RW,
`ML, MR, N3, SN, TD, TG,
`JG, ZM, ZW, AM, AZ, 3Y, KG, KZ, RU, TJ,
`SD, SL, ST, SZ, TZ,
`TM
`US 20180221375
`A1
`20180809
`US 2018—15947840
`20180408
`US 10172862
`32
`20190108
`PRIORITY APPLN.
`
`
`
`
`
`
`
`INFO.:
`
`WO 2019090222
`US 20180221375
`US 10172862
`
`PATENT INFORMATION:
`
`PATENT NO.
`
`
`20190509 Eng'ish
`
`20180809 Eng'ish
`20190108 Eng'ish
`
`
`
`
`A1
`A1
`
`32
`
`PDF | PDF"
`
`PDF | PDF"
`PDF
`
`KIND
`
`
`DATE
`
`APPLICATION NO.
`
`| Interactive
`| Interactive
`
`
`DATE
`
`
`
`
`
`
`
`
`
`20171103
`P
`US 2017-62581478
`20180408
`A
`US 2018—15947840
`A2 20170130
`WO 2017—US15608
`
`_*J
`
`
`
`
`IN LSUS DISPLAY FORMAT
`ASSIGNMENT HISTORY FOR US PATENT AVAILAQL
`A3
`
`
`
`Imipridones selectively modulate Class A G protein-coupled receptors
`(GPCRs),
`such as the D2-like subfamily of dopamine receptors, and are
`useful for treating conditions and disorders in need of such modulation,
`such as cancers. Specifically,
`the cancer involves a midline structure of
`the brain, a cancer having a histone H3 mutation, or both.
`In addition,
`methods of identifying whether a subject having these conditions,
`is
`likely to be responsive to a treatment regimen,
`such as imipridone
`administration, are provided. Furthermore, methods of assessing the
`effectiveness of a treatment regimen,
`such as imipridone administration,
`monitoring, or providing a prognosis for a subject with these condition
`are also provided. Also disclosed is the preparation of compds. of the
`incention.
`Mlgqls;
`
`
`IT
`
`RL: PAC (Pharmacological activity); RCT (Reactant); SPN (Synthetic
`
`
`
`preparation); THU (Therapeutic use); 310% (3iological study); PREP
`
`Page 2
`
`

`

`16/461,512
`
`RN
`
`CN
`
`
`m S
`(Preparation); RACT (Reactant or reagent); US
`(Imipridones for gliomas)
`1777778—83—2
`CAPLUS
`
`(Uses)
`
`Imidazo[1,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`
`2,4,6,7,8,9—hexahydro—4—[(2—methy1pheny1)methy1]-, 2,2,2-trif1uoroacetate
`
`
`(1:1)
`(CA INDfiX NAMfi)
`
`CM
`
`1
`
`CRN
`CMF
`
`1638178-88-7
`C17 H2O N4 0
`
`NH
`
`cw
`N444,
`N site
`
`CH2
`
`Me
`
`CM
`
`2
`
`CRN
`CMF
`
`76-05-1
`C2 H F3 02
`
` ONC202
`
`(V
`
`
`
`
`RL: PAC (Pharmacological activity); SPN (Synthetic preparation); TiU
`
`
`
`
`(Therapeutic use); SIOL (Sio1ogica1 study); PREP (Preparation); USES
`(Uses)
`(Imipridones for gliomas)
`1638178—82—1
`CAPLUS
`
`RN
`
`CN
`
`Imidazo[1,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`
`2,4,6,7,8,9—hexahydro—4—[(2—methy1pheny1)methy1]—7—(pheny1methy1)—,
`
`
`hydrochloride (1:2)
`(CA INDfiX NAMfi)
`
`Page 3
`
`

`

`16/461,512
`
`///CH2’*Ph
`
`N
`
`f1“ \
`\
`N
`N \\\0
`
`CH2
`
`Me
`
`RN
`
`CN
`
`C1
`
`RN
`
`CN
`
`.2 HC1
`
`1638178—83-2
`
`CAPLUS
`
`Imidazo[1,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`
` 4—[(2—chloropheny1)methy1]—2,4,6,7,8,9—hexahydro—7—(phenylmethy1)— (CA
`
`INDNX NAB/1*.)
`
`///CH2’*Ph
`
`N
`
`1638178-89-8
`
`CAPLUS
`
`Imidazo[1,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`
`2,4,6,7,8,9—hexahydro—7—methy1—4—[(2—methy1pheny1)methy1]— (CA INDEX
`
`NAME)
`
`Page 4
`
`

`

`16/461,512
`
`RN
`
`CN
`
`1977539-95-9
`
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`4—[(2—chlorophenyl)methyl]—2,4,6,7,8,9—hexa1ydro—7—(phenylmethyl)—,
`
`(CA INDfiX NAMfi)
`2,2,2-trifluoroacetate (1:1)
`
`CM
`
`1
`
`1638178-83-2
`CRN
`CMF C23 H23 Cl N4 0
`
`///CH2”Ph
`
`N
`
`f1“ \
`\
`N
`N \\\0
`
`CH2
`
`Cl
`
`CM
`
`2
`
`CRN
`CMF
`
`76-05-1
`C2 H F3 02
`
`1F
`F’*CA*C02H
`F
`
`Page 5
`
`

`

`16/461,512
`
`RN
`
`CN
`
`1977539-99-3
`
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—4—[(2—methylphenyl)me:hyl]—7—(2—phenylethyl)—,
`
`
`
`2,2,2-trifluoroacetate (1:1)
`(CA INDfiX NAMfi)
`
`
`
`O\C204
`O\C206
`O\C208
`O\C215
`O\C212
`O\C219
`O\C220
`O\C213
`O\C217
`O\C221
`O\C225
`O\C228
`O\C23O
`O\C233
`O\C236
`O\C237
`O\C232
`
`
`
`CM
`
`1
`
`1638178-90-1
`CRN
`CMF C25 H28 N4 0
`
`N//CH21CH21Ph
`
`\\
`
`\\0
`
`Q;
`
`CH2
`
`CM
`
`2
`
`CRN
`CMF
`
`76-05-1
`C2 H F3 02
`
`
`
`
`O\C203
`O\C205
`O\C207
`O\C209
`O\C216
`O\C211
`O\C223
`O\C210
`O\C214
`O\C218
`O\C224
`O\C227
`O\C229
`O\C23l
`O\C234
`O\C226
`O\C222
`
`Page 6
`
`

`

`16/461,512
`
`RL: RCT (Reactant); SPN (Synthetic preparation); PR
`(Reactant or reagent)
`(Imipridones for gliomas)
`1638178-84-3
`CAPLUS
`
`
`
`Lu'
`
`P
`
`(Preparation); RACT
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—7—(phenylmethyl)—4—(2—thienylmethyl)— (CA INDEX
`
`NAME )
`
`RN
`
`CN
`
`///CH24’Ph
`
`N
`
`fN\
`N
`N <§>O
`
`CH2
`
`S \
`
`RN
`
`CN
`
`1638178-85-4
`
`CAPLUS
`
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`
`2,4,6,7,8,9—hexahydro—4—(2—phenylethyl)—7—(phenylmethyl)— (CA INDfiX NAMfi)
`
`///CH24’Ph
`
`N
`
`m\
`N7 Nko
`
`PntCHthHZ
`
`RN
`
`CN
`
`1638178-86-5
`
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—7—(phenylmetqyl)—4—[2—[4—(phenylmethyl)—l—
`
`
`piperazinyl]ethyl]— (CA INDfiX NAMfi)
`
`Page 7
`
`

`

`16/461,512
`
`V
`
`Ph’*CH2
`
`1638178—87-6
`
`CAPLUS
`
`Imidazo[1,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`
`4—[(2,4—dif1uoropheny1)methy1]—2,4,6,7,8,9—hexahydro—7—(phenylmethy1)—
`
`
`
`(CA INDfiX NAMfi)
`
`///CH2”Ph
`
` F
`
`1638178—88-7
`
`CAPLUS
`
`
`Imidazo[1,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`
`
`
`2,4,6,7,8,9—hexahydro—4—[(2—methy1pheny1)methy1]— (CA INDfiX NAMfi)
`
`RN
`
`CN
`
`RN
`
`CN
`
`Page 8
`
`

`

`16/461,512
`
`NH
`
`Me
`
`RN
`
`CN
`
`1638178-89-8
`
`CAPLUS
`
`Imidazo[1,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`
`2,4,6,7,8,9—hexahydro—7—methy1—4—[(2—methy1pheny1)methy1]— (CA INDEX
`
`NAME)
`
`Me
`
`/
`N
`
`ffl
`\\
`N
`N“
`
`CH2
`
`Me
`
`RN
`
`CN
`
`1638178-90-1
`
`CAPLUS
`
`Imidazo[1,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`
`2,4,6,7,8,9—hexahydro—4—[(2—methy1pheny1)methy1]—7—(2—pheny1ethy1)— (CA
`
`
`INDfiX NAMfi)
`
`Page 9
`
`

`

`16/461,512
`
`CH2’*CH2‘*Ph
`
`/
`N
`
`WM
`N;:::L\
`N
`
`sto
`
`CH2
`
`//
`
`\\
`
`1777785-69-9
`
`CAPLUS
`
`Carbamic acid, N-[Z-[1,2,4,5,8,9—hexahydro—4—[(2—methy1pheny1)methy1]—5—
`
`oxoimidazo[1,2—a]pyrido[3,4—e]pyrimidin—7(6H)—y1]ethy1]—,
`
` fiX NAM *-)
`(CA IND
`1,1—dimethy1ethy1 ester
`
`O 1
`
`1
`
`CHZA’CH24’NH4’C4’03u-t
`
`1777785—70-2
`
`CAPLUS
`
`Imidazo[1,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`
`7—(3—aminopropy1)—2,4,6,7,8,9—hexahydro—4—[(2—methy1pheny1)methy1]—
`
`IND fiX NAM *-)
`
`(CA
`
`RN
`
`CN
`
`Me
`
`RN
`
`CN
`
`Page 10
`
`

`

`16/461,512
`
`N/ (CH2)3*NH2
`
`m \
`N7 N k0
`
`RN
`
`CN
`
`RN
`
`CN
`
`1807861—48-8
`
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—7—(phenylmethyl)—4—[[4—
`
`
`
`(trifluoromethyl)phenlemethyl]— (CA INDfiX NAMfi)
`
`
`
`CF3
`
`1807861—50-2
`
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`4—[(3,4—dichlorophenyl)methyl]—2,4,6,7,8,9—hexahydro—7—(phenylmethyl)—
`
`
`
`(CA IND fiX NAB/1*.)
`
`Page 11
`
`

`

`16/461,512
`
`///CH2”Ph
`
`N
`
`ffi
`NA \
`“0
`
`CH2
`
`C1
`
`1807861—52—4
`
`CAPLUS
`
`Imidazo[1,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`
`4—[(2,4—dichloropheny1)methy1]—2,4,6,7,8,9—hexahydro—7—(phenylmethy1)—
`
`
`
`(CA INDfiX NAMfi)
`
`C1
`
`RN
`
`CN
`
`///CH2’*Ph
`
`N
`
`f1“
`\\
`N4444L\
`N”
`
`CH2
`
`C1
`
`RN
`
`CN
`
`C1
`
`1815609-68-7
`
`CAPLUS
`
`Imidazo[1,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`
`2,4,6,7,8,9—hexahydro—4—[(4—methy1pheny1)methy1]—7—(phenylmethyl)—
`
`
`
`INDfiX NAMfi)
`
`(CA
`
`Page 12
`
`

`

`16/461,512
`
`N///CH2”Ph
`
`m \
`NAN k0
`
`CH2
`
`Me
`
`RN
`
`CN
`
`RN
`
`CN
`
`1815609—71—2
`
`CAPLUS
`
`Imidazo[1,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`
`2,4,6,7,8,9—hexahydro—4—[(4—methoxypheny1)methy1]—7—(phenylmethy1)—
`
`
`
`INDfiX NAMfi)
`
`(CA
`
`OMe
`
`1977540 -O9—2
`
`CAPLUS
`
`Imidazo[1,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`
`4—[(3,5—dif1uoropheny1)methy1]—2,4,6,7,8,9—hexahydro—7—(phenylmethy1)—
`
` fiX NAM *-)
`(CA IND
`
`Page 13
`
`

`

`16/461,512
`
`N//CH21Ph
`
`m\
`N7 NR0
`
`CH2
`
`F
`
`F
`
`1977540—13—8
`
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`4—[(3,4—difluorophenyl)methyl]—2,4,6,7,8,9—hexahydro—7—(phenylmethyl)—
`
`
`
`(CA INDfiX NAMfi)
`
`///CH2”Ph
`
` F
`
`1977540—15—0
`
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—4—[(2—methylphenyl)methyl]—7—(phenyl—2,3,4,5,6—d5-
`
`
`
`methyl-d2)-
`(CA INDfiX NAMfi)
`
`RN
`
`CN
`
`RN
`
`CN
`
`Page 14
`
`

`

`16/461,512
`
`D
`
`N”*CD2
`
`WM
`N
`//\\
`“0
`
`CH2
`
`Me
`
`D
`
`D
`
`D
`
`D
`
`RN
`
`CN
`
`1977540—17—2
`
`CAPLUS
`
`Imidazo[1,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`
` 4—[(2—f1uoropheny1)methy1]—2,4,6,7,8,9—hexahydro—7—(phenylmethy1)— (CA
`
`
`INDfiX NAMfi)
`
`///CH2”Ph
`
`N
`
`ffl
`\\
`N
`N“
`
`CH2
`
`RN
`
`CN
`
`1977540—19—4
`
`CAPLUS
`
`Imidazo[1,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`
`4—[(4—f1uoro—2—methy1pheny1)methyl]—2,4,6,7,8,9—hexahydro—7—(phenylmethy1)—
`
`
`
`(CA INDfiX NAMfi)
`
`Page 15
`
`

`

`16/461,512
`
`///CH2”Ph
`
`N
`
`f1“ \
`\
`N
`“0
`
`CH2
`
`Me
`
`RN
`
`CN
`
`RN
`
`CN
`
`F
`
`1977540-23-0
`
`CAPLUS
`
`Imidazo[1,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`
`2,4,6,7,8,9—hexahydro—4—[[4—(trifluoromethyl)pheny1]methy1]— (CA INDEX
`
`NAME)
`
`NH
`
`CF3
`
`1977540—27—4
`
`CAPLUS
`
`Imidazo[1,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`
`2,4,6,7,8,9—hexahydro—4—[2—(4—morpholiny1)ethy1]—7—(phenylmethyl)— (CA
`
`
`INDfiX NAMfi)
`
`Page 16
`
`

`

`16/461,512
`
` 0
`
`RN
`
`CN
`
`RN
`
`CN
`
`1977540—29—6
`
`CAPLUS
`
`Imidazo[1,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`
`4—[[2—f1uoro—4—(trifluoromethyl)pheny1]methy1]—2,4,6,7,8,9—hexahydro—7-
`
`
`
`(phenylmethy1)— (CA INDfiX NAMfi)
`
`
`
`CF3
`
`1977540—33—2
`
`CAPLUS
`
`Imidazo[1,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`
`2,4,6,7,8,9—hexahydro—4,7—bis[[4—(trifluoromethyl)pheny1]methy1]— (CA
`
`
`
`INDfiX NAB/1*.)
`
`Page 17
`
`

`

`16/461,512
`
`N44’CH2
`
`
`
`CF3
`
`RN
`
`CN
`
`RN
`
`CN
`
`1977540—35—4
`
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`7—[(4—fluorophenyl)methyl]—2,4,6,7,8,9—hexahydro—4—[[4—
`
`
`
`(trifluoromethyl)phenlemethyl]— (CA INDfiX NAMfi)
`
`N44’CH2
`
`
`
`CF3
`
`1977540—37—6
`
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—7—[(4—methoxyphenyl)methyl]—4—[[4—
`
`
`
`(trifluoromethyl)phenlemethyl]— (CA INDfiX NAMfi)
`
`Page 18
`
`

`

`OMe
`
`N44’CH2
`
`16/461,512
`
`
`
`CF3
`
`RN
`
`CN
`
`RN
`
`CN
`
`1977540—39-8
`
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`7—[4—(4—fluorophenyl)—4—oxobutyl]—2,4,6,7,8,9—hexahydro-4-[[4-
`
`
`
`(trifluoromethyl)phenlemethyl]— (CA INDfiX NAMfi)
`
`
`
`CF3
`
`1977540—41—2
`
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—7—(3—pyridinylmethyl)—4—[[4—
`
`
`
`(trifluoromethyl)phenlemethyl]— (CA INDfiX NAMfi)
`
`Page 19
`
`

`

`16/461,512
`
`
`
`CF3
`
`RN
`
`CN
`
`RN
`
`CN
`
`1977540-45-6
`
`CAPLUS
`
`Imidazo[1,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`
`2,4,6,7,8,9—hexahydro—7—(2—pyraziny1methy1)—4—[[4—
`
` fiX NAM *-)
`(CA IND
`(trifluoromethyl)pheny1]methy1]—
`
`CF3
`
`1977540-47-8
`
`CAPLUS
`
`Imidazo[1,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`1ydro—4—[[4—
`7—[(3,4—dichloropheny1)methy1]—2,4,6,7,8,9-hexa
` fiX NAM.
`(CA IND
`(trifluoromethyl)pheny1]methy1]—
`
`Page 20
`
`

`

`16/461,512
`
`Cl
`
`Cl
`
`N”*CH2
`
`RN
`
`CN
`
`RN
`
`CN
`
`CF3
`
`1977540—51—4
`
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—7—(3—thienylmethyl)—4—[[4—
`
`
`(trifluoromethyl)phenlemethyl]— (CA INDfiX NAMfi)
`
`NCHZKi?\)S
`
`CF3
`
`2112855—02—2
`
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`2,4,6,7,8,9—hexahydro—7—(phenylmethyl)—4—(3—pyridinylmethyl)—
`NAME)
`
`
`(CA INDEX
`
`Page 21
`
`

`

`16/461,512
`
`///CH2”Ph
`
`N
`
`f1”
`\
`N
`N“
`
`CH2
`
`/\N‘\
`
`RN
`
`CN
`
`2112855—03-3
`
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—7—(2—hydroxy—2—phenylethyl)—4—[[4—
`
`
`(trifluoromethyl)phenlemethyl]— (CA INDfiX NAMfi)
`
`Ph
`
`CH2 * CHi OH
`
`/N
`
`f1”
`N
`
`\
`
`T
`
`CH2
`
`0
`
`RN
`
`CN
`
`CF3
`
`2241789—77—3
`
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—4—(3—isoxazolidinylmethyl)—7—(phenylmethyl)— (CA
`
`
`INDfiX NAMfi)
`
`Page 22
`
`

`

`16/461,512
`
`///CH2’*Ph
`
`N
`
`f11 \
`N
`
`\
`
`F
`
`CH2
`
`0
`
`NH
`
`/0
`
`RN
`
`CN
`
`2241789—78—4
`
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—7—[(4—methyl—2—thiazolyl)methyl]—4—[[4—
`
`
`
`(trifluoromethyl)phenlemethyl]— (CA INDfiX NAMfi)
`
`N
`
`M
`
`N7 CH2%J/ e
`
`s
`
`
`
`Page 23
`
`

`

`16/461,512
`
`LlO ANSWER 2 OF 24
`
`CAPLUS
`
`COPYRIGHT 2019 ACS on STN
`
`
`
`PatentPak PDF+ I PatentPak Interactive
`Paten:Pak PDF
`
`ACCESSION NUMEER:
`2018:1456733
`CAPLUS
`
`
`
`DOCJWENI NUMEER:
`169:274678
`
`
`
`TITLE:
`INVENTOR(S):
`
`
`
`
`
`PATEMT ASSIGN««(S).
`SOURCE:
`
`
`
`Imipridones for treatment of gliomas
`
`Allen, Joshua E.; Stogniew, Martin; Prabhu, Varun
`Vijay
`OncoceutiCS, Inc., USA
`J.S. Pat. Appl. Publ., 75pp., C0nt.-in-part of Appl.
`M0. PCT/US2017/OI5608.
`CODEN: USXXCO
`Patent
`
`
`DATE
`
`
`LANGUAGE
`
`PatentPak
`
`
`
`
`
`DOCJMENI TYPE:
`
`English
`LANGUAGE:
`4
`FAMILY ACC. MJM. COUNT:
`
`PATENTPAK PATENT INFORMATION:
`
`PATENT MO.
`KIND
`
`US 20180221375
`US 10172862
`W0 2017132661
`W0 2017132661
`W0 2019090222
`US 20190183895
`US 10369154
`
`PATENT INFORMATION:
`
`PATENT NO.
`
`
`
`20180809 Eng'ish
`20190108 Eng'ish
`
`
`20170803 Eng'ish
`20170831 Eng'ish
`
`20190509 Eng'ish
`20190620 Eng'ish
`
`20190806 Eng'ish
`
`
`
`
`A1
`
`32
`A2
`A3
`A1
`A1
`
`32
`
`PDF | PDF"
`PDF
`PDF | PDF"
`PDF
`PDF | PDF"
`PDF
`PDF
`
`
`
`| Interactive
`
`| Interactive
`
`| Interactive
`
`KIND
`
`
`DATE
`
`APPLICATION NO.
`
`
`DATE
`
`US 2018—15947840
`
`20180408
`
`W0 2017—US15608
`
`20170130
`
`
`
`
`
`
`
`
`
`
`
`
`
`20180809
`A1
`US 20180221375
`20190108
`32
`US 10172862
`20170803
`A2
`W0 2017132661
`20170831
`A3
`W0 2017132661
`
`
`W: A3, AG, AL, AM, A0, AT, AJ, AZ, 3A, 33, 3G, 3H, 3N, 3R,
`3W, 3Y,
`
`3Z, CA, CH, CL, CM, CO, CR, CU, CZ, 33, DJ, DK, DM, 30, DZ, EC,
`
`««,
`4G, «S, II, G3, GD, G3, GH, GM, GT,
`4N,
`4R,
`4U,
`ID,
`IL,
`IN,
`IR,
`IS, JP, K3, KG, KH, KM, KP, KR, KW, KZ, LA, LC, LK, LR, LS,
`LJ, LY, MA, M3, M3, MG, MK, MN, MW, Mx, MY, MZ, MA, MG, MI, M0,
`MZ,
`0M, PA, P3, PG, PH, PL, PT, QA, R0, RS, RU, RW, SA, SC, SD,
`SE, SG, SK, SL,
`SM, ST, SV, SY,
`1H, 1J,
`1M,
`1N,
`1R, 11, 1Z,
`JA,
`
`JZ, VC, VM, ZA, ZM,
`JG, US,
`ZW
`
`
`
`4R,
`RW: AL, AT, 33, 3G, Ci, CY, CZ, D3, DK, ««, «S, II,
`IR, G3, GR,
`IT, LT, LU, LV, MC, MK, MI, ML, N0, PL, PT, R0, RS,
`iJ,
`I3,
`IS,
`
`IR, 3P, 3J, CF, CG, CI, CM, GA, GM, GQ, GW, KM,
`SE, SI, SK,
`SM,
`
`3W, G4, GM, K3, LR, LS, MW, MZ, MA, RW,
`ML, MR, M3, SN, TD, TG,
`JG, ZM, ZW, AM, AZ, 3Y, KG, KZ, RU, TJ,
`TM
`SD, SL, ST, SZ, TZ,
`W0 2018—US59209
`20181105
`W0 2019090222
`A1
`20190509
`
`
`W: A3, AG, AL, AM, A0, AT, AJ, AZ, 3A, 33, 3G, 3H, 3N, 3R,
`3W, 3Y,
`
`3Z, CA, CH, CL, CM, CO, CR, CU, CZ, 33, DJ, DK, DM, 30, DZ, 3C,
`
`««,
`4G, «S, II, G3, G3, G3, GH, GM, GT,
`4N,
`4R,
`4U,
`ID,
`IL,
`IN,
`IR,
`IS, J0, JP, K3, KG, Ki, KN, KP, KR, KW, KZ, LA, LC, LK, LR,
`LS, LJ, LY, MA, M3, M3, MG, MK, MN, MW, Mx, MY, MZ, MA, MG, MI,
`M0, MZ,
`0M, PA, P3, PG, Pi, PL, PT, QA, R0, RS, RU, RW, SA, SC,
`S3, S3, SG, SK, SL,
`SM, ST, SV, SY, 14, 1J,
`1M,
`1N,
`1R, 11, 1Z,
`JS,
`JZ, VC, VM, ZA, ZM,
`JA,
`JG,
`ZW
`
`4R,
`IR, G3, GR,
`RW: AL, AT, 33, 3G, Ci, CY, CZ, D3, DK, ««, «S, II,
`
`IT, LT, LJ, LV, MC, MK, MI, ML, N0, PL, PT, R0, RS,
`iJ,
`I3,
`IS,
`
`
`IR, 3P, 3J, CF, CG, CI, CM, GA, GN, GQ, GW, KM,
`SE, SI, SK,
`SM,
`
`3W, G4, GM, K3, LR, LS, MW, MZ, NA, RW,
`ML, MR, M3, SN, TD, TG,
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`Page 24
`
`

`

`16/461,512
`
`INFO.:
`
`
`TM
`SD, SL, ST, SZ, TZ, UG, ZM, ZW, AM, AZ, BY, KG, KZ, RU, TJ,
`US 20190183895
`A1
`20190620
`US 2018-16204964
`20181129
`
`32
`US 10369154
`20190806
`PRIORITY APPLN.
`
`A2 20170130
`WO 2017-US15608
`P
`20171103
`US 2017-62581478
`A
`20160129
`WO 2016-US15817
`P
`20160315
`US 2016-62308325
`P
`20161122
`US 2016-62425403
`A
`20180408
`US 2018-15947840
`
`
`
`
`
`ASSIGNMENT {ISTORY FOR US PATENT AVAILAQL? IN RSUS DISPLAY FORMAT
`
`OTH
`3R SOURCE(S):
`MARPAT 169:274678
`GI
`
`L1‘L27'Lu
`
`(R2)22
`
`I
`
`(R1)zl
`
`
`
`
`
`Imipridones selectively modulate Class A G protein-coupled receptors
`(GPCRs),
`such as the D2-like subfamily of dopamine receptors, and are
`useful for treating conditions and disorders in need of such modulation,
`such as cancers. Specifically,
`the cancer is a midline glioma, a cancer
`having a histone H3 mutation, or both.
`In addition, methods of identifying
`whether a subject having these conditions,
`is likely to be responsive to a
`treatment regimen,
`such as imipridone administration, are provided.
`Furthermore, methods of assessing the effectiveness of a treatment
`regimen,
`such as imipridone administration, monitoring, or providing a
`prognosis for a subject with these condition are also provided. Also
`disclosed is the preparation of compds. of the invention.
`'v\
`1C-“178~93HZP, ONC 202
`RL: PAC (Pharmacological activity); SPN (Synthetic preparation); TiU
`
`
`
`
`
`(Therapeutic use); 310% (Siological study); PREP (Preparation); USES
`(Uses)
`(ONC202;
`1638178—83—2
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`4—[(2—chlorophenyl)methyl]—2,4,6,7,8,9—hexahydro—7—(phenylmethyl)— (CA
`
`
`INDfiX NAMfi)
`
`IT
`
`RN
`CN
`
`Page 25
`
`

`

`16/461,512
`
`///CH24’Ph
`
`N
`
`f)”
`\\
`N
`“0
`
`CH2
`
`Cl
`
`IT
`
`RN
`CN
`
`
`"F, ONC 203
`
`
`
`
`
`-8w8
`
`{U
`RL: PAC (
`Pharmacological activity); SPN (Synthetic preparation); T
` (Therapeutic use); EIOL (Siological study); PREP (Preparation); USES
`(Uses)
`(ONC203;
`1638178—84-3
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`Tmidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`2,4,6,7,8,9—hexahydro—7—(phenylmethyl)—4—(2—thienylmethyl)—
`
`NAME)
`
`
`(CA INDEX
`
`///CH24*Ph
`
`N
`
`f1“
`\\
`N
`“0
`
`CH2
`
`5\
`
`{U
`
`S
`
`aL
`
`
`ONC 204
`i<€31?8»85w£P,
`RL: PAC (Pharmacological activity); SPN (Synthetic preparation); T
`
`
`
`(Therapeutic use); EIOL (Siological study); PREP (Preparation); US
`(Uses)
`(ONC204;
`1638178—85-4
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`Tmidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`2,4,6,7,8,9—hexahydro—4—(2—phenylethyl)—7—(phenylmethyl)—
`
`(CA IND
`
`
`
`EX NAME)
`
`IT
`
`RN
`
`CN
`
`Page 26
`
`

`

`16/461,512
`
`N//CH21Ph
`
`m \
`N7 N X0
`
`PhiCH2*CH2
`
`IT
`
`RN
`
`CN
`
`IT
`
`RN
`
`CN
`
`15351?9M85»5?, ONC 205
`RL: PAC (Pharmacological activity); SPN (Synthetic preparation); TiU
`
`
`
`
`(Therapeutic use); EIOL (Siological study); PREP (Preparation); USES
`(Uses)
`(ONC205;
`1638178-86-5
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—7—(phenylmetqyl)—4—[2—[4—(phenylmethyl)—l—
`
`
`piperaziny1]ethyl]— (CA INDEX NAME)
`
`///CH2”Ph
`
`
`
`~S?WSP, ONC 206
`
`(Pharmacological activity); SPN (Synthetic preparation); TiU
`
`
`
`
`(Therapeutic use); EIOL (Siological study); PREP (Preparation); USES
`(Uses)
`(ONC206;
`1638178—87-6
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`4—[(2,4—difluorophenyl)methyl]—2,4,6,7,8,9—hexahydro—7—(phenylmethyl)—
`
`
`(CA INDEX NAME)
`
`Page 27
`
`

`

`16/461,512
`
`///CH24’Ph
`
`N
`
`ffi
`\
`N
`N“
`
`CH2
`
`F
`
`F
`
`IT
`
`RN
`
`CN
`
`‘8“68m79, ONC 207
`
`RL: PAC (Pharmacological activity);
`RCT (Reac:ant); SPN (Synthetic
`
`
`
`preparation); THU (Therapeutic use); EIOL (Siological study); PREP
`
`(Preparation); RACT (Reactant or reagent);
`JSES (Uses)
`imipridones for treatment of gliomas)
`(ONC207;
`1638178—88—7
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`
`
`2,4,6,7,8,9—hexahydro—4—[(2—methylphenyl)methyl]— (CA INDEX NAME)
`
`NH
`
`f1“ \
`N
`\N \0
`
`\
`
`CH2
`
`Me
`
`:‘L. (“0“, ONC 208
`
`RL: PAC (Pharmacological activity); SPN (Synthetic preparation); TlU
`
`
`
`
`(Therapeutic use); EIOL (Siological study); PREP (Preparation); USES
`(Uses)
`(ONC208;
`1638178-89-8
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`2,4,6,7,8,9—hexahydro—7—methyl—4—[(2—methylphenyl)methyl]—
`
`NAME )
`
`
`(CA IND:
`
`IT
`
`RN
`
`CN
`
`Page 28
`
`
`
`

`

`16/461,512
`
`Me
`
`/
`N
`
`f“
`\\
`N
`N“
`
`CH2
`
`Me
`
`16381?9M%Q»1P, ONC 209
`RL: PAC (Pharmacological activity);
`
`
`(
`QIOR
`(Therapeutic use);
`Qiological
`(Uses)
`(ONC209;
`1638178—90-1
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`{U
`S
`
` eL
`
`T
`US
`
`SPN (Synthetic preparation);
`PR
`3P
`study);
`(Preparation);
`
`Tmidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—4—[(2—methylphenyl)methyl]—7—(2—phenylethyl)—
`
`
`
`INDfiX NAMfi)
`
`(CA
`
`CH2’*CH24*Ph
`
`iéi-GfimEP, ONC 210
`
`PAC (Pharmacological activity);
`
`
`(
`QIOL
`(Therapeutic use);
`Qiological
`(Uses)
`(ONCZlO;
`1977540—09—2
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`{U
`S
`
` eL
`
`T
`US
`
`SPN (Synthetic preparation);
`PR
` 3P
`study);
`(Preparation);
`
`Tmidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`4—[(3,5—difluorophenyl)methyl]—2,4,6,7,8,9—hexahydro—7—(phenylmethyl)—
`
`
`
`(CA INDfiX NAMfi)
`
`IT
`
`RN
`
`CN
`
`RN
`
`CN
`
`Page 29
`
`

`

`16/461,512
`
`N//CH21Ph
`
`m \
`NAN k0
`
`CH2
`
`F
`
`F
`
`IT
`
`RN
`
`CN
`
`1307851M§9»2P, ONC 211
`RL: PAC (Pharmacological activity); SPN (Synthetic preparation); TiU
`
`
`
`
`(Therapeutic use); EIOL (Siological study); PREP (Preparation); USES
`(Uses)
`(ONCle;
`1807861-50-2
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`4—[(3,4—dichlorophenyl)methyl]—2,4,6,7,8,9—hexahydro—7—(phenylmethyl)—
`
`
`(CA INDEX NAME)
`
`///CH24*Ph
`
`N
`
`f1“
`\\
`N
`“0
`
`CH2
`
`C1
`
`C1
`
`IT
`
`RN
`
`CN
`
`
`G “48- E, ONC 212
`‘=
`including toxicity); PAC (Pharmacological
`RL. ADV (Adverse effec:,
`
`activity); SPN (Synthe:ic preparation); THJ
`(Therapeutic use); EIOL
`
`
`(Biological study); PREP (Preparation); USES (Uses)
`(ONC212;
`imipridones for treatment of gliomas)
`1807861—48-8
`CAPLUS
`
`
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—7—(phenylmethyl)—4—[[4—
`
`
`(trifluoromethyl)phenyl]methyl]— (CA INDEX NAME)
`
`Page 30
`
`

`

`16/461,512
`
`N//CH21Ph
`
`cw
`N7 N\o
`
`CH2
`
`CF3
`
`etwl3 SP, ONC 213
`1.
`
`RL: PAC (Pharmacological activity); SPN (Synthetic preparation); TiU
`
`
`
`
`
`(Therapeutic use); EIOL (Siological study); PREP (Preparation); USES
`(Uses)
`(ONC213;
`1977540—13—8
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`Tmidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`
`4—[(3,4—difluorophenyl)methyl]—2,4,6,7,8,9—hexahydro—7—(phenylmethyl)—
`
`
`
`(CA INDEX NAME)
`
`RN
`
`CN
`
`N//CH21Ph
`
`m \
`NAV \0
`
`
`
`CH2
`
`//
`
`F
`
`”077“”S»15wGP, ONC 214
`RL: PAC (Pharmacological activity); SPN (Synthetic preparation); TiU
`
`
`
`
`
`(Therapeutic use); EIOL (Siological study); PREP (Preparation); USES
`(Uses)
`(ONC214;
`1977540—15—0
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`Tmidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(1H)—one,
`
`2,4,6,7,8,9—hexahydro—4—[(2—methylphenyl)methyl]—7—(phenyl—2,3,4,5,6—d5-
`
`
`
`methyl-d2)-
`(CA INDEX NAME)
`
`F
`
`IT
`
`RN
`
`CN
`
`Page 31
`
`

`

`16/461,512
`
`D
`
`NAA’CDZ
`
`WM
`N
`//\\
`N“
`
`CH2
`
`Me
`
`D
`
`D
`
`D
`
`D
`
`IT
`
`RN
`
`CN
`
`¥“~§W-¢E, ONC 215
`
`RL: PAC (Pharmacological activity); SPN (Synthetic preparation); TiU
`
`
`
`
`(Therapeutic use); EIOL (Siological study); PREP (Preparation); USES
`(Uses)
`(ONC215;
`1777785—69-9
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`Carbamic acid, N-[Z-[l,2,4,5,8,9—hexahydro—4—[(2—methylphenyl)methyl]—5—
`
`oxoimidazo[l,2—a]pyrido[3,4—e]pyrimidin—7(6H)—yl]ethyl]—,
`
`
`
`l,l-dimethylethyl ester
`(CA INDEX NAME)
`
`fi
`
`///CH2”CHgt’NH4’C4’03u-t
`
`N
`
`f)”
`\\
`N
`“0
`
`CH2
`
`Me
`
`IT
`
`RN
`
`CN
`
`”“77?85»7Qw2P, ONC 216
`RL: PAC (Pharmacological activity); SPN (Synthetic preparation); TiU
`
`
`
`
`(Therapeutic use); EIOL (Siological study); PREP (Preparation); USES
`(Uses)
`(ONC216;
`1777785—70—2
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`Tmidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`7—(3—aminopropyl)—2,4,6,7,8,9—hexahydro—4—[(2—methylphenyl)methyl]— (CA
`
`
`
`INDEX NAME)
`
`Page 32
`
`

`

`16/461,512
`
`/ (CH2)3*NH2
`
`N
`
`f1“ \
`N
`\N 20
`
`CH2
`
`Me
`
`IT
`
`RN
`
`CN
`
`“MRS, ONC 217
`
`RL: PAC (Pharmacological activity); SPN (Synthetic preparation); TiU
`
`
`
`
`
`(Therapeutic use); EIOL (Siological study); PREP (Preparation); USES
`(Uses)
`(ONC217;
`1977540—17—2
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`4—[(2—fluorophenyl)methyl]—2,4,6,7,8,9—hexahydro—7—(phenylmethyl)— (CA
`
`
`
`INDEX NAME)
`
`///CH24*Ph
`
`N
`
`CM
`\\
`N
`“0
`
`CH2
`
`F
`
`IT
`
`RN
`
`CN
`
`”077“39»1%w4P, ONC 218
`RL: PAC (Pharmacological activity); SPN (Synthetic preparation); TiU
`
`
`
`
`
`(Therapeutic use); EIOL (Siological study); PREP (Preparation); USES
`(Uses)
`(ONC218;
`1977540—19—4
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`4—[(4—fluoro—2—methylphenyl)methyl]—2,4,6,7,8,9—hexahydro—7—(phenylmethyl)—
`
`
`
`(CA INDEX NAME)
`
`Page 33
`
`

`

`l6/46l,5
`
`12
`
`///CH24’Ph
`
`N
`
`ffi
`\\
`N
`N“
`
`CH2
`
`Me
`
`F
`
`IT
`
`RN
`
`CN
`
`
`DSEHSE-QP, ONC 219
`l;
`
`RL: PAC (Pharmacological activity);
`
`
`(
`(Therapeutic use); QIOL
`Qiological
`(Uses)
`(ONC219;
`1807861—52—4
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`SPN (Synthetic preparation);
`
`PREP
`study);
`(Preparation);
`
`T
`US
`
`{U
`fl
`
`LS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`4—[(2,4—dichlorophenyl)methyl]—2,4,6,7,8,9—hexahydro—7—(phenylmethyl)—
`
`
`
`(CA INDfiX NAMfi)
`
`///CH24’Ph
`
`N
`
`ffi
`\\
`N
`V \\\0
`
`
`
`CH2
`
`//
`
`Cl
`
`IT
`
`RN
`
`CN
`
`Cl
`
`1‘
`RL:
`
`DUJ~:1“BE, ONC 220
`
`PAC (Pharmacological activity);
`
`
`(
`(Therapeutic use); QIOL
`Qiological
`(Uses)
`(ONCZZO;
`1815609—71—2
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`SPN (Synthetic preparation);
`PR
` 3P
`study);
`(Preparation);
`
`T
`US
`
`{U
`fl
`
`LS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—4—[(4—methoxyphenyl)methyl]—7—(phenylmethyl)—
`
`IND
` fiX NAM fl)
`
`(CA
`
`Page 34
`
`

`

`16/461,512
`
`///CH24*Ph
`
`N
`
`f1“
`\
`N
`V \\\0
`
`CH2
`
`
`
`//
`
`\\
`
`OMe
`
`IT
`
`RN
`
`CN
`
`
`1 ~ibQCM23»OP, ONC 221
`RL: PAC (Pharmacological activity); SPN (Synthetic preparation); TiU
`
`
`
`
`(Therapeutic use); EIOL (Siological study); PREP (Preparation); USES
`(Uses)
`(ONC221;
`1977540-23-0
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—4—[[4—(trifluoromethyl)phenyl]methyl]— (CA INDEX
`
`NAME)
`
`NH
`
`
`
`IT
`
`
`
`Q0»?7~39
`
`ONC 222
`
`RL:
`
`PAC (Pharmacological activity);
`SPN (Synthetic preparation); TiU
`(Preparation); USES
`
`
`
`(Therapeutic use); EIOL
`(Siological study); PREP
`(Uses)
`(ONC222;
`2241789-77-3
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—4—(3—isoxazolidinylmethyl)—7—(phenylmethyl)— (CA
`
`
`INDEX NAME)
`
`RN
`
`CN
`
`Page 35
`
`

`

`16/461,512
`
`///CH24*Ph
`
`N
`
`ffi
`\\
`N
`“0
`
`CH2
`
`NH
`
`/0
`
`IT
`
`RN
`
`CN
`
`1%???99M681?P, ONC 223
`RL: PAC (Pharmacological activity); SPN (Synthetic preparation); TiU
`
`
`
`
`(Therapeutic use); STOP (Siological study); PREP (Preparation); USES
`(Uses)
`(ONC223;
`1815609-68-7
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`Tmidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—4—[(4—methylphenyl)methyl]—7—(phenylmethyl)— (CA
`
`
`
`INDEX NAME)
`
`N//CH21Ph
`
`cw
`N7 NR0
`
`CH2
`
`Me
`
`IT
`
`RN
`
`CN
`
`
`Séflni7méP, ONC 224
`RL: PAC (Pharmacological activity); SPN (Synthetic preparation); TiU
`
`
`
`
`(Therapeutic use); STOP (Siological study); PREP (Preparation); USES
`(Uses)
`(ONC224;
`1977540—27—4
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`Tmidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—4—[2—(4—morpholinyl)ethyl]—7—(phenylmethyl)— (CA
`
`
`
`INDEX NAME)
`
`Page 36
`
`

`

`16/461,512
`
`///CH2ttPh
`
`N
`
`ffi
`\
`N
`V \\\0
`
`
`
`CH2
`
`CH2
`
`[:w:]0
`
`IT
`
`RN
`
`CN
`
`1.
`'%L~39 IE, ONC 225
`
`
`RL: PAC (Pharmacological activity); SPN (Synthetic preparation); TiU
`
`
`
`(Therapeutic use); EIOL (Siological study); PREP (Preparation); USES
`(Uses)
`(ONC225;
`1977540—29—6
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`4—[[2—fluoro—4—(trifluoromethyl)phenyl]methyl]—2,4,6,7,8,9—hexahydro—7-
`
`
`(phenylmethyl)— (CA INDEX NAME)
`
`///CH2”Ph
`
`N
`
`f)”
`\
`N
`N \\\0
`
`CH2
`
`F
`
`CF3
`
`IT
`
`RN
`
`CN
`
`
`EPRHC-flfi-As, ONC 226
`RL: PAC (Pharmacological activity); SPN (Synthetic preparation);
`
`
`
`(Therapeutic use); EIOL (Siological study); PREP (Preparation);
`(Uses)
`(ONC226;
`2112855—02—2
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`TiU
`USES
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`2,4,6,7,8,9—hexahydro—7—(phenylmethyl)—4—(3—pyridinylmethyl)—
`NAME)
`
`
`(CA IND
`
`Page 37
`
`

`

`16/461,512
`
`///CH2”Ph
`
`N
`
`f)”
`\\
`N
`“0
`
`CH2
`
`WN‘\
`
`{U
`S
`
` AL
`
`T
`US
`
`
`1 ~4o‘4M33»2P, ONC 227
`RL: PAC (Pharmacological activity); SPN (Synthetic preparation);
`
`
`(Therapeutic use); RIOL (Riological study); PREP (Preparation);
`(Uses)
`(ONC227;
`1977540—33—2
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—4,7—bis[[4—(trifluoromethyl)phenyl]methyl]—
`
`
`
`INDfiX NAMfi)
`
`(CA
`
`IT
`
`RN
`
`CN
`
`NtttCHZ
`
`f1“
`Nk\w <§>O
`
`
`
`CH2
`
`//
`
`CF3
`
`{U
`S
`
` AL
`
`T
`US
`
`”977““9»35w4P, ONC 228
`RL: PAC (Pharmacological activity); SPN (Synthetic preparation);
`
`
`(
`RIOL
`)
`; PREP
`(Therapeutic use);
`Riological study
`(Preparation);
`(Uses)
`(ONC228;
`1977540—35—4
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`7—[(4—fluorophenyl)methyl]—2,4,6,7,8,9—hexahydro—4—[[4—
`
`
`
`fiX NAMfi)
`(trifluoromethyl)phenyl]methyl]— (CA IND
`
`IT
`
`RN
`
`CN
`
`Page 38
`
`

`

`16/461,512
`
`FtttCHZ
`
`f“
`N
`//\\
`V \\\0
`
`
`
`CH2
`
`//
`
`\\
`
`IT
`
`RN
`
`CN
`
`CF3
`
`
`
`1;
`ufiGufiVwéP, ONC 229
`RL: PAC (Pharmacological activity);
`
`
`
`(Therapeutic use); QIOL (Qiological
`(Uses)
`(ONC229;
`1977540—37—6
`
`SPN (Synthetic preparation);
`study); PR 3P
`(Preparation);
`
`T
`US
`
`{U
`fl
`
`LS
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—7—[(4—methoxyphenyl)methyl]—4—[[4—
`
` fiX NAM
`(CA IND
`fl)
`(trifluoromethyl)phenyl]methyl]—
`
`OMe
`
`N44cCH2
`
`film
`\\
`N
`N“
`
`CH2
`
`CF3
`
`u.
`r A n ,.
`
`‘3 x: \
`1‘
`3}, ONC 230
`RL: PAC (Pharmacological activity);
`
`
`
`QTOL
`(
`(Therapeutic use);
`Qiological
`(Uses)
`(ONC230;
`1977540—39-8
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`SPN (Synthetic preparation);
`study); PR 3P
`(Preparation);
`
`T
`US
`
`{U
`fl
`
`LS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`RN
`
`CN
`
`Page 39
`
`

`

`16/461,512
`
`
`7—[4—(4—fluorophenyl)—4—oxobutyl]—2,4,6,7,8,9—hexahydro-4-[[4-
`
`
`
`(CA INDfiX NAMfi)
`(trifluoromethyl)phenyl]methyl]—
`
`fi
`
`F
`
`N44*(CH2)34*C
`
`WM
`\\
`N
`N“
`
`CH2
`
`CF3
`
`IT
`
`RN
`
`CN
`
`1;. SQCanmEP, ONC 231
`
`RL: PAC (Pharmacological activity);
`
`
`
`(Therapeutic use); QIOL (Qiological
`(Uses)
`(ONC23l;
`1977540—41—2
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`SPN (Synthetic preparation);
`study); PREP
`(Preparation);
`
`T
`US
`
`{U
`fl
`
`LS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—7—(3—pyridinylmethyl)—4—[[4—
`
`
`
`(CA INDfiX NAMfi)
`(trifluoromethyl)phenyl]methyl]—
`
`N44*CH2
`1
`
`//
`N
`\H
`
`f“
`\\
`N
`V \\\0
`
`
`
`CH2
`
`//
`
`\\
`
`CF3
`
`IT
`
`RN
`
`a;
`‘83~?8-EE, ONC 232
`
`
`RL: PAC (Pharmacological activity);
`
`
`
`(Therapeutic use); QIOL (Qiological
`(Uses)
`(ONC232;
`2241789—78—4
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`SPN (Synthetic preparation);
`study); PREP
`(Preparation);
`
`T
`US
`
`{U
`fl
`
`LS
`
`Page 40
`
`

`

`16/461,512
`
`CN
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—7—[(4—methyl—2—thiazolyl)methyl]—4—[[4—
`
`
`
`(CA INDfiX NAMfi)
`(trifluoromethyl)phenyl]methyl]—
`
`N
`
`M
`
`N44*CH244<%427// e
`
`s
`
`
`
`IT
`
`RN
`
`CN
`
`RN
`
`CN
`
`
`1 ~4o2u 1
`3?, ONC 233
`RL: PAC (Pharmacological activity);
`
`
`
`(Therapeutic use); QIOL (Qiological
`(Uses)
`(ONC233;
`1977540—45—6
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`SPN (Synthetic preparation);
`study); PREP
`(Preparation);
`
`T
`US
`
`{U
`fl
`
`LS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`2,4,6,7,8,9—hexahydro—7—(2—pyrazinylmethyl)—4—[[4—
`
`
`
`(CA INDfiX NAMfi)
`(trifluoromethyl)phenyl]methyl]—
`
`
`SQO“47~99, ONC 234
`1‘
`RL: PAC (Pharmacological activity);
`
`
`(
`QIOL
`(Therapeutic use);
`Qiological
`(Uses)
`(ONC234;
`1977540—47—8
`
`imipridones for treatment of gliomas)
`CAPLUS
`
`SPN (Synthetic preparation);
`
`study); PREP
`(Preparation);
`
`T
`US
`
`{U
`fl
`
`LS
`
`Imidazo[l,2—a]pyrido[3,4—e]pyrimidin—5(lH)—one,
`
`Page 4