- 16 -
`
`CAI el al.
`
`Application No. T0 be Assigned
`
`Amendments to the Claims
`
`This listing of claims will replace all prior versions, and listings, of claims in the application.
`
`1. (Original) A compound having the Formula 1:
`
`R5
`
`R
`
`(1)
`
`or a pharmaceutically acceptable salt or prodrug thereof, wherein:
`
`A is N or CR15,
`
`R1 is H, optionally substituted CH; alkyl, optionally substituted C2-g alkenyl, optionally
`
`substituted C3-g cycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl,
`
`R2 is an optionally substituted heterocyclic group, optionally substituted aryl, or optionally
`
`substituted heteroaryl,
`
`R3-R7 and R15 are independently H, halo, optionally substituted amino, optionally substituted
`
`alkoxy, optionally substituted C140 alkyl, haloalkyl, alkenyl, alkynyl, hydroxyalkyl, aminoalkyl,
`
`carboxyalkyl, nitro, cyano, acylamido, hydroxy,
`
`thiol, acyloxy, azido, carboxy, ethylenedioxo,
`
`hydroxyacylamino or optionally substituted alkylthiol.
`
`2. (Currently Amended) The compound of claim 1, wherein A is N; R1 and R2 are each
`
`independently optionally substituted aryl,; R3-R7 is are each independently H halo or C146 alkyl;
`
`and RE is H or CE alkyl.
`
`Atty. Dkt. No. 3386.0100002
`
`
`
`CAI el al.
`
`Application No. T0 be Assigned
`
`Amendments to the Claims
`
`This listing of claims will replace all prior versions, and listings, of claims in the application.
`
`1. (Original) A compound having the Formula 1:
`
`R5
`
`R
`
`(1)
`
`or a pharmaceutically acceptable salt or prodrug thereof, wherein:
`
`A is N or CR15,
`
`R1 is H, optionally substituted CH; alkyl, optionally substituted C2-g alkenyl, optionally
`
`substituted C3-g cycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl,
`
`R2 is an optionally substituted heterocyclic group, optionally substituted aryl, or optionally
`
`substituted heteroaryl,
`
`R3-R7 and R15 are independently H, halo, optionally substituted amino, optionally substituted
`
`alkoxy, optionally substituted C140 alkyl, haloalkyl, alkenyl, alkynyl, hydroxyalkyl, aminoalkyl,
`
`carboxyalkyl, nitro, cyano, acylamido, hydroxy,
`
`thiol, acyloxy, azido, carboxy, ethylenedioxo,
`
`hydroxyacylamino or optionally substituted alkylthiol.
`
`2. (Currently Amended) The compound of claim 1, wherein A is N; R1 and R2 are each
`
`independently optionally substituted aryl,; R3-R7 is are each independently H halo or C146 alkyl;
`
`and RE is H or CE alkyl.
`
`Atty. Dkt. No. 3386.0100002
`
`
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`- 17 -
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`CAI el al.
`
`Application No. T0 be Assigned
`
`3. (Original) The compound of claim 1, wherein said compound has Formula II:
`
`or pharmaceutically acceptable salts or prodrugs thereof, wherein:
`
`(11)
`
`R3-R7 are independently H, halo, optionally substituted amino, optionally substituted alkoxy,
`
`optionally substituted C140
`
`alkyl, haloalkyl,
`
`alkenyl,
`
`alkynyl, hydroxyalkyl,
`
`aminoalkyl,
`
`carboxyalkyl, nitro, cyano, acylamido, hydroxy,
`
`thiol, acyloxy, azido, carboxy, ethylenedioxo,
`
`hydroxyacylamino or optionally substituted alkylthiol,
`
`Ar1 and Arz are optionally substituted aryl or optionally substituted heteroaryl.
`
`4. (Original) The compound of claim 3, wherein R3-R7 are H, Ar1 and Arz are optionally
`
`substituted phenyl.
`
`5. (Currently Amended) The compound of claim 1, wherein said compound is selected from
`
`the group consisting of:
`
`6-(2-Chlorophenyl)-2-((4-(4-methylpiperazin-l-yl)phenyl)amino)-8,9-dihydroimidazo[1,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Chloro-6-fluorophenyl)-2-((4-(4-methylpiperazin-l-yl)phenyl)amino)-8,9-
`
`dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)—one,
`
`4-(2-Chlorophenyl)-8-((4-(4-methylpiperazin-l-yl)phenyl)amino)-2,4-dihydroimidazo[1,2-
`
`a]pyrido[3,4-e]pyrimidin-5(lH)—one,
`
`6-(2,6-Dichlorophenyl)-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-8,9-dihydroimidazo[l ,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Chloro-6-methylphenyl)-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-8,9-
`
`dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)—one,
`
`Atty. Dkt. No. 3386.0100002
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`
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`- 18 -
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`CAI el al.
`
`Application No. T0 be Assigned
`
`6-(2-Ch1oro-6-fluoropheny1)-2-((4-(4-isopropylpiperazin-1 -y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`2-((4-(4-Acetylpiperazin-1-y1)pheny1)amino)-6-(2-ch1oro—6-fluoropheny1)—8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro-6-fluoropheny1)-2-((2-methy1-1,2,3 ,4-tetrahydroisoquinolin-7-yl)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro—6-fluorophenyl)-2-((2,4,4-trimethy1-1,2,3 ,4-tetrahydroisoquinolin-7-yl)amino)-
`
`8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro-6-fluoropheny1)-2-((2'-methy1-2',3 '-dihydro- 1 'H-spiro(cyclopropane- 1 ,4'-
`
`isoquinolin)-7'-y1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro—6-fluoropheny1)—2-((2'-acety1-2',3'-dihydro—1'H-spiro[cyclopropane-1,4'—
`
`isoquinolin]-7'-y1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,6-Dichloropheny1)-2-((2-methy1-1,2,3 ,4-tetrahydroisoquinolin-7-yl)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,6-Dichloropheny1)-2-((2,4,4-trimethy1-1,2,3 ,4-tetrahydroisoquinolin-7-yl)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,6-Dichlorophenyl)—2-((2'-methy1-2',3'-dihydro-1'H-spiro(cyclopropane-1,4'-isoquinolin)-
`
`7'-y1)amino)—8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,6-Dimethy1pheny1)-2-((2-methyl-1,2,3 ,4-tetrahydroisoquinolin-7-yl)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,6-Dimethy1pheny1)-2-((2,4,4-trimethy1- 1 ,2,3 ,4-tetrahydroisoquinolin-7-y1)amino)—8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,6-Dimethy1phenyl)—2-((2'-methy1-2',3'-dihydro-1'H-spiro[cyclopropane-1,4'—isoquinolin]—
`
`7'-y1)amino)—8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-Isopropy1-2-((4-(4-methy1piperazin-1-y1)pheny1)amino)-8,9-dihydroimidazo[1,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(Tert-buty1)-2-((4-(4-methy1piperazin-1-y1)pheny1)amino)-8,9-dihydroimidazo[1,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-Cyclopropyl-2-((4-(4-methylpiperazin-1-y1)pheny1)amino)—8,9-dihydroimidazo[1,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`Atty. Dkt. No. 33860100002
`
`
`
`- 19 -
`
`CAI el al.
`
`Application No. T0 be Assigned
`
`6-Cyclohexyl-2-((4-(4-methy1piperazin-1-y1)pheny1)amino)-8,9-dihydroimidazo[1,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-A11y1-2-((4-(4-methylpiperazin-1-y1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-
`
`e]pyrimidin-5(6H)-one,
`
`2-((4-(4-Methylpiperazin-1-y1)pheny1)amino)-6-(thiophen-Z-y1)-8,9-dihydroimidazo[1,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(Furan-2-y1)-2-((4-(4-methy1piperazin-1-y1)pheny1)amino)—8,9-dihydroimidazo[1,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`2-((4-(4-Methy1piperazin-1-y1)pheny1)amino)-6-(1H-pyrrol-Z-y1)-8,9-dihydroimidazo[1,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(1H-Imidazol-S-y1)-2-((4-(4-methylpiperazin-1-y1)pheny1)amino)-8,9-dihydroimidazo[1,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro—6-fluoropheny1)—8,8-dimethy1-2-((4-(4-methylpiperazin-1-y1)pheny1)amino)—8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro—6-fluoropheny1)—9,9-dimethy1-2-((4-(4-methylpiperazin-1-y1)pheny1)amino)—8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro—6-fluoropheny1)—2-((4-((2S,6R)-2,6-dimethy1morpholino)pheny1)amino)-8,9-
`
`dihydroimidazo[1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro-6-fluorophenyl)-2-((4-(morpholinomethy1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro-6-fluoropheny1)—2-((4-((3 S, 5R)-3 ,4, 5-trimethy1piperazin- 1 -y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro-6-fluoropheny1)—2-((4-((3 S, 5R)-4-isopropyl-3 ,5-dimethy1piperazin-1-
`
`y1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro-6-fluoropheny1)-2-((2-fluoro-4-(4-methy1piperazin-1-y1)pheny1)amino)—8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro-6-fluoropheny1)-2-((2-fluoro-4-((3 S,5R)—3 ,4, 5-trimethy1piperazin-1-
`
`y1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((2-chloro-4-(4-methy1piperazin-1-y1)pheny1)amino)—8,9-
`
`dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`Atty. Dkt. No. 33860100002
`
`
`
`- 20 -
`
`CAI el al.
`
`Application No. T0 be Assigned
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((2-ch1oro-4-((3 S, 5R)-3 ,4, 5-trimethy1piperazin-1-
`
`y1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro—6-fluorophenyl)-2-((4-(4-methylpiperazin-1-y1)-2-
`
`(trifluoromethy1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1 oro-6-fluoropheny1)-2-((2-trifluoromethy1-4-((3 S, 5R)-3 ,4, 5 -trimethy1piperazin-1-
`
`y1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((2-methy1-4-(4-methy1piperazin-1-y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro-6-fluoropheny1)-2-((2-methy1-4-((3 S,5R)—3 ,4,5-trimethy1piperazin-1-
`
`y1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((3 -fluoro—4-(4-methy1piperazin-1-y1)pheny1)amino)—8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro—6-fluoropheny1)—2-((3 -fluoro-4-((3 S,5R)—3 ,4, 5-trimethy1piperazin-1-
`
`y1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((3 -ch1oro-4-(4-methy1piperazin-1-y1)pheny1)amino)—8,9-
`
`dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`2-((3-Chloro-4-((3 S,5R)—3 ,4, 5-trimethy1piperazin-1-y1)pheny1)amino)-6-(2-ch1oro—6-
`
`fluorophenyl)—8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((4-(4-methy1piperazin-1-y1)-3 -
`
`(trifluoromethy1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((3 -trifluoromethyl-4-((3 S, 5R)-3 ,4, 5 -trimethy1piperazin-1-
`
`y1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((3 -methy1-4-(4-methy1piperazin-1-y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((3 -methy1-4-((3 S,5R)—3 ,4,5-trimethy1piperazin-1-
`
`y1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro-6-fluoropheny1)-2-((4-(4-isopropylpiperazin-1-y1)-3 -methy1pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro-6-fluoropheny1)—2-((4-((3 S, 5R)-4-isopropyl-3 ,5-dimethy1piperazin-1-y1)—3 -
`
`methylpheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`Atty. Dkt. No. 33860100002
`
`
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`- 21 -
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`CAI el al.
`
`Application No. T0 be Assigned
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((3 -methoxy-4-(4-methy1piperazin-1-y1)pheny1)amino)-8,9-
`
`dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro-6-fluoropheny1)-2-((4-(4-methy1piperazin-1 -y1)—3 -nitrophenyl)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((3 , 5-dimethy1-4-(4-methy1piperazin- 1 -y1)pheny1)amino)—8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro-6-fluoropheny1)-2-((6-4-(4-methy1piperazin-1 -y1)pyridin-3 -y1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro—6-fluorophenyl)-2-((2'-isopropyl-Z',3'-dihydro-1'H-spiro[cyclopropane-1,4'—
`
`isoquinolin]-7'-y1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((5-methy1-4, 5,6,7-tetrahydropyrazolo[1,5-a]pyrazin-2-
`
`y1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2, 6-Difluorophenyl)-2-((3 -methy1-4-(4-methy1piperazin- 1 -y1)pheny1)amino)-8, 9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-F1uoro—6-(trifluoromethy1)phenyl)-2-((3 -methy1-4-(4-methy1piperazin-1-
`
`y1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-F1uoro-6-methy1pheny1)-2-((3 -methy1-4-(4-methy1piperazin-1-y1)pheny1)amino)—8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2,6-Dichloropheny1)-2-((4-(4-isopropylpiperazin-1-y1)pheny1)amino)—8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2,6-Dichloropheny1)-2-((4-((3 S, 5R)-3 ,4,5-trimethy1piperazin-1-y1)pheny1)amino)—8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2,6-Dichlorophenyl)—2-((4-((3 S,5R)-4-isopropy1-3 ,5-dimethy1piperazin- 1 -y1)pheny1)amino)-
`
`8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2,6-Dichloropheny1)-2-((2-fluoro-4-((3 S, 5R)-3 ,4,5-trimethy1piperazin-1-y1)pheny1)amino)—
`
`8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2,6-Dichlorophenyl)-2-((2-chloro-4-((3 S, 5R)-3 ,4,5-trimethy1piperazin-1-y1)pheny1)amino)-
`
`8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2,6-Dichloropheny1)-2-((2-trifluoromethy1-4-((3 S, 5R)-3 ,4,5-trimethy1piperazin-1-
`
`y1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`Atty. Dkt. No. 33860100002
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`- 22 -
`
`CAI el al.
`
`Application No. T0 be Assigned
`
`6-(2,6-Dichloropheny1)—2-((3 -fluoro—4-(4-methy1piperazin- 1 -y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2,6-Dichloropheny1)-2-((3 -fluoro-4-((3 S, 5R)-3 ,4,5-trimethy1piperazin-1-y1)pheny1)amino)—
`
`8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2, 6-Dichloropheny1)—2-((3 -ch1ore-4-(4-methy1piperazin-1-y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2, 6-Dichloropheny1)—2-((3 -chloro-4-((3 S, 5R)-3 ,4, 5 -trimethy1piperazin- 1 -y1)pheny1)amino)-
`
`8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2, 6-Dichl oropheny1)-2-((4-(4-methy1piperazin- 1 -y1)—3 -(trifluoromethy1)pheny1)amino)-8, 9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2, 6-Dichloropheny1)—2-((3 -trifluoromethyl-4-((3 S, 5R)-3 ,4, 5 -trimethy1piperazin-1-
`
`y1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2,6-Dichloropheny1)-2-((3 -methy1-4-(4-methy1piperazin-1-y1)pheny1)amino)—8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2,6-Dichloropheny1)-2-((4-(4-isopropylpiperazin- 1 -y1)—3 -methy1phenyl)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2, 6-Dichloropheny1)—2-((3 -methy1-4-((3 S, 5R)—3 ,4, 5 -trimethy1piperazin-1-y1)pheny1)amino)-
`
`8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2,6-Dichlorophenyl)—2-((4-((3 S,5R)-4-isopropy1-3 ,5-dimethy1piperazin-1-y1)-3 -
`
`methylpheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2,6-Dichlorophenyl)—2-((5-methy1-4,5,6,7-tetrahydropyrazolo[ 1 , 5-a]pyrazin-2-y1)amino)-
`
`8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro-6-(trifluoromethy1)pheny1)-2-((3 -methy1-4-(4-methy1piperazin-1-
`
`y1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro—6-methy1pheny1)—2-((3 -methy1-4-(4-methy1piperazin-1-y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2-Ch1oro—6-methoxypheny1)-2-((3 -methy1-4-(4-methy1piperazin-1-y1)pheny1)amino)—8, 9-
`
`dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2,6-Dimethylphenyl)-2-((4-((3 S, 5R)-3 ,4,5-trimethy1piperazin-1-y1)pheny1)amino)—8,9-
`
`dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`Atty. Dkt. No. 33860100002
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`
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`- 23 -
`
`CAI el al.
`
`Application No. T0 be Assigned
`
`6-(4-Ch1oropheny1)-2-((4-(4-methy1piperazin- 1 -y1)pheny1)amino)-8,9-dihydroimidazo[ 1 ,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(3 -Ch1orophenyl)-2-((4-(4-methy1piperazin-1-y1)pheny1)amino)-8,9-dihydroimidazo[1,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,4-Dichlorophenyl)-2-((4-(4-methylpiperazin-1-y1)pheny1)amino)—8,9-dihydroimidazo[1,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro-4-fluorophenyl)-2-((4-(4-methy1piperazin-1-y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1 oro-3 -fluoropheny1)-2-((4-(4-methy1piperazin- 1 -y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2, 5 -Dichl oropheny1)-2-((4-(4-methy1piperazin- 1 -y1)pheny1)amino)—8, 9-dihydroimidazo[1,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2, 3 -Dichl oropheny1)-2-((4-(4-methy1piperazin- 1 -y1)pheny1)amino)—8, 9-dihydroimidazo[1,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(Pyrimidin-2-y1)-2-((4-(4-methy1piperazin-1-y1)pheny1)amino)-8,9-dihydroimidazo[1,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`2-((4-(4-Methylpiperazin-1-y1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-
`
`e]pyrimidin-5(6H)-one;
`
`6-Cyclobuty1-2-((4-(4-methy1piperazin-1-y1)pheny1)amino)—8,9-dihydroimidazo[1,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-Cyclopentyl-2-((4-(4-methy1piperazin-1-y1)pheny1)amino)-8,9-dihydroimidazo[1,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one);
`
`6-Pheny1-2-((4-(4-methylpiperazin-1-y1)pheny1)amino)-8,9-dihydroimidazo[1,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(Pyridin-2-yl)—2-((4-(4-methy1piperazin-1-y1)pheny1)amino)-8,9-dihydroimidazo[1,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(Pyridin-3 -y1)-2-((4-(4-methy1piperazin-1-y1)pheny1)amino)-8,9-dihydroimidazo[1,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(Pyridin-4-yl)—2-((4-(4-methy1piperazin-1-y1)pheny1)amino)-8,9-dihydroimidazo[1,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`Atty. Dkt. No. 33860100002
`
`
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`- 24 -
`
`CAI el al.
`
`Application No. T0 be Assigned
`
`6-(2,6-Difluoropheny1)-2-((3-ch1oro—4-(4-methy1piperazin- 1 -y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,6-Difluorophenyl)-2-((3 ,5-dimethy1-4-(4-methylpiperazin- 1 -y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((4-(lH-imidazol-l -y1)pheny1)amino)-8,9-dihydroimidazo[ 1 ,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((4-(4-methyl-1,4-diazepan-1-y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro-6-fluoropheny1)-2-((4-((4-methy1piperazin-1-y1)methy1)pheny1)amino)-8,9-
`
`dihydroimidazo[1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro—6-fluorophenyl)-2-((4-(2-(dimethy1amino)ethoxy)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro-6-fluoropheny1)-2-((4-(3-(dimethy1amino)propoxy)pheny1)amino)-8,9-
`
`dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro-6-fluoropheny1)-2-((4-((1-methy1piperidin-4-y1)oxy)pheny1)amino)—8,9-
`
`dihydroimidazo[1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro-6-fluoropheny1)-2-((4-((2-(dimethy1amino)ethy1)amino)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro-6-fluoropheny1)-2-((4-((2-(dimethy1amino)ethyl)(methyl)amino)pheny1)amino)-
`
`8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro-6-fluoropheny1)-2-((4-((3 -(dimethy1amino)propy1)amino)pheny1)amino)—8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro-6-fluoropheny1)-2-((4-((3 -(dimethy1amino)propy1)(methyl)amino)phenyl)amino)-
`
`8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro-6-fluoropheny1)-2-((4-(( 1 -methy1piperidin-4-y1)amino)pheny1)amino)—8,9-
`
`dihydroimidazo[1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro-6-fluoropheny1)-2-((4-(methy1(1 -methy1piperidin-4-y1)amino)pheny1)amino)-8,9-
`
`dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((4-(1-methy1piperidin-4-y1)phenyl)amino)—8,9-
`
`dihydroimidazo[1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`Atty. Dkt. No. 33860100002
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`
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`- 25 -
`
`CAI el al.
`
`Application No. T0 be Assigned
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((4-(4-(dimethy1amino)piperidin- 1 -y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((4-(4-(dimethy1amino)piperidin- 1 -y1)-3 -fluoropheny1)amino)-
`
`8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro—6-fluoropheny1)—2-((3 -ch1 oro—4-(4-(dimethy1amino)piperi din- 1 -y1)pheny1)amino)-
`
`8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1 oro—6-fluoropheny1)-2-((3 -bromo—4-(4-(dimethy1amino)piperidin-1-y1)pheny1)amino)—
`
`8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((4-(4-(dimethy1amino)piperidin- 1 -y1)-3 -methy1phenyl)amino)—
`
`8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((3 -fluoro-5-methy1-4-(4-(dimethy1amino)piperidin- 1 -
`
`y1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1 oro—6-fluoropheny1)-2-((5 -(4-methy1piperazin-1-y1)pyrazin-Z-y1)amin0)-8, 9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((3 , 5 -dichloro—4-(4-methy1piperazin- 1 -y1)pheny1)amino)—8, 9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((3 -fluoro-5-methy1-4-(4-methy1piperazin-1-y1)pheny1)amino)—
`
`8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro—6-fluoropheny1)—2-((3 -fluoro—5 -methoxy-4-(4-methy1piperazin-1-
`
`y1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((3 -chloro-5-methy1-4-(4-methy1piperazin-1-y1)pheny1)amino)-
`
`8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((3 -chloro-5-methoxy-4-(4-methy1piperazin-1-
`
`y1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((3 -bromo-5-methoxy-4-(4-methy1piperazin-1-
`
`y1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((3 -methyl-4-(4-methylpiperazin-1-y1)-5-
`
`(trifluoromethy1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro—6-fluoropheny1)-2-((3 -methoxy-5-methy1-4-(4-methy1piperazin-1-
`
`y1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`Atty. Dkt. No. 33860100002
`
`
`
`- 26 -
`
`CAI el al.
`
`Application No. T0 be Assigned
`
`6-(2,6-Dichloropheny1)—2-((5-chloro-2-methy1-1,2,3,4-tetrahydroisoquinolin-7-y1)amino)-8,9-
`
`dihydroimidazo[l,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`7
`7
`7
`6-(2,6-Dichloropheny1)—2-((2,5-dimethy1-1 2 3 4-tetrahydroisoquinolin-7-y1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`
`
`6-(2,6-Dichlorophenyl)—2-((2,4,4, 5-tetramethy1-1,2,3 ,4-tetrahydroisoquinolin-7-y1)amin0)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2,6-Dichloropheny1)—2-((5'-chloro-2'-methyl-2',3'-dihydro-1'H-spiro(cyclopropane-1,4'—
`
`isoquinolin)-7'-y1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2,6-Dichloropheny1)-2-((2',5'—dimethy1-2',3'-dihydro—1'H-spiro[cyclopropane-1,4'-
`
`isoquinolin]-7'-y1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2,6-Dichloropheny1)—2-((3 ,5-dichloro-4-((3 S,5R)-3 ,4, 5-trimethy1piperazin-1-
`
`y1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2,6-Dichloropheny1)—2-((3 -chloro-5-methy1-4-((3 S,5R)—3 ,4, 5-trimethy1piperazin-1-
`
`y1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2,6-Dichloropheny1)-2-((4-(4-(dimethy1amino)piperidin-1 -y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2, 6-Dichloropheny1)-2-((3 -ch1oro—4-(4-(dimethy1amino)piperidin-1-y1)phenyl)amino)-8, 9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2, 6-Dichloropheny1)-2-((3 -bromo—4-(4-(dimethy1amino)piperidin-1-y1)pheny1)amino)—8, 9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2,6-Dichloropheny1)-2-((4-(4-(dimethy1amino)piperidin-1 -y1)-3 -methy1phenyl)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2, 6-Dichloropheny1)-2-((3 , 5 -dichloro-4-(4-(dimethy1amino)piperidin-1-y1)pheny1)amino)—
`
`8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`6-(2,6-Dichloropheny1)-2-((4-(4-(dimethy1amino)piperidin-1-y1)-3 -fluoro-5-
`
`methylpheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one,
`
`Atty. Dkt. No. 33860100002
`
`
`
`- 27 -
`
`CAI el al.
`
`Application No. T0 be Assigned
`
`6-(2,6-Dichloropheny1)-2-((3 -ch1oro-4-(4-(dimethylamino)piperidin-1-y1)-5-
`
`methoxypheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)—one;
`
`6-(2, 6-Dichloropheny1)-2-((3 -bromo-4-(4-methy1piperazin- 1 -y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2, 6-Dichloropheny1)-2-((3 -methoxy-4-(4-methy1piperazin-1-y1)pheny1)amino)-8, 9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,6-Dichloropheny1)—2-((3 -chloro-5-fluoro—4-(4-methy1piperazin- 1 -y1)pheny1)amino)—8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,6-Dichloropheny1)—2-((3 -fluoro—5-methy1-4-(4-methylpiperazin-1-y1)pheny1)amino)—8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,6-Dichloropheny1)-2-((3 -fluoro-5-methoxy-4-(4-methy1piperazin-1-y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,6-Dichloropheny1)—2-((3 ,5-dichloro-4-(4-methy1piperazin-1-y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,6-Dichloropheny1)—2-((3 -chloro-5-methy1-4-(4-methy1piperazin-1-y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,6-Dichloropheny1)-2-((3 -ch1oro—4-(4-methy1piperazin-1-y1)-5-
`
`(trifluoromethy1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,6-Dichloropheny1)—2-((3 -chloro-5-methoxy-4-(4-methy1piperazin-1-y1)pheny1)amino)—8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,6-Dichloropheny1)—2-((3 -bromo—5-fluoro-4-(4-methy1piperazin-1-y1)pheny1)amino)—8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,6-Dichloropheny1)—2-((3 -bromo-5-ch1ore-4-(4-methy1piperazin-1-y1)pheny1)amino)—8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,6-Dichloropheny1)—2-((3 -bromo—5-methy1-4-(4-methy1piperazin-1-y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,6-Dichloropheny1)—2-((3 -bromo-5-methoxy-4-(4-methy1piperazin-1-y1)pheny1)amino)—
`
`8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,6-Dichloropheny1)-2-((3 , 5-dimethy1-4-(4-methy1piperazin- 1 -y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`Atty. Dkt. No. 33860100002
`
`
`
`- 28 -
`
`CAI el al.
`
`Application No. T0 be Assigned
`
`6-(2,6-Dichloropheny1)—2-((3 -methoxy-5-methy1-4-(4-methy1piperazin-1-y1)pheny1)amino)-
`
`8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Bromo-6-chlorophenyl)-2-((4-(4-(dimethy1amino)piperidin-1-y1)-3-fluoro—5-
`
`methylpheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-B romo—6-chloropheny1)-2-((3 -ch1oro-4-(4-methy1piperazin-1-y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Bromo—6-chloropheny1)-2-((3 -bromo-4-(4-methy1piperazin-1-y1)pheny1)amino)-8, 9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-B romo—6-chloropheny1)-2-((3 -methy1-4-(4-methy1piperazin-1-y1)pheny1)amino)—8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Bromo—6-chloropheny1)-2-((3 ,5-dichloro-4-(4-methy1piperazin-1-y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Bromo—6-chloropheny1)-2-((3 -fluoro—5-methy1-4-(4-methy1piperazin-1-y1)pheny1)amino)-
`
`8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Bromo—6-chloropheny1)-2-((3 -ch1oro—5-methy1-4-(4-methy1piperazin-1-y1)pheny1)amino)—
`
`8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Bromo—6-chloropheny1)-2-((3 -bromo—5-methy1-4-(4-methy1piperazin- 1 -y1)pheny1)amino)—
`
`8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-F1uoro-6-methy1pheny1)-2-((3 -ch1oro—4-(4-methy1piperazin- 1 -y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-F1uoro-6-methy1pheny1)—2-((3 , 5 -dimethy1-4-(4-methy1piperazin-1-y1)pheny1)amino)-8, 9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1ore-6-methy1pheny1)-2-((4-(4-(dimethy1amino)piperidin- 1 -y1)-3-fluoro-5-
`
`methylpheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro—6-methy1pheny1)—2-((3 -ch1oro-4-(4-methy1piperazin-1-y1)pheny1)amino)—8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro-6-methy1pheny1)-2-((3 , 5-dichloro-4-(4-methy1piperazin-1-y1)pheny1)amino)-8,9-
`
`dihydroimidazo[ 1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Ch1oro—6-methy1pheny1)—2-((3 -ch1oro—5-methy1-4-(4-methy1piperazin- 1 -
`
`y1)pheny1)amino)-8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`Atty. Dkt. No. 33860100002
`
`
`
`- 29 -
`
`CAI el al.
`
`Application No. T0 be Assigned
`
`6-(2-Chloro—6-methylphenyl)-2-((3 ,5-dimethyl-4-(4-methylpiperazin-1-yl)phenyl)amino)—8,9-
`
`dihydroimidazo[ l ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,6-Dichlorophenyl)—2-((4-(piperazin-1-yl)phenyl)amino)-8,9-dihydroimidazo[1,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2, 6-Dichlorophenyl)—2-((3 -chloro-4-(piperazin-1-yl)phenyl)amino)-8,9-dihydroimidazo[1,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2, 6-Dichlorophenyl)—2-((3 -methyl-4-(piperazin- l -yl)phenyl)amino)—8,9-
`
`dihydroimidazo[ l ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2, 6-Dichlorophenyl)—2-((3 -methoxy-4-(piperazin-1-yl)phenyl)amino)-8,9-
`
`dihydroimidazo[ l ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Chloro—6-fluorophenyl)-2-((3 -(hydroxymethyl)-4-(piperazin-1-yl)phenyl)amino)-8,9-
`
`dihydroimidazo[ l ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2, 6-Dichlorophenyl)—2-((3 -(hydroxymethyl)-4-(piperazin-1-yl)phenyl)amino)—8, 9-
`
`dihydroimidazo[ l ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`
`
`6-(2,6-Dichlorophenyl)—2-((4-(4-(2-hydroxyethyl)piperazin- l -yl)phenyl)amino)—8,9-
`
`dihydroimidazo[ l ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,6-Dichlorophenyl)-2-((4-morpholinophenyl)amino)-8,9-dihydroimidazo[ l ,2-
`
`a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2,6-Dichlorophenyl)—2-((3 -((methylamino)methyl)-4-morpholinophenyl)amino)—8,9-
`
`dihydroimidazo[1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2-Bromo—6-chlorophenyl)-2-((3 -chloro-4-(4-(dimethylamino)piperidin-1 -yl)phenyl)amino)-
`
`8,9-dihydroimidazo[1 ,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one;
`
`6-(2, 6-Dichlorophenyl)—2-((3 -chloro-4-(4-methylpiperazin-1-yl)phenyl)amino)-8,9-
`
`dihydroimidazo[l,2-a]pyrimido[5,4-e]pyrimidin-5(6H)—one dihydrochloride;
`
`or a pharmaceutically acceptable salt or prodrug thereof.
`
`Atty. Dkt. No. 33860100002
`
`
`
`- 3O -
`
`CAI el al.
`
`Application No. T0 be Assigned
`
`6-7.
`
`(Canceled).
`
`8. (Currently Amended) A pharmaceutical composition comprising the compound of any—ef‘
`
`el-ai-ms claim l—teé and a pharmaceutically acceptable carrier.
`
`9. (Original) The pharmaceutical composition of claim 8, further comprising at least one
`
`known anticancer agent, or a pharmaceutically acceptable salt of said anticancer agent.
`
`10. (Currently Amended) The pharmaceutical composition of claim 8+9, wherein said
`
`composition includes at
`
`least one of the following anticancer drugs: busulfan, melphalan,
`
`chlorambucil, cyclophosphamide, ifosfamide, temozolomide, bendamustine, cis-platin, mitomycin
`
`C,
`
`bleomycin,
`
`carboplatin,
`
`camptothecin,
`
`irinotecan,
`
`topotecan,
`
`doxorubicin,
`
`epirubicin,
`
`aclarubicin, mitoxantrone,
`
`elliptinium,
`
`etoposide, 5-azacytidine, gemcitabine, 5-fluorouracil,
`
`methotrexate, 5-fluoro-2'—deoxy-uridine, fludarabine, nelarabine, ara-C, pralatrexate, pemetrexed,
`
`hydroxyurea, thioguanine, colchicine, Vinblastine, Vincristine, Vinorelbine, paclitaxel, ixabepilone,
`
`cabazitaxel,
`
`docetaxel,
`
`campath,
`
`panitumumab, metazotuzumab,
`
`navuzumab,
`
`pymzumab,
`
`remoluzumab, bevacizumab, partuzumab,
`
`trastuzumab, cetuXimab, obinutuzumab, olfamzumab,
`
`rituXimab, alemtuzumab, tiemuzumab, toximab, bentuXimab, daremuzumab, errotuzumab, T-DMl,
`
`ofatumumab, dinutuXimab, blinatumomab,
`
`ipilimma, avastin,
`
`trastuzumab,
`
`rituXimab,
`
`imatinib,
`
`gefitinib, erlotinib, osimertinib, afatinib, ceritinib, aletinib, crizotinib, erlotinib, lapatinib, sorafenib,
`
`sunitinib, nilotinib, dasatinib, pazopanib,
`
`temsirolimus,
`
`everolimus, vorinostat,
`
`romidepsin,
`
`panobinostat, belinostat, tamoxifen, letrozole, fulvestrant, mitoguazone, octreotide, retinoic acid,
`
`arsenic trioxide, zoledronic acid, bortezomib, carfilzomib,
`
`ixazomib, Vismodegib,
`
`sonidegib,
`
`denosumab, thalidomide, lenalidomide, venetoclaX, aldesleukin (recombinant human interleukin-2),
`
`sipueucel-T (prostate cancer therapeutic vaccine), palbociclib, olaparib, niraparib, rucaparib and
`
`talazoparib.
`
`11. (New) The compound of claim 3, wherein Arz is phenyl optionally substituted by one,
`
`two, three or four groups selected from the group consisting of: optionally substituted piperazinyl,
`
`optionally substituted piperazinyl-Cl-C4 alkyl, optionally substituted piperidinyl,
`
`imidazolyl,
`
`Atty. Dkt. No. 3386.0100002
`
`
`
`- 31 -
`
`CAI el al.
`
`Application No. T0 be Assigned
`
`optionally substituted 1,4-diazaheterocycloheptyl, C1-C6 alkyl, C1-C6 acyl, optionally substituted
`
`morpholinyl, morpholinyl-Cl-C4 alkyl, halo, halo C1-C6 alkyl, optionally substituted C1-C6 alkoxy,
`
`optionally substituted hydroxy C1-C6 alkyl, optionally substituted amino C1-C6 alkyl, optionally
`
`substituted piperidinylamino, optionally substituted C1-C6 alkyl amino, opt
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