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US 2016/0106743 A1Published application
Topoisomerase ii poisons and methods of making and using same
AssigneeUniversity of Rochester
InventorDavid Goldfarb
Life of this patent
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Abstract
Disclosed herein are compositions of Formula I and an optional anticancer drug. Also disclosed herein are methods of treating or preventing cancer using the same.
Claims21
A composition, comprising:
- a topoisomerase II poison of Formula I:
- wherein
- each R1 is, independently, F, Cl, Br, I, OH, SH, (CH2)kCO2R5, (CH2)kOC(O)R5, (CH2)kNR5R6, or CN;
- or C1-8 alkyl or cycloalkyl optionally substituted with one or more F, Cl, Br, I, OH, SH, ═O, ═S, NH2, (CH2)kCO2R5, (CH2)kNR5R6, OC1-8 alkyl, or CN;
- n is 0, 1, 2, 3, or 4;
- each R2 is, independently, F, Cl, Br, I, OH, SH, (CH2)kCO2R5, or (CH2)kOC(O)R5, (CH2)kNR5R6, or CN;
- or C1-8 alkyl or cycloalkyl optionally substituted with one or more F, Cl, Br, I, OH, SH, ═O, ═S, NH2, (CH2)kCO2R5, (CH2)kNR5R6, OC1-8 alkyl, or CN;
- m is 0, 1, 2, 3, or 4;
- X is N, NH, NC1-8 alkyl, NC(O)R5, CH2, CH—C1-8 alkyl, C(C1-8 alkyl)2, CO, O, S, SO, or SO2;
- Y is N, NH, or CH;
- R5 and R6 are, independently, H, C1-8 alkyl, OC1-8 alkyl, or cycloalkyl;
- k is 0, 1, 2, 3, or 4;
- a (+), (−), or (±) isomer thereof, or a pharmaceutically acceptable salt or prodrug thereof.
10 more elements
A composition, comprising:
- (a) 6H-indolo[2,3-b]quinoxaline, 11H-indeno[1,2-b]quinoxalin-11-one, or a combination thereof, and (b) doxorubicin, doxil, myocet, or a combination thereof.
A method of treating cancer in a subject, comprising:
- administering to the subject a pharmaceutically effective amount of (a) a topoisomerase II poison of Formula I
- wherein
- each R1 is, independently, F, Cl, Br, I, OH, SH, (CH2)kCO2R5, (CH2)kOC(O)R5, (CH2)kNR5R6, or CN;
- or C1-8 alkyl or cycloalkyl optionally substituted with one or more F, Cl, Br, I, OH, SH, ═O, ═S, NH2, (CH2)kCO2R5, (CH2)kNR5R6, OC1-8 alkyl, or CN;
- n is 0, 1, 2, 3, or 4;
- each R2 is, independently, F, Cl, Br, I, OH, SH, (CH2)kCO2R5, (CH2)kOC(O)R5, (CH2)kNR5R6, or CN;
- or C1-8 alkyl or cycloalkyl optionally substituted with one or more F, Cl, Br, I, OH, SH, ═O, ═S, NH2, (CH2)kCO2R5, (CH2)kNR5R6, OC1-8 alkyl, or CN;
- m is 0, 1, 2, 3, or 4;
- X is NH, NC1-8 alkyl, NC(O)R5, CH2, CH—C1-8 alkyl, C(C1-8 alkyl)2, CO, O, S, SO, SO2;
- Y is N, CH;
- R5 and R6 are, independently, H, C1-8 alkyl, OC1-8 alkyl, or cycloalkyl;
- k is 0, 1, 2, 3, or 4;
- a (+), (−), or (±) isomer thereof, or a pharmaceutically acceptable salt or prodrug thereof;
- and
- (b) an anticancer drug.
12 more elements
Dependencies are inferred from the claim text.