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US 2004/0110760 A1Published application
Nitro and amino substituted topoisomerase agents
AssigneeRutgers, The State University of New Jersey
InventorsEdmond J. LaVoie, Sudhir K. Singh, Leroy F. Liu
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Abstract
The invention provides compounds of formula I: 1 wherein R1-R9, W, and X have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating cancer using compounds of formula I.
Claims57
A compound of formula I:
- 3
- wherein:
- one of R1, R2 and R3 is nitro or NRaRb;
- and the remaining R1, R2, and R3 are each independently hydrogen, (C1-C6)alkyl, (C3-C6)cycloalkyl, NRaRb, COORc, ORd;
- or R1 and R2, or R2 and R3 taken together are methylenedioxy, 1,2-ethylenedioxy, or 1,3-propylenedioxy;
- R4 is hydrogen, hydroxy, or fluoro;
- each R5, R6, R7, and R8 is independently hydrogen, (C1-C6)alkyl, (C3-C6)cycloalkyl, NRaRb, COORc, ORd;
- or R5 and R6, R6 and R7, or R7 and R8 taken together are methylenedioxy, 1,2-ethylenedioxy, or 1,3-propylenedioxy;
- R9 is (C1-C6)alkyl substituted with one or more solubilizing groups;
- W is N or CH;
- X is two hydrogens, ═O, ═S, or ═NRe;
- Ra and Rb are each independently hydrogen or (C1-C6)alkyl, or Ra and Rb together with the nitrogen to which they are attached form a pyrrolidino, piperidino or morpholino ring;
- each Rc is hydrogen, (C1-C6)alkyl, aryl, or aryl(C1-C6)alkyl;
- each Rd is hydrogen, (C1-C6)alkyl, (C1-C6)alkanoyl, aryl, or aryl(C1-C6)alkyl;
- and
- Re is hydrogen, (C1-C6)alkyl, aryl, or aryl(C1-C6)alkyl;
- or a pharmaceutically acceptable salt thereof.
14 more elements
Any one of compounds 4a, 4b, 5a, 5b, 6a, and 6b;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.