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US 2006/0189631 A1Published application
Substituted imidazopyrimidines for the prevention and treatment of cancer
AssigneeLaboratorios Salvat, S.A.
InventorsJuan Catena Ruiz, Carles Gallemi, Anna Serrat, Carmen Comas, Dolors Balsa Lopez, Carmen Lagunas Arnal, Carolina Salcedo Roca, Andres Fernandez Garcia
Life of this patent
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Abstract
Compounds of general formula (I), wherein from A1 to A5, and from B1 to B5 are H, alkyl, alkoxyl, halogen, carboxylic derivatives or sulfur derivatives, among others; and from P1 to P3 are H, halogen, alkyl or alkoxyl, among others. Said compounds may be used for the chemoprevention and treatment of both precancerous lesions and cancer.
Claims26
A compound of general formula (I),
- stereoisomers and mixtures thereof, polymorphs and mixtures thereof, and pharmaceutically acceptable solvates and addition salts of them all,
- wherein:
- A1, A2, A3, A4, A5, B1, B2, B3, B4 and B5 are radicals independently selected from the group consisting of H, (C1-C4)-alkyl, (C3-C7)-cycloalkyl, CF3, OCF3, CN, (CH2)nOR1, (CH2)nNR1R2, CONR1R2, F, Cl, Br, I, NR1R2, NR2COR1, OR1, COR1, COOR1, COSR1, OCOR1, SR1, SOR1, S(O)OH, SO2R1, SO2NR2R3, SO2NHCOR1, and SCOR1;
- wherein n is an integer from 1 to 3;
- R1 is a radical selected from H, CH2OCOR2, CF3, (C1-C4)-alkyl, and (C3-C7)-cycloalkylmethyl and (C3-C7)-cycloalkyl;
- R2 is a radical selected from H, and (C1-C4)-alkyl;
- R3 is a radical selected from COR1, and SO2R1;
- alternatively, A2, A3, B2 or B3 may represent NO2;
- alternatively, either A2 and A3, or B2 and B3 may be forming a R4—(C1-C3)-alkyl-R5 biradical, wherein R4 and R5 are independently selected from CR1R2, O, NR1, S;
- and
- P1, P2, and P3 are radicals independently selected from the group consisting of H, NR1R2, NR2COR1, CF3, F, Cl, Br, OH, SH, (C1-C4)-alkyl, (C1-C4)-alkoxyl and (C1-C4)-alkylsulfanyl,
- with the proviso that formula (I) does not include any of the following compounds:
- (a) simultaneously B3 is SO2NH2 or SO2CH3, A3, A4 or A5 are H, F, Cl, Br, (C1-C3)-alkyl, CF3, (C1-C3)-alkoxyl or OCF3, and P1 or P2 are H, CH3, Cl, Br or CH3O;
- (b) simultaneously B3 is CH3O or H, A3 is CH3O or H, and P1, P2 and P3 are H;
- (c) simultaneously B3 is F, A3 is SO2CH3, and P1 is methyl;
- (d) simultaneously A1, A2, A3, A4, A5, B1, B2, B3, B4, B5 are H, P1 is methyl, P2 is H and P3 is OH;
- (e) simultaneously A3 and B3 are CH3O, A1, A2, A4, A5, B1, B2, B4 and B5 are H, and one of the groups P1, P2 or P3 are H, OH, (C1-C4)-alkyl or (C1-C4)-alkoxyl, being the remaining two groups P1, P2 or P3 representing H;
- or
- (f) simultaneously A3 and B3 are CH3O, A1, A2, A4, A5, B1, B2, B4 and B5 are H, P1 is OH or (C1-C4)-alkoxyl, P2 is H and P3 is (C1-C4)-alkyl.
16 more elements
The ethod according to claim 19 wherein the compound is administered orally, parenterally or topically.
Dependencies are inferred from the claim text.