205984-57-2Relevant academic research and scientific papers
TRICYCLIC COMPOUNDS HAVING ACTIVITY AS Ras-FPT INHIBITORS
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, (2008/06/13)
Compounds of formula (I), wherein: X is hydrogen, halogen, CF3, nitro, NH2 or lower alkyl; each X is independently selected from the group consisting of hydrogen, halogen, lower alkoxy and lower alkyl; n is 1 or 2; Y is selected from the group consisting of S(O)p, O, and NR, wherein p is 0, 1 or 2, and R is hydrogen, alkyl, aryl, cycloalkyl, loweralkoxycarbonyl, aminocarbonyl or acyl; R and R, which may be the same or different, are selected from the group consisting of hydrogen and lower alkyl groups, or taken together can form an oxygen atom when Y is NR; A..... is C=, CH- or N-; R is -CZ-Y-Y-R, wherein: Z is O, =CH-CN, or =N-CN; one of Y and Y is a bond, -CO-, O, S, or -NR-, and the other is (CH2)m, where m is 0 or an integer of 1 to 4, and R is H or alkyl, with the previso that when Z is O and m is 0 then Y or Y is selected form -CO-, O, S, or -NR; R is aryl, heteroaryl or heterocycloalkyl, with proviso that R can also be lower alkyl when Z is =N-CN; and their pharmaceutically acceptable acid additions salts; have activity as Ras-FPT inhibitors. They can be used, e.g., in pharmaceutical compositions, for inhibiting the abnormal growth of cells and for inhibiting proliferative diseases. Processes for their preparation, and useful intermediates, are also disclosed.
Tricyclic compounds having activity as RAS-FPT inhibitors
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, (2008/06/13)
Compounds of Formula I: wherein: X1 is hydrogen, halogen, CF3, nitro, NH2 or lower alkyl; each X2 is independently selected from the group consisting of hydrogen, halogen, lower alkoxy and lower alkyl; n is 1 or 2; Y is selected from the group consisting of S(O)p, O, and NR5, wherein p is 0, 1 or 2, and R5 is hydrogen, alkyl, aryl, cycloalkyl, loweralkoxycarbonyl, aminocarbonyl or acyl; R1 and R2, which may be the same or different, are selected from the group consisting of hydrogen and lower alkyl groups, or taken together can form an oxygen atom when Y is NR5; A . . . is C=, CH- or N-; R is -CZ-Y1-Y2-R3, wherein: Z is O, =CH-CN, or =N-CN; one of Y1 and Y2 is a bond, -CO-, O, S, or -NR4-, and the other is (CH2)m, where m is 0 or an integer of 1 to 4, and R4 is H or alkyl, with the proviso that when Z is O and m is 0 then Y1 or Y2 is selected from -CO-, O, S, or -NR4; R3 is aryl, heteroaryl or heterocycloalkyl, with the proviso that R3 can also be lower alkyl when Z is =N-CN; and their pharmaceutically acceptable acid addition salts; have activity as Ras-FPT inhibitors. They can be used, e.g., in pharmaceutical compositions, for inhibiting the abnormal growth of cells and for inhibiting proliferative diseases. Processes for their preparation, and useful intermediates, are also disclosed.
