Tricyclic compounds having activity as RAS-FPT inhibitors

Details Tricyclic compounds having activity as RAS-FPT inhibitors Tricyclic compounds having activity as RAS-FPT inhibitors

1997-10-07

2000-10-10

Bernhardt, Emily

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514215, 514254, 540577, 544361, 546 80, 546 89, A61K 31445, C07D49504, C07D49104

Patent

active

061302295

ABSTRACT:
Compounds of Formula I: ##STR1## wherein: X.sup.1 is hydrogen, halogen, CF.sub.3, nitro, NH.sub.2 or lower alkyl;
each X.sup.2 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).sub.p, O, and NR.sup.5, wherein p is 0, 1 or 2, and R.sup.5 is hydrogen, alkyl, aryl, cycloalkyl, loweralkoxycarbonyl, aminocarbonyl or acyl;
R.sup.1 and R.sup.2, 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.sup.5 ;
A . . . is C=, CH-- or N--;
R is --CZ--Y.sup.1 --Y.sup.2 --R.sup.3, wherein:
Z is O, =CH--CN, or =N--CN;
one of Y.sup.1 and Y.sup.2 is a bond, --CO--, O, S, or --NR.sup.4 --, and the other is (CH.sub.2).sub.m, where m is 0 or an integer of 1 to 4, and R.sup.4 is H or alkyl, with the proviso that when Z is O and m is 0 then Y.sup.1 or Y.sup.2 is selected from --CO--, O, S, or --NR.sup.4 ;
R.sup.3 is aryl, heteroaryl or heterocycloalkyl, with the proviso that R.sup.3 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.

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