Patent number: 6130229
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.
Type:
Grant
Filed:
October 7, 1997
Date of Patent:
October 10, 2000
Assignee:
Schering Corporation
Inventors:
Adriano Afonso, Joseph M. Kelly, Stuart B. Rosenblum, Ronald L. Wolin, Jay Weinstein
Patent number: 5703090
Abstract: A method of inhibiting Ras function and therefore inhibiting cellular growth is disclosed. The method comprises the administration of a novel compound of the formula (Ia), (Ib) or (Ic) ##STR1## wherein: R and R.sup.1 are H, alkyl, halogeno, OH, alkoxy, NH.sub.2, alkylamino, dialkylamino, CF.sub.3, SO.sub.3 H, CO.sub.2 R.sup.3, NO.sub.2, SO.sub.2 NH.sub.2, or CONHR.sup.4 ;n is 0 or 1;R.sup.2 is a group of the formula R.sup.5 C(O)--, R.sup.5 CH.sub.2 C(O)--, R.sup.5 C(R.sup.6).sub.2 C(O)--, R.sup.5 SO.sub.2 --, R.sup.5 CH.sub.2 SO.sub.2 --, R.sup.5 SCH.sub.2 C(O)--, R.sup.5 OC(O)--, R.sup.5 NHC(O)--, R.sup.5 C(O)C(O)-- or R.sup.5 SC(O)--;R.sup.5 is alkyl, aryl, arylalkyl, arylalkenyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl or heterocycloalkyl; andR.sup.6 is alkyl or C(R.sup.6).sub.2 is a carbocyclic ring;or pharmaceutically aceptable salts thereof.
Type:
Grant
Filed:
September 11, 1996
Date of Patent:
December 30, 1997
Assignee:
Schering Corporation
Inventors:
Adriano Afonso, Joseph M. Kelly, Ronald L. Wolin