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US 6,143,766 AGranted
Benzopyranone and quinolone inhibitors of ras farnesyl transferase
AssigneeWarner-Lambert Company
InventorsJames Stanley Kaltenbronn, Daniele Marie Leonard, Joseph Thomas Repine
Life of this patent
Estimating the term…
Abstract
The present invention provides ras farnesyl transferase inhibiting compounds of Formula I ##STR1## The present invention also provides a method of treating cancer and treating or preventing restenosis or atherosclerosis. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula I.
Claims14
A compound having the Formula I:
- ##STR69## and the pharmaceutically acceptable salts thereof, wherein X is --N--R.sup.3 or O;
- R.sup.2 is alkyl, alkenyl, aryl, substituted aryl, aralkyl, substituted aralkyl, heteroaryl, substituted heteroaryl, heteroaralkyl, or substituted heteroaralkyl;
- R.sup.3 is hydrogen, alkyl, alkenyl, aralkyl, substituted aralkyl, aryl, or substituted aryl;
- R.sup.4 is hydrogen, alkyl, alkenyl, aryl, substituted aryl, aralkyl, substituted aralkyl, heteroaralkyl, or substituted heteroaralkyl;
- one of R.sup.5 and R.sup.6 is hydrogen, and the other is --O--R.sup.1 ;
- R.sup.1 is ##STR70## R.sup.7 is hydrogen, alkyl, aralkyl or substituted aralkyl;
- and R.sup.8 and R.sup.9 are independently hydrogen, alkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, aralkyl, or substituted aralkyl;
- provided, however, that when R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl, X is O, R.sup.4 is hydrogen, R.sup.5 or R.sup.6 is --O--R.sup.1, and R.sup.1 is ##STR71## then, R.sup.7, R.sup.8, and R.sup.9 are not all hydrogen.
5 more elements
A compound selected from the group consisting of:
- 4-(3-Chloro-phenyl)-6-(2-imidazol-1-yl-1-phenyl-ethoxy)-1-methyl-8-propyl-1 H-quinolin-2-one;
- 4-(3-Chloro-phenyl)-6-(2-imidazol-1-yl-1-phenyl-ethoxy)-1-methyl-8-phenethy l-1H-quinolin-2-one;
- 6-[2-(3-Benzyl-3H-imidazol-4-yl)-ethoxy]-4-(3-chloro-phenyl)-1-methyl-1H-qu inolin-2-one;
- 6-[2-(3-Benzyl-3H-imidazol-4-yl)-ethoxy]-4-(3-chloro-phenyl)-1-methyl-8-pro pyl-1H-quinolin-2-one;
- 6-[2-(3-Benzyl-3H-imidazol-4-yl)-ethoxy]-4-(3-chloro-phenyl)-1-methyl-8-phe nethyl-1H-quinolin-2-one;
- 4-(3-Chloro-phenyl)-7-(2-imidazol-1-yl-1-phenyl-ethoxy)-1-methyl-8-propyl-1 H-quinolin-2-one;
- 4-(3-Chloro-phenyl)-7-(2-imidazol-1-yl-1-phenyl-ethoxy)-1-methyl-8-phenethy l-1H-quinolin-2-one;
- 7-[2-(3-Benzyl-3H-imidazol-4-yl)-ethoxy]-4-(3-chloro-phenyl)-1-methyl-1H-qu inolin-2-one;
- 7-[2-(3-Benzyl-3H-imidazol-4-yl)-ethoxy]-4-(3-chloro-phenyl)-1-methyl-8-pro pyl-1H-quinolin-2-one;
- 7-[2-(3-Benzyl-3H-imidazol-4-yl)-ethoxy]-4-(3-chloro-phenyl)-1-methyl-8-phe nethyl-1H-quinolin-2-one;
- 4-(2-Chloro-phenyl)-7-(2-imidazol-1-yl-1-phenyl-ethoxy)-8-propyl-chromen-2- one;
- 4-(2-Chloro-phenyl)-7-(2-imidazol-1-yl-1-phenyl-ethoxy)-8-phenethyl-chromen -2-one;
- 7-[2-(3-Benzyl-3H-imidazol-4-yl)-ethoxy]-4-(2-chloro-phenyl)-chromen-2-one;
- 7-[2-(3-Benzyl-3H-imidazol-4-yl)-ethoxy]-4-(2-chloro-phenyl)-8-propyl-chrom en-2-one;
- and
- 7-[2-(3-Benzyl-3H-imidazol-4-yl)-ethoxy]-4-(2-chloro-phenyl)-8-phenethyl-ch romen-2-one.
13 more elements
Dependencies are inferred from the claim text.