1-cyclopropyl-4-pyridyl-quinolinones
AssigneeSterling Winthrop Inc.
InventorsMichael A. Eissenstat, John D. Weaver, III, Gee-Hong Kuo, Mark P. Wentland
Life of this patent
Estimating the term…
Abstract
Compounds of formula ##STR1## wherein R.sub.1 is hydrogen, lower-alkyl, or trifluoromethyl; R.sub.2 is lower-alkyl, trifluoromethyl or CH.sub.2 Z where Z is hydroxy, chloro, lower-alkylamino or dilower-alkylamino; R.sub.3 and R.sub.4 are each individually hydrogen or fluoro; and Ar is phenyl, an aromatic 5- or 6-membered heterocycle or any of these substituted at one or more positions with lower-alkyl, fluoro, chloro, hydroxy, amino, lower-alkylamino, dilower-alkylamino, carboxy, sulfonamido, lower alkylsulfonamido, methylenedioxy, trifluoroacetamido, lower-alkanoylamino, or carbamoyl; and their pharmaceutically acceptable acid addition salts are useful as anticancer agents.
Claims24
A compound of formula ##STR27## wherein R.sub.1 is hydrogen, lower-alkyl, or trifluoromethyl;
- R.sub.2 is lower-alkyl, trifluoromethyl or CH.sub.2 Z where Z is hydroxy, chloro, lower-alkylamino or dilower-alkylamino;
- R.sub.3 and R.sub.4 are each independently hydrogen or fluoro;
- and
- Ar is phenyl, an aromatic 5- or 6-membered heterocycle having carbon and up to two heteroatoms chosen from nitrogen and oxygen;
- or any of these substituted at one to three positions with lower-alkyl, fluoro, chloro, hydroxy, amino, lower-alkylamino, dilower-alkylamino, carboxy, sulfonamido, lower aklylsulfonamido, methylenedioxy, trifluoroacetamido, lower-alkanoylamino, or carbanoyl;
- or a pharmaceutically acceptable acid addition salt thereof.
A compound of formula ##STR28## wherein R.sub.1 is hydrogen, lower-alkyl, or trifluoromethyl;
- R.sub.2 is lower-alkyl, trifluoromethyl or CH.sub.2 Z where Z is hydroxy, chloro, lower-alkylamino or dilower-alkylamino and
- R.sub.3 and R.sub.4 are each independently hydrogen or fluoro.
A compound of formula ##STR29## wherein R.sub.1 is hydrogen, lower-alkyl, or trifluoromethyl;
- R.sub.2 is lower-alkyl, trifluoromethyl or CH.sub.2 Z where Z is hydroxy, chloro, lower-alkylamino of dilower-alkylamino
- R.sub.3 and R.sub.4 are each independently hydrogen or fluoro;
- and
- Ar' is phenyl substituted with one or more of lower-alkoxy or benzyloxy wherein Ar' also includes 3,5-(CH.sub.3 O).sub.2 -4-OH-phenyl.
Dependencies are inferred from the claim text.