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US 5,789,427 AGranted
Methods and compositions for inhibiting cell proliferative disorders
AssigneesSugen, Inc., Yissum Research Development Company of the Hebrew University of Jerusalem
InventorsHui Chen, Aviv Gazit, Klaus Peter Hirth, Elaina Mann, Laura K. Shawver, Jianming Tsai, Peng Cho Tang
Life of this patent
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Abstract
The present invention concerns compounds and their use to inhibit the activity of a receptor tyrosine kinase. The invention is preferably used to treat cell proliferative disorders such as cancers characterized by over-activity or inappropriate activity HER2 or EGFR.
Claims16
A compound having the chemical formula:
- ##STR22## or a pharmaceutically acceptable salt thereof, wherein R.sub.1, R.sub.2, and R.sub.3 are each independently selected from the group consisting of alkyl, alkenyl, alkynyl, alkoxy, alkylaryl, OH, amine, thioether, SH, halogen, hydrogen, NO.sub.2 and NH.sub.2 ;
- Y is either nothing, --C(CN).dbd.C--, -alkyl- or --NH-alkyl-;
- and
- R.sub.5 is either CN or aryl;
- provided that if R.sub.5 is aryl and said aryl is phenyl, then a) R.sub.1, R.sub.2, and R.sub.3 are not alkoxy or OH, and b) at least one of R.sub.1, R.sub.2, and R.sub.3 is not hydrogen.
2 more elements
A compound having the chemical formula:
- ##STR23## or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is t-butyl or isopropyl;
- R.sub.2 is OH;
- R.sub.3 is t-butyl or isopropyl;
- Y is either nothing or a lower alkyl;
- and
- R.sub.5 is either phenyl or pyridyl.
3 more elements
A compound selected from the group consisting of
- (E)-3-(3,5-diisopropyl-4-hydroxyphenyl-2-(pyrid-2-yl)sulfonyl!acrylonitril e;
- (E)-2-cyanomethylsulfonyl-3-(3,5-diisopropyl-4-hydroxyphenyl)acrylonitrile) ;
- (E,E)-2-1-cyano-2-(3,5-diisopropyl-4-hydroxyphenyl)ethenyl!sulfonyl!-3-(3 ,5-diisopropyl-4-hydroxyphenyl)acrylonitrile);
- (E)-3-(3,5-diisopropyl-4-hydroxyphenyl)-2-(phenylsulfonyl)acrylonitrile);
- (E)-3-(3,5-dimethyl-4-hydroxyphenyl)-2-(pyrid-2-yl)sulfonyl!acrylonitrile) ;
- (E)-3-(3,5-di-t-butyl-4-hydroxyphenyl)-2-(phenylsulfonyl)acrylonitrile;
- (E)-3-(3,5-di-t-butyl-4-hydroxyphenyl)-2-(pyrid-2-yl)sulfonyl!acrylonitril e;
- (E,E)-2-1-cyano-2-(3,5-diisopropyl-4-hydroxyphenyl)ethenyl!sulfonyl!-3-(3 ,5-di-t-butyl-4-hydroxyphenyl)acrylonitrile;
- (E)-2-(benzylaminosulfonyl)-3-(3,5-di-t-butyl-4-hydroxyphenyl)acrylonitrile );
- (E)-2-(benzylaminosulfonyl)-3-(3,5-diisopropyl-4-hydroxyphenyl)acrylonitril e);
- (E)-2-(benzylaminosulfonyl)-3-(3,5-dimethyl-4-hydroxyphenyl)acrylonitrile
- (E)-3-(3,5-di-t-butyl-4-hydroxyphenyl)-2-(3-phenyl-n-propyl)aminosulfonyl! acrylonitrile);
- (E)-3-(3,5-diisopropyl-4-hydroxyphenyl)-2-(3-phenyl-n-propyl)aminosulfonyl !acrylonitrile;
- and
- (E)-3-(3,5-dimethyl-4-hydroxyphenyl)-2-(3-phenyl-n-propyl)aminosulfonyl!ac rylonitrile,
- or a pharmaceutically acceptable salt thereof.
13 more elements
Dependencies are inferred from the claim text.