3-(2'-halobenzylidenyl)-2-indolinone compounds for the treatment of disease
AssigneeSugen, Inc.
InventorsPeng Cho Tang, Li Sun, Gerald McMahon
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Abstract
The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
Claims24
A compound of the formula ##STR11## and pharmaceutically acceptable salts thereof, wherein:
- R.sub.1 is H or alkyl;
- R.sub.2 is O or S;
- R.sub.3 is hydrogen,
- R.sub.4, R.sub.5, R.sub.6, and R.sub.7 are each independently selected from the group consisting of hydrogen, alkyl, alkoxy, aryl, aryloxy, alkaryl, alkaryloxy, halogen, trihalomethyl, S(O)R, SO.sub.2 NRR', SO.sub.3 R, SR, NO.sub.2, NRR', OH, CN, C(O)R, OC(O)R, NHC(O)R, (CH.sub.2).sub.n CO.sub.2 R, and CONRR';
- R.sub.3 'and R.sub.5 'd R.sub.6 '! are each independently selected from the group consisting of hydrogen, alkyl, alkoxy, aryl, aryloxy, alkaryl, alkaryloxy, halogen, trihalomethyl, S(O)R, SO.sub.2 NRR', SO.sub.3 R, SR, NO.sub.2, NRR', OH, CN, C(O)R, OC(O)R, NHC(O)R, (CH.sub.2).sub.n CO.sub.2 R, and CONRR';
- R.sub.6 ' is selected from the group consisting of hydrogen, alkyl, alkoxy, aryl, aryloxy, alkaryl, alkaryloxy, halogen, trihalomethyl, S(O)R, SO.sub.2 NRR', SO.sub.3 R, SR, NO.sub.2, OH, CN, C(O)R, OC(O)R, NHC(O)R, (CH.sub.2).sub.n CO.sub.2 R, and CONRR',
- n is 0-3;
- X is Br, Cl, F or I;
- R is H, alkyl or aryl;
- and
- R' is H, alkyl or aryl.
A compound of the formula ##STR12## or a pharmaceutically acceptable salt thereof, wherein:
- R.sub.1 is H or alkyl;
- R.sub.2 is O or S;
- R.sub.3 is hydrogen;
- R.sub.4, R.sub.5, R.sub.6, and R.sub.7 are each independently selected from the group consisting of hydrogen, alkyl, alkoxy, aryl, aryloxy, alkaryl, alkaryloxy, halogen, trihalomethyl, S(O)R, SO.sub.2 NRR', SO.sub.3 R, SR, NO.sub.2, NRR', OH, CN, C(O)R, OC(O)R, NHC(O)R, (CH.sub.2).sub.n CO.sub.2 R, and CONRR';
- n is 0-3;
- X is Br, Cl, F or I;
- R is H, alkyl or aryl;
- and
- R' is H, alkyl or aryl,
- with the proviso that if R.sub.6 ' is NRR', then R and R' are not alkyl substituted with N(CH.sub.3).sub.2 or amino.
The compound 3-(2-chloro-4-hydroxybenzylidenyl)-2-indolinone or a pharmaceutically acceptable salt thereof.
The compound 3-(2-chloro-4-methoxybenzylidenyl)-2-indolinone or a pharmaceutically acceptable salt thereof.
A pharmaceutical composition comprising the compound 3-(2-chloro-4-hydroxybenzylidenyl)-2-indolinone or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient.
A pharmaceutical composition comprising the compound 3-(2-chloro-4-methoxybenzylidenyl)-2-indolinone or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient.
Dependencies are inferred from the claim text.