Tyrphostin like compounds
AssigneeSugen, Inc.
InventorsPeng Cho Tang, Li Sun, Asaad S. Nematalla, Gerald McMahon
Life of this patent
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Abstract
The present invention relates to molecules capable of modulating tyrosine signal transduction to prevent and treat cell proliferative disorders or cell differentiation disorders associated with particular tyrosine kinases by inhibiting one or more abnormal tyrosine kinase activities.
Claims16
A compound of the formula ##STR5## or a pharmaceutically acceptable salt thereof, wherein:
- X is NH;
- m is 0 or 1;
- n is 0,1,2, or 3;
- Q is a 5-membered heteroaryl ring optionally substituted with one or more substituents selected from the group consisting of halo, trihalo, alkyl, alkoxy, hydroxy, H, nitro, cyano, amide, sulfonyl, sulfonamide, carboxy, carboxamide, and amino;
- and
- R.sub.1-4 are independently selected from the group consisting of halo, trihalo, alkyl, alkoxy, hydroxy, H, nitro, cyano, amide, sulfonyl, sulfonamide, carboxy, carboxamide, and amino,
- with the proviso that if both m and n are 0, then Q is not furanyl.
A compound of the formula ##STR6## or a pharmaceutically acceptable salt thereof, wherein:
- X is NH;
- m is 0 or 1;
- n is 0, 1, 2, or 3;
- Q is thienyl optionally substituted with one or more substituents selected from the group consisting of halo, trihalo, alkyl, alkoxy, hydroxy, H, nitro, cyano, amide, sulfonyl, sulfonamide, carboxy, carboxamide, and amino;
- and
- R.sub.1-4 are independently selected from the group consisting of halo, trihalo, alkyl, alkoxy, hydroxy, H, nitro, cyano, amide, sulfonyl, sulfonamide, carboxy, carboxamide, and amino.
A compound selected from the group consisting of
- (E)-3-(3,5-Di-t-butyl-4-hydroxyphenyl)-2-(thien-2-yl)sulfonyl!acrylonitril e;
- (E)-3-(3,5-Diisopropyl4-hydroxyphenyl)-2-(thien-2-yl)sulfonyl!acrylonitril e;
- (E)-3-(3,4-Dihydroxyphenyl)-2-(thien-2-yl)sulfonyl!acrylonitrile;
- (E)-3-(3,5-Di-t-butyl-4-hydroxyphenyl)-2-(thien-3-yl)sulfonyl!acrylonitril e;
- (E)-3-(3,5-Diisopropyl-4-hydroxyphenyl)-2-(thien-3-yl)sulfonyl!acrylonitri le;
- or a pharmaceutically acceptable salt of said compound.
A pharmaceutical composition, comprising an effective amount of a compound of the formula:
- ##STR7## or a pharmaceutically acceptable salt thereof, wherein:
- X is NH;
- m is 0 or 1;
- n is 0,1,2, or 3;
- Q is a 5-membered heteroaryl ring optionally substituted with one or more substituents selected from the group consisting of halo, trihalo, alkyl, alkoxy, hydroxy, H, nitro, cyano, amide, sulfonyl, sulfonamide, carboxy, carboxamide, and amino;
- and
- R.sub.1-4 are independently selected from the group consisting of halo, trihalo, alkyl, alkoxy, hydroxy, H, nitro, cyano, amide, sulfonyl, sulfonamide, carboxy, carboxamide, and amino;
- with a proviso that if both m and n are 0, the Q is not furanyl;
- and
- a pharmaceutically acceptable carrier or diluent.
A method of inhibiting uncontrolled cell proliferation or differentiation, comprising the step of administering to an animal or a human an effective amount of a compound of the formula:
- ##STR8## or a pharmaceutically acceptable salt thereof, wherein:
- X is NH;
- m is 0 or 1;
- n is 0,1,2, or 3;
- Q is a 5-membered heteroaryl ring optionally substituted with one or more substituents selected from the group consisting of halo, trihalo, alkyl, alkoxy, hydroxy, H, nitro, cyano, amide, sulfonyl, sulfonamide, carboxy, carboxamide, and amino;
- and
- R.sub.1-4 are independently selected from the group consisting of halo, trihalo, alkyl, alkoxy, hydroxy, H, nitro, cyano, amide, sulfonyl, sulfonamide, carboxy, carboxamide, and amino,
- with proviso that m and n are 0, then Q is not furanyl.
Dependencies are inferred from the claim text.