Thienyl compounds for inhibition of cell proliferative disorders
AssigneeSugen, Inc.
InventorsPeng Cho Tang, Asaad S. Nematalla, Gerald McMahon
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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.
Claims24
A compound of the formula ##STR4## or a pharmaceutically acceptable salt thereof, wherein:
- X is selected from the group consisting of oxygen, CH.sub.2, NH, substituted alkene, and CH.sub.2 CN,
- n is selected from the group consisting of 0, 1, 2, and 4,
- R.sub.1 is an aryl or heteroaryl 5 or 6 membered ring optionally substituted with one or more member of the group consisting of hydroxy, halo, alkoxy, trihalomethyl, nitro, carboxy, amide, sulfonyl, and sulfonamide;
- and
- R.sub.2, R.sub.3, and R.sub.4 are independently selected from the group consisting of hydroxy, halo, alkoxy, trihalomethyl, nitro, carboxy, amide, sulfonyl, and sulfonamide.
A compound of the formula ##STR5## wherein R.sub.2, R.sub.3, and R.sub.4 are each independently selected from the group consisting of 2-nitro;
- 3-phenoxy;
- 2-methylmercapto;
- 2-aminocarbonyl;
- and
- R.sub.1 is selected from the group consisting of phenyl;
- 2-pyridine;
- 4-fluorobenzene;
- 3-trifluoromethylphenyl;
- 4-trifluoromethylphenyl;
- 3-trifluoromethylbenzyl;
- thien-2-yl;
- thien-3-yl;
- cyanomethyl;
- and 1-cyano-2-(nitrothien-5-yl)ethenyl.
A compound named (E)-2-(benzylaminosulfonyl)-3-(2-nitrothien-5-yl)acrylonitrile.
A compound named (E)-2-(benzylaminosulfonyl)-3-(3-phenoxythien-2-yl)acrylonitrile.
A compound named (E)-3-(2-nitrothien-5-yl)-2-(3-phenyl-n-propyl)aminosulfonyl!acrylonitril e.
A compound named (E)-3-(2-methylmercaptothien-5-yl)-2-(3-phenyl-n-propyl)aminosulfonyl!acr ylonitrile.
Dependencies are inferred from the claim text.