| 摘要 |
Compounds of the formula and pharmaceutically acceptable salts thereof. As used in formula I, and throughout the specification, the symbols have the following meanings: R1=R2, COR3, CONH2, CONR2R3, COOR2, or SO2R2; R2=alkyl, cycloalkyl, heterocycloalkyl, cycloalkylalkyl, heterocycloalkylalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl; R3=H, alkyl, cycloalkyl, heterocycloalkyl, cycloalkylalkyl, heterocycloalkylalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl; , where n=0,1,2; m=1,2 but both n and m cannot be 2, or , where i, j=0 or 1 but cannot both be 1, and Y=optionally substituted alkene, alkyne, or any 2 adjacent carbon atoms of a cycloalkyl or cycloheteroalkyl ring of 3-7 atoms; R4=alkyl with two or more carbon atoms, cycloalkyl, heterocycloalkyl, cycloalkylalkyl, heterocycloalkylalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, or R9 with the proviso that when R1 is acetyl or propionyl and Y=alkene, then R4 cannot be nitrofuryl or 2-quinolinyl; R5, R6, R7, R8=independently H, alkyl, cycloalkyl, heterocycloalkyl, cycloalkylalkyl, heterocycloalkylalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, halo, or hydroxy, alkoxy, amino, NR12R13, thio, or alkylthio with the proviso that only one such heteroatom group is bonded to any one carbon atom; R9= where Z=O, NR14, S; R10, R11=independently H, alkyl, cycloalkyl, heterocycloalkyl, cycloalkylalkyl, heterocycloalkylalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, halo, hydroxy, alkoxy, alkylcarbonyloxy, carboxy, alkyloxycarbonyl, amino, NR15R16, carbamoyl, ureido, thio, or alkylthio; R12, R13, R14, R15, R16=independently H, alkyl, cycloalkyl, heterocycloalkyl, cycloalkylalkyl, heterocycloalkylalkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl. The compounds of formula I are protein kinase inhibitors and are useful in the treatment of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of Alzheimer's disease, and cardiovascular disease.
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