| 摘要 |
A compound which comprises a prodrug of a protein tyrosine kinase inhibitor (PTKi) linked to a protecting group, said group being capable of being cleaved from said compound to release the protein tyrosine kinase inhibitor. Protein tyrosine kinase inhibitors include tyrphostins, preferably those of formula (I), where X represents carbon, a nitrogen or a group N?O, n is an integer from 1 to 3; each group R1, which may be the same or different is hydrogen, hydroxy, mercapto, carboxy, formyl, C1-4alkyl, C2-4 alkenyl, C1-4alkoxy, C1-4alkylthio, carboxy, C1-4alkyl, carboxyC2-4 alkenyl, C1-4alkylsulphoxy, halo (i.e. fluoro, chloro, bromo or iodo), nitro, amino, C1-4alkylamino, or C1-4dialkylamino, or when n is 2 or 3 two R1 groups may together form a methylenedioxy or ethylenedioxy group; R2 is hydrogen, hydroxy, C1-4alkyl or together with position 2 of the ring to which the group(s) R1 is (are) attached forms a 5 or 6 membered aliphatic or heterocyclic ring, said 5 or 6 membered ring optionally containing a ketone group; and R3 is cyano, carboxy, carbamoyl, thiocarbamoyl, a group C(O)HNCH2CN, a group C(NH2)=C(CN2), an alpha keto group C(O)R4 where R4 is 3,4-dihydroxyphenyl or 2-thiophene or an alpha amido group C(O)NHR5 where R5 is benzyl, phenyl, or 2,4-dimethoxyphenyl, provided that at least one of the groups R1 and R2 are mercapto, hydroxy or amino.
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