PRODRUGS OF PROTEIN TYROSINE KINASE INHIBITORS; SUCH COMPOUNDS LINKED TO A PROTECTING GROUP CAPABLE OF BEING CLEAVED TO RELEASE THE INHIBITOR
PCT No. PCT/GB94/01532 Sec. 371 Date Jul. 1, 1996 Sec. 102(e) Date Jul. 1, 1996 PCT Filed Jul. 15, 1994 PCT Pub. No. WO95/02420 PCT Pub. Date Jan. 26, 1995A compound which comprises a prodrug of a protein tyrosine kinase inhibitor (PTKi) linked to a protecting group which is capable of being cleaved...
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Main Authors | , |
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Format | Patent |
Language | English |
Published |
24.10.1997
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Edition | 6 |
Subjects | |
Online Access | Get full text |
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Summary: | PCT No. PCT/GB94/01532 Sec. 371 Date Jul. 1, 1996 Sec. 102(e) Date Jul. 1, 1996 PCT Filed Jul. 15, 1994 PCT Pub. No. WO95/02420 PCT Pub. Date Jan. 26, 1995A compound which comprises a prodrug of a protein tyrosine kinase inhibitor (PTKi) linked to a protecting group which is capable of being cleaved from the compound to release the PTKi, said PTKi prodrugs including tyrphostins, of formula (I), N->O, n is 1 to 3; each group R1, which may be the same or different is H, OH, mercapto, carboxy, formyl, C1-4 alkyl, C2-4 alkenyl, C1-4 alkoxy, C1-4 alkylthio, carboxyC1-4 alkyl, carboxyC2-4 alkenyl, C1-4 alkylsulphoxy, halo, nitro, amino, C1-4 alkylamino, or C1-4 dialkylamino, or when n is 2 or 3 two R1 groups may together form a methylenedioxy or ethylenedioxy group; R2 is H, OH, C1-4 alkyl 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, optionally containing a ketone group; and R3 is cyano, carboxy, carbamoyl, thiocarbamoyl, C(O)HNCH2CN, C(NH2)=C(CN2), an alpha keto C(O)R4 where R4 is 3,4-dihydroxyphenyl or 2-thiophene or an alpha amido C(O)NHR5 where R5 is benzyl, phenyl, or 2,4-dimethoxyphenyl; provided that at least one of R1 and R2 is mercapto, hydroxy or amino. |
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Bibliography: | Application Number: NZ19940268629 |