Patent ID: 6124303
Filing Date: 2000-09-26
Classification: A61K

Abstract:
A method for inhibiting the growth of neoplastic cells comprising exposing the cells to an amount of a compound of Formula I effective to inhibit growth of said cells: ##STR120## wherein A is selected from the group consisting of the formula ##STR121## and (CH.sub.2).sub.a --CH.sub.3, and ""a"" is an integer from 9-15; R.sub.1 is selected from the group consisting of a straight-chain or branched alkyl group with 2 to 10 carbon atoms, which is optionally substituted by phenyl, which in turn may be substituted by halogen, nitro, cyano, straight-chain or branched alkyl with up to 6 carbon atoms, and by a group with the formula --SO.sub.2 NR.sub.9 R.sub.10 ;wherein R.sub.9 and R.sub.10 are the same or different, and are each selected from the group consisting of hydrogen, phenyl, and straight-chain or branched alkyl with up to 6 carbon atoms, which is optionally substituted by hydroxy, or together with the nitrogen atom R.sub.9 and R.sub.10 form a 5- to 6-membered saturated heterocyclic ring with up to 2 other hetero atoms from the group consisting of S, N, and/or O, which is also optionally substituted through a free N function by a straight-chain or branched alkyl with up to 6 carbon atoms, which in turn may be substituted by hydroxy, and/or is alkyl optionally substituted by a group with the formula --NR.sub.11 R.sub.12 ;wherein R.sup.2 is selected from the group consisting of hydrogen, azido, straight-chain or branched alkyl with up to 6 carbon atoms and a group with the formula --OR.sub.13, --O--SO.sub.2 R.sub.14, and --NR.sub.15 R.sub.16 ;wherein R.sub.13 is selected from the group consisting of hydrogen, a hydroxy-protecting group, straight-chain or branched alkyl with up to 6 carbon atoms, benzoyl and straight-chain or branched alkyl with up to 6 carbon atoms, which is optionally substituted by carboxy or straight-chain or branched alkoxycarbonyl with up to 6 carbon atoms, or by a group with the formula --CO--NR.sub.17 R.sub.18 ;wherein R.sub.17 and R.sub.18 are the same or different and are selected from the group consisting of hydrogen and straight-chain or branched alkyl with up to 4 carbon atoms,R.sub.14 is selected from the group consisting of straight-chain or branched alkyl with up to 4 carbon atoms and phenyl;R.sub.15 and R.sub.16 are the same or different and are selected from a group consisting of hydrogen, an amine-protecting group, straight-chain or branched alkyl or acyl, each with up to 6 carbon atoms, formyl, benzoyl, and a group with the formula --SO.sub.2 R.sub.19, wherein R.sub.19 has the meaning given above for R.sub.14 and is the same as or different from it,R.sub.3 is selected from a group consisting of hydrogen, or R.sup.2 and R.sup.3 together form a group of the formula .dbd.O or .dbd.N--OR.sub.20 ;wherein R.sub.20 is selected from a group consisting of hydrogen and straight-chain or branched alkyl with up to 6 carbon atoms, which is optionally substituted by phenyl or by a group with the formula --NR.sub.21 R.sub.22,wherein R.sub.21 and R.sub.22 are the same or different and are selected from a group consisting of hydrogen, phenyl, and straight-chain or branched alkyl with up to 6 carbon atoms,R.sub.4 is selected from a group consisting of hydrogen and straight-chain or branched alkyl with up to 4 carbon atoms,R.sub.5 and R.sub.8 are the same or different and are selected from the group consisting of hydrogen and straight-chain or branched alkyl with up to 3 carbon atoms,R.sub.6 is selected from a group consisting of hydrogen and straight-chain or branched alkyl with up to 5 carbon atoms, which is optionally substituted by hydroxy,R.sub.7 is selected from the group consisting of straight-chain or branched alkyl with 2 to 8 carbon atoms, which is substituted by a group with the formula --NR.sub.23 R.sub.24,wherein R.sub.23 and R.sub.24 are the same or different and are selected from the group consisting of hydrogen and straight-chain or branched alkyl with up to 5 carbon atoms, which is optionally substituted by hydroxy, or is optionally substituted by phenyl, which in turn is substituted by the group with the formula --SO.sub.2 --NR.sub.25 R.sub.26 ;wherein R.sub.25 and R.sub.26 have the meanings given above for R.sub.9 and R.sub.10 ;D is selected from a group consisting of hydrogen and a group with the formula --SO.sub.2 --NR.sub.27 R.sub.28 ;wherein R.sub.27 and R.sub.28 are the same or different and have the meanings given above for R.sub.9 and R.sub.10, and are the same as them or different from them; andE is selected from a group consisting of straight-chain or branched alkyl with up to 8 carbon atoms, and their tautomers and salts.