Camptothecin with a modified lactone ring

PK140542AUndetermined Publication Date: 2010-03-11SIGMA TAU IND FARMACEUTICHE RIUNITE SPA +1
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Patent Information

Application Number
PK200300456
Authority / Receiving Office
PK · PK
Patent Type
Applications
Current Assignee / Owner
Publication Date
2010-03-11
Patent Text Reader

Abstract

A compound of Formula (I) where:R1 is a -C(R5)=N-O-R4 group, in which R4 is hydrogen or a straight or branched C1-C5 alkyl or C1-C5 alkenyl group, or a C3-C10 cycloallvl group, or a straight or branched (C3-C10) cycloalkyl (C1-C5) alkyl group, or a C6-C14 aryl group, or a straight or branched (C6-C14) aryl - (C1-C5) alkyl group, or a heterocyclic group or a straight or branched heterocyclo - (C1-C5) alkyl group, said. heterocyclic group containing at least one heteroatom selected from an atom . of nitrogen, optionally substituted with an (C1-C3) alkyl group, and / or an atom. of oxygen and / or of sulphur; said alkyl, allrenyl, cycloalkyl, cycloalkyl-alkyl, aryl, aryl-alkyl, heterocyclic or heterocyclo-alkyl groups can optionally be substituted with one or more groups selected from the group consisting of halogen, hydroxy, C1-C3 alkyl, C1-C5 alkoxy, phenyl, cyano, nitro, and –NR6R7, where R6 and R7 which may be the same or different, are hydrogen, straight or branched (C1-C5) alkyl, the –COOH group or one of its pharmaceutically acceptable esters; or the, - CONR8R9 group, where R8 and R9, which may be the same or different, are hydrogen, straight or branched (C1-C5) alkyl; or R4 is a (C6-C10) aroyl or (C6-C10) arylsulphonyl residue) optionally substituted with one or more groups selected from: halogen, hydroxy, straight or branched C1-C5 alkyl, straight or branched C1-C5 alkoxy, phenyl, cyano, nitro, -NR10R11, where R10 and R11 which may be the same or different, are hydrogen, straight or branched C1-C5 alkyl; or: R4 is a polyazninoalkyl residue; or R5 is a glycosyl residue; R5 is hydrogen., straight or branched C1-C5 alkyl, straight or branched C1-C5 alkenyl, C3-C10 cycloalkyl, straight or branched (C3-C10) cydoally1 - (C1-C5) alkyl, C8-C14 aryl, straight or branched (C6-C14) aryl - (C1-C6) alkyl; R2 and R3 which may be the same or different, are hydrogen, hydroxy, straight or branched C1-C5 alkoxy, with the proviso that, in formula. (I), R1, R2 and R8 cannot be simultaneously hydrogen.
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