5-Fluoruoracil Derivatives

专利名称：5-Fluoruoracil Derivatives发明人：Rosemeyer, Helmut,Malecki, Edith申请号：EP121865.6申请日：20120928公开号：EP2712868A1公开日：20140402

摘要：The present invention relates to a compound represented by formula (I)wherein X is selected from the group of formulae (II) to (IV) wherein R is H or C-C chainwhich may be branched or linear and which may be saturated or unsaturated and whichmay optionally be interrupted and/or substituted by one or more hetero atom(s) (Het1)and/or functional group(s)(G1); or R is a C-C moiety which comprises at least one cyclicstructure and which may be saturated or unsaturated and which may optionally beinterrupted and/or substituted by one or more hetero atom(s) (Het1) and functionalgroup(s)(G1); R is H; or R is a Mono-phosphate, Di-phosphate, Tri-phosphate or

phosphoramidite moiety; or R is -Y-X or -Y-L-Y- X; Y and Y are independently from eachother a single bond or a functional connecting moiety, X is a colloid-active compound (CA)or a fluorescence marker (FA) or a polynucleotide moiety having up to 50 nucleotideresidues, preferably 10 to 25 nucleotides, especially a polynucleotide having an antisenseor antigen effect; L is a linker by means of which Y and X are covalently linked together; Rand R represent independently from each other a C-C-alkyl moiety which may optionallybe substituted or interrupted by one or more heteroatom(s) and/or functional

group(s);or R and R form a ring having at least 5 members, preferably a ring having 5 to 8carbon atoms and wherein the ring may be substituted or interrupted by one or more

hetero atom(s) and/or functional group(s); or R and R represent independently from eachother a C-C-alkyl moiety substituted with one or more moieties selected from the group-Y-X or -Y-L-Y-X; or R and R represent independently from each other -Y-X or -Y-L-Y- X; Rand R represent independently from each other a C-C-alkyl moiety which may optionallybe substituted or interrupted by one or more heteroatom(s) and/or functional group(s);or R and R represent independently from each other a C-C-alkyl moiety substituted withone or more moieties selected from the group -Y-X or -Y-L-Y-X; or R and R form a ringhaving at least 5 members, preferably a ring having 5 to 18 carbon atoms and wherein thering may be substituted or interrupted by one or more hetero atom(s) and/or functionalgroup(s); and/or one or more moieties selected from the group -Y-X or -Y-L-Y- X; R and Rrepresent independently from each other -Y-X or -Y-L-Y- X; R is a hydrogen atom or -O-R;R is H or C-C chain which may be branched or linear and which may be saturated orunsaturated and which may optionally be interrupted and/or substituted by one or morehetero atom(s) (Het1) and/or functional group(s)(G1); or R is -Y-X or -Y-L-Y- X, with theproviso that R and R are not both H and/or with the proviso that the compoundcomprises at least two chains each of which having 4 or more carbon atoms.

申请人：B. Braun Melsungen AG

地址：Carl-Braun-Strasse 1 34212 Melsungen DE

国籍：DE

代理机构：von Kreisler Selting Werner

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