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    • 2. 发明申请
    • DISUBSTITUTED P-FLUOROBENZOLSULFONAMIDES AND THEIR USE IN NMR DIAGNOSTICS
    • 二取代P FLUORBENZOSULFONAMIDE和它们在核磁共振诊断
    • WO1996019447A1
    • 1996-06-27
    • PCT/EP1995004825
    • 1995-12-08
    • SCHERING AKTIENGESELLSCHAFT
    • SCHERING AKTIENGESELLSCHAFTNIEDBALLA, UlrichPLATZEK, JohannesRADÜCHEL, BerndFRENZEL, ThomasBAUER, Hans
    • C07C311/08
    • A61K49/06C07C311/08
    • Disubstituted p-fluorobenzolsulfonamides containing a CF3 group have the general formula (I), in which Z is a CF3 group or a hydrogen atom; Y is a C1-C6 alkyl group that may be substituted by 1 to 4 hydroxy groups or interrupted by 1 to 2 oxygen atoms, a (CH2)oCOOH or (CH2)oCONR R group in which o equals 0 or 1 and R and R represent independently from each other hydrogen and a C1-C6 alkyl group optionally substituted by 1 to 4 hydroxy groups; X is a hydrogen atom or has one of the meanings given for Y; W is a C0-C6 alkylene group that may be substituted by 1 to 4 hydroxy groups or interrupted by 1 to 2 oxygen atoms; n equals 0 or 1; A is one of the rests -OH, OR , -CF3, -CH2CF3, -NH-CH2-COOH, -NH-CR (CF3)-COOH, in which R is a hydrogen atom or a straight or branched chain C1-C6 alkyl group optionally substituted by 1 to 2 hydroxy groups, provided that X stands for a hydrogen atom when Z is a CF3 group, that X has one of the meanings given for Y when Z stands for a hydrogen atom and that the optional acid groups in the molecule be present as their amides or salts with organic or inorganic bases. These compounds are useful as NMR diagnostic agents.
    • 二取代的,一CF 3 P-Fluorbenzolsulfonamide通式(I)其中Z是CF 3基团或氢原子基团的,Y代表可被1至4个羟基基团或由1至2个取代的C1-C6烷基 氧原子可以被中断,一(CH 2)oCOOH-或(CH 2)OCONR <1> [R <2>组O含义数字0或1,R <1>和R <2>在独立的含义彼此的 氢和任选被1至4个羟基C1-C6烷基取代的,X为氢原子或Y的给定的含义之一,W为可被1至4个羟基基团从1是取代的或由一个C 0 -C 6亚烷基 2个氧原子可被中断,n是数字0或1,A表示基团OH或<3>,-CF 3,-CH 2 CF 3,-NH-CH 2 -COOH,-NH-CR <3>(CF 3) - COOH取代的直链或者与R <3>中的氢原子的含义或一个任选地被1至2个羟基取代的(S) 支链C1-C6烷基,条件是X是Wasserstoffatour当Z是X具有用于Y给出的含义中的一个的CF 3基团,条件中,当Z是氢原子,和,如果需要的话,在分子中, 存在于它们的酰胺的形式或与有机或无机碱的盐的形式的酸基团是适合作为NMR诊断试剂。