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    • 148. 发明公开
    • Novel sulfonyl derivatives
    • 新磺酰化
    • EP0493642A1
    • 1992-07-08
    • EP91100035.4
    • 1991-01-02
    • Takayanagi, Takeo, Dr.
    • Takayanagi, Takeo, Dr.
    • C07C335/42A61K31/63C07D203/12C07F3/02C07F1/08C07C311/48C07C309/76C07C311/53C07C309/88C07F3/10
    • C07D203/08C07C309/76C07C309/88C07C311/49C07C311/53C07C335/42C07D239/69C07D473/38C07F1/005C07F3/003C07H19/16
    • The present invention relates to novel sulfonyl compounds

      wherein R' and R'' are the same or different and are each hydrogen, -COCHR⁴, -COC(R⁴)₃ -SO₂CH₃, -COOCH₂CH₃, -CH₂-CH₂-R⁴, -CONH-CH₂CH₂R⁴, -CONHCH₂COOCH₂CH₃, -CH₂CH₂OCONH₂, and R₄ is Cl or a residue selected from

      -NHCOCH₂CH₂OH, -NHCOCH₂CH₃, -NHOH, -NHCH₃, and

      R¹ and R² are the same or different and are each selected from

      6-mercaptopurinyl, 5-fluorouracily, prednisolyl, salicyl-. hydrazidyl, 1-allyl-2-thiouracilyl, hydroxylamine, isoamidyl, or is an inorganic group consisting of -OH, -SH, -F, -J, -CCl₃, or an organic group consisting of -O-CH₃, -O-CH₂CH₃, -O-CH=CH₂, -O-C₆H₅ or benzhydrol; or an aminoehtyl residue, or an ether group forming oxonium salts consisting of ClCH₂OCH₂Cl, CH₃OCH₂CH₂OCH₃, CH₂ClCH₂OCH₂CH₂Cl, C₄H₉OCH₃, (C₆H₅)₂O,

      (CH₂=CHCH₂)₂O, CH₂=CHOCH=CH₂, C₄H₉OC₄H₉, C₆H₅OCH₃, CH₃-O-CHCl₂, ClCH₂-O-C₂H₅, OHCH₂CH₂-O-CH₂CH₂Cl, ClCH₂CHCl-C₂H, and Mt as a metal atom; and wherein the

      residue can optionally be changed to a linear, branched or cyclic alkyl having 1 to 6 carbon atoms, halogen or a Hg:N-(C₁-C₆) alkyl group.
      The invention further relates to a process for the preparation of the novel sulfonyl compounds and derivatives thereof, as well as for a process for manufacturing a pharmaceutical composition containing the novel sulfonyl compound as an active ingredient. Such novel sulfonyl compound are for example capable in the use for inhibitung tissue growth.
    • 本发明涉及新的磺酰化合物,其中R'和R“相同或不同,各自为氢,-COCHR 4,-COC(R 4)3 -SO 2 CH 3,-COOCH 2 CH 3, CH 2 -CH 2 -CH 2 R 4,-CONH-CH 2 CH 2 R 4,-CONHCH 2 COOCH 2 CH 3,-CH 2 CH 2 OCONH 2和R 4是Cl或选自下列的残基:CHCO 2 -NHCOCH 2 CH 2 OH,-NHCOCH 2 CH 3,-NHOH,-NHCH 3和CHEM R 1和R 2相同或不同,各自选自6-巯基嘌呤,5-氟尿苷,泼尼松
      林,水杨酰基。 或者是由-OH,-SH,-F,-J,-CCl 3或由-O-CH 3,-O-(C 1 -C 3)组成的有机基团的无机基团, CH 2 CH 3,-O-CH = CH 2,-O-C 6 H 5或二苯基甲醇; 或C 6 H 9 OCH 3,(C 6 H 5)2 O,CH CH 2(CH 2 = CHCH 2)2 O,CH 2 = CHOCH = CH 2,C 4 H 9 OC 4 H 9,C 6 H 5 OCH 3,CH 3 -O(CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2) -CHCl 2,ClCH 2 -O-C 2 H 5,OHCH 2 CH 2 -O-CH 2 CH 2 Cl,ClCH 2 CHCl-C 2 H和Mt作为金属原子; 并且其中所述残基可任选地改变为具有1至6个碳原子的直链,支链或环状烷基,卤素或Hg:N-(C 1 -C 6)烷基。 本发明还涉及制备新的磺酰基化合物及其衍生物的方法,以及制备含有新型磺酰化合物作为活性成分的药物组合物的方法。 这样的新型磺酰化合物例如能够用于抑制组织生长。