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    • 3. 发明授权
    • Tricyclic cefem sulphones
    • 三环头孢磺酸钠
    • US5585372A
    • 1996-12-17
    • US367319
    • 1995-01-20
    • Marco AlpegianiPierluigi BissolinoEttore PerroneVincenzo Rizzo
    • Marco AlpegianiPierluigi BissolinoEttore PerroneVincenzo Rizzo
    • A61K31/545A61K31/546A61P11/00A61P25/04A61P29/00C07D501/00C07D501/62
    • C07D501/00
    • The present invention provides compounds of formula (I) and pharmaceutically or veterinarily salts thereof; ##STR1## wherein R.sub.1 is hydrogen or halogen or an organic group; R.sub.2 is hydrogen or an optionally substituted C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.14 aralkyl group;R.sub.3 is hydrogen or halogen, or an organic groupR.sub.4 is hydrogen or a group defined as R.sub.2 above or R.sub.4 taken together with R.sub.3 constitutes a C.sub.2 -C.sub.6 alkanediyl or an alkanediyl radical optionally substituted by methyl or phenyland X is either oxygen or sulphur or NR.sub.6, wherein R.sub.6 is either hydrogen or a group as defined for R.sub.2. A process for their preparation by cyclization of appropriate intermediates is also described.The compounds of formula I and the pharmaceutically and veterinarily acceptable salts thereof are elastase inhibitors.
    • PCT No.PCT / EP94 / 01643 Sec。 371 1995年1月20日第 102(e)1995年1月20日PCT PCT 1994年5月17日PCT公布。 WO94 / 28003 PCT出版物 日期:1994年12月8日本发明提供式(I)化合物及其药学上或兽用盐; (I)其中R1是氢或卤素或有机基团; R 2是氢或任选取代的C 1 -C 6烷基,C 3 -C 6环烷基,C 6 -C 10芳基或C 7 -C 14芳烷基; R3是氢或卤素,或有机基团R4是氢或被定义为R2上面的R2或与R4一起构成的基团构成任选被甲基或苯基取代的C 2 -C 6烷二基或烷二基,X是氧或硫或 NR 6,其中R 6是氢或根据R 2定义的基团。 还描述了通过合适的中间体的环化制备其方法。 式I化合物及其药学上和兽医学上可接受的盐是弹性蛋白酶抑制剂。
    • 4. 发明授权
    • 2,2-disubstituted cephem sulphones
    • 2,2-二取代的头孢烯砜
    • US5580865A
    • 1996-12-03
    • US43023
    • 1993-04-05
    • Marco AlpegianiPierluigi BissolinoEttore PerroneVincenzo Rizzo
    • Marco AlpegianiPierluigi BissolinoEttore PerroneVincenzo Rizzo
    • A61K31/545A61K31/546A61P11/00A61P17/00A61P19/06A61P29/00C07D501/00C07D501/04C07D501/16C07D501/20C07D501/36C07D501/22C07D501/24
    • C07D501/00
    • The present invention provides cephalosporin sulphones or formula (I), and pharmaceutically or veterinarily acceptable salts thereof; ##STR1## wherein n is zero, one or two; R.sub.1 is hydrogen, halogen or an optionally substituted C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio or C.sub.1 -C.sub.4 carboxamido group;R.sub.2 is hydrogen or an optionally substituted C.sub.1 -C.sub.8 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.2 -C.sub.5 alkenyl or C.sub.3 -C.sub.6 cycloalkyl group;R.sub.3 is hydrogen or acetoxymethyl, methoxymethyl, methyl or an optionally substituted heterocyclylthiomethyl group;R.sub.4 is an optionally substituted C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.6 alkenyl, aryl(C.sub.1 -C.sub.8)alkyl or heterocyclyl(C.sub.1 -C.sub.8)alkyl group; andR.sub.5 is an optionally substituted C.sub.6 -C.sub.10 aryl or a heterocyclyl group.The compounds of formula I and the pharmaceutically and veterinarily acceptable salts thereof are elastase inhibitors.
    • 本发明提供头孢菌素砜或式(I)化合物及其药学或兽医学上可接受的盐; (I)其中n为0,1或2; R 1是氢,卤素或任选取代的C 1 -C 4烷基,C 2 -C 4烯基,C 1 -C 4烷氧基,C 1 -C 4烷硫基或C 1 -C 4甲酰氨基; R 2是氢或任选取代的C 1 -C 8烷基,C 6 -C 10芳基,C 2 -C 5烯基或C 3 -C 6环烷基; R3是氢或乙酰氧基甲基,甲氧基甲基,甲基或任意取代的杂环硫基甲基; R4是任选取代的C 1 -C 8烷基,C 2 -C 6烯基,芳基(C 1 -C 8)烷基或杂环基(C 1 -C 8)烷基; 并且R 5是任选取代的C 6 -C 10芳基或杂环基。 式I化合物及其药学上和兽医学上可接受的盐是弹性蛋白酶抑制剂。