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    • 82. 发明授权
    • 7-D-(.alpha.-Acylamino-arylacetamido)-cephalosporanic acid derivatives
    • 7-D - ({6-羧基 - 芳基乙酰氨基) - 头孢烷酸衍生物
    • US4058610A
    • 1977-11-15
    • US720101
    • 1976-09-03
    • David A. CoxBraham Shroot
    • David A. CoxBraham Shroot
    • C07D265/32C07D501/36A61K31/545
    • C07D265/32
    • Novel antibacterial agents; namely, 7-(.alpha.-acylamino-arylacetamido)-cephalosporanic acid derivatives having the formula: ##STR1## wherein R.sup.1 is thienyl, 2-furyl, phenyl, substituted thienyl or substituted phenyl; R is hydroxyl; R.sup.2 is hydrogen, hydroxy, acetoxy, carbamoyloxy, N-pyridyl, azido or heterocyclic thio group; R and R.sup.2 when taken together represent an oxygen atom; R.sup.3 is sulpho or COOR.sup.4' wherein R.sup.4' is hydrogen or R.sup.4 wherein R.sup.4 is lower alkyl, 5-indanyl, naphthyl, phenyl, or substituted phenyl, CONR.sup.5 R.sup.6, wherein each of R.sup.5 and R.sup.6 is hydrogen, lower alkyl or cycloalkyl; or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached form a saturated heterocyclic group; X is oxygen or sulphur, a direct link, carbonyl, methylene, hydroxymethylene, sulphinyl, sulphonyl or an imino group of the formula --NR.sup.7 --, wherein R.sup.7 is hydrogen, lower alkyl, lower alkenyl, or benzyl; and each of alk.sup.1 and alk.sup.2 is a divalent saturated aliphatic hydrocarbon group containing from 1 to 3 carbon atoms; the pharmaceutically acceptable salts thereof, and methods for their preparation.
    • 新型抗菌剂; 即具有下式的7-(α-酰基氨基 - 芳基乙酰胺基) - 头孢烷酸衍生物:其中R 1是噻吩基,2-呋喃基,苯基,取代的噻吩基或取代的苯基; R是羟基; R2是氢,羟基,乙酰氧基,氨基甲酰氧基,N-吡啶基,叠氮基或杂环硫基; 当R和R 2一起表示氧原子时; R 3是磺基或COOR 4',其中R 4'是氢或R 4,其中R 4是低级烷基,5-二氢化茚基,萘基,苯基或取代的苯基,CONR 5 R 6,其中R 5和R 6各自是氢,低级烷基或环烷基; 或R 5和R 6与它们所连接的氮原子一起形成饱和杂环基; X是氧或硫,直链,羰基,亚甲基,羟亚甲基,亚磺酰基,磺酰基或式-NR7-的亚氨基,其中R7是氢,低级烷基,低级烯基或苄基; alk1和alk2各自为含有1至3个碳原子的二价饱和脂族烃基; 其药学上可接受的盐及其制备方法。
    • 83. 发明授权
    • 7-D-(.alpha.-acylamino-arylacetamido)-cephalosporanic acid derivatives
    • 7-D - ({ - 酰基氨基 - 芳基乙酰氨基) - 头孢烷酸衍生物
    • US4006230A
    • 1977-02-01
    • US635297
    • 1975-11-26
    • David A. CoxBraham Shroot
    • David A. CoxBraham Shroot
    • C07D265/32C07D501/20C07D501/24C07D501/32
    • C07D265/32
    • Novel antibacterial agents; namely, 7-(.alpha.-acylamino-arylacetamido)-cephalosporanic acid derivatives having the formula: ##STR1## wherein R.sup.1 is thienyl, 2-furyl, phenyl, substituted thienyl or substituted phenyl; R is hydroxyl; R.sup.2 is hydrogen, hydroxy, acetoxy, carbamoyloxy, N-pyridyl, azido or heterocyclic thio group; R and R.sup.2 when taken together represent an oxygen atom; R.sup.3 is sulpho or COOR.sup.4.sup.' wherein R.sup.4.sup.' is hydrogen or R.sup.4 wherein R.sup.4 is lower alkyl, 5-indanyl, naphthyl, phenyl, or substituted phenyl, CONR.sup.5 R.sup.6, wherein each of R.sup.5 and R.sup.6 is hydrogen, lower alkyl or cycloalkyl; or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached form a saturated heterocyclic group; X is oxygen or sulphur, a direct link, carbonyl, methylene, hydroxymethylene, sulphinyl, sulphonyl or an imino group of the formula --NR.sup.7 --, wherein R.sup.7 is hydrogen, lower alkyl, lower alkenyl, or benzyl; and each of alk.sup.1 and alk.sup.2 is a divalent saturated aliphatic hydrocarbon group containing from 1 to 3 carbon atoms; the pharmaceutically acceptable salts thereof, and methods for their preparation.
    • 新型抗菌剂; 即具有下式的7-(α-酰基氨基 - 芳基乙酰胺基) - 头孢烷酸衍生物:其中R 1是噻吩基,2-呋喃基,苯基,取代的噻吩基或取代的苯基; R是羟基; R2是氢,羟基,乙酰氧基,氨基甲酰氧基,N-吡啶基,叠氮基或杂环硫基; 当R和R 2一起表示氧原子时; R 3是磺基或COOR 4,其中R 4'是氢或R 4,其中R 4是低级烷基,5-二氢化茚基,萘基,苯基或取代的苯基,CONR 5 R 6,其中R 5和R 6各自是氢,低级烷基或环烷基 ; 或R 5和R 6与它们所连接的氮原子一起形成饱和杂环基; X是氧或硫,直链,羰基,亚甲基,羟亚甲基,亚磺酰基,磺酰基或式-NR7-的亚氨基,其中R7是氢,低级烷基,低级烯基或苄基; alk1和alk2各自为含有1至3个碳原子的二价饱和脂族烃基; 其药学上可接受的盐及其制备方法。