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    • 6. 发明授权
    • Cephalosporin derivatives
    • 头孢菌素衍生物
    • US4520193A
    • 1985-05-28
    • US322961
    • 1981-11-19
    • Christian BergerDaniel FargeClaude MoutonnierGerard Wolff
    • Christian BergerDaniel FargeClaude MoutonnierGerard Wolff
    • A61K31/545A61K31/546A61P31/04C07D501/20C07D501/24C07D501/38
    • C07D501/24
    • The invention provides new cephalosporin derivatives of the general formula, ##STR1## which are in the form of a bicyclooct-2-ene or bicyclooct-3-ene, in which formula R.sub.1 is a radical of the general formula ##STR2## [in which R.sub.5 is hydrogen, alkyl, vinyl, cyanomethyl, protected carboxyalkyl or a protective radical and R.sub.6 is a protective radical] or an amino-protecting radical, R.sub.2 is an acid-protecting radical and R.degree. represents various organic radicals, or alternatively R.sub.1 is an amino-protecting radical or various acyl radicals, R.sub.2 is a protective radical and R.degree. represents various organic radicals, and R.sub.3 and R.sub.4 are alkyl radicals optionally substituted by alkoxy or dialkylamino, or phenyl radicals, or --NR.sub.3 R.sub.4 forms a heterocyclic ring. These products are intermediates for the synthesis of cephalosporins having antibacterial activity.
    • 本发明提供了通式为(IMA)(I)的新型头孢菌素衍生物,其为双环-2-烯或双环辛-3-烯的形式,其中式R1为通式为“IMAGE” (II)[其中R5为氢,烷基,乙烯基,氰基甲基,被保护的羧基烷基或保护基,R6为保护基]或氨基保护基,R2为酸保护基,R DEG为各种有机基团 或者R 1为氨基保护基或各种酰基,R 2为保护基,R≠表示各种有机基团,R 3和R 4为任选被烷氧基或二烷基氨基取代的烷基或苯基或-NR 3 R 4形式 杂环。 这些产品是合成具有抗菌活性的头孢菌素的中间体。