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Oximes derived from erythromycin A, their preparation, their application in pharmaceuticals and pharmaceutical compositions containing them

机译:衍生自红霉素A的肟,其制备方法,在药物中的应用以及含有它们的药物组合物

摘要

The invention relates to derivatives 1 and their salts with acids A is an alkylene (1 to 6 carbons), R is alkyloxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio (at most 6 carbons), the sulfur being optionally oxidized, aryloxy, aralkyloxy, arylthio, aralkylthio, the sulfur being optionally oxidized, NR 1 R 2 , where R 1 and R 2 are hydrogen, alkyl (1 to 6 carbons) or form a heterocycle, or R is a quaternary ammonium, a halogen, a 1,2, -epoxyethyl radical optionally substituted and optionally opened with a nucleophile, O-CO-B where B is alkyl, alkyloxy (1 to 6 carbons), aryl, aralkyl, aryloxy, aralkyloxy, or R is a free or protected formyl, a free carbonyl, esterified or salified, a thiocyanate , nitrile, acyl, carbamoyl, and R is hydrogen or acyl, their preparation from erythromycin or its 9-oxime, their use as antibiotic drugs and the compositions containing them.
机译:本发明涉及 衍生物1及其与酸的盐 A是亚烷基(1至6个碳), R是烷氧基,烯氧基,炔基氧基,烷硫基,烯基硫基,炔基硫基(最多6个碳),硫原子可选被氧化,芳氧基,芳烷氧基,芳硫基,芳烷硫基,硫可选被氧化, NR 1 R 2 ,其中R 1 和R 2是氢,烷基(1至6个碳)或形成杂环,或R是季铵盐铵,卤素,可被亲核试剂O-CO-B任选取代并任选打开的1,2-环氧乙基基团,其中B为烷基,烷氧基(1-6个碳原子),芳基,芳烷基,芳氧基,芳烷氧基或R是游离或受保护的甲酰基,游离的羰基,酯化或成盐的硫氰酸盐,腈,酰基,氨基甲酰基,R为氢或酰基,由红霉素或其9-肟制得,用作抗生素药物和包含它们的组合物。

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