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Polycyclic derivatives of phthalazine, use of polycyclic derivatives of phthalazine and medicine

机译:酞嗪的多环衍生物,酞嗪的多环衍生物和药物的用途

摘要

"POLYCYCLICAL DERIVATIVES OF FTALAZINA, USE OF POLYCYCLIC DERIVATIVES OF PHALAZINE AND MEDICINE". The present invention relates to new derivatives of polycyclic phthalazines, especially 2 - substituted mature phthalazines (10, 12, 15, 16 - tetrahydroxy - 8 - methoxy - 11 - methyl - 1, 9, 14 - trioxo - 1, 2, 6, 7, 9, 14 - hexahydronaphtacene - [1,2-g] - phthalazine) of formula (I) and its use. The bonds according to the present invention are active against gram-positive bacteria, particularly against multiresistant staphylococci (MRSA) as well as resistant to glycopeptides, such as enterococci, and are therefore suitable for the manufacture of antibacterial drugs. In formula (I) R ^ 1 ^ is carboxyalkyl or carboxyaryl as well as one of its salts, starches or esters and R ^ 2 ^ and R ^ 3 ^ are H or acyl (for example CO-Alkyl, COO-alkyl), being R ^ 1 ^ is different from substituted carboxyphenyl, when R ^ 3 ^ is C ~ 1-8 ~ alkanoyl.
机译:“法拉嗪的多环衍生物,使用多嗪和药物的多环衍生物”。本发明涉及多环酞嗪的新衍生物,特别是2-取代的成熟酞嗪(10、12、15、16-四羟基-8-甲氧基-11-甲基-1、9、14-三氧杂--1、2、6,式(I)的7、9、14-六氢萘-[1,2-g]-酞嗪)及其用途。根据本发明的键对革兰氏阳性细菌具有活性,特别是对多重耐药葡萄球菌(MRSA)以及对糖肽如肠球菌具有耐药性,因此适用于制造抗菌药物。在式(I)中,R ^ 1 ^是羧烷基或羧基芳基及其盐,淀粉或酯之一,R ^ 2 ^和R ^ 3 ^是H或酰基(例如CO-烷基,COO-烷基),当R ^ 3 ^为C〜1-8〜烷酰基时,R ^ 1 ^与取代的羧基苯基不同。

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