OR YAT SUN,OR YAT SUN,MA ZHENKUN,MA ZHENKUN,CLARK F. RICHARD,CLARK F. RICHARD,CHU T. DANIEL,CHU T. DANIEL,PLATTNER J. JACOB,PLATTNER J. JACOB
申请号：
RO200700230
公开号：
RO123591B1
申请日:
1997.09.02
申请国别(地区):
RO
年份:
2014
代理人:
摘要：
The invention relates to a 6-O-substituted ketolide derivative or a pharmaceutically acceptable salt thereof, to a pharmaceutical composition containing the same and to a process for preparing the said derivative. The claimed 6-O-substituted ketolide derivative represented by the formula (V), where the substitutes are those presented in the description, is employed in the preparation of a medicament for the control of bacterial infection in mammals. According to the invention, the pharmaceutical composition comprises a therapeutically effective amount of the said derivative, in combination with a pharmaceutically acceptable carrier. The process for preparing the derivative consists in treating a compound of the formula , where the substitutes are those described by the invention, with a combination of reagents selected from an alkali metal hydride and a phosgene reagent, selected from phosgene, diphosgene and triphosgene, under anhydrous conditions, followed by the decarboxylation catalyzed by an aqueous base and the reaction with a methane-sulphonic anhydride in pyridine, the treatment with an amine, an alkali metal hydride and carbonyl-diimidazole, or the optional treatment of the so obtained compound with an amine and optional deprotection, and, finally the isolation of the resulting compound.Invenţia se referă la un derivat cetolidic 6-O substituit sau la o sare acceptabilă farmaceutic a acestuia, la o compoziţie farmaceutică ce conţine acest derivat, şi la un procedeu pentru prepararea acestuia. Derivatul cetolidic 6-O substituit, reprezentat de o formulă (V) în care substituenţii sunt cei prezentaţi în descriere, este utilizat pentru prepararea unui medicament pentru controlul infecţiei bacteriene la un mamifer. Compoziţia farmaceutică, conform invenţiei, cuprinde o cantitate eficientă terapeutic din acest derivat, în combinaţie cu un purtător acceptabil farmaceutic. Procedeul pentru preparararea acestui derivat constă în tratarea unui compus cu formula, în ca
