首页> 外国专利> PROCESS FOR PRODUCING NEW BETA-LACTAM ANTIBIOTICS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SUCH COMPOUNDS AS ACTIVE INGREDIENT

PROCESS FOR PRODUCING NEW BETA-LACTAM ANTIBIOTICS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SUCH COMPOUNDS AS ACTIVE INGREDIENT

机译:制备包含此类化合物作为活性成分的新型β-内酰胺类抗生素和药物组合物的过程

摘要

There is disclosed a novel beta -lactam antibiotics represented by the formula: IMAGE (I) wherein A is a group represented by the formulae -NHCO-, -NHCONHCO-, -NHCOCH=CH- or IMAGE where R6 is a hydrogen atom or a lower alkyl group; R1 and R2 are independently a hydrogen atom or a protective group; R3 is a hydrogen atom or a methoxy group; X is a hydrogen atom, a hydroxyl group, a protected hydroxyl group, a halogen atom, a lower alkoxy group or a nitro group; n is an integer of 1 or 2; Y is a group represented by the formulae: IMAGE provided that a carbon atom which is bonded by a carboxyl group being bonded to nitrogen atom; M is a hydrogen atom, a protective group or an easily hydrolyzable group in a human body; R7 is a hydrogen atom, a methyl group a lower alkoxy-methyl group or a group represented by the formula: -CH2-T where T is an acyloxy group, a carbamoyloxy group, a quaternary ammonium, a substituted or unsubstituted heterocyclic ring or a formula: -S-R8 where R8 is an acyl group or a substituted or unsubstituted heterocyclic ring, R4 and R5 are each hydrogen atoms or combined with each other to form additional direct bond; Z is a direct bond or a carbonyl group when R4 and R5 are hydrogen atoms, or a formula: -O-B- where the oxygen atom is bonded to nitrogen atom and B is a straight, branched or cyclic alkylene group when R4 and R5 are combined with each other to form additional direct bond, or its pharmaceutically acceptable salt.
机译:公开了一种新的由式:表示的β-内酰胺抗生素(I),其中A是由式-NHCO-,-NHCONHCO-,-NHCOCH = CH-或表示的基团,其中R6是氢原子或低级烷基; R1和R2独立地是氢原子或保护基; R3是氢原子或甲氧基。 X是氢原子,羟基,被保护的羟基,卤素原子,低级烷氧基或硝基; n是1或2的整数; Y是下述式所表示的基团:是将通过羧基与碳原子结合而成的碳原子与氮原子结合而成的基团。 M是人体中的氢原子,保护基或易水解基团; R 7是氢原子,甲基,低级烷氧基-甲基或下式表示的基团:-CH 2 -T其中T是酰氧基,氨基甲酰氧基,季铵,取代或未取代的杂环或式:-S-R8其中R8是酰基或取代或未取代的杂环,R4和R5各自是氢原子或彼此结合形成另外的直接键;当R4和R5为氢原子时,Z为直键或羰基,或式:-OB-,其中R4和R5结合时,氧原子与氮原子键合,且B为直链,支链或环状亚烷基彼此形成额外的直接键或其药学上可接受的盐。

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