4-thia-1-aza-bicyclo�4,2,0!oct-2-ene antibiotics
    19.
    发明授权
    4-thia-1-aza-bicyclo�4,2,0!oct-2-ene antibiotics 失效
    4-硫杂-1-氮杂 - 双环[4,2,0]辛-2-烯抗生素

    公开(公告)号:US5683996A

    公开(公告)日:1997-11-04

    申请号:US335163

    申请日:1994-11-07

    CPC分类号: C07D513/04

    摘要: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R is selected from the group consisting of ##STR2## and R.sub.b --NH--, Ra is an organic radical, Ri and Rj are individually selected from the group consisting of hydrogen, aliphatic hydrocarbon, aromatic hydrocarbon and heterocycle or taken together with the nitrogen atom to which they are attached form an optionally substituted ring, Rb is selected from the group consisting of carbocyclic aryl and heterocyclic aryl, both optionally substituted, R.sub.1A is selected from the group consisting of ##STR3## and ##STR4## are individually selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, Z.sub.A is selected from the group consisting of a simple bond, --O-- and optionally oxidized sulfur, R.sub.3A is selected from the group donsisting of optionally substituted carbocyclic aryl and heterocyclic aryl, optionally substitute quaternary ammonium, acetyle, carbamoyl, alkoxycarbonyl, alkyl and haloalkyl of 1 to 4 carbon atoms, --CN and azido, R.sub.4 is selected from the group consisting of hydrogen and methoxy, A is selected from the group consisting of hydrogen, alkali metal, alkaline earth metal, magnesium, --NH.sub.4, an organic amine and esterified carboxy or COOA is --COO.sup.--, n.sub.2 is an integer from 0 to 2 and their non-toxic, pharmaceutical acceptable acid addition salts having excellent antibiotic activity.

    摘要翻译: 选自下列化合物的化合物:其中R选自由下列组成的组成的组分:其中R选自由下列组成的组:R a-NH-,R a是有机基团,R 1和R j分别选自 由氢,脂族烃,芳族烃和杂环组成的组或与它们所连接的氮原子一起形成任选取代的环,R b选自碳环芳基和杂环芳基,二者均为取代基,R 1A 选自分别选自氢和1至4个碳原子的烷基,ZA选自简单的键,-O-和任选被氧化的 硫,R3A选自任选取代的碳环芳基和杂环芳基,任选地取代季铵,乙酰基,氨基甲酰基,烷氧基羰基,烷基和卤代 1至4个碳原子的烷基,-CN和叠氮基,R 4选自氢和甲氧基,A选自氢,碱金属,碱土金属,镁,-NH 4,有机胺 酯化的羧基或COOA为-COO + E,crc - + EE,n2为0〜2的整数,其无毒的药学上可接受的酸加成盐具有优异的抗生素活性。