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    • 2. 发明授权
    • 4-thia-1-aza-bicyclo[4,2,0]oct-2-ene derivatives
    • 4-硫杂-1-氮杂 - 双环[4,2,0]辛-2-烯衍生物
    • US5385897A
    • 1995-01-31
    • US855324
    • 1992-03-20
    • Jean-Georges TeutschAlain BonnetJozsef AszodiSolange Gouin d'Ambrieres
    • Jean-Georges TeutschAlain BonnetJozsef AszodiSolange Gouin d'Ambrieres
    • C07D513/04C07D519/00C07D417/12A61K31/54
    • C07D513/04
    • 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## R.sub.A ' and R.sub.B ' 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 oxidize sulfur, R.sub.3A is selected from the group consisting of optionally substituted carbocyclic aryl and heterocyclic aryl, optionally substitute quaternary ammonium, acetyl, 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..crclbar., n.sub.2 is an integer from 0 to 2 and their non-toxic, pharmaceutical acceptable acid addition salts having excellent antibiotic activity.
    • 选自由下列化合物组成的组的化合物:其中R选自由下列组成的组成的组合:IMA和Rb-NH-,R a是有机基团,R 1和R j分别选自 氢,脂族烃,芳族烃和杂环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,两者均为任选取代的,R 1A选自 由“IMAGE”RA“和”RB“组成的组分别选自氢和1至4个碳原子的烷基,ZA选自简单键,-O-和任选地氧化硫, 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,烷基和卤代烷基1 至4个碳原子,-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,有机胺和酯化羧基 或-COOA为-COO( - ),n2为0〜2的整数,其无毒性,药学上可接受的酸加成盐具有优异的抗生素活性。
    • 6. 发明授权
    • Cephalosporins
    • 头孢菌素
    • US5936083A
    • 1999-08-10
    • US625910
    • 1996-04-01
    • Jozsef AszodiJean-Francois ChantotSolange Gouin D'Ambrieres
    • Jozsef AszodiJean-Francois ChantotSolange Gouin D'Ambrieres
    • C07D501/00C07D501/22C07D501/24C07D501/56
    • C07D501/00
    • A compound selected from the group consisting of a syn isomer of a compound of the formula ##STR1## in the R or S form or in the form of an R, S mixture wherein R us selected from the group consisting of ##STR2## R and R' are individually selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen, CO.sub.2 --Q, ##STR3## CH.sub.2 --SQ, Q and Q' are individually hydrogen or alkyl of 1 to 4 carbon atoms, P, P' and P" are individually alkyl of 1 to 4 carbon atoms optionally substituted by one of the substituents R and R' the dotted line indicating that P and P' can optionally form with the nitrogen atom to which they are linked a heterocycle with 5 or 6 links, R.sub.b and R.sub.c are individually selected from the group consisting of an equivalent of an alkali metal, an alkaline earth metal, magnesium, ammonium and an amine organic base or A and A' are the remainder of an easily cleavable ester group or CO.sub.2 A is CO.sub.2 --and the wavy line indicates that CH.sub.2 R.sub.1 is in the E or Z position and their non-toxic, pharmaceutically acceptable acid addition salts having anti-bacterial activity.
    • 选自R或S形式的式的化合物的顺式异构体或R,S混合物形式的化合物,其中R us选自R和R'的化合物分别选自 由氢,1-4个碳原子的烷基,1-4个碳原子的烷氧基,卤素,CO2-Q,CH2-SQ,Q和Q'分别是氢或1-4个碳原子的烷基,P, P'和P“分别是1至4个碳原子的烷基,任选被一个取代基R和R'取代,虚线表示P和P'可以任选地与它们连接的氮原子一起形成杂环与 5或6链,Rb和Rc分别选自碱金属,碱土金属,镁,铵和胺有机碱的当量,A和A'是易裂解酯基的剩余部分 或CO 2 A是CO 2 - 而波浪线表示CH 2 R 1在E或Z位置a 它们具有抗菌活性的无毒的,药学上可接受的酸加成盐。