Antibacterial penem esters derivatives
    4.
    发明授权
    Antibacterial penem esters derivatives 失效
    抗菌青蒿酯衍生物

    公开(公告)号:US5885981A

    公开(公告)日:1999-03-23

    申请号:US470944

    申请日:1995-06-06

    CPC分类号: C07D499/88

    摘要: Antibiotic penem compounds are represented by the following formula: ##STR1## wherein R represents a group of the general formula: ##STR2## in which R.sub.1 is a hydrogen atom or linear or branched C.sub.1 --C.sub.6 alkyl group, R.sub.2 is a particular substituted or unsubstituted alkyl, aryl or aralkyl group, n is an integer of 1-6, Y is a 5- or 6-membered heterocyclic aliphatic group having 1 or 2 oxygen atoms in the ring thereof, and Z is a specific 5-substituted 2-oxo-1,3-dioxolen-4-yl group. Antibiotic compositions for oral administration are also described.

    摘要翻译: 抗生素penem化合物由下式表示:其中R表示下列通式的基团:其中R 1为氢原子或直链或支链C 1 -C 6烷基,R 2为特定的取代或未取代的 烷基,芳基或芳烷基,n为1-6的整数,Y为其环中具有1或2个氧原子的5或6元杂环脂族基团,Z为特定的5-取代的2-氧代 -1,3-二氧杂环戊烯-4-基。 还描述了用于口服给药的抗生素组合物。

    Process for preparing .beta.-lactam derivative and synthetic
intermediate thereof
    6.
    发明授权
    Process for preparing .beta.-lactam derivative and synthetic intermediate thereof 失效
    制备β-内酰胺衍生物及其合成中间体的方法

    公开(公告)号:US5414081A

    公开(公告)日:1995-05-09

    申请号:US18407

    申请日:1993-02-17

    摘要: Disclosed is a process for preparing a .beta.-lactam compound represented by the formula: ##STR1## wherein R.sup.1 represents a hydroxy-substituted lower alkyl group or an amino group each of which may be protected; R.sup.2 represents hydrogen atom or an ester residue; X represents a methylene group which may be substituted by a lower alkyl group, sulfur atom or a group represented by the formula: --A--CH.sub.2 -- where A represents sulfur atom, oxygen atom or methylene group; and W represents an active ester residue of hydroxyl group, or a salt thereof, which comprises the steps of treating a 1-aza-3-thia-bicycloalkane compound represented by the formula: ##STR2## wherein R.sup.1, R.sup.2 and X have the same meanings as defined above, or a salt thereof with a base in the presence of a desulfurizing agent and then reacting the resulting compound with an active esterifying agent of hydroxyl group.

    摘要翻译: 公开了一种制备由下式表示的β-内酰胺化合物的方法:低级烷基或各自可被保护的氨基; R2表示氢原子或酯残基; X表示可以被低级烷基,硫原子或由下式表示的基团取代的亚甲基:-A-CH2-,其中A表示硫原子,氧原子或亚甲基; W表示羟基的活性酯残基或其盐,其包括如下步骤:处理由下式表示的1-氮杂-3-硫杂 - 双环烷烃化合物:其中R1,R2和X 具有与上述相同的含义,或其盐与脱碱剂存在下的碱,然后使所得化合物与羟基的活性酯化剂反应。

    Pharmaceutically-acceptable amine salts of 6-.beta.-halopenicillanic
acids
    7.
    发明授权
    Pharmaceutically-acceptable amine salts of 6-.beta.-halopenicillanic acids 失效
    6-β-卤代青霉烷酸的药学上可接受的胺盐

    公开(公告)号:US4594246A

    公开(公告)日:1986-06-10

    申请号:US564901

    申请日:1983-12-23

    申请人: Welf von Daehne

    发明人: Welf von Daehne

    CPC分类号: C07D499/00

    摘要: This invention relates to penicillanic acid derviatives of the formula I ##STR1## in which X stands for chlorine, bromine or iodine, to pharmaceutically acceptable, non-toxic salts of the compounds of formula I, to pharmaceutically acceptable, easily hydrolyzable esters thereof, including salts of such esters, to pharmaceutical compositions containing the compounds of the invention and dosage units thereof, to methods for the preparation of the compounds of the invention, and to methods of using the said new compounds in the human and veterinary therapy.The 6.beta.-halopenicillanic acids of formula I are potent inhibitors of .beta.-lactamases from a variety of gram-positive and gram-negative bacteria, making the 6.beta.-halopenicillanic acids as well as their salts and easily hydrolyzable esters valuable in human and veterinary medicine.

    摘要翻译: 本发明涉及式I的青霉烷酸衍生物,其中X代表氯,溴或碘,以及式I化合物的药学上可接受的无毒盐,其药学上可接受的,易水解的酯, 包括这些酯的盐,含有本发明化合物的药物组合物及其剂量单位,以及制备本发明化合物的方法,以及在人和兽医疗法中使用所述新化合物的方法。 式I的6个β-卤代青霉烷酸是来自多种革兰氏阳性和革兰氏阴性细菌的β-内酰胺酶的有效抑制剂,使6β-卤代青霉烷酸及其盐和容易水解的酯在人和兽医中有价值 医学。

    Process for the preparation of faropenem
    10.
    发明授权
    Process for the preparation of faropenem 失效
    制备法罗培南的方法

    公开(公告)号:US07977475B2

    公开(公告)日:2011-07-12

    申请号:US12089159

    申请日:2006-10-05

    IPC分类号: C07D499/893

    CPC分类号: C07D499/893

    摘要: The present invention is related to processes for the preparation of faropenem, which comprises treating the compound of Formula II, with an alkali metal salt of a substituted or unsubstituted C5-10 carboxylic acid and a catalytic amount of a palladium complex in the presence of an organic solvent, followed by the treatment of the reaction mixture of with water and a water miscible solvent, and isolating a hydrate of an alkali metal salt of faropenem from the reaction mass, wherein water is not removed from the reaction mixture in water treatment or isolation steps.

    摘要翻译: 本发明涉及制备法罗培南的方法,该方法包括在取代或未取代的C 5-10羧酸的碱金属盐和催化量的钯络合物的存在下处理式II化合物 有机溶剂,然后用水和水混溶性溶剂处理反应混合物,并从反应物质中分离法罗培南碱金属盐的水合物,其中在水处理或分离中不从反应混合物中除去水 脚步。