CONDENSED CARBAPENEM DERIVATIVES
    72.
    发明公开
    CONDENSED CARBAPENEM DERIVATIVES 失效
    简明碳青霉烯类。

    公开(公告)号:EP0656899A1

    公开(公告)日:1995-06-14

    申请号:EP93919157.0

    申请日:1993-08-25

    申请人: GLAXO S.p.A.

    IPC分类号: A61K31 A61P31 C07D477

    CPC分类号: C07D477/00

    摘要: The present invention relates to compounds of formula (I) and salts and metabolically labile esters thereof; wherein R is a 5 or 6 membered nitrogen containing heteroaryl group, which heteroaryl group optionally contains 1 or 2 additional heteroatoms selected from nitrogen, oxygen or sulphur and said heteroaryl group is linked to the alkylene chain (CH2)n via a nitrogen atom in the heteroaryl group; n is an integer from 2 to 4, to processes for their preparation and to their use as antibacterial agents.

    ANTIBACTERIAL CONDENSED CARBAPENEMES
    76.
    发明公开
    ANTIBACTERIAL CONDENSED CARBAPENEMES 失效
    抗菌简明碳青霉烯类。

    公开(公告)号:EP0589886A1

    公开(公告)日:1994-04-06

    申请号:EP92905563.0

    申请日:1992-03-02

    申请人: GLAXO S.p.A.

    IPC分类号: A61K31 A61P31 C07D477

    CPC分类号: C07D477/00 Y02P20/55

    摘要: Composés de formule (I) dans laquelle R1 représente un atome d'hydrogène ou un groupe protecteur hydroxyle; R2 représente un atome d'hydrogène, un groupe protecteur carboxyle ou un cation dérivé d'une base inorganique ou d'une base organique; R3 représente le groupe O(CH2)nR4 dans lequel n est un nombre entier pouvant aller de 2 à 6 et R4 représente un atome d'halogène ou un hydroxy, un alcoxy C1-3, un alkythio C1-3, un azido, un cyano, un nitro ou un groupe ammonium quaternaire N+R5R6R7X- dans lequel R5 et R6 représentent indépendamment un groupe alkyle C1-3, R7 représente un groupe alkyle C1-2 et X- est un anion pharmaceutiquement acceptable. On décrit également des esters métaboliquement labiles, leurs sels et leurs solvates ainsi que des procédés de production de ceux-ci.

    Antibiotic carbapenem compounds
    77.
    发明公开
    Antibiotic carbapenem compounds 失效
    抗生素碳青霉烯

    公开(公告)号:EP0581502A1

    公开(公告)日:1994-02-02

    申请号:EP93305609.5

    申请日:1993-07-16

    摘要: The present invention relates to carbapenems and provides a compound of the formula (I)

    wherein :

    R 1 is i-hydroxyethyl, 1-fluoroethyl or hydroxymethyl ;
    R 2 is hydrogen or C 1-4 alkyl;
    R 3 is hydrogen or C 1-4 alkyl;
    A is a 5-membered heteroaryl ring containing one nitrogen atom and up to two additional heteroatoms selected from nitrogen, oxygen and sulphur ; and is bonded to the nitrogen of the linking carbamoyl group by a carbon atom in the ring, is substituted with the carboxy group on a carbon atom in the ring and is optionally further substituted on a carbon atom in the ring ; and

    in any ring -NH-, H is optionally replaced by C 1-4 alkyl;
    or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them are also described.

    摘要翻译: 本发明涉及碳青霉烯并提供式(I)化合物其中:R 1是1-羟乙基,1-氟乙基或羟甲基; R 2是氢或C 1-4烷基; R 3是氢或C 1-4烷基; A是含有一个氮原子和多达两个另外选自氮,氧和硫的杂原子的5元杂芳基环; 并且通过环中的碳原子与连接的氨基甲酰基的氮键合,被环中的碳原子上的羧基取代,并且任选地在环中的碳原子上进一步取代; 并且在任何环-NH-中,H任选被C 1-4烷基取代; 或其药学上可接受的盐或体内可水解的酯。 还描述了其制备方法,其制备中的中间体,它们作为治疗剂的用途和含有它们的药物组合物。

    Method for removing the protecting group for hydroxy group
    78.
    发明公开
    Method for removing the protecting group for hydroxy group 失效
    维尔法伦,嗯,伊朗geschützteHO-Gruppe freizumachen。

    公开(公告)号:EP0567949A1

    公开(公告)日:1993-11-03

    申请号:EP93106643.5

    申请日:1993-04-23

    摘要: A method for removing tri-substituted silyl group from β-lactam compound having a tri-substituted silyl group-protecting hydroxy group, which comprises treating with an acid and a fluoride selected from alkali metal fluoride, alkaline earth metal fluoride and hydrogenfluoride of organic or inorganic amine, by which the tri-substituted silyl group can be easily and effectively removed under moderate conditions so that the desired compound can be obtained in high yield at low cost.

    摘要翻译: 一种从具有三取代甲硅烷基保护羟基的β-内酰胺化合物中除去三取代甲硅烷基的方法,该方法包括用酸和选自碱金属氟化物,碱土金属氟化物和氟化氢的有机或 无机胺,通过其可以在中等条件下容易且有效地除去三取代甲硅烷基,从而可以低成本高收率地获得所需化合物。