Cephem compounds, their production and use
    51.
    发明公开
    Cephem compounds, their production and use 失效
    头孢烯化合物,它们的生产和使用

    公开(公告)号:EP0304858A2

    公开(公告)日:1989-03-01

    申请号:EP88113679.0

    申请日:1988-08-23

    CPC分类号: C07D501/46 C07D519/00

    摘要: Novel cephem compounds of the general formula :
    wherein R¹ is a lower alkyl group, and salts and esters thereof, showing excellent and balanced antibacterial activity against a broad spectrum of bacteria, especially by rectal administration, and their production and use as antimicrobial agents are described.

    摘要翻译: 描述了具有以下通式的新型头孢烯化合物:其中R 1为低级烷基及其盐和酯,其对广谱细菌,特别是直肠给药,以及它们作为抗微生物剂的生产和用途显示出优异和平衡的抗菌活性 。

    Antibacterial compounds, their production and use
    54.
    发明公开
    Antibacterial compounds, their production and use 失效
    Antibakterielle Verbindungen,ihre Herstellung und Verwendung。

    公开(公告)号:EP0203271A2

    公开(公告)日:1986-12-03

    申请号:EP86102584.9

    申请日:1986-02-27

    摘要: A compound of the formula;
    wherein R 1 is an amino group which may be protected, R 3 is a hydrogen atom or an optionally substituted hydrocarbon residue; Z is S, S → O, O or CH 2 , R 4 is a hydrogen atom, methoxy group or formamido group, R 13 is a hydrogen atom, methyl group, hydroxyl group or halogen atom and A⊕ is an optionally substituted imidazolium-1-yl group forming a condensed ring at the 2,3- or 3,4-position or a pharmaceutically acceptable salt or ester thereof is novel and has excellent antibacterial activity.

    摘要翻译: 式的化合物; 其中R 1为可被保护的氨基,R 3为氢原子或任选取代的烃残基; Z是S,S - > O,O或CH 2,R 4是氢原子,甲氧基或甲酰氨基,R 1是氢原子,甲基,羟基或卤原子,A 在(2,3)或3,4位上形成稠环的任选被取代的咪唑鎓-1-基,或其药学上可接受的盐或酯是新的并且具有优异的抗菌活性。

    Cephalosporin esters, their production and use
    56.
    发明公开
    Cephalosporin esters, their production and use 失效
    CEPHOROSPORIN ESTERS,他们的生产和使用

    公开(公告)号:EP0128027A3

    公开(公告)日:1985-11-21

    申请号:EP84303702

    申请日:1984-06-01

    IPC分类号: C07D501/36 A61K31/545

    CPC分类号: C07D501/36

    摘要: A compound of the formula
    wherein (1) R 1 is a lower alkyl group of 2 to 6 carbon atoms or a cycloalkyl group of 5 to 7 carbon atoms and R 2 is a cycloalkyl group of 5 to 7 carbon atoms or a lower alkyl group of 1 to 3 carbon atoms which is substituted by a cycloalkyl group of 5 to 7 carbon atoms or by a phenyl group, or (2) R, is a cycloalkyl group of 5 to 7 carbon atoms and R 2 is a lower alkyl group of 1 to 5 carbon atoms, or a pharmaceutically acceptable salt thereof, processes for preparing the same and a pharmaceutical composition thereof are provided. The compound can orally be applied as antibiotics having improved bioavailability.

    Cephem compounds
    57.
    发明公开
    Cephem compounds 失效
    Cephemverbindungen。

    公开(公告)号:EP0160969A2

    公开(公告)日:1985-11-13

    申请号:EP85105579.8

    申请日:1985-05-07

    IPC分类号: C07D501/46

    CPC分类号: C07D501/46

    摘要: A cephem compound of the formula:
    wherein R, is an optionally protected amino group; Q is a nitrogen atom or a C-R 2 group; R 2 is a hydrogen or halogen atom; R 3 is a hydrogen atom or a hydrocarbon residue which may be substituted; R 4 is a hydrogen atom or a methoxy group; R 5 is a nitrogen-containing aromatic heterocyclic group which may be substituted; A denotes that further substituted or substituents may be present on the pyridine ring; n is 0 or 1 or a physiologically or pharmaceutically acceptable salt or ester thereof.
    This compound is novel and has an excellent antibacterial activity.

    摘要翻译: 化学式为下式的头孢烯化合物:其中R 1为任选保护的氨基; Q是氮原子或C-R2基团; R2是氢或卤素原子; R3是氢原子或可被取代的烃残基; R4是氢原子或甲氧基; R5是可以被取代的含氮芳族杂环基; A表示进一步取代或取代基可以存在于吡啶环上; n为0或1,或其生理或药学上可接受的盐或酯。 该化合物是新颖的,具有优异的抗菌活性。

    Method for producing 1-iodoalkyl acylates
    58.
    发明公开
    Method for producing 1-iodoalkyl acylates 失效
    Herstellungsverfahren von 1-Iodalkyl-Acylaten。

    公开(公告)号:EP0143601A2

    公开(公告)日:1985-06-05

    申请号:EP84308067.2

    申请日:1984-11-21

    摘要: 1-lodoalkyl acylates, which are useful as raw materials for the esterification of cephalosporins and penicillins, are prepared in a high degree of purity and in high yield by reacting a carboxylic acid iodide with an aldehyde. The carboxylic acid iodide may be prepared in situ by reacting a carboxylic acid chloride with a salt of hydriodic acid and then reacting the resulting product with an aldehyde, or by simultaneously reacting a carboxylic acid chloride, a salt of hydriodic acid I and an aldehyde with one another.

    摘要翻译: 可用作头孢菌素和青霉素酯化原料的1-碘代烷基酰化物通过羧酸碘化物与醛的反应以高纯度和高收率制备。 羧酸碘化物可以通过使羧酸氯化物与氢碘酸盐反应然后使所得产物与醛反应,或通过同时使羧酸氯化物,氢碘酸和醛与一种 另一个。

    1-Sulfo-2-azetidinone derivatives, their production and use
    59.
    发明公开
    1-Sulfo-2-azetidinone derivatives, their production and use 失效
    1-Sulfo-2-azetidinon-Derivate,ihre Herstellung und Verwendung。

    公开(公告)号:EP0100041A1

    公开(公告)日:1984-02-08

    申请号:EP83106993.5

    申请日:1983-07-16

    摘要: 1-Sulfo-2-azetidinone derivative of the formula:
    wherein

    R 1 is an amino group which may optionally be acylated or protected; and
    R 2 is a five- or six-membered ring-forming primary or secondary amido group which may contain at least one of nitrogen, sulfur and oxygen atoms as a ring-constituting element; or a pharmaceutically acceptable salt thereof, is novel and possesses excellent antimicrobial activity and b-lactamase inhibitory activity, and is useful as a treatment agent against infections in man and mammals.

    摘要翻译: 1-磺基-2-氮杂环丁酮衍生物,其结构式为:CHEM,其中R 1是任选被酰化或保护的氨基; R 2是可以含有氮,硫和氧原子中的至少一个作为构成环的元素的五元或六元环形的伯或仲酰胺基; 或其药学上可接受的盐是新颖的并且具有优异的抗微生物活性和β-内酰胺酶抑制活性,并且可用作抗人和哺乳动物感染的治疗剂。