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8 条记录 (耗时 0.02 秒)

    Processes for preparing .beta.-lactams
    2.
    发明授权
    Processes for preparing .beta.-lactams 失效
    制备β-内酰胺的方法

    公开(公告)号：US4407751A

    公开(公告)日：1983-10-04

    申请号：US291081

    申请日：1981-08-07

    申请人： Wagn O. Godtfredsen ,  Welf von Daehne

    发明人： Wagn O. Godtfredsen ,  Welf von Daehne

    IPC分类号： C07D499/00 ,  C07D499/32 ,  C07D503/00 ,  C07D519/00 ,  C07D499/04

    CPC分类号： C07D503/00 ,  C07D499/00

    摘要： The present invention relates to hitherto unknown compounds of the general formula I: ##STR1## in which R.sub.1 stands for a phenyl, 4-hydroxyphenyl, 1,4-cyclohexadienyl or a 3-thienyl group; R.sub.2 represents a primary amino or a carboxy group; R.sub.3 is a hydrogen atom, or a lower alkyl, aryl or aralkyl radical, and A stands for a radical of a .beta.-lactamase inhibitor containing a .beta.-lactam ring as well as a carboxy group, A being connected via the carboxy group.The present invention provides new compounds useful in the treatment of bacterial infections. The new compounds are in particular strongly active against .beta.-lactamase producing bacteria.

    摘要翻译： 本发明涉及迄今未知的通式Ⅰ化合物：其中R1代表苯基，4-羟基苯基，1,4-环己二烯基或3-噻吩基; R2表示伯氨基或羧基; R3是氢原子或低级烷基，芳基或芳烷基，A代表含有β-内酰胺基的羧基的羧基，A通过羧基连接。 本发明提供了可用于治疗细菌感染的新化合物。 新化合物特别对β-内酰胺酶生产细菌具有强烈的活性。

    6-Amidinopenicillanic acid derivatives including the radical of a .beta.-lactamase inhibitor
    3.
    发明授权
    6-Amidinopenicillanic acid derivatives including the radical of a .beta.-lactamase inhibitor 失效
    包括β-内酰胺酶抑制剂基团的6-脒基青霉烷酸衍生物

    公开(公告)号：US4325960A

    公开(公告)日：1982-04-20

    申请号：US116651

    申请日：1980-01-29

    申请人： Wagn O. Godtfredsen ,  Welf von Daehne

    发明人： Wagn O. Godtfredsen ,  Welf von Daehne

    IPC分类号： C07D499/80 ,  A61K31/431 ,  A61P31/04 ,  C07D499/00 ,  C07D499/21 ,  C07D499/32 ,  C07D499/42 ,  C07D503/00 ,  C07D519/00

    CPC分类号： C07D503/00 ,  C07D499/00

    摘要： The present invention relates to hitherto unknown compounds of the general formula I: ##STR1## in which R.sub.1 stands for a five- to ten-membered azacycloalkyl or azabicycloalkyl residue attached via the nitrogen atom and optionally being substituted by one or two, the same or different, lower alkyl groups; R.sub.2 represents a hydrogen atom or a lower alkyl, aryl, or aralkyl radical; and A represents a radical of a .beta.-lactamase inhibitor containing a .beta.-lactam ring as well as a carboxy group, A being connected via the carboxy group.The present compounds are useful in the treatment of bacterial infections. The new compounds are in particular strongly active against .beta.-lactamase producing bacteria.

    摘要翻译： 本发明涉及迄今为止未知的通式I化合物：其中R1代表通过氮原子连接并任选被一个或两个相同的5至10元氮杂环烷基或氮杂双环烷基取代的相同 或不同的低级烷基; R2表示氢原子或低级烷基，芳基或芳烷基; 而A代表含有β-内酰胺环以及羧基的β-内酰胺酶抑制剂的基团，A通过羧基连接。

    Crystalline penicillin derivative tosylate hydrates
    5.
    发明授权
    Crystalline penicillin derivative tosylate hydrates 失效
    结晶青霉素衍生物甲苯磺酸盐水合物

    公开(公告)号：US4831025A

    公开(公告)日：1989-05-16

    申请号：US24858

    申请日：1987-03-13

    申请人： Wagn O. Godtfredsen ,  Welf von Daehne

    发明人： Wagn O. Godtfredsen ,  Welf von Daehne

    IPC分类号： C07D499/08 ,  A61K31/43 ,  A61P31/04 ,  C07D499/00 ,  C07D499/32 ,  C07D499/68 ,  C07D499/86 ,  C07D519/06

    CPC分类号： C07D499/00

    摘要： The present invention relates to a crystalline hydrate of a salt of the antimicrobial agent 1,1-dioxopenicillanoyloxymethyl 6-(D-.alpha.-amino-.alpha.-phenylacetamido)penicillanate with p-toluenesulfonic acid, more particularly the mono- and dihydrate.The hydrates are easily obtained in a crystalline state devoid of organic solvent residues, they show good stability on storage, they are effectively absorbed and hydrolyzed in vivo, and they are thus specifically suitable for medical treatment of patients, in particular for oral administration.

    摘要翻译： 本发明涉及6-（D-α-氨基-α-苯基乙酰氨基）青霉素与对甲苯磺酸的抗微生物剂1,1-二氧代青霉酰氨基甲酸盐的结晶水合物，更特别是一水合物和二水合物。 水合物在没有有机溶剂残留物的结晶状态下容易获得，它们在储存时显示出良好的稳定性，它们在体内被有效地吸收和水解，因此它们特别适用于患者的医疗，特别是用于口服给药。

    Penicillin esters, salts thereof and methods for their preparation
    7.
    发明授权
    Penicillin esters, salts thereof and methods for their preparation 失效
    青霉素酯，其盐及其制备方法

    公开(公告)号：US4554160A

    公开(公告)日：1985-11-19

    申请号：US554423

    申请日：1975-03-03

    申请人： Wagn O. Godtfredsen

    发明人： Wagn O. Godtfredsen

    IPC分类号： C07D295/088 ,  C07D499/00 ,  A61K35/00

    CPC分类号： C07D295/088 ,  C07D499/00

    摘要： The invention relates to a new series of penicillin esters and salts thereof, to methods of their preparation and to intermediates in the production of the esters of the general formula ##STR1## in which R.sub.1 and R.sub.2 represent an alkyl radical having from 1 to 6 carbon atoms, a cycloalkyl or cycloalkylalkyl radical the cycloalkyl part having from 3 to 10 carbon atoms, or R.sub.1 and R.sub.2 together with the nitrogen atom represent a heterocyclic ring with from 4 to 8 carbon atoms; R.sub.3 represents radicals known from natural, biosynthetic, and semisynthetic penicillins; and pharmaceutically acceptable salts thereof.The new compounds are efficiently absorbed from the gastrointestinal tract and after the absorption they are rapidly transformed into the corresponding free penicillins and amidinopenicillanic acids, whereby a broad-spectrum infection can be combated.

    摘要翻译： 本发明涉及一系列新的青霉素酯及其盐，其制备方法和中间体在制备通式ⅠA的酯中，其中R 1和R 2表示具有1至6个的烷基 碳原子，环烷基或环烷基烷基，具有3至10个碳原子的环烷基部分，或R1和R2与氮原子一起代表具有4至8个碳原子的杂环; R3表示天然，生物合成和半合成青霉素已知的基团; 及其药学上可接受的盐。 新化合物被有效地从胃肠道吸收，吸收后迅速转化为相应的游离青霉素和脒基青霉烷酸，从而可以对抗广泛感染。

    Topical preparation for treatment of alopecia
    8.
    发明授权
    Topical preparation for treatment of alopecia 失效
    治疗脱发的专题准备

    公开(公告)号：US5244664A

    公开(公告)日：1993-09-14

    申请号：US817816

    申请日：1992-01-08

    申请人： Wagn O. Godtfredsen

    发明人： Wagn O. Godtfredsen

    IPC分类号： A61K8/49 ,  A61Q7/00

    CPC分类号： A61K8/4926 ,  A61Q7/00

    摘要： This invention relates to pharmaceutical compositions for treatment of alopecia comprising a compound of formula, in the form of the free base or acid addition salts thereof, in association with a pharmaceutical carrier adapted for topical application to mammalian skin. The compounds used have general formula ##STR1## in which the R.sub.1 -substituted cyanoguanidyl radical is placed in the 3- or 4-position of the pyridine ring, and in which R.sub.1 stands for a straight or branched, saturated or unsaturated, aliphatic hydrocarbon radical having from 1 to 8 carbon atoms, a cycloalkyl or cycloalkenyl radical having from 3 to 7 carbon atoms, or an aryl or an aralkyl radical. R.sub.2 stands for hydrogen, halogen, hydroxy, lower alkyl or alkoxy radicals. The present compositions find applications both in the human and veterinary use.

    摘要翻译： 本发明涉及用于治疗脱发的药物组合物，其包含与游离碱或其酸加成盐形式的式的化合物，其与适于局部施用于哺乳动物皮肤的药物载体结合。 所使用的化合物具有通式“IMAGE”，其中R1取代的氰基胍基位于吡啶环的3-或4-位，其中R1代表直链或支链饱和或不饱和的脂族烃基 具有1至8个碳原子，具有3至7个碳原子的环烷基或环烯基，或芳基或芳烷基。 R2代表氢，卤素，羟基，低级烷基或烷氧基。 本发明的组合物在人类和兽医学应用中都有应用。