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6 条记录 (耗时 0.021 秒)

    3,7-Disubstituted cephalosporins
    1.
    发明授权
    3,7-Disubstituted cephalosporins 失效
    3,7-二取代头孢菌素

    公开(公告)号：US4148996A

    公开(公告)日：1979-04-10

    申请号：US797606

    申请日：1977-05-16

    申请人： Giorgio Palamidessi ,  Franco Zarini ,  Giovanni Franceschi ,  Giovanna Schioppacassi ,  Federico Arcamone

    发明人： Giorgio Palamidessi ,  Franco Zarini ,  Giovanni Franceschi ,  Giovanna Schioppacassi ,  Federico Arcamone

    IPC分类号： C07D501/04 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/24 ,  C07D501/36

    CPC分类号： C07D501/36 ,  A61K31/545

    摘要： 7-Acylamino-3-pyrazinylthiomethyl-3-cephem-4-carboxylic acids are disclosed having the general formula: ##STR1## wherein R is an alkyl having from 1 to 5 carbon atoms or ##STR2## wherein Y = Y.sup.1 = HY = y.sup.1 = clY = cl, Y.sup.1 = FY = h,y .sup.1 = cl andIn which n is an integer from 1 to 4, X is O or S, and R.sub.2 is thienyl, phenyl, 1,4-cyclohexadienyl, phenoxy, pyrazinyl and substituted phenyl, thienyl, pyrazinyl and phenoxy, the substituent being selected from the group consisting of hydroxy, chlorine, bromine, and alkyl and alkoxy having from 1 to 4 carbon atoms;R.sub.3 is alkali metal such as sodium or potassium, hydrogen, alkyl having from 1 to 4 carbon atoms, benzyl, trichloroethyl, methoxybenzyl, benzhydryl, pivaloyloxymethyl, and an alkaline earth metal; R.sup.1 may be a pyrazinyl of the general formulae: ##STR3## in which R.sup.4, R.sup.5, R.sup.6 are equal or different and are selected from the group consisting of F, Cl, Br, hydrogen, alkyl, phenyl, cyano, thiocyano, carboxyl, carboxyalkyl, carboxamido, thiocarboxamido, hydroxy, alkoxy, thiol, alkylthio, amino, alkylamino, phenylamino. By the terms alkyl, an alkyl having from 1 to 4 carbon atoms is intended. Processes for making them are also disclosed.The new cephalosporin derivatives of formula (I) exhibit a broad spectrum antibacterial activity and are useful as therapeutic agents in the treatment of infectious diseases caused by gram-negative and gram-positive bacteria.

    摘要翻译： 公开了具有以下通式的7-酰基氨基-3-吡嗪基硫甲基-3-头孢烯-4-羧酸：其中R是具有1至5个碳原子的烷基或者具有1或5个碳原子的烷基 其中Y = Y1 = HY = Y1 = C1 Y = C1，Y1 = FY = H，Y1 = C1和IN，其中N为1至4的整数，X为O或S，R2为噻吩基， 苯基，1,4-环己二烯基，苯氧基，吡嗪基和取代的苯基，噻吩基，吡嗪基和苯氧基，所述取代基选自羟基，氯，溴以及具有1至4个碳原子的烷基和烷氧基; R3是碱金属如钠或钾，氢，具有1至4个碳原子的烷基，苄基，三氯乙基，甲氧基苄基，二苯甲基，新戊酰氧基甲基和碱土金属; R 1可以是以下通式的吡嗪基：其中R 4，R 5，R 6相同或不同，并且选自F，Cl，Br，氢，烷基，苯基，氰基，硫氰基，羧基， 羧基烷基，甲酰氨基，硫代甲酰胺基，羟基，烷氧基，硫醇，烷硫基，氨基，烷基氨基，苯基氨基。 术语烷基是指具有1至4个碳原子的烷基。 还披露了制作它们的过程。

    Azole compounds endowed with antimycotic activity for human and veterinary use
    4.
    发明授权
    Azole compounds endowed with antimycotic activity for human and veterinary use 失效
    唑类化合物具有抗真菌活性，适用于人和兽用

    公开(公告)号：US6103909A

    公开(公告)日：2000-08-15

    申请号：US138904

    申请日：1998-08-24

    申请人： Mauro Napoletano ,  Cristina Fraire ,  Enrico Albini ,  Giovanna Schioppacassi

    发明人： Mauro Napoletano ,  Cristina Fraire ,  Enrico Albini ,  Giovanna Schioppacassi

    IPC分类号： A61K31/00 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4196 ,  A61P31/00 ,  A61P31/10 ,  C07D233/60 ,  C07D249/08 ,  C07D521/00

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： Compounds of formula ##STR1## wherein R.sub.1 is chloro, fluoro, bromo or trifluoromethyl;R.sub.2 is hydrogen, chloro , fluoro, bromo or trifluoromethyl;Z is CH or N;R.sub.3, R.sub.4 and R.sub.5, which are the same or different, are hydrogen or C.sub.1 -C.sub.4 alkyl, with the proviso that R.sub.4 is different from R.sub.5 when R.sub.3 is hydrogen;X is O, S, SO or SO.sub.2 ;R.sub.6 is a C.sub.1 -C.sub.5 polyfluoroalkyl group containing at least two fluorine atoms and optionally other halogen atoms selected from the group consisting of chloro and bromo; processes for their preparation and pharmaceutical compositions containing them are described.The compounds of formula II-A are endowed with a marked wide range antimycotic acitivity.

    摘要翻译： 式的化合物其中R 1是氯，氟，溴或三氟甲基; R2是氢，氯，氟，溴或三氟甲基; Z是CH或N; R 3，R 4和R 5相同或不同，是氢或C 1 -C 4烷基，条件是当R3是氢时，R 4不同于R 5; X是O，S，SO或SO 2; R6是含有至少两个氟原子和任选地其它选自氯和溴的卤素原子的C1-C5多氟烷基; 描述了其制备方法和含有它们的药物组合物。 式II-A的化合物具有显着的广泛的抗真菌活性。

    Azole compounds with antimycotic activity for human and veterinary use
    6.
    发明授权
    Azole compounds with antimycotic activity for human and veterinary use 失效
    用于人类和兽医用途的具有抗真菌活性的唑类化合物

    公开(公告)号：US5869512A

    公开(公告)日：1999-02-09

    申请号：US806149

    申请日：1997-02-25

    申请人： Mauro Napoletano ,  Cristina Fraire ,  Enrico Albini ,  Giovanna Schioppacassi

    发明人： Mauro Napoletano ,  Cristina Fraire ,  Enrico Albini ,  Giovanna Schioppacassi

    IPC分类号： A61K31/00 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4196 ,  A61P31/00 ,  A61P31/10 ,  C07D233/60 ,  C07D249/08 ,  C07D521/00

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： Compounds of formula ##STR1## wherein R.sub.1 is chloro, fluoro, bromo or trifluoromethyl;R.sub.2 is hydrogen, chloro, fluoro, bromo or trifluoromethyl;Z is CH or N;R.sub.3, R.sub.4 and R.sub.5, which are the same or different, are hydrogen or C.sub.1 -C.sub.4 alkyl, with the proviso that R.sub.4 is different from R.sub.5 when R.sub.3 is hydrogen;X is O, S, SO or S0.sub.2 ;R.sub.6 is a C.sub.1 -C.sub.5 polyfluoroalkyl group containing at least two fluorine atoms and optionally other halogen atoms selected from the group consisting of chloro and bromo; processes for their preparation and pharmaceutical compositions containing them are described.The compounds of formula II-A are endowed with a marked wide range antimycotic acitivity.

    摘要翻译： 式（II-A）的化合物，其中R 1是氯，氟，溴或三氟甲基; R2是氢，氯，氟，溴或三氟甲基; Z是CH或N; R 3，R 4和R 5相同或不同，是氢或C 1 -C 4烷基，条件是当R 3是氢时，R 4不同于R 5; X是O，S，SO或SO 2; R6是含有至少两个氟原子和任选地其它选自氯和溴的卤素原子的C1-C5多氟烷基; 描述了其制备方法和含有它们的药物组合物。 式II-A的化合物具有显着的广泛的抗真菌活性。