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    3-vinyl-cephalosporins and their preparations
    12.
    发明授权
    3-vinyl-cephalosporins and their preparations 失效
    3-乙烯基头孢菌素及其制剂

    公开(公告)号：US4622393A

    公开(公告)日：1986-11-11

    申请号：US610175

    申请日：1984-05-14

    申请人： Daniel Farge ,  Pierre Le Roy ,  Claude Moutonnier ,  Jean-Francois Peyronel

    发明人： Daniel Farge ,  Pierre Le Roy ,  Claude Moutonnier ,  Jean-Francois Peyronel

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D253/07 ,  C07D501/24

    CPC分类号： C07D253/065 ,  C07D253/07

    摘要： New 3-vinylcephalosporins of the general formula (I), ##STR1## in which n=0 or 1, R.sub.1 is a radical of the general formula (II), ##STR2## in which R.sub.4 is hydrogen or a protective radical and R.sub.5 represents a radical of the general formula (IIa) ##STR3## in which R.sup.a.sub.5 and R.sup.b.sub.5 are hydrogen or alkyl or together form an alkylene radical and R.sup.c.sub.5 is hydrogen or a protective radical, R.sub.2 is hydrogen, a protective radical or a radical which can easily be removed by an enzymatic method, and R.sub.3 is a halogen atom or a radical R'.sub.3 SO.sub.2 O-- or R".sub.3 CO--O--, in which radicals R'.sub.3 and R".sub.3 are substituted or unsubstituted alkyl or phenyl radicals, or alternatively R.sub.1 is a hydrogen atom or a radical of the general formula (II) in which R.sub.4 is defined as above and R.sub.5 is hydrogen, alkyl, vinyl, cyanomethyl or a protective radical, and R.sub.2 is defined as above, or R.sub.1 is hydrogen or a variously substituted acyl radical and R.sub.2 is hydrogen or a protective radical, and R.sub.3 is a halogen atom.These new products are useful as intermediates for the preparation of antibiotic cephalosporins.

    摘要翻译： 通式（I）的新的3-乙酰头孢菌素，其中n = 0或1的其中R 1是通式（II）的基团，其中R 4是氢或 保护基，R 5表示通式（IIa）（IIa）的基团，其中Ra5和Rb5为氢或烷基或一起形成亚烷基，Rc5为氢或保护基，R2为氢， 保护基或可以通过酶法容易地除去的基团，R3是卤素原子或基团R'3SO2O-或R'3CO-O-，其中基团R'3和R'3被取代 或未取代的烷基或苯基，或者R 1是氢原子或通式（II）的基团，其中R 4如上定义，R 5是氢，烷基，乙烯基，氰基甲基或保护基，并且R 2被定义 如上所述，或R 1为氢或各种取代的酰基，R 2为氢或保护基，R 3为卤素原子。 这些新产品可用作制备抗生素头孢菌素的中间体。

    Cephalosporin derivatives
    13.
    发明授权
    Cephalosporin derivatives 失效
    头孢菌素衍生物

    公开(公告)号：US4503220A

    公开(公告)日：1985-03-05

    申请号：US408674

    申请日：1982-08-16

    申请人： Daniel Farge ,  Pierre L. Roy ,  Claude Moutonnier ,  Jean-Francois Peyronel

    发明人： Daniel Farge ,  Pierre L. Roy ,  Claude Moutonnier ,  Jean-Francois Peyronel

    IPC分类号： C07D501/18 ,  C07F9/6561 ,  C07D501/14 ,  A61K31/545

    CPC分类号： C07F9/65613

    摘要： 3-Vinylcephalosporin derivatives of the formula: ##STR1## in which the symbols R.sub.1 are phenyl radicals or radicals --OZ.sub.1 (it being possible for Z.sub.1 to be alkyl, 2,2,2-trichloroethyl or optionally substituted phenyl or benzyl, or for the radicals Z.sub.1 to form an alkylene radical), R.sub.2 is a radical which can be removed by an enzymatic method, or a protecting radical, and R.sub.3 and R.sub.4 are optionally substituted alkyl, or phenyl, or together form a saturated 5-membered or 6-membered heterocyclic ring optionally containing another hetero-atom, are new, crystallizable intermediates useful for the preparation of anti-bacterial cephalosporins.

    摘要翻译： 其中符号R1是苯基或基团-OZ1（Z1可以是烷基，2,2,2-三氯乙基或任选取代的苯基或苄基）的下式的3-乙烯基头孢菌素衍生物： 或基团Z 1形成亚烷基），R 2为可通过酶法或保护基除去的基团，且R 3和R 4为任选取代的烷基或苯基，或一起形成饱和的5元环 或任选含有另一个杂原子的6元杂环是可用于制备抗菌头孢菌素的新的可结晶中间体。

    Cephalosporin derivatives, and pharmaceutical compositions containing them
    14.
    发明授权
    Cephalosporin derivatives, and pharmaceutical compositions containing them 失效
    头孢菌素衍生物和含有它们的药物组合物

    公开(公告)号：US4496560A

    公开(公告)日：1985-01-29

    申请号：US408676

    申请日：1982-08-16

    申请人： Daniel Farge ,  Pierre Le Roy ,  Claude Moutonnier ,  Jean-Francois Peyronel ,  Bernard Plau

    发明人： Daniel Farge ,  Pierre Le Roy ,  Claude Moutonnier ,  Jean-Francois Peyronel ,  Bernard Plau

    IPC分类号： A61K31/535 ,  A61P31/04 ,  C07D501/20 ,  C07D501/24 ,  C07D505/00 ,  A61K31/545

    CPC分类号： C07D505/00

    摘要： New cephalosporin derivatives, of the formula: ##STR1## in which R.sub.1 is a heterocyclic, phenyl, p-hydroxyphenyl, phenoxy or dichlorophenylthio radical and R.sub.2 is a hydrogen atom, or R.sub.1 is phenyl or p-hydroxyphenyl and R.sub.2 is an amino radical, R.sub.3 is hydrogen, phenyl, substituted phenyl, alkylthio or substituted amino or a radical of the structure --A--R'.sub.3, which A is --CH.sub.2 --, --NH-- or --NHCO-- and R'.sub.3 is a substituted pyridinio radical, R is a carboxyl radical or a carboxylato radical if R.sub.3 is a --AR'.sub.3 radical and X is a sulphur or oxygen atom, the said alkyl moieties or radicals containing 1 to 4 carbon atoms each in their D, L and D,L forms, where these exist, and their salts are narrow-spectrum anti-bacterial agents which are active against gram-positive bacteria.

    摘要翻译： 新的头孢菌素衍生物，其结构式如下：其中R1是杂环，苯基，对羟基苯基，苯氧基或二氯苯硫基，R2是氢原子，或R1是苯基或对羟基苯基，R2是 氨基，R3是氢，苯基，取代的苯基，烷硫基或取代的氨基或结构-A-R'3的基团，其中A是-CH 2 - ， - NH-或-NHCO-，R'3是取代的 吡啶基，R为羧基或羧基，如果R3为-AR'3基，X为硫或氧原子，则所述烷基部分或含有1至4个碳原子的基团各自为D，L和D L形式，其中存在这些盐，其盐是对革兰氏阳性细菌具有活性的窄谱抗菌剂。

    Oxacephalosporins
    15.
    发明授权
    Oxacephalosporins 失效
    牛蒡子

    公开(公告)号：US4370478A

    公开(公告)日：1983-01-25

    申请号：US323112

    申请日：1981-11-19

    申请人： Daniel Farge ,  Pierre L. Roy ,  Claude Moutonnier ,  Bernard Plau ,  Jean-Francois Peyronel

    发明人： Daniel Farge ,  Pierre L. Roy ,  Claude Moutonnier ,  Bernard Plau ,  Jean-Francois Peyronel

    IPC分类号： A61K31/535 ,  A61P31/04 ,  C07D501/24 ,  C07D505/00 ,  C07D498/04

    CPC分类号： C07D505/00

    摘要： New oxacephalosporins of the general formula: ##STR1## in which either R.sub.1 is hydrogen or a protective radical, R.sub.4 is hydrogen or substituted 2-(2-aminothiazol-4-yl)-acetyl or .alpha.-carboxyarylacetyl, of which the amine and acid groups are free or protected, and R" is hydrogen or methoxy in the 7.alpha.-position, or R.sub.1 is a protective radical, R.sub.4 is a radical which can easily be removed and R" is hydrogen or methoxy in the 7.alpha.-position or hydrogen in the 7.beta.-position, and R.sub.2 is a radical --O SO.sub.2 --R.sub.3 or --O CO--R'.sub.3 (R.sub.3 and R'.sub.3 being substituted or unsubstituted alkyl radicals, or phenyl radicals) or a halogen atom, are useful as intermediates for the preparation of antimicrobial oxacephalosporins.

    摘要翻译： 新的通式为：其中R 1为氢或保护基的式（Ⅰ）的化合物，R4为氢或取代的2-（2-氨基噻唑-4-基） - 乙酰基或α-羧基芳基乙酰基，其中 胺和酸基是游离的或被保护的，并且R“在7α-位中是氢或甲氧基，或者R1是保护基，R4是可以容易地除去的基团，R”是氢或甲氧基， 7个α位或7位β-中的氢，R2是-O-SO 2 -R 3或-OCO-R'3（R3和R'3是取代或未取代的烷基或苯基）或 卤素原子，可用作制备抗微生物头孢菌素的中间体。

    Oxacephalosporins
    16.
    发明授权
    Oxacephalosporins 失效
    牛蒡子

    公开(公告)号：US4369314A

    公开(公告)日：1983-01-18

    申请号：US322951

    申请日：1981-11-19

    申请人： Daniel Farge ,  Pierre L. Roy ,  Claude Moutonnier ,  Bernard Plau ,  Jean-Francois Peyronel

    发明人： Daniel Farge ,  Pierre L. Roy ,  Claude Moutonnier ,  Bernard Plau ,  Jean-Francois Peyronel

    IPC分类号： A61K31/535 ,  A61P31/04 ,  C07D501/24 ,  C07D505/00 ,  C07D498/04

    CPC分类号： C07D505/00

    摘要： New oxacephalosporin derivative of the general formula: ##STR1## in which R.sub.1 is a protective radical, R.sub.2 is either a radical of the general formula: ##STR2## [in which R.sub.5 is hydrogen, alkyl, vinyl, protected carboxyalkyl or a protective radical and R.sub.6 is a protective radical] or an .alpha.-carboxyarylacetyl radical and R" is hydrogen or methoxy in the 7.alpha.-position, or alternatively R.sub.2 is a protective radical and R" is either hydrogen or methoxy in the 7.alpha.-position or hydrogen in the 7.beta.-position, and R.sub.3 and R.sub.4 are optionally substituted alkyl, or phenyl, or form a heterocyclic ring with the nitrogen atom, their E and Z forms and mixtures thereof and also their preparation.These new products are useful as intermediates for the preparation of biologically active oxacephalosporins.

    摘要翻译： （I）其中R1是保护基团的新的类似于以下通式的式（II）的新的类鞘氨醇衍生物：R2是以下通式的基团：其中R 5是氢，烷基，乙烯基，保护基 羧基烷基或保护基，R 6为保护基]或α-羧基芳基乙酰基，R“为7位上的氢或甲氧基，或者R2为保护基，R”为氢或甲氧基 7个β-位中的7个α-位或氢，R3和R4是任选取代的烷基或苯基，或与氮原子，它们的E和Z形式及其混合物形成杂环，以及它们的制备。 这些新产品可用作制备生物活性的羟基头孢菌素的中间体。