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    Penicillin derivatives
    4.
    发明授权
    Penicillin derivatives 失效
    青霉素衍生物

    公开(公告)号：US4235774A

    公开(公告)日：1980-11-25

    申请号：US11347

    申请日：1979-02-12

    申请人： Michael Preiss ,  Hans-Bodo Konig ,  Karl G. Metzger ,  Gunter Schmidt

    发明人： Michael Preiss ,  Hans-Bodo Konig ,  Karl G. Metzger ,  Gunter Schmidt

    IPC分类号： A61K31/43 ,  A61P31/04 ,  C07D499/00 ,  C07D499/64 ,  C07D499/70

    CPC分类号： C07D499/00

    摘要： New penicillin derivatives, or esters or salts thereof, of the formula ##STR1## in which R is H or alkoxy,B is a heterocyclic radical,A is an ethylene, trimethylene or o-phenylene radical,D is --co-- or a direct bond, andZ is a hydrogen atom, an optionally substituted alkyl or alkenyl group, an optionally substituted cycloalkyl, cycloalkenyl or cycloalkadienyl group, an optionally substituted aryl group, an optionally substituted hetercyclyl group or an acyl radical.

    摘要翻译： 新颖的青霉素衍生物或其酯或其盐，其中R为H或烷氧基，B为杂环基，A为乙烯，三亚甲基或邻亚苯基，D为 - 或直接 键，Z是氢原子，任选取代的烷基或烯基，任选取代的环烷基，环烯基或环二烯基，任选取代的芳基，任选取代的杂环基或酰基。

    .beta.-Lactam antibiotics and their medicinal use
    6.
    发明授权
    .beta.-Lactam antibiotics and their medicinal use 失效
    β-内酰胺抗生素及其药用

    公开(公告)号：US4386089A

    公开(公告)日：1983-05-31

    申请号：US276762

    申请日：1981-06-24

    申请人： Hans-Bodo Konig ,  Karl G. Metzger ,  Michael Preiss

    发明人： Hans-Bodo Konig ,  Karl G. Metzger ,  Michael Preiss

    IPC分类号： C07D499/70 ,  A61K31/43 ,  A61P31/04 ,  C07D233/38 ,  C07D277/20 ,  C07D277/48 ,  C07D499/00 ,  C07D499/46 ,  C07D499/64 ,  C07D501/20 ,  C07D501/34 ,  C07D501/36 ,  A61K31/545

    CPC分类号： C07D277/20 ,  C07D233/38 ,  C07D277/48 ,  C07D499/00

    摘要： .beta.-Lactam compounds of the formula ##STR1## in which B denotes an optionally substituted heterocyclic 5-membered or 6-membered ring or an optionally substituted phenyl ring,Z denotes a hydrogen atom or a C.sub.1 to C.sub.4 alkoxy group, ##STR2## Y, E.sub.1 and E.sub.2 independently of one another denote a divalent organic radical andR.sub.1, R.sub.2, R.sub.3 and R.sub.4 independently of one another denote a hydrogen atom or an alkyl, alkenyl, alkinyl, alkadienyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, aryl or heterocyclyl radical, it also being possible for the above-mentioned radicals, with the exception of hydrogen, to be substituted, or an acyl radical,are antibacterial agents with a broad antibacterial spectrum and are useful as agents for promoting growth and for improving feed utilization in animals and as antioxidants.

    摘要翻译： 式（I）的β-内酰胺化合物，其中B表示任选取代的杂环5元或6元环或任选取代的苯环，Z表示氢原子或C1至C4烷氧基， Y，E1和E2彼此独立地表示二价有机基团，R 1，R 2，R 3和R 4彼此独立地表示氢原子或烷基，烯基，炔基，链烯基，环烷基，环烯基 ，环链二烯基，芳基或杂环基，除了氢被取代以外，上述基团也可以是酰基，是具有广谱抗菌谱的抗菌剂，并且可用作促进生长的试剂 并提高动物和抗氧化剂的饲料利用率。

    Beta-lactam antibiotics
    7.
    发明授权
    Beta-lactam antibiotics 失效
    β-内酰胺类抗生素

    公开(公告)号：US4200576A

    公开(公告)日：1980-04-29

    申请号：US862466

    申请日：1977-12-20

    申请人： Peter Feyen ,  Michael Preiss ,  Karl G. Metzger

    发明人： Peter Feyen ,  Michael Preiss ,  Karl G. Metzger

    IPC分类号： C07D499/66 ,  A61K31/415 ,  A61K31/42 ,  A61K31/43 ,  A61K31/435 ,  A61K31/505 ,  A61K31/535 ,  A61K31/545 ,  A61P31/04 ,  C07D233/38 ,  C07D499/00 ,  C07D499/64 ,  C07D499/68 ,  C07D501/20 ,  C07D501/57

    CPC分类号： C07D233/38 ,  C07D499/00 ,  Y02P20/55

    摘要： Antibacterially active and animal feedstuff supplement .beta.-lactam antibiotics of the formula ##STR1## in which R is H or --UR',U is O or S,R' is optionally substituted alkyl, alkenyl, alkinyl, aralkyl, aryl or cycloalkyl,Z is ##STR2## R.sup.1 and R.sup.2 individually are hydrogen or, individually or together with the carbon atom to which they are bonded, are any of various radicals,A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 -- or ##STR3## B is optionally substituted phenyl or is cyclohexenyl or cyclohexadienyl; X is S, O, SO, SO.sub.2 or --CH.sub.2 --; andY is a group of the formula ##STR4## T is hydrogen, alkyl--CO--O--, pyridinium, aminopyridinium, carbamoyloxy, azido, cyano, hydroxyl or optionally substituted --S--phenyl, or is --S--Het, in whichHet is an optionally substituted heterocyclic 5-membered or 6-membered ring; and whereinE is hydrogen, a radical forming, with the carboxyl group to which it is attached, a carboxy ester group, a cation of a salt, or a protective group,or a hydrate thereof. A process is also given for converting R directly from H to UR' employing a base, a halogenating agent and R'UH .

    摘要翻译： 抗菌活性和动物饲料补充式为其中R为H或-UR'的式（I）的β-内酰胺抗生素，U为O或S，R'为任选取代的烷基，烯基，炔基，芳烷基，芳基或 环烷基，Z是R 1和R 2各自独立地是氢，或者与它们所键合的碳原子单独或一起是各种基团中的任何一个，A是-CH 2 -CH 2 - ， - CH 2 -CH 2 -CH 2 - 或 - B是任选取代的苯基或环己烯基或环己二烯基; X是S，O，SO，SO 2或-CH 2 - ; 并且Y是下式的基团：T是氢，烷基-CO-O-，吡啶鎓，氨基吡啶鎓，氨基甲酰氧基，叠氮基，氰基，羟基或任选取代的-S-苯基，或者是-S-Het，其中 Het是任选取代的杂环5元或6元环; 其中E为氢，与其连接的羧基形成的自由基为羧基酯基，盐的阳离子或保护基或其水合物。 还给出了使用碱，卤化剂和R'UH将R直接从H转化为UR'的方法。

    .beta.-Lactam antibiotics
    8.
    发明授权
    .beta.-Lactam antibiotics 失效
    β-内酰胺抗生素

    公开(公告)号：US4251524A

    公开(公告)日：1981-02-17

    申请号：US53655

    申请日：1979-06-29

    申请人： Peter Feyen ,  Michael Preiss ,  Karl G. Metzger

    发明人： Peter Feyen ,  Michael Preiss ,  Karl G. Metzger

    IPC分类号： C07D499/66 ,  A61K31/415 ,  A61K31/42 ,  A61K31/43 ,  A61K31/435 ,  A61K31/505 ,  A61K31/535 ,  A61K31/545 ,  A61P31/04 ,  C07D233/38 ,  C07D499/00 ,  C07D499/64 ,  C07D499/68 ,  C07D501/20 ,  C07D501/57 ,  A61K31/655

    CPC分类号： C07D233/38 ,  C07D499/00 ,  Y02P20/55

    摘要： Antibacterially active and animal feedstuff supplement .beta.-lactam antibiotics of the formula ##STR1## in which R is H or --UR',U is O or S,R' is optionally substituted alkyl, alkenyl, alkinyl, aralkyl, aryl or cycloalkyl, ##STR2## R.sup.1 and R.sup.2 individually are hydrogen or, individually or together with the carbon atom to which they are bonded, are any of various radicals,A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 -- or ##STR3## B is optionally substituted phenyl or is cyclohexenyl or cyclohexadienyl; X is S, O, SO, SO.sub.2 or --CH.sub.2 --; andY is a group of the formula ##STR4## T is hydrogen, alkyl-CO-O-, pyridinium, aminopyridinium, carbamoyloxy, azido, cyano, hydroxyl or optionally substituted -S-phenyl, or is -S-Het,in whichHet is an optionally substituted heterocyclic 5-membered or 6-membered ring;and whereinE is hydrogen, a radical forming, with the carboxyl group to which it is attached, a carboxy ester group, a cation of a salt, or a protective group,or a hydrate thereof. A process is also given for converting R directly from H to UR' employing a base, a halogenating agent and R'UH.

    摘要翻译： 抗菌活性和动物饲料补充式为其中R为H或-UR'的式（I）的β-内酰胺抗生素，U为O或S，R'为任选取代的烷基，烯基，炔基，芳烷基，芳基或 环烷基，R 1和R 2分别是氢或者与它们所键合的碳原子单独或一起是各种基团中的任何一个，A是-CH 2 -CH 2 - ， - CH 2 -CH 2 -CH 2 - 或

    Penicillin 1,1-dioxides
    10.
    发明授权
    Penicillin 1,1-dioxides 失效
    青霉素1,1-二氧化物

    公开(公告)号：US4344955A

    公开(公告)日：1982-08-17

    申请号：US158975

    申请日：1980-06-12

    申请人： Ekkehard Niemers ,  Hans-Bodo Konig ,  Wilfried Schrock ,  Karl G. Metzger

    发明人： Ekkehard Niemers ,  Hans-Bodo Konig ,  Wilfried Schrock ,  Karl G. Metzger

    IPC分类号： A61K31/43 ,  A61P31/04 ,  C07D499/00 ,  C07D499/04 ,  C07D499/44 ,  C07D499/46 ,  C07D499/56 ,  C07D499/60 ,  C07D499/64 ,  C07D499/68 ,  C07D499/70 ,  C07D499/72 ,  C07D499/74 ,  C07D499/76 ,  C07D499/78

    CPC分类号： C07D499/00 ,  A61K31/43

    摘要： Anti-bacterially active penicillin 1,1-dioxides of the formula ##STR1## or a salt thereof, in which R.sub.1 denotes a hydrogen atom or an ester-forming radical,R.sub.2 denotes a hydrogen atom or optionally substituted alkoxy group,R.sub.3 denotes a hydrogen atom, COR.sub.4, SO.sub.2 -alkyl, SO.sub.2 -aryl or an optionally substituted alkyl group, but R.sub.2 and R.sub.3 do not simultaneously denote hydrogen atoms, andR.sub.4 denotes a hydrogen atom or any of many possible organic radicals.The compounds are also inhibitors of .beta.-lactamases so they can be used in conjunction with .beta.-lactamase-susceptible antibiotics. They are useful in fighting bacterial infection, in promoting animal growth and in preserving various materials.

    摘要翻译： 其中R1表示氢原子或成酯基团的式为“IMAGE”或其盐的抗细菌活性青霉素1,1-二氧化物，R 2表示氢原子或任选取代的烷氧基，R 3表示氢 原子，COR 4，SO 2 - 烷基，SO 2 - 芳基或任选取代的烷基，但R 2和R 3不同时表示氢原子，R 4表示氢原子或许多可能的有机基团中的任何一种。 这些化合物也是β-内酰胺酶的抑制剂，因此它们可以与β-内酰胺酶敏感的抗生素联合使用。 它们有助于消灭细菌感染，促进动物生长和保存各种材料。