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33 条记录 (耗时 0.03 秒)

    Penicillins
    21.
    发明授权
    Penicillins 失效

    公开(公告)号：US3972870A

    公开(公告)日：1976-08-03

    申请号：US502835

    申请日：1974-09-03

    申请人： Hans-Bodo Konig ,  Wilfried Schrock ,  Karl-Georg Metzger

    发明人： Hans-Bodo Konig ,  Wilfried Schrock ,  Karl-Georg Metzger

    IPC分类号： C07D499/00 ,  C07D499/64 ,  C07D499/46

    CPC分类号： C07D499/00

    摘要： Penicillins of the formula ##EQU1## or pharmaceutically acceptable non-toxic salts thereof, wherein C* is a carbon atom constituting a center of chirality;A is a moiety of the formula ##EQU2## or ##EQU3## wherein X is ##EQU4## Y is ##EQU5## or wherein Aryl is an aryl moiety; Z is ##EQU6## Q.sub.1 is ##EQU7## or ##SPC1##Q.sub.2 is ##EQU8## ##SPC2##or ##SPC3##R is straight- chain or branched alkyl of 1 to 5 carbon atoms;R.sub.1 is alkyl of 1 to 10 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, alkenyl of 2 to 10 carbon atoms, cycloalkenyl of 3 to 10 carbon atoms. vinyl, arylvinyl, mono-, di-, or tri-halo-lower alkyl, H.sub.2 N--, R--NH--, (R).sub.2 N--, aryl--NH--, aryl-lower alkylamino, alkoxy of 1 to 8 carbon atoms, aralkoxy of 1 to 8 carbon atoms in the alkoxy portion, cycloalkoxy of 3 to 7 carbon atoms, aryloxy, R--O--V--, R--S--V--, N=C--V--, R--O--CO--V--, H.sub.2 N--CO--V--, R--NH--CO--V--, R--O--CO--NH--, R--SO.sub.2 --NH--, (R).sub.2 N--CO--V--, wherein R is as above defined, ##SPC4## ##SPC5##provided that when X is --SO.sub.2 --, R.sub.1 is not alkoxy, aralkoxy, cycloalkoxy or aryloxy, and further provided that R.sub.1 can also be hydrogen when X is --CO--;V is a divalent organic radical of 1 to 3 carbon atoms;n is 0, 1 or 2;R.sub.2 and R.sub.3 are the same or different and are each hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl of 2 to 8 carbon atoms, vinyl, allyl, propenyl, cycloalkyl of 3 to 6 carbon atoms, cycloalkenyl of 3 to 6 carbon atoms, mono-, di- or tri-halo lower alkyl or aryl;R.sub.4, r.sub.5 and R.sub.6 are the same or different and are each hydrogen, nitro, cyano, (R).sub.2 N--, (R).sub.2 N--CO--, R--CO--NH--, R--O--CO--, R--CO--O--, R--, R--O--, wherein R is as above defined, H.sub.2 N--SO.sub.2 --, chlorine, bromine, iodine, fluorine or trifluoromethyl;G is hydrogen or straight or branched chain alkyl of 1 to 5 carbon atoms; andB is a moiety of the formula ##SPC6##whereinR.sub.7, r.sub.8 and R.sub.9 are the same or different and are each hydrogen, halogen, nitro, hydroxy, R--, R--O--, R--S--, R--SO-- , R--SO.sub.2 --, (R).sub.2 N--, R--CO--NH--, or R--CO--O-- , wherein R is as above defined;the arrow in the divalent linking group .rarw.Q.sub.2 .fwdarw. means that the linkage of two atoms by the free valencies of this group must take place as indicated by the arrow;exhibit activity against both Gram-positive and Gram-negative bacteria.

    Penicillin 1,1-dioxides
    26.
    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。

    .beta.-Lactam antibiotics and their medicinal use
    30.
    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。