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33 条记录 (耗时 0.042 秒)

    Cephalosporins
    1.
    发明授权
    Cephalosporins 失效
    头孢菌素

    公开(公告)号：US4626535A

    公开(公告)日：1986-12-02

    申请号：US566975

    申请日：1983-12-30

    申请人： Rolf Angerbauer ,  Michael Boberg ,  Gunther Kinast ,  Karl G. Metzger ,  Wilfried Schrock ,  Hans-Joachim Zeiler

    发明人： Rolf Angerbauer ,  Michael Boberg ,  Gunther Kinast ,  Karl G. Metzger ,  Wilfried Schrock ,  Hans-Joachim Zeiler

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D285/08 ,  C07D417/06 ,  C07D501/20 ,  C07D501/34 ,  C07D501/36 ,  C07D501/46 ,  C07D501/59 ,  C07D501/38

    CPC分类号： C07D285/08 ,  C07D417/06

    摘要： Novel antibacterially active cephalosporins of the formula ##STR1## in which R.sup.1 denotes hydrogen, optionally substituted alkyl, a substituted or unsubstituted phenyl ring, a polycyclic aromatic ring or an optionally substituted heterocyclic 5- or 6-member ring having 1-4 heteroatoms,R.sup.2 represents hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkenyl, halogen, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, hydroxymethyl, formyloxymethyl, C.sub.1 -C.sub.4 -alkylcarbonyloxymethyl, aminocarbonyloxymethyl, pyridiniummethyl, 4-carbamoylpyridiniummethyl, 4-sulphonylethylpyridiniummethyl, 4-carboxylmethylpyridiniummethyl or heterocyclylthiomethyl, heterocyclyl representing a radical of the formula ##STR2## wherein R.sup.8 denotes hydrogen, methyl, 2-dimethylaminoethyl, carboxymethyl, sulphomethyl, carboxyethyl or sulphoethyl andR.sup.9 denotes hydrogen or methyl,or pharmaceutically tolerated salts or esters thereof.

    摘要翻译： 式中，R1表示氢，任选取代的烷基，取代或未取代的苯基环，多环芳环或具有1-4个杂原子的任选取代的杂环的5-或6-元环的新型抗菌活性头孢菌素，R2 表示氢，C 1 -C 4 - 烷基，C 1 -C 4 - 烯基，卤素，C 1 -C 4 - 烷氧基，C 1 -C 4 - 烷硫基，羟甲基，甲酰氧基甲基，C 1 -C 4 - 烷基羰氧基甲基，氨基羰基氧基甲基，吡啶鎓甲基，4-氨基甲酰基吡啶鎓甲基，4-磺基乙基吡啶鎓甲基 ，4-羧基甲基吡啶鎓甲基或杂环硫基甲基，代表下式基团的杂环基，其中R8表示氢，甲基，2-二甲基氨基乙基，羧甲基，磺基甲基，羧乙基或磺基，R9表示氢或甲基， 或其药学上可耐受的盐或酯。

    Penicillins
    3.
    发明授权
    Penicillins 失效

    公开(公告)号：US4009272A

    公开(公告)日：1977-02-22

    申请号：US605742

    申请日：1975-08-18

    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 ,  A61K31/505

    CPC分类号： C07D499/00

    摘要： Penicillins of the formula ##STR1## 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 ##STR2## wherein X is ##STR3## Y is ##STR4## WHEREIN Aryl is an aryl moiety; Z is ##STR5## Q.sub.1 is ##STR6## Q.sub.2 is ##STR7## 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, ##STR8## 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 ##STR9## wherein R.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 Q.sub.2 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.This is a division of Ser. No. 502,956, filed Sept. 3, 1974, now U.S. Pat. No. 3,974,142, which in turn is continuation-in-part of our then copending but now abandoned applications Ser. Nos. 299,246 and 300,776, each of which was filed Oct. 20, 1972.