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33 条记录 (耗时 0.029 秒)

    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.

    Penicillins and cephalosporins and their production
    7.
    发明授权
    Penicillins and cephalosporins and their production 失效
    青霉素和头孢菌素及其生产

    公开(公告)号：US4081539A

    公开(公告)日：1978-03-28

    申请号：US763728

    申请日：1977-01-31

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

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

    IPC分类号： C07D499/00 ,  A61K31/545

    CPC分类号： C07D499/00

    摘要： .beta.-Lactams of the formula ##STR1## and pharmaceutically acceptable nontoxic salts thereof wherein A is hydrogen or alkyl of 1 to 4 carbon atoms;B is phenyl, methylphenyl, chlorophenyl, hydroxyphenyl or cyclohexa-1,4-dien-1-yl;R is a moiety of the formula ##STR2## wherein E is hydrogen, --OH or --O--CO--CH.sub.3 ; andC* constitutes a center of chirality; are produced which exhibit antibiotic activity.

    摘要翻译： 式“IMAGE”的β-内酰胺及其药学上可接受的无毒盐，其中A为氢或1至4个碳原子的烷基; B是苯基，甲基苯基，氯苯基，羟基苯基或环己-1,4-二烯-1-基; R是下式的部分：其中E是氢，-OH或-O-CO-CH 3; 和C *构成手性中心; 产生具有抗生素活性。

    Penicillins and processes for their preparation and use
    8.
    发明授权
    Penicillins and processes for their preparation and use 失效
    青霉素及其制备和使用的过程

    公开(公告)号：US4031229A

    公开(公告)日：1977-06-21

    申请号：US692930

    申请日：1976-06-04

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

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

    IPC分类号： C07D499/10 ,  C07D233/32 ,  C07D233/38 ,  C07D499/00 ,  C07D499/04 ,  C07D499/64 ,  C07D499/66 ,  C07D499/68 ,  C07D499/70 ,  A61K31/43

    CPC分类号： C07D233/32 ,  C07D233/38 ,  C07D499/00

    摘要： 6-[.alpha.-(Imidazolidin-2-on-1-carbonylamido)acetamido]-penicillanic acids substituted in the 3-position of the imidazolidinone ring with phenyl or a substituted phenyl group and on the .alpha.-carbon atom of the acetamido bridge with a phenyl, thienyl, cyclohexenyl or cyclohexadienyl group, and their salts, are antibacterial agents. The compounds, of which .alpha.-(3-phenylimidazolidin-2-on-1-ylcarbonylamino)benzylpenicillin is a representative example, are prepared by acylation of the corresponding 6-(.alpha.-aminoacetamido)penicillanic acid or a derivative thereof.

    摘要翻译： 在咪唑啉酮环的3位被苯基或取代的苯基取代的6- [α-（咪唑烷-2-酮-1-羰基酰氨基）乙酰氨基] - 青霉烷酸和乙酰氨基桥的α-碳原子上， 苯基，噻吩基，环己烯基或环己二烯基及其盐是抗菌剂。 通过酰化相应的6-（α-氨基乙酰氨基）青霉烷酸或其衍生物，制备其中α-（3-苯基咪唑烷-2-酮-1-基羰基氨基）苄青霉素的代表性实例的化合物。

    Penicillins
    9.
    发明授权
    Penicillins 失效
    青霉素

    公开(公告)号：US3993642A

    公开(公告)日：1976-11-23

    申请号：US538753

    申请日：1975-01-06

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

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

    IPC分类号： C07D499/66 ,  A23K20/195 ,  A61K31/50 ,  A61P31/04 ,  C07D231/08 ,  C07D231/20 ,  C07D499/00 ,  C07D499/12 ,  C07D499/16 ,  C07D499/64 ,  C07D499/68 ,  C07D499/70

    CPC分类号： C07D231/08 ,  C07D231/20 ,  C07D499/00

    摘要： A compound of the formula: ##SPC1##Or a pharmaceutically acceptable nontoxic salt thereof whereinR.sub.1 is hydrogen, straight or branched chain alkyl of 1 to 5 carbon atoms, monoaralkyl of up to 8 carbon atoms, monoaryl, substituted monoaryl, or thienyl;A is a moiety of the formula: ##EQU1## wherein R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are the same or different and each is hydrogen, straight or branched chain alkyl of 1 to 5 carbon atoms, monoaralkyl of up to 8 carbon atoms, monoaryl, substituted monoaryl, or thienyl;B is a moiety of the formula: ##SPC2##WhereinR.sub.8, r.sub.9 and R.sub.10 are the same or different and each is hydrogen, fluorine, chlorine, bromine, iodine, lower alkyl, lower alkoxy, lower alkythio, lower alkylsulphonyl, sulphamyl, nitro, cyano, di(lower alkyl)amino, lower alkanoylamino, lower alkanoyloxy, lower alkylsulphonylamino, trifluoromethyl or hydroxy;E is oxygen or sulphur; andC is a carbon atom constituting a center of chirality, are useful for their antibacterial activity.

    摘要翻译： 下式的化合物：

    Penicillins
    10.
    发明授权
    Penicillins 失效

    公开(公告)号：US3972869A

    公开(公告)日：1976-08-03

    申请号：US502765

    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 ad R.sub.9 are the same or different and are each hydrogen, halogen, nitro, hydroxy, R--, R--0--, 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 .fwdarw.means that the linkage of two atoms by the free valencies of his group must take place as indicated by the arrow; exhibit activity against both Gram-positive and Gram-negative bacteria.