Penicillins
    8.
    发明授权
    Penicillins 失效
    青霉素

    公开(公告)号:US3993770A

    公开(公告)日:1976-11-23

    申请号:US629526

    申请日:1975-11-06

    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 alkylthio, 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: 化学式为:+ q,10或其药学上可接受的非对映盐,其中R1为氢,1至5个碳原子的直链或支链烷基,至多8个碳原子的单烷基,单芳基,取代的单芳基或噻吩基; A是下式的部分:R4R2O || PARALLEL -CCC-,|| R5R3 R3R2O || PARALLEL -CC = NC-,| R4 R6R4R2O R3R2O R2O ||| PARALLEL || PARALLEL | PARALLEL -CCCC-,-C = CC-,-C = NC-,||| R7R5R3 R5R3R2O R4R3R2O OR2O ||| PARALLEL ||| PARALLEL PARALLEL | PARALLEL -CCNC-,-C = CNC-,-CNC-,|| R6R4 OR2R3O平行角度平行+ TR 或-C-C-C-,其中R 2,R 3,R 4,R 5,R 6和R 7相同或不同,各自为氢,1至5个碳原子的直链或支链烷基,至多8个碳原子的直链烷基 原子,单芳基,取代的单芳基或噻吩基; B是下式的部分:

    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

    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

    公开(公告)号:US3972869A

    公开(公告)日:1976-08-03

    申请号:US502765

    申请日:1974-09-03

    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.