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    • 7. 发明授权
    • Penicillins
    • US4009272A
    • 1977-02-22
    • US605742
    • 1975-08-18
    • Hans-Bodo KonigWilfried SchrockKarl-Georg Metzger
    • Hans-Bodo KonigWilfried SchrockKarl-Georg Metzger
    • C07D499/00A61K31/505
    • C07D499/00
    • 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.