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公开(公告)号：US3972870A
公开(公告)日：1976-08-03
申请号：US502835
申请日：1974-09-03
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.
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公开(公告)号：US3966709A
公开(公告)日：1976-06-29
申请号：US518178
申请日：1974-10-25
IPC分类号： C07D499/66 , A23K20/195 , A61K31/43 , C07D499/00 , C07D499/64 , C07D499/68 , C07D501/18 , C07D501/20 , C07D501/22 , C07D501/34 , C07D499/70
CPC分类号： C07D499/00
摘要： .beta.-Lactams of the formula ##SPC1##And pharmaceutically acceptable nontoxic salts thereof whereinA 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 ##SPC2##WhereinE 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： β-内酰胺和其药学上可接受的非酮性盐，其中A是氢或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; C构成手性中心; 产生具有抗生素活性。
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公开(公告)号：US3936442A
公开(公告)日：1976-02-03
申请号：US426308
申请日：1973-12-19
IPC分类号： A61K31/43 , C07C275/60 , C07D499/64 , C07D499/58
CPC分类号： C07D499/64 , A61K31/43 , C07C275/60 , C07D499/68
摘要： 6-(.alpha.-3-Acyl-ureidoacetamido)-penicillanic acids and pharmaceutically acceptable non-toxic salts thereof in which the hydrogen atom of the nitrogen atom present in the 3-position is substituted, are effective against Gram-positive and Gram-negative infections, particularly Klebsiella aerobacter infections.
摘要翻译： 6-（α-3-酰基 - 脲基乙酰胺基） - 青霉烷酸及其药学上可接受的无毒盐，其中存在于3-位的氮原子的氢原子被取代，对革兰氏阳性和革兰氏阴性有效 感染，特别是克雷伯杆菌感染。
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