Oxo-imidazolidine substituted cephalosporins and antibacterial
compositions and methods of combatting bacteria employing them
    2.
    发明授权
    Oxo-imidazolidine substituted cephalosporins and antibacterial compositions and methods of combatting bacteria employing them 失效
    氧代 - 咪唑烷取代的头孢菌素和抗菌组合物和使用它们的抗菌药物的方法

    公开(公告)号:US4107304A

    公开(公告)日:1978-08-15

    申请号:US590794

    申请日:1975-06-27

    CPC分类号: C07D501/20

    摘要: Cephalosporins of the formula ##STR1## their pharmaceutically-acceptable, nontoxic salts, and hydrates thereof are produced, whereinA is hydrogen; unsubstituted or substituted alkyl; aryl; or R.sub.1 --X--, whereinX is --CO-- or --SO.sub.2 --, andR.sub.1 is hydrogen, unsubstituted or substituted alkyl; aryl; thienyl; furyl; amino; alkylamino; dialkylamino; pyrrolidyl; or piperidyl;Or whenX is --CO--,R.sub.1 can also be alkoxy;B is phenyl, methylphenyl, chlorophenyl, hydroxyphenyl or the moiety ##STR2## E is hydrogen, hydroxyl or acetoxy; and C is a center of chirality.These compounds are particularly useful for their antimicrobial and, particularly, antibacterial effects.

    摘要翻译: 生产下式的头孢菌素:其药学上可接受的无毒盐及其水合物,其中A是氢; 未取代或取代的烷基; 芳基; 或R 1 -X-,其中X是-CO-或-SO 2 - ,并且R 1是氢,未取代或取代的烷基; 芳基; 噻吩基 呋喃 氨基; 烷基氨基; 二烷基氨基; 吡咯烷基 或哌啶基; 或当X为-CO-时,R 1也可为烷氧基; B是苯基,甲基苯基,氯苯基,羟基苯基或部分E是氢,羟基或乙酰氧基; C是手性的中心。

    Cephalosporins and their production
    3.
    发明授权
    Cephalosporins and their production 失效
    头孢菌素及其生产

    公开(公告)号:US4086340A

    公开(公告)日:1978-04-25

    申请号:US685706

    申请日:1976-05-12

    CPC分类号: C07D501/20

    摘要: Cephalosporins of the formula ##STR1## their pharmaceutically-acceptable, nontoxic salts, and hydrates thereof are produced, whereinA is hydrogen; unsubstituted or substituted alkyl; aryl; or R.sub.1 --X--, whereinX is --CO-- or --SO.sub.2 --, andR.sub.1 is hydrogen, unsubstituted or substituted alkyl; aryl; thienyl; furyl; amino; alkylamino; dialkylamino; pyrrolidyl; or piperidyl;Or whenX is --CO--,R.sub.1 can also be alkoxy;B is phenyl, methylphenyl, chlorophenyl, hydroxyphenyl or the moiety ##STR2## E is hydrogen, hydroxyl or acetoxy; and C is a center of chirality.These compounds are particularly useful for their antimicrobial and, particularly, antibacterial effects.

    摘要翻译: 生产下式的头孢菌素:其药学上可接受的无毒盐及其水合物,其中A是氢; 未取代或取代的烷基; 芳基; 或R 1 -X-,其中X是-CO-或-SO 2 - ,并且R 1是氢,未取代或取代的烷基; 芳基; 噻吩基 呋喃 氨基; 烷基氨基; 二烷基氨基; 吡咯烷基 或哌啶基; 或当X为-CO-时,R 1也可为烷氧基; B是苯基,甲基苯基,氯苯基,羟基苯基或部分E是氢,羟基或乙酰氧基; C是手性的中心。

    Penicillins
    6.
    发明授权

    公开(公告)号:US4009272A

    公开(公告)日:1977-02-22

    申请号:US605742

    申请日:1975-08-18

    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
    10.
    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

    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。