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1.发明授权Sulfonylimidazolidone substituted cephalosporins, antibacterial compositions containing them, and methods of combatting bacteria employing them 失效磺酰基咪唑烷酮取代的头孢菌素，含有它们的抗菌组合物，以及使用它们的抗菌药物的方法
公开(公告)号：US4093722A
公开(公告)日：1978-06-06
申请号：US686103
申请日：1976-05-13
IPC分类号： A61K31/545 , C07D501/20 , C07D501/24 , C07D501/34
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。
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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
IPC分类号： A61K31/545 , C07D501/20 , C07D501/24 , C07D501/34
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。
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公开(公告)号：US4086340A
公开(公告)日：1978-04-25
申请号：US685706
申请日：1976-05-12
IPC分类号： A61K31/545 , C07D501/20 , C07D501/24 , C07D501/34
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。
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公开(公告)号：US3980792A
公开(公告)日：1976-09-14
申请号：US568477
申请日：1975-04-16
IPC分类号： A61K31/43 , C07C275/60
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.
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公开(公告)号：US3939149A
公开(公告)日：1976-02-17
申请号：US426188
申请日：1973-12-19
IPC分类号： A61K31/43 , C07C275/60 , C07D499/64 , C07D499/46
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.
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公开(公告)号：US3983105A
公开(公告)日：1976-09-28
申请号：US502662
申请日：1974-09-03
IPC分类号： C07D233/38 , C07D275/02 , C07D333/34 , C07D499/00 , C07D499/64 , C07D499/46
CPC分类号： C07D275/02 , C07D233/38 , C07D333/34 , C07D499/00
摘要： Arylmethyl- and cyclohexenylmethyl- penicillins, substituted on the .alpha.-carbon atom of the side chain by a 2,3-disubstituted imidazolidinylcarbamido or a 2,3-disubstituted imidazolidinylthiocarbamido group, or by the corresponding 2,3-disubstituted 1,3-diazacyclohexylcarbamido or thiocarbamido groups are anti-bacterial agents.
摘要翻译： 通过2,3-二取代的咪唑烷基氨基甲酰基或2,3-二取代的咪唑烷基硫代氨基甲酰基取代在侧链的α-碳原子上的芳基甲基和环己烯基甲基 - 青霉素，或通过相应的2,3-二取代的1,3-二氮杂环己基氨基甲酰基 或硫代氨基甲酰基是抗菌剂。
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公开(公告)号：US3959258A
公开(公告)日：1976-05-25
申请号：US425966
申请日：1973-12-19
IPC分类号： A61K31/43 , C07C275/60 , C07D233/38 , C07D261/18 , C07D307/68 , C07D333/24 , C07D333/38 , C07D499/68 , C07F7/08
CPC分类号： C07D499/64 , A61K31/43 , C07C275/60 , C07D233/38 , C07D261/18 , C07D307/68 , C07D333/24 , C07D333/38 , C07D499/68 , C07F7/08
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.
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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。
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公开(公告)号：US4031229A
公开(公告)日：1977-06-21
申请号：US692930
申请日：1976-06-04
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。
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10.发明授权Oxoimidazolidinylthiocarbonyl derivatives of ceph-3-em-4-carboxylic acids 失效ceph-3-em-4-羧酸的氧杂咪唑烷基硫代羰基衍生物
公开(公告)号：US4071683A
公开(公告)日：1978-01-31
申请号：US643542
申请日：1975-12-22
IPC分类号： C07D499/00 , C07D499/64 , C07D501/20 , C07D501/22
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; C构成手性中心; 生产出抗生素活性。
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