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1. 发明授权

US4093722A Sulfonylimidazolidone substituted cephalosporins, antibacterial compositions containing them, and methods of combatting bacteria employing them 失效
标题翻译：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
申请人： Wilfried Schrock , Hans-Bodo Konig , Michael Preiss , Karl Georg Metzger , Michael Walkowiak
发明人： Wilfried Schrock , Hans-Bodo Konig , Michael Preiss , Karl Georg Metzger , Michael Walkowiak
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。

2. 发明授权

US4107304A Oxo-imidazolidine substituted cephalosporins and antibacterial compositions and methods of combatting bacteria employing them 失效
标题翻译：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
申请人： Wilfried Schrock , Hans-Bodo Konig , Michael Preiss , Karl Georg Metzger , Michael Walkowiak
发明人： Wilfried Schrock , Hans-Bodo Konig , Michael Preiss , Karl Georg Metzger , Michael Walkowiak
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。

3. 发明授权

US4086340A Cephalosporins and their production 失效
标题翻译：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
申请人： Wilfried Schrock , Hans-Bodo Konig , Michael Preiss , Karl Georg Metzger , Michael Walkowiak
发明人： Wilfried Schrock , Hans-Bodo Konig , Michael Preiss , Karl Georg Metzger , Michael Walkowiak
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。

4. 发明授权

US3978056A Penicillins 失效
标题翻译：青霉素
公开(公告)号：US3978056A
公开(公告)日：1976-08-31
申请号：US502770
申请日：1974-09-03
申请人： Hans-Bodo Konig , Wilfried Schrock , Karl-Georg Metzger
发明人： Hans-Bodo Konig , Wilfried Schrock , Karl-Georg Metzger
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 imidazolidinylcarbamide 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酰胺或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。

5. 发明授权

US3959258A Ureidoacetamido-penicillins 失效
公开(公告)号：US3959258A
公开(公告)日：1976-05-25
申请号：US425966
申请日：1973-12-19
申请人： Hans-Bodo Konig , Wilfried Schrock , Hans Disselnkotter , Karl Georg Metzger
发明人： Hans-Bodo Konig , Wilfried Schrock , Hans Disselnkotter , Karl Georg Metzger
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.

6. 发明授权

US4009272A Penicillins 失效
公开(公告)号：US4009272A
公开(公告)日：1977-02-22
申请号：US605742
申请日：1975-08-18
申请人： Hans-Bodo Konig , Wilfried Schrock , Karl-Georg Metzger
发明人： Hans-Bodo Konig , Wilfried Schrock , Karl-Georg Metzger
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.

7. 发明授权

US3980792A Ureidoacetamido-penicillins 失效
公开(公告)号：US3980792A
公开(公告)日：1976-09-14
申请号：US568477
申请日：1975-04-16
申请人： Hans-Bodo Konig , Wilfried Schrock , Hans Disselnkotter , Karl Georg Metzger
发明人： Hans-Bodo Konig , Wilfried Schrock , Hans Disselnkotter , Karl Georg Metzger
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.

8. 发明授权

US3974142A Penicillins 失效
标题翻译：青霉素
公开(公告)号：US3974142A
公开(公告)日：1976-08-10
申请号：US502956
申请日：1974-09-03
申请人： Hans-Bodo Konig , Wilfried Schrock , Karl-Georg Metzger
发明人： Hans-Bodo Konig , Wilfried Schrock , Karl-Georg Metzger
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。

9. 发明授权

US3939149A Ureidoacetamido-penicillins 失效
公开(公告)号：US3939149A
公开(公告)日：1976-02-17
申请号：US426188
申请日：1973-12-19
申请人： Hans-Bodo Konig , Wilfried Schrock , Hans Disselnkotter , Karl Georg Metzger
发明人： Hans-Bodo Konig , Wilfried Schrock , Hans Disselnkotter , Karl Georg Metzger
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.

10. 发明授权

US4081539A Penicillins and cephalosporins and their production 失效
标题翻译：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
申请人： Hans-Bodo Konig , Karl Georg Metzger , Wilfried Schrock
发明人： Hans-Bodo Konig , Karl Georg Metzger , Wilfried Schrock
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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