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1. 发明授权

US4111978A Cyanomethylthioacetylcephalosporin intermediates 失效
标题翻译：氰基甲基硫代乙酰头孢菌素中间体
公开(公告)号：US4111978A
公开(公告)日：1978-09-05
申请号：US829707
申请日：1977-09-01
申请人： Hermann Breuer , Uwe Treuner
发明人： Hermann Breuer , Uwe Treuner
IPC分类号： C07D501/20 , C07C121/16 , C07C121/66
CPC分类号： C07D501/20
摘要： New compounds of the following general formula, and their salts ##STR1## wherein R.sub.1 and R.sub.2 each is hydrogen, lower alkyl, lower alkenyl, phenyl, hydroxyphenyl, chlorophenyl, benzyl, phenethyl, or R.sub.1 and R.sub.2 together complete a cyclopentyl or cyclohexyl group; R.sub.3 is hydrogen, lower alkyl, lower alkenyl, cyclopentyl, cyclohexyl, phenyl, hydroxyphenyl, aminophenyl, chlorophenyl, benzyl, furyl, thienyl, pyrrolidyl or pyridyl; and R.sub.5 is hydrogen or lower alkyl; are intermediates for the production of cephalosporin derivatives.
摘要翻译：下列通式的新化合物及其盐，其中R 1和R 2各自为氢，低级烷基，低级烯基，苯基，羟基苯基，氯苯基，苄基，苯乙基或R 1和R 2一起完成环戊基或环己基; R3是氢，低级烷基，低级烯基，环戊基，环己基，苯基，羟基苯基，氨基苯基，氯苯基，苄基，呋喃基，噻吩基，吡咯烷基或吡啶基。 R5是氢或低级烷基; 是用于生产头孢菌素衍生物的中间体。

2. 发明授权

US4086422A Carbamoylalkylureido cephalosporins 失效
标题翻译：氨基甲酰基烷基脲基头孢菌素
公开(公告)号：US4086422A
公开(公告)日：1978-04-25
申请号：US714420
申请日：1976-08-16
申请人： Hermann Breuer , Uwe Treuner
发明人： Hermann Breuer , Uwe Treuner
IPC分类号： C07D501/20 , C07D501/34 , C07D501/36 , C07D501/38 , C07D501/44
CPC分类号： C07D501/36 , C07D501/20
摘要： Carbamoyalkylureido cephalosporins of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion, or the group ##STR2## R.sub.1 is hydrogen or methoxy; A is straight or branched chain alkylene of 1 to 6 carbons; R.sub.2 and R.sub.3 are independently selected from hydrogen and straight chain alkyl of 1 to 4 carbons, or R.sub.2 is hydrogen and R.sub.3 is branched chain alkyl of 3 or 4 carbons, phenyl, benzyl or phenethyl, or R.sub.2 and R.sub.3 taken together with N atom to which they are attached form ##STR3## R.sub.4 is hydrogen or lower alkyl; R.sub.5 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl, or certain heterocyclic groups; R.sub.6 is hydrogen or lower alkyl; R.sub.7 is lower alkyl; and X is hydrogen, lower alkanoyloxy, ##STR4## or certain heterothio groups; are disclosed. These compounds are useful as antibacterial agents.
摘要翻译：其中R为氢，低级烷基，苯基 - 低级烷基，二苯基 - 低级烷基，三（低级烷基）甲硅烷基，三卤代乙基，成盐离子或基团R1为氢或碳原子数为1的碳原子数1〜8的烷硫基烷基脲基头孢菌素甲氧基 A是1至6个碳的直链或支链亚烷基; R2和R3独立地选自氢和1至4个碳的直链烷基，或者R2是氢，R3是3或4个碳的支链烷基，苯基，苄基或苯乙基，或R2和R3与N原子一起它们是连接的，其中R 4是氢或低级烷基; R5是氢，低级烷基，环烷基，环烯基，环链二烯基，苯基，苯基 - 低级烷基，取代的苯基，取代的苯基 - 低级烷基或某些杂环基; R6是氢或低级烷基; R7是低级烷基; X是氢，低级烷酰氧基，或者某些杂硫基; 被披露。这些化合物可用作抗菌剂。

3. 发明授权

US3944546A Cyanomethylthioacetylcephalosporins 失效
标题翻译：氰基甲基硫代乙酰头孢菌素
公开(公告)号：US3944546A
公开(公告)日：1976-03-16
申请号：US513675
申请日：1974-10-10
申请人： Hermann Breuer , Uwe Treuner
发明人： Hermann Breuer , Uwe Treuner
IPC分类号： C07D501/20
CPC分类号： C07D501/20
摘要： New cyanomethylthioacetylcephalosporins of the following general formula, and their salts ##EQU1## wherein R is hydrogen or a salt forming ion of the group consisting of aluminum, alkali metal, alkaline earth metal, lower alkylamine, phenyl-lower alkylamine, N,N-dibenzylethylenediamine, procaine or lower alkylpiperidine; R.sub.1 and R.sub.2 each is hydrogen, lower alkyl, lower alkenyl, phenyl, hydroxyphenyl, chlorophenyl, benzyl, phenethyl, or R.sub.1 and R.sub.2 together complete a cyclopentyl or cyclohexyl group; R.sub.3 is phenyl, substituted phenyl or thienyl, said phenyl substituents being halogen, lower alkyl, amino or lower alkoxy; and X is hydrogen, lower alkoxy, lower alkylthio or lower alkanoyloxy; are useful as antibacterial agents.
摘要翻译：新的具有下列通式的氰基甲基硫代乙酰头孢菌素及其盐R3OS | PARALLEL ANGLE CH-C-NH-CH-CHCH2 ||||||||C-NC-CH2X R1-C-CN PARALLEL ANGLE |OC || R2| COOR其中R是氢或由铝，碱金属，碱土金属，低级烷基胺，苯基 - 低级烷基胺，N，N-二苄基乙二胺，普鲁卡因或低级烷基哌啶组成的组的成盐离子; R 1和R 2各自为氢，低级烷基，低级烯基，苯基，羟基苯基，氯苯基，苄基，苯乙基或R 1和R 2一起形成环戊基或环己基; R3是苯基，取代的苯基或噻吩基，所述苯基取代基是卤素，低级烷基，氨基或低级烷氧基; X为氢，低级烷氧基，低级烷硫基或低级烷酰氧基; 作为抗菌剂是有用的。

4. 发明授权

US3932397A Cyanomethylthioacetylcephalosporins 失效
标题翻译：氰基甲基硫代乙酰头孢菌素
公开(公告)号：US3932397A
公开(公告)日：1976-01-13
申请号：US513677
申请日：1974-10-10
申请人： Hermann Breuer , Uwe Treuner
发明人： Hermann Breuer , Uwe Treuner
IPC分类号： C07D501/24 , C07D501/28 , C07D501/36
CPC分类号： C07D501/20
摘要： New cyanomethylthioacetylcephalosporins of the following general formula, and their salts ##SPC1##Wherein R is hydrogen or a salt forming ion of the group consisting of aluminum, alkali metal, alkaline earth metal, lower alkylamine, phenyl-lower alkylamine, N,N'-dibenzylethylenediamine, procaine or lower alkylpiperidine; R.sub.1 and R.sub.2 each is hydrogen, lower alkyl, lower alkenyl, phenyl, hydroxyphenyl, chlorophenyl, benzyl, phenethyl, or R.sub.1 and R.sub.2 together complete a cyclopentyl or cyclohexyl group; R.sub.3 is hydrogen, lower alkyl or lower alkenyl; and X is lower alkoxy or lower alkylthio; are useful as antibacterial agents.
摘要翻译：新的具有以下通式的氰甲基硫代乙酰头孢菌素及其盐，其中R为氢或由铝，碱金属，碱土金属，低级烷基胺，苯基 - 低级烷基胺，N，N'-二苄基乙二胺，普鲁卡因或低级烷基哌啶; R 1和R 2各自为氢，低级烷基，低级烯基，苯基，羟基苯基，氯苯基，苄基，苯乙基或R 1和R 2一起形成环戊基或环己基; R3是氢，低级烷基或低级烯基; X为低级烷氧基或低级烷硫基; 作为抗菌剂是有用的。

5. 发明授权

US3932396A Cyanomethylthioacetylcephalosporins 失效
标题翻译：氰基甲基硫代乙酰头孢菌素
公开(公告)号：US3932396A
公开(公告)日：1976-01-13
申请号：US513676
申请日：1974-10-10
申请人： Hermann Breuer , Uwe Treuner
发明人： Hermann Breuer , Uwe Treuner
IPC分类号： C07D501/20 , C07D501/26 , C07D501/36
CPC分类号： C07D501/20
摘要： New cyanomethylthioacetylcephalosporins of the following general formula, and their salts ##SPC1##Wherein R is hydrogen or a salt forming ion of the group consisting of aluminum, alkali metal, alkaline earth metal, lower alkylamine, phenyl-lower alkylamine, N,N'-dibenzylethylenediamine, procaine or lower alkylpiperidine; R.sub.1 and R.sub.2 each is hydrogen, lower alkyl, lower alkenyl, phenyl, hydroxyphenyl, chlorophenyl, benzyl, phenethyl or R.sub.1 and R.sub.2 together complete a cyclopentyl or cyclohexyl group; R.sub.3 is cyclo-lower alkyl, cyclo-lower alkenyl or cyclo-lower alkadienyl; and X is hydrogen, lower alkanoyloxy, lower alkoxy or lower alkylthio.
摘要翻译：新的具有以下通式的氰甲基硫代乙酰头孢菌素及其盐，其中R为氢或由铝，碱金属，碱土金属，低级烷基胺，苯基 - 低级烷基胺，N，N'-二苄基乙二胺，普鲁卡因或低级烷基哌啶; R 1和R 2各自为氢，低级烷基，低级烯基，苯基，羟基苯基，氯苯基，苄基，苯乙基或R 1和R 2一起形成环戊基或环己基; R3是环低级烷基，环低级烯基或环 - 低级亚烷基; X为氢，低级烷酰氧基，低级烷氧基或低级烷硫基。

6. 发明授权

US4670553A 2-oxo-1-(aminocarbonylaminosulfonyl-aminocarbonyl)azetidines 失效
公开(公告)号：US4670553A
公开(公告)日：1987-06-02
申请号：US444771
申请日：1982-11-26
申请人： Hermann Breuer , Theodor Denzel
发明人： Hermann Breuer , Theodor Denzel
IPC分类号： C07D205/085 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D205/08 , A61K31/395 , C07D401/12
CPC分类号： C07D403/12 , C07D205/085 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Antibacterial activity is exhibited by compounds having the formula ##STR1## and salts thereof, wherein R.sub.1 is acyl;R.sub.2 is hydrogen or methoxy;R.sub.3 and R.sub.4 are the same or different and each is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl or a 5,6 or 7-membered heterocycle or one of R.sub.3 and R.sub.4 is hydrogen and the other is azido, halomethyl, dihalomethyl, trihalomethyl, alkoxycarbonyl, 2-phenylethenyl, 2-phenylethynyl, carboxyl, ##STR2## X.sub.1 is azido, amino, hydroxy, alkanoylamino, alkylsulfonyloxy, arylsulfonyloxy, aryl, cyano, --S--X.sub.2 or --O--X.sub.2 ;X.sub.2 is alkyl, substituted alkyl, aryl, arylalkyl, alkanoyl, substituted alkanoyl, arylcarbonyl or heteroarylcarbonyl;one of X.sub.3 and X.sub.4 is hydrogen and the other is hydrogen or alkyl, or X.sub.3 and X.sub.4 when taken together with the carbon atom to which they are attached from a cycloalkyl group;X.sub.5 is formyl, alkanoyl, arylcarbonyl, arylalkylcarbonyl, carboxyl, alkoxycarbonyl, aminocarbonyl, (substituted amino)carbonyl, or cyano;A is --CH.dbd.CH--, --CH.sub.2 --CH.dbd.CH--, --(CH.sub.2)--.sub.m, --(CH.sub.2).sub.m' --O--, --(CH.sub.2).sub.m' --NH--, --(CH.sub.2).sub.m' --S--CH.sub.2 --, or --(CH.sub.2).sub.m --O--CH.sub.2 --;m is 0, 1, 2 or 3;m' is 1 or 2;X.sub.6 and X.sub.7 are the same or different and each is hydrogen or alkyl, or X.sub.6 is hydrogen and X.sub.7 is amino, substituted amino, acylamino or alkoxy;R.sub.5 is hydrogen, alkyl or aryl;R.sub.6 is hydrogen, alkyl, aryl, a 5,6 or 7-membered heterocycle, --NR.sub.7 R.sub.8, or --(CH.sub.2).sub.n --X wherein n is 1,2,3 or 4 and X is halogen, aryl, alkoxy, aryloxy or --NR.sub.9 R.sub.10 ;R.sub.7 and R.sub.8 are the same or different and each is hydrogen, alkyl or aryl, or R.sub.7 is hydrogen and R.sub.8 is a 5,6 or 7-membered heterocycle or --(CH.sub.2).sub.n --Y wherein n is 1,2,3 or 4 and Y is alkoxy, amino, alkylthio or halogen; andR.sub.9 and R.sub.10 are the same or different and each is hydrogen or alkyl, or R.sub.9 is hydrogen and R.sub.10 is a 5,6 or 7-membered heterocycle.

7. 发明授权

US4499016A 2-Oxo-1-[(acylamino)sulfonyl]azetidines 失效
标题翻译： 2-氧代-1 - [（酰氨基）磺酰基]氮杂环丁烷
公开(公告)号：US4499016A
公开(公告)日：1985-02-12
申请号：US290648
申请日：1981-08-06
申请人： Hermann Breuer , Theodor Denzel , Uwe D. Treuner
发明人： Hermann Breuer , Theodor Denzel , Uwe D. Treuner
IPC分类号： C07D205/08 , A61K31/397 , A61K31/425 , A61K31/505 , A61P31/04 , C07D205/085 , C07D403/12 , C07D417/12 , C07F7/10 , A61K31/395
CPC分类号： C07D403/12 , C07D205/085 , C07D417/12 , C07F7/10
摘要： Antibacterial activity is exhibited by .beta.-lactams having an --SO.sub.2 --NH--C--R substituent in the 1-position and an acylamino substituent in the 3-position wherein R is alkyl, phenyl, substituted phenyl, phenylalkyl, (substituted phenyl)alkyl, alkoxy, phenyloxy, (substituted phenyl)oxy, phenylalkoxy, or (substituted phenyl)alkoxy.
摘要翻译：在1-位上具有-SO2-NH-CR取代基的β-内酰胺和3-位的酰氨基取代基，其中R是烷基，苯基，取代的苯基，苯基烷基，（取代的苯基）烷基，烷氧基，苯氧基，（取代苯基）氧基，苯基烷氧基或（取代的苯基）烷氧基。

8. 发明授权

US4217348A Cephalosporins having an oxazolidonyloxamido substituted acyl sidechain 失效
标题翻译：头孢菌素具有恶唑烷二硫酰氨基取代的酰基侧链
公开(公告)号：US4217348A
公开(公告)日：1980-08-12
申请号：US946479
申请日：1978-09-28
申请人： Uwe D. Treuner , Hermann Breuer
发明人： Uwe D. Treuner , Hermann Breuer
IPC分类号： C07D263/26 , C07D501/20 , A61K31/545 , C07D501/34 , C07D501/36 , C07D501/46
CPC分类号： C07D263/26
摘要： Cephalosporins of the formula ##STR1## wherein R is hydrogen, sodium, potassium, or certain ester groups; R.sub.1 is in the .alpha.-configuration and is hydrogen or methoxy; R.sub.2 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, substituted or unsubstituted phenyl, benzyl, phenethyl, thienyl, furyl, or pyridyl, or 2-amino-4-thiazolyl; X is --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, ##STR2## R.sub.3 is hydrogen, ##STR3## --O--lower alkyl, or certain substituted or unsubstituted heterothio groups; are disclosed. These compounds possess useful antibacterial activity.
摘要翻译：其中R是氢，钠，钾或某些酯基团的式“IMAGE”的头孢菌素; R1为α构型，为氢或甲氧基; R2是氢，低级烷基，环烷基，环烯基，环烷二烯基，取代或未取代的苯基，苄基，苯乙基，噻吩基，呋喃基或吡啶基，或2-氨基-4-噻唑基; X是-CH 2 - ， - CH 2 -CH 2 - ， - R 3是氢， - 低级烷基或某些取代或未取代的杂硫基; 被披露。这些化合物具有有效的抗菌活性。

9. 发明授权

US4128724A Hydrazinocarbonylamino cephalosporins 失效
标题翻译：肼基氨基头孢菌素
公开(公告)号：US4128724A
公开(公告)日：1978-12-05
申请号：US868781
申请日：1978-01-12
申请人： Hermann Breuer , Uwe D. Treuner
发明人： Hermann Breuer , Uwe D. Treuner
IPC分类号： C07D333/24 , C07D501/20 , C07D501/36 , C07D501/32 , C07D501/56
CPC分类号： C07D333/24
摘要： New .alpha.-hydrazinocarbonylamino cephalosporins which have the formula ##STR1## are useful as antimicrobial agents.
摘要翻译：具有式“IMAGE”的新的α-肼基羰基氨基头孢菌素可用作抗微生物剂。

10. 发明授权

US4096329A 7-Cyanoalkylureido 3 heterocylic thio methyl cephalosporins 失效
标题翻译： 7-氰基烷基脲基3杂环硫代甲基头孢菌素
公开(公告)号：US4096329A
公开(公告)日：1978-06-20
申请号：US765037
申请日：1977-02-02
申请人： Hermann Breuer , Uwe D. Treuner
发明人： Hermann Breuer , Uwe D. Treuner
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D333/24 , C07D501/20 , C07D501/36
CPC分类号： C07D333/24
摘要： Cyanoalkylureido cephalosporins of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion, or the group ##STR2## R.sub.1 is hydrogen or methoxy; A is straight or branched chain alkylene or ##STR3## R.sub.2 is phenyl, 2-thienyl, or 3-thienyl; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl, or certain heterocyclic groups; R.sub.5 is hydrogen or lower alkyl; R.sub.6 is lower alkyl; and X is hydrogen, lower alkanoyloxy, ##STR4## or certain heterothio groups; are disclosed. These compounds are useful as antibacterial agents.
摘要翻译：其中R是氢，低级烷基，苯基 - 低级烷基，二苯基 - 低级烷基，三（低级烷基）甲硅烷基，三卤代乙基，形成成盐离子或基团R 1的氰基烷基脲基头孢菌素是氢或甲氧基 A是直链或支链亚烷基或者R 2是苯基，2-噻吩基或3-噻吩基; R3是氢或低级烷基; R4是氢，低级烷基，环烷基，环烯基，环链二烯基，苯基，苯基 - 低级烷基，取代的苯基，取代的苯基 - 低级烷基或某些杂环基; R5是氢或低级烷基; R6是低级烷基; X是氢，低级烷酰氧基，或者某些杂硫基; 被披露。这些化合物可用作抗菌剂。

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