公开(公告)号：US3886149A

公开(公告)日：1975-05-27

申请号：US25868672

申请日：1972-06-01

申请人： SQUIBB & SONS INC

发明人： TREUNER UWE D ,  BREUER HERMANN

IPC分类号： C07D499/62 ,  C07D501/20 ,  C07D99/24

CPC分类号： C07D501/20

摘要： Amino substituted dithiocarbonylthioacetylcephalosporins of the general formula
R1 is hydrogen, lower alkyl, aralkyl, aryl or certain heterocyclic groups; R2 and R3 each is hydrogen or lower alkyl; R4 is lower alkyl, aryl or aralkyl; R5 is hydrogen or lower alkyl; R6 is hydrogen, cycloalkyl, lower alkyl; or together R5 and R6 complete certain nitrogen heterocyclics; X is hydrogen, hydroxy, lower alkanoyloxy, aroyloxy, aralkanoyloxy, SR7, OR7, the radical of a nitrogen base, a quaternary ammonium radical, or together X and R represent a bond linking carbon and oxygen in a lactone ring; R7 is lower alkyl; and n is 1, 2, 3 or 4; are useful as antibacterial agents.

WHEREIN R is hydrogen, lower alkyl, aralkyl, tri(lower alkyl)silyl, tri(lower alkyl)stannyl, a salt forming ion or the group

摘要翻译： 氨基取代的二硫代羰基硫代乙酰头孢菌素，通式为WHEREIN R为氢，低级烷基，芳烷基，三（低级烷基）甲硅烷基，三（低级烷基）甲锡烷基，成盐离子或R1为氢，低级烷基，芳烷基，芳基或某些 杂环基; R2和R3各自为氢或低级烷基; R4是低级烷基，芳基或芳烷基; R5是氢或低级烷基; R6为氢，环烷基，低级烷基; 或者R5和R6一起完成某些氮杂环化合物; X是氢，羟基，低级烷酰氧基，芳酰氧基，芳烷酰氧基，SR7，OR7，氮基的基团，季铵基，或一起X和R表示内酯环中碳和氧连接的键; R7是低级烷基; n为1,2,3或4; 作为抗菌剂是有用的。

公开(公告)号：US3926979A

公开(公告)日：1975-12-16

申请号：US46501374

申请日：1974-04-29

申请人： SQUIBB & SONS INC

发明人： TREUNER UWE D ,  BREUER HERMANN

IPC分类号： A61K31/545 ,  C07D501/20 ,  C07D501/28

CPC分类号： C07D501/36 ,  C07D501/20

摘要： R1 is hydrogen, lower alkyl or cyclo-lower alkyl; R2 is a salt forming metal, lower alkyl or cyclo-lower alkyl; R3 is lower alkyl or phenyl-lower alkyl; and X is hydrogen, hydroxy or lower alkanoyloxy, are useful as antibacterial agents.

wherein R is hydrogen, lower alkyl, trimethylsilyl alkali metal or

Dithiocarbonylthio cephalosporin derivatives of the formula

摘要翻译： 式S的二硫羰基硫代头孢菌素衍生物AN-R1-CH ----- CO-NH-CH-CHCH2 ||| SCS-R2 PARALLEL C-NC-CH2-X平行O角SC | C或OR并行O其中R 是氢，低级烷基，三甲基甲硅烷基碱金属或O并原-CH2-OC-R3; R1是氢，低级烷基或环 - 低级烷基; R2是形成盐的金属，低级烷基或环 - 低级烷基; R3是低级烷基或苯基 - 低级烷基; X为氢，羟基或低级烷酰氧基，可用作抗菌剂。

公开(公告)号：US3926983A

公开(公告)日：1975-12-16

申请号：US50190574

申请日：1974-08-30

申请人： SQUIBB & SONS INC

发明人： TREUNER UWE D ,  BREUER HERMANN

IPC分类号： A61K31/545 ,  C07D501/36 ,  C07D501/50

CPC分类号： C07C329/00

摘要： R is lower alkyl, phenyl, or phenyl-lower alkyl; R4 is a fiveor six-membered nitrogen and/or sulfur or oxygen-containing ring system; are useful as antibacterial agents.

wherein R1 is hydrogen, lower alkyl, phenyl or certain heterocyclic groups; R2 is lower alkyl or phenyl-lower alkyl; R3 is hydrogen, lower alkyl, phenyl-lower alkyl, tri(lower alkyl)silyl, tri(lower alkyl)stannyl, a salt forming ion, or

3-Heterothio((alkoxycarbonyl)thioacetyl)cephalosporin derivatives which have the formula

摘要翻译： 3-异硫代[（烷氧基羰基）硫代乙酰基]头孢菌素衍生物，其具有式R1 | R2-O-C-S-CH-CO-NH并行化O，其中R1是氢，低级烷基，苯基或某些杂环基; R2是低级烷基或苯基 - 低级烷基; R3是氢，低级烷基，苯基 - 低级烷基，三（低级烷基）甲硅烷基，三（低级烷基）甲锡烷基，成盐离子或O并原-CH2-O-C-R; R为低级烷基，苯基或苯基 - 低级烷基; R4是五或六元氮和/或硫或含氧环系; 作为抗菌剂是有用的。

公开(公告)号：US3875153A

公开(公告)日：1975-04-01

申请号：US36581673

申请日：1973-05-31

申请人： SQUIBB & SONS INC

发明人： TREUNER UWE D ,  BREUER HERMANN

IPC分类号： C07D501/20 ,  C07D99/24

CPC分类号： C07D501/22 ,  C07D501/26

摘要： New cephalosporin derivatives of the formula

WHEREIN R is hydrogen, lower alkyl, phenyl-lower alkyl, tri(lower alkyl)silyl, alkali metal, alkaline earth metal or amine group or the group

R1 is cyano; R2 is cyano or phenylsulfonyl; R3 is hydrogen, lower alkyl, phenyl or thienyl; R4 is hydrogen or lower alkyl; R5 is lower alkyl, phenyl or phenyl-lower alkyl; and X is hydrogen, hydroxy or lower alkanoyloxy; are useful as antibacterial agents.

摘要翻译： 式WHEREIN R的新型头孢菌素衍生物为氢，低级烷基，苯基 - 低级烷基，三（低级烷基）甲硅烷基，碱金属，碱土金属或胺基，或R1为氰基; R2是氰基或苯基磺酰基; R3是氢，低级烷基，苯基或噻吩基; R4是氢或低级烷基; R5是低级烷基，苯基或苯基 - 低级烷基; X为氢，羟基或低级烷酰氧基; 作为抗菌剂是有用的。

公开(公告)号：US3929778A

公开(公告)日：1975-12-30

申请号：US49559774

申请日：1974-08-08

申请人： SQUIBB & SONS INC

发明人： BREUER HERMANN ,  TREUNER UWE D

IPC分类号： A61K31/545 ,  C07D501/20 ,  C07D501/28

CPC分类号： C07D501/20

摘要： WHEREIN R is hydrogen, lower alkyl, phenyl-lower alkyl, tri(lower alkyl)silyl, a salt forming ion, or the group


((Acylcarbamoyl)thioacetyl)cephalosporin derivatives of the formula
R1 is hydrogen, lower alkyl, phenyl, thienyl or furyl; R2 is lower alkyl, lower alkoxy, phenyl or phenyl-lower alkyl; R3 is hydrogen, hydroxy or lower alkanoyloxy; R4 is lower alkyl, phenyl or phenyl-lower alkyl; and R5 is hydrogen or lower alkyl, are useful as antimicrobial agents.

D R A W I N G

摘要翻译： [（酰基氨基甲酰基）硫代乙酰基]头孢菌素衍生物，式WHEREIN R为氢，低级烷基，苯基 - 低级烷基，三（低级烷基）甲硅烷基，成盐离子或基团R 5 O |平行-CH-O-C-R 4; R 1是氢，低级烷基，苯基，噻吩基或呋喃基; R2是低级烷基，低级烷氧基，苯基或苯基 - 低级烷基; R3是氢，羟基或低级烷酰氧基; R4是低级烷基，苯基或苯基 - 低级烷基; 和R5是氢或低级烷基，可用作抗微生物剂。

公开(公告)号：US3929776A

公开(公告)日：1975-12-30

申请号：US46872774

申请日：1974-05-10

申请人： SQUIBB & SONS INC

发明人： TREUNER UWE D ,  BREUER HERMANN

IPC分类号： A61K31/545 ,  C07D501/36 ,  C07D501/50

CPC分类号： C07D501/36

摘要： R1 is hydrogen, lower alkyl, phenyl, pyridyl, thienyl or furyl; R2 is lower alkyl, R3 is lower alkylthio or a five-membered heterocycle containing only nitogen and carbon or nitrogen, carbon and sulfur in the ring; R4 is lower alkyl, phenyl or phenyl-lower alkyl; are useful as antibacterial agents.

WHEREIN R is hydrogen, lower alkyl, phenyl, phenyl-lower alkyl, tri(lower alkyl)stannyl, tri(lower alkyl)silyl, a salt forming ion or the group

3-Alkylthio- and 3-heterothio derivatives of ((thioalkoxycarbonyl)thioacetyl)cephalosporins having the general formula

摘要翻译： 苯基，苯基，低级烷基，三（低级烷基）甲锡烷基，三（低级烷基）甲硅烷基，三（低级烷基）甲硅烷基，三（低级烷基）甲硅烷基， 成盐离子或基团O并原-CH2-OC-R4; R 1是氢，低级烷基，苯基，吡啶基，噻吩基或呋喃基; R 2是低级烷基，R 3是低级烷硫基或在环中仅含有硝基和碳或氮，碳和硫的五元杂环; R4是低级烷基，苯基或苯基 - 低级烷基; 作为抗菌剂是有用的。

公开(公告)号：US3897423A

公开(公告)日：1975-07-29

申请号：US33780673

申请日：1973-03-05

申请人： SQUIBB & SONS INC

发明人： TREUNER UWE D ,  BREUER HERMANN

IPC分类号： A23K20/195 ,  A61K31/545 ,  C07D501/20 ,  C07F7/22 ,  C07D99/24

CPC分类号： C07D501/20

摘要： Amino substituted acylthio cephalosporins of the general formula

wherein R is hydrogen, lower alkyl, aralkyl, tri(lower alkyl)silyl, tri(lower alkyl)stannyl, a salt forming ion or the group

R1 is hydrogen, lower alkyl, aryl or certain heterocyclic groups; R2 and R3 each is hydrogen, lower alkyl or phenyl R4 is lower alkyl, aryl or aralkyl; R5 is hydrogen or lower alkyl; R6 is hydrogen or lower alkyl; or together R5 and R6 complete certain nitrogen heterocyclics; X is hydrogen, hydroxy, azido, lower alkanoyloxy, lower alkoxy, lower alkylthio, lower alkylthiadiazolythio, the radical of a nitrogen base, or together X and R represent a bond linking carbon and oxygen in a lactone ring; and n is 1, 2 or 3; are useful as antibacterial agents.

摘要翻译： 氨基取代的酰基硫代头孢菌素通式S ANGLE R1-CH ----- CO-NH-CH-CHCH2 | R2|||||R5C-NC-CH2-XSC-（C）-N 角度平行角平行| R660 OR3| C-OR并行O其中R是氢，低级烷基，芳烷基，三（低级烷基）甲硅烷基，三（低级烷基）甲锡烷基，成盐离子或基团O并列-CH2-OC -R4; R1是氢，低级烷基，芳基或某些杂环基; R2和R3各自为氢，低级烷基或苯基R4为低级烷基，芳基或芳烷基; R5是氢或低级烷基; R6是氢或低级烷基; 或者R5和R6一起完成某些氮杂环化合物; X是氢，羟基，叠氮基，低级烷酰氧基，低级烷氧基，低级烷硫基，低级烷基噻二唑硫代，氮碱基，或一起X和R代表连接内酯环中的碳和氧的键; n为1,2或3; 作为抗菌剂是有用的。

公开(公告)号：US3892735A

公开(公告)日：1975-07-01

申请号：US33780573

申请日：1973-03-05

申请人： SQUIBB & SONS INC

发明人： TREUNER UWE D ,  BREUER HERMANN

IPC分类号： A23K20/195 ,  C07C67/00 ,  C07C325/00 ,  C07C333/10 ,  C07D501/20

CPC分类号： C07D501/20

摘要： New cyanodithiocarbamic acid derivatives of cephalosporins of the following general formula, and their salts

WHEREIN R is hydrogen, lower alkyl, aralkyl, tri (lower alkyl)silyl, a salt forming ion or the group

R1 is lower alkyl or phenyl-lower alkyl; R2 is hydrogen, lower alkyl, phenyl (which may be substituted) or certain heterocyclic groups; R3 is lower alkyl, phenyl or phenyl-lower alkyl and X is hydrogen, hydroxy, lower alkanoyloxy, lower alkoxy, lower alkylthio, aroyloxy, aralkanoyloxy, the radical of a nitrogen base, or together X and R represent a bond linking carbon and oxygen in a lactone ring; are useful as antibacterial agents.

摘要翻译： 下列通式的头孢菌素的新型氰基二硫代氨基甲酸衍生物及其盐，其中R为氢，低级烷基，芳烷基，三（低级烷基） - 甲硅烷基，成盐离子或基团R 1为低级烷基或苯基 - 低级烷基; R2是氢，低级烷基，苯基（可被取代）或某些杂环基; R3是低级烷基，苯基或苯基 - 低级烷基，X是氢，羟基，低级烷酰氧基，低级烷氧基，低级烷硫基，芳酰氧基，芳烷酰氧基，氮碱基，或一起X和R表示连接碳和氧的键 在内酯环中 作为抗菌剂是有用的。

公开(公告)号：US3880846A

公开(公告)日：1975-04-29

申请号：US31662372

申请日：1972-12-19

申请人： SQUIBB & SONS INC

发明人： BREUER HERMANN ,  TREUNER UWE D

IPC分类号： C07D499/00 ,  C07D499/04 ,  C07D499/64 ,  C07D499/68 ,  C07D499/70 ,  C07D501/20 ,  C07D99/24 ,  C07D99/16

CPC分类号： C07D499/00

摘要： New vinylaminoacetylpenicillins and vinylaminoacetyl cephalosporins have the formula
A is the 6-aminopenicillanic acid moiety and certain derivatives thereof or the 7-aminocephalosporanic acid moiety and certain derivatives thereof. R1 is -CN or -COR5. R2 is -CN, -COR5, -SO2R6 or -PO(R7)2. R3 is hydrogen, lower alkyl, phenyl, hydroxyphenyl, thienyl, furyl or pyridyl. R5, R6 and R7 each is lower alkoxy or phenyl. These products are useful as antibacterial agents.

摘要翻译： 新的乙烯基氨基乙酰基青霉素和乙烯基氨基乙酰头孢菌素具有式A是6-氨基青霉烷酸部分及其某些衍生物或7-氨基头孢烷酸部分及其某些衍生物。

公开(公告)号：US3926980A

公开(公告)日：1975-12-16

申请号：US47312374

申请日：1974-05-24

申请人： SQUIBB & SONS INC

发明人： TREUNER UWE D ,  BREUER HERMANN

IPC分类号： A61K31/545 ,  C07D501/20 ,  C07D501/34

CPC分类号： C07D501/36 ,  C07D501/20

摘要： Dithiocarbonylthioacetyl cephalosporin derivatives of the formula

WHEREIN R is hydrogen, lower alkyl, trimethylsilyl, alkali metal or

R1 is thienyl; R2 is a salt forming metal, lower alkyl or cyclolower alkyl; R3 is lower alkyl or phenyl-lower alkyl; and X is hydrogen, hydroxy or lower alkanoyloxy, are useful as antibacterial agents.

摘要翻译： 二硫代羰基硫代乙酰基头孢菌素衍生物，式为WHEREIN R为氢，低级烷基，三甲基甲硅烷基，碱金属或O平行-CH 2 -O-C-R 3; R1是噻吩基; R2是形成盐的金属，低级烷基或环 - 低级烷基; R3是低级烷基或苯基 - 低级烷基; X为氢，羟基或低级烷酰氧基，可用作抗菌剂。