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1. 发明公开

EP0200159A3 3-Acylamino-2-oxo-1-azetidinesulfonic acids 失效
标题翻译： 3-氨基亚氨基-2-氧代-1-氮杂环丙烷酸
公开(公告)号：EP0200159A3
公开(公告)日：1988-09-07
申请号：EP86105653
申请日：1986-04-24
申请人： E.R. Squibb & Sons, Inc.
发明人： Zahler, Robert , Breuer, Hermann , Jacobs, Glenn Anthony
IPC分类号： C07D417/12 , C07D277/40 , C07D205/08 , C07C131/00
CPC分类号： C07D277/587 , C07D417/12 , C07K5/06139
摘要： Antibacterial activity is exhibited by 2-azetidinones activated in the 1-position with an -S0 3 H group and having in the 3-position an acylamino group of the formula

2. 发明授权

EP0068466B1 4-Aryl or heteroaryl thio-2-oxo-1-azetidinesulfonic acid salts and process for their preparation 失效
标题翻译： 4-芳基或杂芳基硫代-2-氧代-1-氮杂环丁烷酸的制备及其制备方法
公开(公告)号：EP0068466B1
公开(公告)日：1987-01-14
申请号：EP82105647.0
申请日：1982-06-25
申请人： E.R. Squibb & Sons, Inc.
发明人： Treuner, Uwe D. , Denzel, Theodor , Breuer, Hermann
IPC分类号： C07D417/14 , C07D403/14 , C07D403/12 , C07D409/12 , C07D413/14 , C07D413/12 , C07D401/12 , C07D205/08 , A61K31/505 , A61K31/495 , A61K31/44
CPC分类号： C07D403/12 , C07D403/14 , C07D409/12 , C07D413/14 , C07D417/14

3. 发明公开

EP0127177A3 [[(3-Acylamino-2-oxo-1-azetidinyl)oxy]methyl]phosphinic acids 失效
标题翻译： ÛÛ（3-乙酰氨基-2-氧代-1-氮杂）氧代甲基 - 磷酸
公开(公告)号：EP0127177A3
公开(公告)日：1985-08-07
申请号：EP84106131
申请日：1984-05-29
申请人： E.R. Squibb & Sons, Inc.
发明人： Koster, William H. , Breuer, Hermann
IPC分类号： C07F09/65 , A61K31/675
CPC分类号： C07F9/5683 , C07D205/085 , C07F9/3211 , C07F9/4006
摘要： Antibacterial activity is exhibited by ß-lactams having a 3-acylamino substituent and in the 1-position a substituent having the formula
wherein
R 5 and R. are the same or different and each is hydrogen, alkyl, alkenyl, alkynyl, phenyl, substituted phenyl, cycloalkyl or a 4, 5, 6 or 7-membered heterocycle, or R 6 and R 6 together with the carbon atom to which they are attached are cycloalkyl or a 4, 5, 6 or 7-membered heterocycle, or one of R 6 and R. is hydrogen and the other is azido, halomethyl, dihalomethyl, trihalomethyl, alkoxycarbonyl, alkenyl, alkynyl, 2-phenylethenyl, 2-phenylethynyl, carboxyl, -CH 2 X 1 , -S-X 2 ,
R 7 is hydrogen, alkyl, substituted alkyl, phenyl, substituted phenyl, 1-(ethoxycarbonyloxy)ethyl, 1,3-dihydro-3-oxo-1-isobenzofuranyl,
wherein R' is hydrogen or alkyl, R" is alkyl or phenyl, R"' is hydrogen, methyl or phenyl, and R iv is hydrogen or together with R"' is
and R. is hydroxy, alkoxy, (substituted alkyl)-oxy, phenyloxy, (substituted phenyl)oxy, alkyl, substituted alkyl, phenyl, substituted phenyl, heteroaryl, amino, substituted amino, alkylthio, (substituted alkyl)thio, phenylthio. (substituted phenyl)thio, or

4. 发明授权

EP0127177B1 [[(3-Acylamino-2-oxo-1-azetidinyl)oxy]methyl]phosphinic acids 失效
标题翻译： ÛÛ（3-乙酰氨基-2-氧代-1-氮杂）氧代 - 甲基 -
公开(公告)号：EP0127177B1
公开(公告)日：1988-12-21
申请号：EP84106131.0
申请日：1984-05-29
申请人： E.R. Squibb & Sons, Inc.
发明人： Koster, William H. , Breuer, Hermann
IPC分类号： C07F9/65 , A61K31/675
CPC分类号： C07F9/5683 , C07D205/085 , C07F9/3211 , C07F9/4006

5. 发明授权

EP0062876B1 2-Oxo-1-(((substituted sulfonyl)amino)carbonyl)azetidines 失效
标题翻译： 2-OXO-1 - （（（取代的磺酰基）氨基）羰基）氨基甲酸酯
公开(公告)号：EP0062876B1
公开(公告)日：1986-09-24
申请号：EP82102908.9
申请日：1982-04-05
申请人： E.R. Squibb & Sons, Inc.
发明人： Breuer, Hermann , Slusarchiyk, William A. , Denzel, Theodor , Treuner, Uwe D.
IPC分类号： C07D205/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D417/12 , C07D417/14 , C07D413/12 , C07D413/14
CPC分类号： C07D231/12 , C07D205/085 , C07D233/56 , C07D249/08

6. 发明公开

EP0062876A1 2-Oxo-1-(((substituted sulfonyl)amino)carbonyl)azetidines 失效
标题翻译： 2-（（（取代的磺酰基）氨基）羰基）氮杂环丁烷。
公开(公告)号：EP0062876A1
公开(公告)日：1982-10-20
申请号：EP82102908.9
申请日：1982-04-05
申请人： E.R. Squibb & Sons, Inc.
发明人： Breuer, Hermann , Slusarchiyk, William A. , Denzel, Theodor , Treuner, Uwe D.
IPC分类号： C07D205/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D417/12 , C07D417/14 , C07D413/12 , C07D413/14
CPC分类号： C07D231/12 , C07D205/085 , C07D233/56 , C07D249/08
摘要： Antibacterial activity is exhibited by β-lactams having a
substituent in the 1-position and an acylamino substituent in the 3-position wherein Z is oxygen or sulfur and R is alkyl, alkenyl, alkynyl, substituted alkyl, phenyl, substituted phenyl, a 5,6 or 7-membered heterocycle (R c ), phenylalkyl. (substituted-phenyl)alkyl, R c -alkyl or-NR,Rb wherein R. and R b are the same or different and each is hydrogen, alkyl, substituted alkyl, phenyl, substituted phenyl, phenylalkyl, (substituted phenyl)alkyl or one of R, and R b is hydrogen, alkyl, phenyl, substituted phenyl, phenylalkyl or (substituted phenyl)alkyl and the other is amino (-NH 2 ), alkanoylamino, arylcarbonylamino, alkoxycarbonylamino, alkylsulfonylamino, alkylamino, dialkylamino, phenylamino, (substituted phenyl)- amino, hydroxy, cyano (-C=N), alkoxy, phenyloxy, (substituted phenyl)oxy, phenylalkoxy, (substituted phenyl)alkoxy, R c as defined, above R c -alkyl, R c -alkoxy, alkylsulfonyl, alkylmethyleneamino, (alkyl-CH=N-), pheny-Imethyleneamino or (substituted phenyl)methyleneamino.
摘要翻译：在1-位具有-n-NH-SO2R取代基的β-内酰胺和3-位的酰氨基取代基，其中Z是氧或硫，R是烷基，烯基，炔基，取代的烷基，苯基，取代的苯基，5,6或7-元杂环（Rc），苯基烷基，（取代的 - 苯基）烷基，R c - 烷基或-NR a R b，其中R a和R b相同或不同，各自为氢，烷基，取代的烷基，苯基，取代的苯基，苯基烷基，（取代的苯基）烷基或Ra和Rb之一是氢，烷基，苯基，取代的苯基，苯基烷基或（取代的苯基）烷基，另一个是氨基（-NH 2），烷酰基氨基，芳基羰基氨基，烷氧基羰基氨基，烷基磺酰基氨基，烷基氨基，二烷基氨基，苯基氨基，（取代的苯基 - 氨基，羟基，氰基（-CIDENTICAL N），烷氧基，苯氧基，（取代的苯基）氧基，苯基烷氧基，（取代的苯基）烷氧基， - 烷基，R C- - 烷氧基，烷基磺酰基，烷基亚甲基氨基，（烷基） CH = N-），苯基亚甲基氨基或（取代的苯基）亚甲基氨基。

7. 发明公开

EP0085291A1 2-Oxo-1-(aminocarbonylaminosulfonylaminocarbonyl)azetidines 失效
标题翻译： 2-氧代-1-（aminocarbonylaminosulfonylaminocarbonyl）氮杂环丁烷
公开(公告)号：EP0085291A1
公开(公告)日：1983-08-10
申请号：EP83100006.2
申请日：1983-01-03
申请人： E.R. Squibb & Sons, Inc.
发明人： Breuer, Hermann , Denzel, Theodor
IPC分类号： C07D205/08 , C07D403/12 , C07D403/14 , C07D413/14 , C07D417/12 , C07D417/14 , A61K31/64
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
and salts thereof, wherein R 1 , R 2 , R 3 , R 4 , R 6 and R 6 represent various organic groups.
摘要翻译：具有下式的化合物及其盐具有抗菌活性，其中R1，R2，R3，R4，R6和R6代表各种有机基团。

8. 发明公开

EP0068466A1 4-Aryl or heteroaryl thio-2-oxo-1-azetidinesulfonic acid salts and process for their preparation 失效
标题翻译： 4-芳基 - 杂芳基 - 硫代-2-氧代-1-氮杂环丁烷磺酸酯和Verfahren zu deren Herstellung。
公开(公告)号：EP0068466A1
公开(公告)日：1983-01-05
申请号：EP82105647.0
申请日：1982-06-25
申请人： E.R. Squibb & Sons, Inc.
发明人： Treuner, Uwe D. , Denzel, Theodor , Breuer, Hermann
IPC分类号： C07D417/14 , C07D403/14 , C07D403/12 , C07D409/12 , C07D413/14 , C07D413/12 , C07D401/12 , C07D205/08 , A61K31/505 , A61K31/495 , A61K31/44
CPC分类号： C07D403/12 , C07D403/14 , C07D409/12 , C07D413/14 , C07D417/14
摘要： Described are 4-aryl or heteroarylthio-2-oxo-1-azetidinesulfonic acid salts having the formula
wherein R is hydrogen or methoxy;

R 1 is acyl;
R 2 is aryl, 1H-tetrazol-5-yl, 1-alkyl-1H-tetrazol-5-yl, 1,3,4-thiadiazol-2-yl, 5-alkyl-1,3,4-thiadiazol-2-yl, 1,2,4-thia- diazol-5-yl, 3-alkyl-1,2,4-thiadiazol-5-yl, 1,3,4-oxadiazol-2-yl, 5-alkyl-1,3,4-oxadiazol-2-yl, 1,2,4-oxadiazol-5-yl, 3-alkyl-1,2,4--oxadiazol-5-yl, 2-pyridinyl, 3-pyridinyl, 4-pyridinyl, 2-pyrimidinyl, benzothiazol-2-yl, 4H-1,2,3-triazol-5-yl, 5-alkyl-4H--1,2,3-triazol-5-yl, 1H-imidazol-2-yl, or 1-alkyl-1H-imidazol--2-yl; and
M⊕ is hydrogen or a cation, with the proviso that if M⊕ is hydrogen the R, group contains a basic function;

having antibacterial activity. Described is also a process for their preparation.
摘要翻译：描述了具有式CHEM的4-芳基或杂芳硫基-2-氧代-1-氮杂环丁烷磺酸盐，其中R是氢或甲氧基; R1是酰基; R2是芳基，1H-四唑-5-基，1-烷基-1H-四唑-5-基，1,3,4-噻二唑-2-基，5-烷基-1,3,4-噻二唑-2-基， 1,2,4-噻二唑-5-基，3-烷基-1,2,4-噻二唑-5-基，1,3,4-恶二唑-2-基，5-烷基-1,3， 4-二唑-2-基，1,2,4-恶二唑-5-基，3-烷基-1,2,4-恶二唑-5-基，2-吡啶基，3-吡啶基，4-吡啶基，2-吡啶基，嘧啶基，苯并噻唑-2-基，4H-1,2,3-三唑-5-基，5-烷基-4H-1,2,3-三唑-5-基，1H-咪唑-2-基或1 烷基-1H-咪唑-2-基; 并且M（+）是氢或阳离子，条件是如果M（+）是氢，则R1基团含有基本的官能团; 具有抗细菌活性。描述的也是它们的制备过程。

9. 发明公开

EP0061763A1 4-Substituted mercapto-2-oxo-1-azetidinesulfonic acid salts and process for their preparation 失效
标题翻译： 4-取代基巯基-2-氧代-1-氮杂环己烷磺酸盐和Verfahren zu ihrer Herstellung。
公开(公告)号：EP0061763A1
公开(公告)日：1982-10-06
申请号：EP82102644.0
申请日：1982-03-29
申请人： E.R. SQUIBB & SONS, INC.
发明人： Treuner, Uwe D. , Denzel, Theodor , Breuer, Hermann , Cimarusti, Christopher M.
IPC分类号： C07D205/08 , C07D403/12 , C07D407/12 , C07D407/14 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14 , A61K31/395
CPC分类号： C07D205/095
摘要： Antibacterial activity is exhibited by β-lactams having a sulfonic acid salt substituent in the 1-position, an acylamino substituent in the 3-position and a substituted mercapto substituent in the 4-position.
摘要翻译：在1-位具有磺酸盐取代基的β-内酰胺，3-位的酰基氨基取代基和4-位的取代的巯基取代基表现出抗菌活性。

10. 发明授权

EP0076758B1 4-Ether derivatives of 2-azetidinone-1-sulfonic acids 失效
标题翻译： 2-氮杂环丁酮-1-磺酸的4-醚衍生物
公开(公告)号：EP0076758B1
公开(公告)日：1987-01-07
申请号：EP82401804.8
申请日：1982-10-04
申请人： E.R. Squibb & Sons, Inc.
发明人： Kronenthal, David R. , Breuer, Hermann
IPC分类号： C07D417/12 , C07D403/12
CPC分类号： C07D403/12 , C07D205/085 , C07D417/12

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