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1. 发明公开

EP0484881A2 Heteroaroyl derivatives of monocyclic beta-lactam antibiotics 失效
标题翻译：异ero酰化冯单克隆β-内酰胺抗生素。
公开(公告)号：EP0484881A2
公开(公告)日：1992-05-13
申请号：EP91118838.1
申请日：1991-11-05
申请人： E.R. SQUIBB & SONS, INC.
发明人： Koster, William H. , Sundeen, Joseph E. , Straub, Henner , Ermann, Peter Hans , Treuner, Uwe D.
IPC分类号： C07D417/14 , A61K31/495 , C07D241/44 , C07D491/04 , C07F9/6509 , C07C271/66 , C07C217/86
CPC分类号： C07D241/52 , C07C217/86 , C07C271/66 , C07D241/44 , C07D417/14 , C07D491/04 , C07F9/650994 , Y02P20/55
摘要： Antibacterial activity is exhibited by novel compounds having the formula
摘要翻译：具有式CHEM的新化合物表现出抗菌活性

2. 发明公开

EP0095394A3 2-Oxo-1-(thiophosphonic or thiophosphinic)-azetidines 失效
标题翻译： 2-OXO-1-（硫代磷酸或硫代磷酸） - 淀粉酶
公开(公告)号：EP0095394A3
公开(公告)日：1984-05-16
申请号：EP83400750
申请日：1983-04-15
申请人： E.R. Squibb & Sons, Inc.
发明人： Zahler, Robert , Koster, William H.
IPC分类号： C07F09/65 , A61K31/675
CPC分类号： C07F9/5683
摘要： β-Lactams having the formula
R 2 is hydrogen or methoxy; R 3 and R 4 are the same or different and each is hydrogen, alkyl, substituted alkyl or aryl; R 5 is hydrogen, alkyl, substituted alkyl, or aryl; and R e is hydroxy, alkoxy, (substituted alkyl)oxy, aryloxy, alkyl, substituted alkyl, aryl, amino, substituted amino, alkylthio or arylthio; have antibacterial activity.

3. 发明公开

EP0086556A1 Process for preparing (3S)-3-(((2-amino-4-thiazolyl)((1-carboxy-1-methylethoxy)imino)-acetyl)amino)-2-oxo-1-azetidinesulfonic acid and 4-substituted derivatives 失效
标题翻译：一种的制备方法，（3S）-3 - （（（2-氨基-4-噻唑基） - （（1-羧基-1-甲基乙氧基）亚氨基）乙酰基）氨基）-2-氧代-1-氮杂环丁烷磺酸和 4-取代的衍生物。
公开(公告)号：EP0086556A1
公开(公告)日：1983-08-24
申请号：EP83300191.0
申请日：1983-01-14
申请人： E.R. Squibb & Sons, Inc.
发明人： Cimarusti, Christopher M. , Fox, Rita T. , Fritz, Alan W. , Koster, William H. , Moniot, Jerome L.
IPC分类号： C07D417/12
CPC分类号： C07D277/587 , C07D417/12 , Y02P20/55
摘要： Disclosed herein is a process for preparing a compound having the formula
which comprises coupling a compound having the formula
or a salt thereof, with a compound having the formula
to obtain a compound having the formula
reacting that compound with 2-aminooxy-2-methyl- propanoic acid, or a salt thereof, to obtain a compoung having the formula
and, if R is an amino protecting group, deprotecting that compound to yield the desired product; wherein

R is hydrogen or an amino protecting group;
R 1 is hydrogen, methyl or ethyl;
M⊕ is an inorganic cation or a substituted ammonium ion; and
M 1 ⊕ is hydrogen, an inorganic cation or a substituted ion.

4. 发明公开

EP0484881A3 Heteroaroyl derivatives of monocyclic beta-lactam antibiotics 失效
标题翻译：单克隆抗坏血酸的异恶唑衍生物
公开(公告)号：EP0484881A3
公开(公告)日：1992-10-14
申请号：EP91118838.1
申请日：1991-11-05
申请人： E.R. SQUIBB & SONS, INC.
发明人： Koster, William H. , Sundeen, Joseph E. , Straub, Henner , Ermann, Peter Hans , Treuner, Uwe D.
IPC分类号： C07D417/14 , A61K31/495 , C07D241/44 , C07D491/04 , C07F9/6509 , C07C271/66 , C07C217/86
CPC分类号： C07D241/52 , C07C217/86 , C07C271/66 , C07D241/44 , C07D417/14 , C07D491/04 , C07F9/650994 , Y02P20/55
摘要： Antibacterial activity is exhibited by novel compounds having the formula

5. 发明授权

EP0086556B1 Process for preparing (3S)-3-(((2-amino-4-thiazolyl)((1-carboxy-1-methylethoxy)imino)-acetyl)amino)-2-oxo-1-azetidinesulfonic acid and 4-substituted derivatives 失效
标题翻译：制备（3S）-3 - （（（2-氨基-4-噻唑烷基）（（1-羧甲基-1-甲基乙基）亚氨基） - 乙基）氨基）-2-氧代-1-氮杂卓酸和4-取代的衍生物
公开(公告)号：EP0086556B1
公开(公告)日：1986-05-07
申请号：EP83300191.0
申请日：1983-01-14
申请人： E.R. Squibb & Sons, Inc.
发明人： Cimarusti, Christopher M. , Fox, Rita T. , Fritz, Alan W. , Koster, William H. , Moniot, Jerome L.
IPC分类号： C07D417/12
CPC分类号： C07D277/587 , C07D417/12 , Y02P20/55

6. 发明公开

EP0127177A2 [[(3-Acylamino-2-oxo-1-azetidinyl)oxy]methyl]phosphinic acids 失效
标题翻译： [[（3-酰氨基-2-氧代-1-氮杂环丁烷基）氧基]甲基]-Phosphinsäure。
公开(公告)号：EP0127177A2
公开(公告)日：1984-12-05
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
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
摘要翻译：具有3-酰基氨基取代基的β-内酰胺和1-位具有式CHEM的取代基表现出抗菌活性，其中R 5和R 6相同或不同，各自为氢，烷基，烯基，炔基，苯基，取代的苯基，环烷基或4,5,6或7-元杂环，或R5和R6与它们所连接的碳原子一起为环烷基或4,5,6或7-元杂环，或R5中的一个并且R6是氢，另一个是叠氮基，卤代甲基，二卤代甲基，三卤甲基，烷氧基羰基，烯基，炔基，2-苯基乙烯基，2-苯基乙炔基，羧基，-CH2X1 -S-X2，-O-X2或-A- NX6X7; R 7是氢，烷基，取代的烷基，苯基，取代的苯基，1-（乙氧基羰氧基）乙基，1,3-二氢-3-氧代-1-异苯并呋喃基，其中R min是氢或烷基，R sec是烷基或苯基，R“'是氢，甲基或苯基，并且R iv是氢或与R”'一起是 - （CH 2）3 - 或-CH 2）（取代的烷基） - 氧基，苯氧基，（取代的苯基）氧基，烷基，取代的烷基，苯基，取代的苯基，杂芳基，氨基，取代的氨基，烷硫基，（取代的烷基）取代的苯基）硫基或R sec-O-CH 2 -CH 2 -O。

7. 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

8. 发明公开

EP0132356A1 Process for preparing 2-azetidinones 失效
标题翻译： Verfahren zur Herstellung von 2-Azetidinonen。
公开(公告)号：EP0132356A1
公开(公告)日：1985-01-30
申请号：EP84304834.9
申请日：1984-07-16
申请人： E.R. Squibb & Sons, Inc.
发明人： Koster, William H.
IPC分类号： C07D205/08
CPC分类号： C07D205/085
摘要： A compound having the formula
can be prepared by heating an anion having the formula

or a cation having the formula
with a cation having the formula
摘要翻译：具有式的化合物可以通过用具有式CHEM的阳离子或具有式CHEM e的阳离子加热具有式CHEM的阴离子来制备

9. 发明公开

EP0095394A2 2-Oxo-1-(thiophosphonic or thiophosphinic)-azetidines 失效
标题翻译： 2-氧代-1-（硫代磷酸二硫代磷酸钠） - 氮杂环丁烷。
公开(公告)号：EP0095394A2
公开(公告)日：1983-11-30
申请号：EP83400750.2
申请日：1983-04-15
申请人： E.R. Squibb & Sons, Inc.
发明人： Zahler, Robert , Koster, William H.
IPC分类号： C07F9/65 , A61K31/675
CPC分类号： C07F9/5683
摘要： β-Lactams having the formula

R 2 is hydrogen or methoxy;
R 3 and R 4 are the same or different and each is hydrogen, alkyl, substituted alkyl or aryl;
R 5 is hydrogen, alkyl, substituted alkyl, or aryl; and
R e is hydroxy, alkoxy, (substituted alkyl)oxy, aryloxy, alkyl, substituted alkyl, aryl, amino, substituted amino, alkylthio or arylthio; have antibacterial activity.
摘要翻译：具有式CH 2 R 2的β-内酰胺是氢或甲氧基; R3和R4相同或不同，各自为氢，烷基，取代的烷基或芳基; R5是氢，烷基，取代的烷基或芳基; 并且R 6是羟基，烷氧基，（取代的烷基）氧基，芳氧基，烷基，取代的烷基，芳基，氨基，取代的氨基，烷硫基或芳硫基; 具有抗菌活性。

10. 发明公开

EP0061765A1 Beta-Lactams 失效
标题翻译： β-Laktame。
公开(公告)号：EP0061765A1
公开(公告)日：1982-10-06
申请号：EP82102646.5
申请日：1982-03-29
申请人： E.R. SQUIBB & SONS, INC.
发明人： Koster, William H. , Cimarusti, Christopher M.
IPC分类号： C07F9/65 , A61K31/675
CPC分类号： C07F9/5683
摘要： Antibacterial activity is exhibited by β-lactams having a phosphinic or phosphonic substituent in the 1-position and an acylamino substituent in the 3-position.
摘要翻译：在1-位具有次膦酸或膦酸取代基的β-内酰胺和3-位的酰氨基取代基表现出抗菌活性。

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