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1. 发明授权

US4587047A 2-oxo-1-[[(substituted sulfonyl)amino]-carbonyl]azetidines 失效
标题翻译： 2-氧代-1 - [[（取代的磺酰基）氨基]羰基]氮杂环丁烷
公开(公告)号：US4587047A
公开(公告)日：1986-05-06
申请号：US364352
申请日：1982-04-01
申请人： Hermann Breuer , William A. Slusarchyk , Theodor Denzel , Uwe D. Treuner
发明人： Hermann Breuer , William A. Slusarchyk , Theodor Denzel , Uwe D. Treuner
IPC分类号： C07D205/085 , C07D521/00 , C07D205/08 , A61K31/395 , C07D401/12 , C07D403/12
CPC分类号： C07D231/12 , C07D205/085 , C07D233/56 , C07D249/08
摘要： Antibacterial activity is exhibited by .beta.-lactams having a ##STR1## 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.sub.c), phenylalkyl, (substituted phenyl)alkyl, R.sub.c -alkyl or --NR.sub.a R.sub.b wherein R.sub.a and R.sub.b are the same or different and each is hydrogen, alkyl, substituted alkyl, phenyl, substituted phenyl, phenylalkyl, or (substituted phenyl)alkyl or one of R.sub.a and R.sub.b is hydrogen, alkyl, phenyl, substituted phenyl, phenylalkyl or (substituted phenyl)alkyl and the other is amino, alkanoylamino, arylcarbonylamino, alkoxycarbonylamino, alkylsulfonylamino, alkylamino, dialkylamino, phenylamino, (substituted phenyl)amino, hydroxy, cyano, alkoxy, phenyloxy, (substituted phenyl)oxy, phenylalkoxy, (substituted phenyl)alkoxy, R.sub.c, R.sub.c -alkyl, R.sub.c -alkoxy, alkylsulfonyl, alkylmethyleneamino, phenylmethyleneamino or (substituted phenyl)methyleneamino.
摘要翻译：在1-位具有取代基的β-内酰胺和3-位上的酰氨基取代基，其中Z是氧或硫，R是烷基，烯基，炔基，取代的烷基，苯基，被取代的抗菌活性表现出抗菌活性苯基，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，苯基烷基或（取代的苯基）烷基或Ra和Rb中的一个是氢，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，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，（取代苯基）氨基，羟基，氰基，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，Rc，Rc-烷基，Rc-烷氧基，烷基磺酰基，烷基亚甲基氨基，苯基亚甲基氨基或苯基）亚乙基氨基。

2. 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。

3. 发明授权

US4734496A 4-amino derivatives of 2-oxo-1-azetidinesulfonic acid salts 失效
标题翻译： 2-氧代-1-氮杂二磺酸盐的4-氨基衍生物
公开(公告)号：US4734496A
公开(公告)日：1988-03-29
申请号：US268305
申请日：1981-05-29
申请人： Uwe D. Treuner , Theodor Denzel , Hermann Breuer
发明人： Uwe D. Treuner , Theodor Denzel , Hermann Breuer
IPC分类号： C07D403/04 , C07D403/14 , C07D405/14 , C07D409/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D205/08 , C07D403/12
CPC分类号： C07D403/04 , C07D403/14 , C07D405/14 , C07D409/12 , C07D417/12 , C07D417/14 , C07D471/04
摘要： .beta.-Lactams having a sulfonic acid salt substituent in the 1-position, an acylamino substituent in the 3-position and an --NR.sub.2 R.sub.3 substituent in the 4-position wherein R.sub.2 and R.sub.3 are the same or different and each is ##STR1## or R.sub.2 and R.sub.3 together with the nitrogen atom to which they are attached are ##STR2## R.sub.4 is alkyl, aryl or arylalkyl; and R.sub.5 and R.sub.6 are the same or different and each is hydrogen, halogen, alkyl, alkoxy, alkylthio, alkoxycarbonyl, carboxyl or a carboxyl salt; have antibacterial activity.
摘要翻译：在1-位具有磺酸盐取代基的β-内酰胺，3-位的酰氨基取代基和4-位的-NR2R3取代基，其中R2和R3相同或不同，并且各自为或和R 3与它们所连接的氮原子一起是R 4是烷基，芳基或芳基烷基; R 5和R 6相同或不同，各自为氢，卤素，烷基，烷氧基，烷硫基，烷氧基羰基，羧基或羧基盐; 具有抗菌活性。

4. 发明授权

US4461767A Iminothiazolyl ureido cephalosporins 失效
标题翻译：亚氨基噻唑基脲基头孢菌素
公开(公告)号：US4461767A
公开(公告)日：1984-07-24
申请号：US46068
申请日：1979-06-06
申请人： Hermann Breuer , Uwe D. Treuner , Theodor Denzel
发明人： Hermann Breuer , Uwe D. Treuner , Theodor Denzel
IPC分类号： C07D277/20 , C07D501/36 , A61K31/545 , C07D501/56
CPC分类号： C07D277/20
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, ##STR2## R.sub.4 is hydrogen or lower alkyl; R.sub.5 is hydrogen, lower alkyl, ##STR3## or --(CH.sub.2).sub.n --N--(lower alkyl).sub.2 ; R.sub.6 is hydrogen, sodium, or potassium; n is an integer from 1 to 4; are disclosed. These compounds are useful as anti-bacterial agents.
摘要翻译：其中R为氢，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，R4是氢或低级烷基; R4是氢或低级烷基; R5是氢，低级烷基，或者 - （CH2）n-N-（低级烷基）2; R6是氢，钠或钾; n是1至4的整数; 被披露。这些化合物可用作抗细菌剂。

5. 发明授权

US4501743A Iminothiazolyl ureido cephalosporins 失效
标题翻译：亚氨基噻唑基脲基头孢菌素
公开(公告)号：US4501743A
公开(公告)日：1985-02-26
申请号：US588831
申请日：1984-03-12
申请人： Hermann Breuer , Uwe D. Treuner , Theodor Denzel
发明人： Hermann Breuer , Uwe D. Treuner , Theodor Denzel
IPC分类号： C07D277/20 , A61K31/545
CPC分类号： C07D277/20
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, ##STR2## X is hydrogen, ##STR3## R.sub.4 is hydrogen or lower alkyl; R.sub.5 is hydrogen, lower alkyl, ##STR4## --(CH.sub.2).sub.n --N--(lower alkyl).sub.2 ; R.sub.6 is hydrogen, sodium, or potassium; n is an integer from 1 to 4; are disclosed. These compounds are useful as anti-bacterial agents.
摘要翻译：其中R为氢，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，X是氢，R4是氢或低级烷基; R5是氢，低级烷基， - （CH2）n-N-（低级烷基）2; R6是氢，钠或钾; n是1至4的整数; 被披露。这些化合物可用作抗细菌剂。

6. 发明授权

US4801705A 2-oxo-1-(((substituted sulfonyl)amino)-carbonyl)azetidines 失效
标题翻译： 2-氧代-1 - （（（取代的磺酰基）氨基） - 羰基）氮杂环丁烷
公开(公告)号：US4801705A
公开(公告)日：1989-01-31
申请号：US877599
申请日：1986-06-23
申请人： Hermann Breuer , Jakob-Matthias Drossard , Peter H. Ermann , Henner Straub , Uwe D. Treuner
发明人： Hermann Breuer , Jakob-Matthias Drossard , Peter H. Ermann , Henner Straub , Uwe D. Treuner
IPC分类号： A61K31/395 , A61K31/397 , A61K31/495 , A61P31/04 , C07D205/08 , C07D205/085 , C07D403/12 , C07D417/12 , C07D417/14 , A61K31/415
CPC分类号： C07D417/12 , C07D417/14
摘要： Antibacterial activity is exhibited by .beta.-lactams having a 3-acylamino substituent and having in the 1-position an activating group of the formula ##STR1## wherein R is

7. 发明授权

US4762922A 2-oxo-1-[[(substituted sulfonyl)amino]-carbonyl]azetidines 失效
标题翻译： 2-氧代-1 - [[（取代的磺酰基）氨基]羰基]氮杂环丁烷
公开(公告)号：US4762922A
公开(公告)日：1988-08-09
申请号：US70286
申请日：1987-07-01
申请人： Hermann Breuer , Uwe D. Treuner
发明人： Hermann Breuer , Uwe D. Treuner
IPC分类号： C07D401/14 , A61K31/44 , A61K31/4427 , A61P31/04 , C07D401/12 , C07D417/14 , A61K31/395 , A61K31/425
CPC分类号： C07D401/12 , C07D417/14
摘要： Antibacterial activity is exhibited by 2-azetidinones having a 3-acylamino substituent and having an activating group in the 1-position of the formula ##STR1## wherein R is ##STR2## A.sub.1 is --NH-- or ##STR3## A.sub.2 is ##STR4## or --CH.dbd.CH--.
摘要翻译：具有3-酰基氨基取代基的2-氮杂环丁酮和具有式Ia的1位的具有活化基团的抗菌活性表现为其中R为“IMA”或“IMA”> A1为-NH-或 A2 是 + TR 或-CH = CH-。

8. 发明授权

US4127716A 3-HETEROTHIOMETHYL UREIDO CEPHALOSPORINS 失效
标题翻译： 3-HETEROTHOMETHYL UREIDO CEPHALOSPORINS
公开(公告)号：US4127716A
公开(公告)日：1978-11-28
申请号：US764134
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： C07D307/54 , C07D333/24 , C07D501/36 , C07D501/56 , A61K31/545 , C07D501/54
CPC分类号： C07D333/24 , C07D307/54
摘要： L-Isomer compounds of the formula ##STR1## wherein R.sub.1 is phenyl, thienyl or furyl; R.sub.4 represents certain heterocyclic groups; R.sub.3 is hydrogen, lower alkyl, phenyl-lower alkyl, substituted phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)stannyl, tri(lower alkyl)silyl, a salt forming ion, or the group ##STR2## wherein R is lower alkyl, phenyl, phenyl-lower alkyl, or substituted phenyl and phenyl-lower alkyl are disclosed. These compounds are useful as antibacterial agents.
摘要翻译：其中R1是苯基，噻吩基或呋喃基的式（Ⅰ）的L-异构体化合物; R4表示某些杂环基; R3是氢，低级烷基，苯基 - 低级烷基，取代的苯基 - 低级烷基，二苯基 - 低级烷基，三（低级烷基）甲锡烷基，三（低级烷基）甲硅烷基，成盐离子或基团，其中R 是低级烷基，苯基，苯基 - 低级烷基或取代的苯基和苯基 - 低级烷基。这些化合物可用作抗菌剂。

9. 发明授权

US4100345A 3-(Carbamoyl)pyridino derivatives of 7a-methoxy ureidocephalosporins 失效
标题翻译： 7-甲氧基脲基头孢菌素的3-（氨基甲酰基）吡啶衍生物
公开(公告)号：US4100345A
公开(公告)日：1978-07-11
申请号：US761914
申请日：1977-01-24
申请人： Hermann Breuer , Uwe D. Treuner
发明人： Hermann Breuer , Uwe D. Treuner
IPC分类号： C07D333/24 , C07D501/38 , C07D501/44 , C07D501/40
CPC分类号： C07D333/24
摘要： Ureido cephalosporin derivatives of the formula ##STR1## wherein R.sub.1 is hydrogen or methoxy; R.sub.2 is hydrogen or lower alkyl; R.sub.3 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl; or certain heterocyclic groups; are disclosed. These compounds are useful as antibacterial agents.
摘要翻译：其中R1是氢或甲氧基的式“IMAGE”的脲基头孢菌素衍生物; R2是氢或低级烷基; R3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; 或某些杂环基团; 被披露。这些化合物可用作抗菌剂。

10. 发明授权

US4093801A [[[(2,4-Dioxo-1-imidazolidinyl)amino]carbonyl]amino]-acetylcephalosporin derivatives 失效
标题翻译： {8 {8（2,4-二氧代-1-咪唑啉基）氨基{9羰基{9氨基{9-乙酰头孢菌素衍生物
公开(公告)号：US4093801A
公开(公告)日：1978-06-06
申请号：US819648
申请日：1977-07-27
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 , C07D233/80 , C07D333/24 , C07D501/20 , C07D501/36 , C07D501/34 , C07D501/46
CPC分类号： C07D333/24 , C07D233/80
摘要： [[[(2,4-Dioxo-1-imidazolidinyl)amino]carbonyl]amino]-acetylcephalosporin derivatives having 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; R.sub.2, R.sub.3 and R.sub.5 each is hydrogen or lower alkyl; R.sub.4 is hydrogen, lower alkyl, cyclo-lower alkyl, cyclo-lower alkenyl, cyclo-lower alkadienyl, phenyl, phenyl-lower alkyl, substitutted phenyl, substituted phenyl-lower alkyl, or certain heterocyclic groups; R.sub.6 is lower alkyl; and X is hydrogen, lower alkanoyloxy, ##STR3## or certain heterothio groups; are useful as antibacterial agents.
摘要翻译：具有下式的[[[（2,4-二氧代-1-咪唑烷基）氨基]羰基]氨基] - 乙酰头孢菌素衍生物其中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，成盐离子，或基团R 1是氢或甲氧基; R2，R3和R5各自为氢或低级烷基; R4是氢，低级烷基，环低级烷基，环低级烯基，环低级亚烷基，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是低级烷基; X是氢，低级烷酰氧基，或者某些杂硫基; 作为抗菌剂是有用的。

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