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1. 发明授权

US5145853A Bactericidal formulations for use in veterinary medicine 失效
标题翻译：用于兽药的杀菌剂
公开(公告)号：US5145853A
公开(公告)日：1992-09-08
申请号：US635817
申请日：1991-01-02
申请人： Karl G. Metzger , Hans-Joachim Zeiler , Martin Scheer , Herbert Voege , Klaus Grohe
发明人： Karl G. Metzger , Hans-Joachim Zeiler , Martin Scheer , Herbert Voege , Klaus Grohe
IPC分类号： C07D215/56 , A61K20060101 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/535 , A61P31/00 , A61P31/04
CPC分类号： A61K31/47 , A61K31/44 , A61K31/535
摘要： A method of treating livestock infected with, or protecting livestock against infection from, bacteria which comprises administering to such livestock an antibacterially effective amount of a quinolonecarboxylic acid or derivative of the formula ##STR1## in which A represents nitrogen or .dbd.C--R.sup.4,R.sup.4 represents hydrogen, fluorine, chlorine, nitro or methyl,B represents ##STR2## and B also represents ##STR3## when R.sup.1 does not denote cyclopropyl, and R.sup.5 represents hydrogen, a branched or unbranched alkyl group which has 1 to 4 carbon atoms and which can optionally be substituted by a hydroxyl or methoxy group,R.sup.6 represents hydrogen, methyl or phenyl,R.sup.7 represents hydrogen or methyl,R.sup.8 represents amino, alkyl- or dialkylamino having 1 or 2 carbon atoms in the alkyl group, aminomethyl, alkyl- or dialkylaminomethyl having 1 or 2 carbon atoms in the alkyl group,R.sup.1 represents an alkyl radical having 1 to 3 carbon atoms, cyclopropyl, 2-fluoroethyl vinyl, methoxy, 4-fluorophenyl or methylamino,R.sup.2 represents hydrogen, alkyl having 1 to 6 carbon atoms, and cyclohexyl, benzyl, 2-oxopropyl, phenacyl and ethoxycarbonylmethyl,R.sup.3 represents hydrogen, methyl or ethyl, Z represents oxygen, nitrogen which is substituted by methyl or phenyl, and .dbd.CH.sub.2 --,or a pharmaceutically utilizable salt thereof.
摘要翻译：一种治疗感染或保护家畜免受细菌感染的牲畜的方法，其包括向所述家畜施用抗菌有效量的喹诺酮羧酸或其中A表示氮或= C的式“IMAGE”或“IMAGE”的衍生物 -R4，R4表示氢，氟，氯，硝基或甲基，当R1不表示环丙基时，B表示“IMAGE”，并且B也表示“IMAGE”，R5表示氢，支链或非支链烷基，其具有1至4个碳原子，并且其可以任选被羟基或甲氧基取代，R6表示氢，甲基或苯基，R7表示氢或甲基，R8表示氨基，烷基中具有1或2个碳原子的烷基或二烷基氨基，氨基甲基，烷基中具有1或2个碳原子的烷基 - 或二烷基氨基甲基，R 1表示具有1至3个碳原子的烷基，环丙基，2-氟乙基乙烯基，甲氧基，4-氟苯基或我二氨基，R2代表氢，具有1-6个碳原子的烷基，环己基，苄基，2-氧代丙基，苯甲酰甲基和乙氧羰基甲基，R3代表氢，甲基或乙基，Z代表氧，被甲基或苯基取代的氮， CH2-或其药学上可用的盐。

2. 发明授权

US5571812A 7-amino-1-cyclopropyl-6,8-dihalogeno- 1,4-dihydro-4-oxo-3-quinolinecarboxylic acid antibacterial agents 失效
标题翻译： 7-氨基-1-环丙基-6,8-二卤代-1,4-二氢-4-氧代-3-喹啉羧酸抗菌剂
公开(公告)号：US5571812A
公开(公告)日：1996-11-05
申请号：US875572
申请日：1992-04-27
申请人： Uwe Petersen , Klaus Grohe , Hans-Joachim Zeiler , Karl G. Metzger
发明人： Uwe Petersen , Klaus Grohe , Hans-Joachim Zeiler , Karl G. Metzger
IPC分类号： A61K31/47 , A61K31/495 , A61K31/535 , A61K31/54 , A61P31/04 , C07D215/56 , C07D401/04 , C07D409/04 , C07D409/12 , C07D413/04 , C07D417/04
CPC分类号： C07D215/56 , C07D401/04 , C07D409/12 , C07D413/04
摘要： The invention is related to 7-amino-1-cyclopropyl-6,8- dihalogeno-1,4-dihydro-4-oxo-3-quinoline-carboxylic acids of the formula (I) ##STR1## in which X.sup.1, X.sup.2, R.sup.1 and R.sup.2 have the meaning as pointed out in the following specification. Moreover, the invention is related to a process for the production of the compounds of formula (I) and to antibacterial agents containing them.
摘要翻译：本发明涉及式（I）的7-氨基-1-环丙基-6,8-二卤代-1,4-二氢-4-氧代-3-喹啉羧酸（Ⅰ），其中X1 ，X2，R1和R2具有以下说明书中指出的含义。此外，本发明涉及制备式（I）化合物的方法和含有它们的抗菌剂。

3. 发明授权

US5284842A Quinolone- and naphthridone carboxylic acid derivatives, process for their production, antibacterial compositions and feed additives containing them 失效
标题翻译：喹诺酮和萘啶酮羧酸衍生物，其制备方法，抗菌组合物和含有它们的饲料添加剂
公开(公告)号：US5284842A
公开(公告)日：1994-02-08
申请号：US931746
申请日：1992-08-18
申请人： Uwe Petersen , Thomas Schenke , Klaus Grohe , Michael Schriewer , Ingo Haller , Karl G. Metzger , Rainer Endermann , Hans-Joachim Zeiler
发明人： Uwe Petersen , Thomas Schenke , Klaus Grohe , Michael Schriewer , Ingo Haller , Karl G. Metzger , Rainer Endermann , Hans-Joachim Zeiler
IPC分类号： C07D207/12 , C07D211/42 , C07D211/48 , C07D401/04 , C07D405/14 , C07D455/04 , C07D471/04 , C07D487/10 , C07D491/10 , C07D498/06 , C07D498/10 , C07D513/10 , C07D519/00 , A61K31/47
CPC分类号： C07D401/04 , C07D207/12 , C07D211/42 , C07D211/48 , C07D405/14 , C07D455/04 , C07D471/04 , C07D487/10 , C07D491/10 , C07D513/10
摘要： An antibacterially active quinolone or naphthyridonecarboxylic acid derivative of the formula ##STR1## in which R.sup.1 stands for various organic radical,R.sup.2 stands for hydrogen, alkyl having 1 to 4 carbon atoms or (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl,R.sup.3 stands for hydrogen or amino,R.sup.4 stands for a radical of the formula ##STR2## A stands for N or C--R.sup.5, whereinR.sup.5 stands for hydrogen, halogen methyl, cyano or nitro or else together with R.sup.1 can form a bridge of the structure ##STR3## or a pharmaceutically utilizable hydrate, acid addition salt, alkali metal salt, alkaline earth metal salt, silver salt or guanidinium salt of the carboxylic acid when R.sup.2 is hydrogen.
摘要翻译：其中R1代表各种有机基团，R2代表氢，具有1至4个碳原子的烷基或（5-甲基-2-氧代-1,3-二氧杂环戊烯）的式为“IMAGE”的抗菌活性喹诺酮或萘啶酮羧酸衍生物 -4-基）甲基，R3代表氢或氨基，R4代表下式基团A表示N或C-R5，其中R5代表氢，卤素甲基，氰基或硝基，或者与当R 2为氢时，R 1可以形成结构或可药用的水合物，酸加成盐，碱金属盐，碱土金属盐，银盐或胍盐的桥。

4. 发明授权

US5252734A Antibacterial 5-alkylquinolonecarboxylic acids 失效
标题翻译：抗菌5-烷基喹诺酮羧酸
公开(公告)号：US5252734A
公开(公告)日：1993-10-12
申请号：US831778
申请日：1992-02-05
申请人： Michael Schriewer , Klaus Grohe , Andreas Krebs , Uwe Petersen , Thomas Schenke , Ingo Haller , Karl G. Metzger , Rainer Endermann , Hans-Joachim Zeiler
发明人： Michael Schriewer , Klaus Grohe , Andreas Krebs , Uwe Petersen , Thomas Schenke , Ingo Haller , Karl G. Metzger , Rainer Endermann , Hans-Joachim Zeiler
IPC分类号： C07D215/56 , C07D471/04 , C07D487/04 , C07D487/08 , C07D498/04 , C07D498/06 , C07D513/06 , C07F1/10
CPC分类号： C07D215/56 , C07D471/04 , C07D487/04 , C07D487/08
摘要： Antibacterial 5-alkylquinolonecarboxylic acids of the formula ##STR1## in which R.sup.3 is C.sub.1 -C.sub.4 - alkyl,R.sup.1 is optionally substituted alkyl or cycloalkyl, alkenyl, alkoxy, amino or alkylamino or optionally substituted phenyl,R.sup.2 is hydrogen or optionally substituted alkyl,R.sup.4 is a nitrogen-containing heterocyclic radical, andA is hydrogen, halogen, methyl, cyano or nitro, or forms a bridge with R.sup.1.and hydrates and salts thereof.
摘要翻译：式为“IMAGE”的抗菌5-烷基喹诺酮羧酸，其中R 3为C 1 -C 4烷基，R 1为任选取代的烷基或环烷基，烯基，烷氧基，氨基或烷基氨基或任选取代的苯基，R 2为氢或任选取代的烷基，R 4 是含氮杂环基，A是氢，卤素，甲基，氰基或硝基，或与R1形成桥。及其水合物和盐。

5. 发明授权

US5202337A 7-(2,7-diazabicyclo[3.3.0]octyl)-3-quinoline- and -naphthyridone-carboxylic acid derivatives 失效
标题翻译： 7-（2,7-二氮杂双环（3.3.0）十八烷基）-3-喹啉 - 和 - 邻苯二甲酰基羧酸衍生物
公开(公告)号：US5202337A
公开(公告)日：1993-04-13
申请号：US771700
申请日：1991-10-03
申请人： Uwe Petersen , Thomas Schenke , Michael Schriewer , Klaus Grohe , Andreas Krebs , Ingo Haller , Karl G. Metzger , Klaus-Dieter Bremm , Rainer Endermann , Hans-Joachim Zeiler
发明人： Uwe Petersen , Thomas Schenke , Michael Schriewer , Klaus Grohe , Andreas Krebs , Ingo Haller , Karl G. Metzger , Klaus-Dieter Bremm , Rainer Endermann , Hans-Joachim Zeiler
IPC分类号： A01N43/40 , A01N43/42 , A23K20/116 , A23L3/3544 , A61K31/47 , A61P31/04 , C07D471/14 , C07D487/04 , C07D487/08 , C07D487/14 , C07D513/04 , C07D513/14 , C07D519/00
CPC分类号： C07D471/14 , A23K20/116 , A23L3/3544 , A61K31/47 , C07D487/04 , C07D487/14 , C07D513/14
摘要： The invention relates to new 7-(2,7-Diazabicyclo[3.3.0]octyl)-3-quinolone- and -naphthyridonecarboxylic acid derivatives, processes for their preparation, and antibacterial agents and feed additives containing them.
摘要翻译：本发明涉及新的7-（2,7-二氮杂双环[3.3.0]辛基）-3-喹诺酮和 - 萘啶酮羧酸衍生物，其制备方法，以及含有它们的抗菌剂和饲料添加剂。

6. 发明授权

US4990517A 7-(1-pyrrolidinyl)-3-quinolone- and -naphthyridonecarboxylic acid derivatives as antibacterial agents and feed additives 失效
标题翻译： 7-（1-吡咯烷基）-3-喹诺酮和 - 萘啶酮羧酸衍生物作为抗菌剂和饲料添加剂
公开(公告)号：US4990517A
公开(公告)日：1991-02-05
申请号：US375434
申请日：1989-06-30
申请人： Uwe Petersen , Thomas Schenke , Andreas Krebs , Klaus Grohe , Michael Schriewer , Ingo Haller , Karl G. Metzger , Rainer Endermann , Hans-Joachim Zeiler
发明人： Uwe Petersen , Thomas Schenke , Andreas Krebs , Klaus Grohe , Michael Schriewer , Ingo Haller , Karl G. Metzger , Rainer Endermann , Hans-Joachim Zeiler
IPC分类号： A23K20/195 , A61K31/435 , A61K31/47 , A61K31/535 , A61P31/04 , C07D207/14 , C07D215/56 , C07D401/04 , C07D403/04 , C07D407/14 , C07D413/04 , C07D471/04 , C07D487/04 , C07D498/04 , C07D498/06 , C07D513/04 , C07D513/06 , C07D519/00
CPC分类号： C07D215/56 , C07D207/14 , C07D401/04 , C07D407/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： 7-(1-Pyrrolidinyl)-3-quinolone- and -naphthyridonecarboxylic acid derivatives as antibacterial agents and feed additives, of the formula ##STR1## in which X.sup.1 is halogen,X.sup.2 is hydrogen, halogen, amino or other radical,R.sup.1 is alkyl, cycloalkyl, optionally substituted phenyl or other radical,R.sup.2 is hydrogen, alkyl or a dioxolylmethyl radical,R.sup.3 is ##STR2## A is N, CH, C-halogen, or the like, or forms a bridge with R.sup.1, and addition products thereof.
摘要翻译： 7-（1-吡咯烷基）-3-喹诺酮和 - 萘啶酮羧酸衍生物作为抗菌剂和饲料添加剂，其中X1是卤素，X2是氢，卤素，氨基或其它基团，R1是烷基，环烷基，任选取代的苯基或其它基团，R 2是氢，烷基或二氧杂环戊基甲基，R 3是N，CH，C-卤素等，或与R 1形成桥，及其加成产物。

7. 发明授权

US4908366A Antibacterial 8-cyano-1-cyclopropyl-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids 失效
标题翻译：抗菌8-氰基-1-环丙基-1,4-二氢-4-氧代-3-喹啉羧酸
公开(公告)号：US4908366A
公开(公告)日：1990-03-13
申请号：US144884
申请日：1988-01-14
申请人： Michael Schriewer , Klaus Grohe , Uwe Petersen , Ingo Haller , Karl G. Metzger , Rainer Endermann , Hans-Joachim Zeiler
发明人： Michael Schriewer , Klaus Grohe , Uwe Petersen , Ingo Haller , Karl G. Metzger , Rainer Endermann , Hans-Joachim Zeiler
IPC分类号： A61K31/47 , A61K31/495 , A61P31/04 , C07D215/56 , C07D401/04 , C07D487/08
CPC分类号： C07D215/56 , C07D401/04 , C07D487/08
摘要： Antibacterial 8-cyano-1-cyclopropyl-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid derivatives of the formula ##STR1## in which Y represents a carboxyl group, a nitrile group, an ester group --COOR.sup.1 or an acid amide group --CONR.sup.2 R.sup.3,X.sup.1 represents hydrogen nitro, alkyl or halogenX.sup.4 can be hydrogen or halogen, or alkyl,R.sup.4 and R.sup.5, together with the nitrogen atom to which they are bonded, form a 5- or 6-membered heterocyclic ring which can additionally contain the atoms or groups --O--, --S--, --SO--, --SO.sub.2 --, ##STR2## as ring members or the group ##STR3## can also represent a ring system of the structure ##STR4## which can optionally be substituted on the ring carbons by methyl and pharmaceutically usable hydrates, salts or esters thereof.These compounds have a high antibacterial activity and are therefore suitable as active compounds for human and veterinary medicine.
摘要翻译：其中Y表示羧基，腈基，酯基-COOR1或酸的式“IMAGE”的抗菌8-氰基-1-环丙基-1,4-二氢-4-氧代-3-喹啉羧酸衍生物酰胺基-CONR2R3，X1表示氢硝基，烷基或卤素X4可以是氢或卤素，或烷基，R4和R5与它们所键合的氮原子一起形成5-或6-元杂环，其可以另外还包含原子或基团-O - ， - S - ， - SO - ， - SO 2 - ，作为环成员或组也可以表示结构 + TR

8. 发明授权

US4620007A 6-fluoro-7-chloro-1-cyclopropyl-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid 失效
标题翻译： 6-氟-7-氯-1-环丙基-4-氧代-1,4-二氢 - 喹啉-3-羧酸
公开(公告)号：US4620007A
公开(公告)日：1986-10-28
申请号：US807554
申请日：1985-12-11
申请人： Klaus Grohe , Hans-Joachim Zeiler , Karl G. Metzger
发明人： Klaus Grohe , Hans-Joachim Zeiler , Karl G. Metzger
IPC分类号： C07D215/56 , C07D471/04 , C07D215/14
CPC分类号： C07D471/04 , C07D215/56
摘要： The invention relates to 7-amino-1-cyclo-propyl-4-oxo-1,4-dihydro-naphthyridine (or quinoline)-3-carboxylic acids of Formula I as defined in the specifications. Also included in the invention is a process for the preparation of said compounds of Formula I and Ia. Further, the invention includes compositions containing the compounds of Formula I or Ia and the use of said compounds and compositions as antibacterial agents.
摘要翻译：本发明涉及规格中定义的式I的7-氨基-1-环丙基-4-氧代-1,4-二氢 - 萘啶（或喹啉）-3-羧酸。本发明还包括制备所述式I和Ia化合物的方法。此外，本发明包括含有式I或Ia化合物的组合物以及所述化合物和组合物作为抗菌剂的用途。

9. 发明授权

US4599334A 7-(3-aryl-1-piperazinyl)- and 7-(3-cyclohexyl-1-piperazinyl)-3-quinolonecarboxylic acid antibacterials 失效
标题翻译： 7-（3-芳基-1-哌嗪基） - 和7-（3-环己基-1-哌嗪基）-3-喹诺酮羧酸抗菌剂
公开(公告)号：US4599334A
公开(公告)日：1986-07-08
申请号：US735493
申请日：1985-05-17
申请人： Uwe Petersen , Klaus Grohe , Hans-Joachim Zeiler , Karl G. Metzger
发明人： Uwe Petersen , Klaus Grohe , Hans-Joachim Zeiler , Karl G. Metzger
IPC分类号： A61K31/495 , A61P3/00 , A61P31/04 , C07D215/56 , C07D333/00 , C07D401/04 , C07D409/14
CPC分类号： C07D215/56 , C07D401/04 , C07D409/14
摘要： Novel 1-cyclopropyl-4-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acid antibacterials of the formula ##STR1## in which R.sup.1 is hydrogen, alkyl with 1 to 4 carbon atoms and optionally substituted by hydroxyl, methoxy, amino, dimethylamino, halogen, cyano or alkoxycarbonyl having 1 or 2 carbon atoms in the alkyl moiety, or is oxoalkyl having up to 4 carbon atoms, phenacyl, or acyl having 1 to 4 carbon atoms, phenacyl, or acyl having 1 to 4 carbon atoms,R.sup.2 is phenyl or cyclohexyl optionally substituted up to three times by halogen, methyl, phenyl, cyano, hydroxyl, methoxy, benzyloxy, amino, methylamino, dimethylamino, piperidino or nitro, or is methylenedioxyphenyl, methylenedioxycyclohexyl, furyl, tetrahydrofuryl or thienyl, andX.sup.1 is hydrogen or fluorine,or pharmaceutically ultizable hydrates, acid addition salts, alkali metal salts or alkaline earth metal salts thereof.
摘要翻译：具有式“IMAGE”的新颖的1-环丙基-4-氟-1,4-二氢-4-氧代-7-（1-哌嗪基）-3-喹啉羧酸抗菌剂，其中R 1是氢，具有1至4个的烷基任选地被羟基，甲氧基，氨基，二甲基氨基，卤素，氰基或在烷基部分中具有1或2个碳原子的烷氧基羰基取代，或具有至多4个碳原子的氧代烷基，苯甲酰甲基或具有1至4个碳原子的酰基，苯甲酰基或具有1至4个碳原子的酰基，R 2是苯基或任选被卤素，甲基，苯基，氰基，羟基，甲氧基，苄氧基，氨基，甲基氨基，二甲基氨基，哌啶子基或硝基取代至多三次的苯基或环己基，亚甲二氧基苯基，亚甲二氧基环己基，呋喃基，四氢呋喃基或噻吩基，X 1为氢或氟，或其药学上可接受的水合物，酸加成盐，碱金属盐或碱土金属盐。

10. 发明授权

US4559341A Quinolonecarboxylic acids and antibacterial agents containing these compounds 失效
标题翻译：喹诺酮羧酸和含有这些化合物的抗菌剂
公开(公告)号：US4559341A
公开(公告)日：1985-12-17
申请号：US576595
申请日：1984-02-03
申请人： Uwe Petersen , Klaus Grohe , Engelbert Kuhle , Hans-Joachim Zeiler , Karl G. Metzger
发明人： Uwe Petersen , Klaus Grohe , Engelbert Kuhle , Hans-Joachim Zeiler , Karl G. Metzger
IPC分类号： C07D215/56 , C07D401/04 , C07D401/12 , C07D521/00 , A61K31/495 , C07D401/14
CPC分类号： C07D215/56 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12
摘要： The invention relates to quinolone carboxylic acids, pharmaceutical compositions containing said quinolone carboxylic acids and the use of said compounds and compositions for treatment of bacterial infection. Also included in the invention are process for the manufacture of the active quinolone carboxylic acids.
摘要翻译：本发明涉及喹诺酮羧酸，含有所述喹诺酮羧酸的药物组合物以及所述化合物和组合物用于治疗细菌感染的用途。本发明还包括制备活性喹诺酮羧酸的方法。

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