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31. 发明授权

US4548934A 4H-1,4-Benzothiazine derivatives 失效
标题翻译： 4H-1,4-苯并噻嗪衍生物
公开(公告)号：US4548934A
公开(公告)日：1985-10-22
申请号：US518901
申请日：1983-08-01
申请人： Gerd Fengler , Dieter Arlt , Klaus Grohe , Hans-Joachim Zeiler , Karl G. Metzger
发明人： Gerd Fengler , Dieter Arlt , Klaus Grohe , Hans-Joachim Zeiler , Karl G. Metzger
IPC分类号： A61K31/43 , C07D279/16 , A61K31/54
CPC分类号： A61K31/43 , A61K31/70 , C07D279/16
摘要： The present invention relates to novel 4H-1,4-benzothiazine derivatives and a method for their synthesis. The invention also relates to the pharmaceutical use of said derivatives, in particular their use as anti-infective agents, as agents for promoting growth and for improving feed stuff utilization in animals, and as preservations.
摘要翻译：本发明涉及新的4H-1,4-苯并噻嗪衍生物及其合成方法。本发明还涉及所述衍生物的药物用途，特别是其作为抗感染剂的用途，作为用于促进生长和改善动物饲料利用的试剂以及作为保存物。

32. 发明授权

US5284855A 7-(2,7-diazabicyclo[3.3.0]octyl)-3-quinolone-and-naphthyridonecarboxylic acid derivatives 失效
标题翻译： 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
公开(公告)号：US5284855A
公开(公告)日：1994-02-08
申请号：US974446
申请日：1992-11-12
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 , A61K31/505 , C07D401/14
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 anti-bacterial 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。

33. 发明授权

US5190955A 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：US5190955A
公开(公告)日：1993-03-02
申请号：US645751
申请日：1991-01-25
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： 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-quinolinecarboxlyic 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-喹啉代羧酸衍生物酰胺基-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，其可以还包含原子或基团-O + 13，-S + 13，-SO-，-SO 2 - ，作为环成员或组也可以表示结构的环系统

34. 发明授权

US4841059A Pyridine-enamines 失效
标题翻译：吡啶 - 烯胺
公开(公告)号：US4841059A
公开(公告)日：1989-06-20
申请号：US108839
申请日：1987-10-15
申请人： Michael Schriewer , Klaus Grohe , Hans-Joachim Zeiler , Karl G. Metzger
发明人： Michael Schriewer , Klaus Grohe , Hans-Joachim Zeiler , Karl G. Metzger
IPC分类号： A23K20/116 , A61K31/495 , A61K31/535 , A61K31/55 , A61P31/04 , C07C67/00 , C07C213/00 , C07C225/16 , C07C227/00 , C07C227/08 , C07C229/34 , C07C231/00 , C07C231/12 , C07C237/16 , C07C237/20 , C07C237/30 , C07C253/00 , C07C255/42 , C07C313/00 , C07C315/04 , C07C317/48 , C07C323/25 , C07C323/32 , C07C323/36 , C07C323/37 , C07C323/62 , C07C323/67 , C07D213/73 , C07D471/06 , C07D498/06 , C07D498/16
CPC分类号： C07D213/73 , A23K20/116 , C07D471/06
摘要： Antibacterially active new 1,8-bridged 4-quinolone-3-carboxylic acid derivatives of the formula ##STR1## in which Y is carboxyl or a derivative thereofR.sup.1, R.sup.2, R.sup.3, R.sup.4, X.sup.1, X.sup.2 and X.sup.5 are H or various radicals,Z is O, NH, substituted NH, ##STR2## m and n are 0 or 1, andA, B, D, and E are CH or substituted C or up to three of them are N,and physiologically acceptable salts thereof. Novel intermediates are described as well as processes for making the intermediates and end products.
摘要翻译：其中Y为羧基或其衍生物R1，R2，R3，R4，X1，X2和X5的式为“IMAGE”的抗菌活性新的1,8-桥桥4-喹诺酮-3-羧酸衍生物为H或各种基团，Z是O，NH，取代的NH，m和n是0或1，A，B，D和E是CH或取代的C，或者最多三个是N，并且生理上可接受的盐。描述了新的中间体以及制备中间体和终产物的方法。

35. 发明授权

US4840954A 6,7-disubstituted 1-cycloproply-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids 失效
标题翻译： 6,7-二取代的1-环丙-1,4-二氢-4-氧代-1,8-二氮杂萘-3-羧酸
公开(公告)号：US4840954A
公开(公告)日：1989-06-20
申请号：US815440
申请日：1985-12-31
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： A61K31/33 , A61K31/435 , A61K31/495 , A61P31/04 , C07D20060101 , C07D213/61 , C07D213/77 , C07D213/78 , C07D213/80 , C07D471/04
CPC分类号： C07D213/78 , C07D213/61 , C07D213/77 , C07D213/80 , C07D471/04
摘要： New 6,7-disubstituted-1-cyclopropyl-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxy lic acids of the formula (I) ##STR1## in which X represents halogen or nitro and A represents ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are defined hereinbelow are disclosed as well as their usefulness as antibacterial agents.
摘要翻译：式（I）的新的6,7-二取代-1-环丙基-1,4-二氢-4-氧代-1,8-二氮杂萘-3-羧酸，其中X表示卤素或硝基，A 表示其中R1，R2，R3和R4如下文定义的以及它们作为抗菌剂的用途。

36. 发明授权

US4753925A Antibacterial 1,7-diamino-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids 失效
标题翻译：抗细菌的1,7-二氨基-1,4-二氢-4-氧代-3-喹啉羧酸
公开(公告)号：US4753925A
公开(公告)日：1988-06-28
申请号：US899458
申请日：1986-08-22
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： A61K31/435 , A61K31/47 , A61K31/495 , A61K31/535 , A61P31/04 , C07D215/58 , C07D471/04 , C07D401/04
CPC分类号： C07D471/04 , C07D215/58
摘要： Antibacterially effective 1,7-diamino-1,4-dihydro-4-oxo-3-(aza)quinolinecarboxylic acids of the formula ##STR1## in which A is nitrogen or C--R.sup.1,R.sup.1 is nitro or halogen,R.sup.2 and R.sup.3 each independently is C.sub.1 -C.sub.3 -alkyl, or together with the nitrogen atom to which they are bonded, form a 5-membered or 6-membered heterocyclic ring, which can additionally contain the atoms or groups --O--, --S--, --SO--, --SO.sub.2 -- or .dbd.N--R.sup.4 as a ring member and can optionally be mono-, di- or tri-substituted on the carbon atoms by C.sub.1 -C.sub.3 -alkyl, hydroxyl, alkoxy with 1-3 carbon atoms, amino, methylamino or ethylamino, it being possible for a carbon atom in each case to carry only one substituent,R.sup.4 is hydrogen, an alkyl or alkenyl group which has 1 to 4 carbon atoms and is optionally substituted by a hydroxyl, alkoxy, alkylmercapto, alkylamino or dialkylamino group with 1 to 3 carbon atoms per alkyl radical, the cyano group or an alkoxycarbonyl group with 1 to 4 carbon atoms in the alcohol part, or a benzyloxycarbonyl group.
摘要翻译：其中A为氮或C-R 1，R1为硝基或卤素的式为“IMAGE”的抗菌有效的1,7-二氨基-1,4-二氢-4-氧代-3-（氮杂）喹啉羧酸，R2和R3 各自独立地为C 1 -C 3 - 烷基，或与它们所键合的氮原子一起形成5元或6元杂环，其可另外含有原子或基团-O - ， - S - ， - SO - ， - SO 2 - 或= N-R 4作为环成员，并且可以任选地在C 1 -C 3烷基，羟基，具有1-3个碳原子的烷氧基，碳原子上被单，二或三取代，氨基，甲基氨基或乙基氨基，每种情况下碳原子可能仅携带一个取代基，R4是氢，具有1至4个碳原子并任选被羟基，烷氧基，烷基巯基，烷基氨基取代的烷基或烯基或每个烷基具有1至3个碳原子的二烷基氨基，在醇部分中具有1至4个碳原子的氰基或烷氧基羰基，或苄氧基羰基。

37. 发明授权

US4725595A 1,8-bridged 4-quinolone-3-carboxylic acid antibacterials 失效
标题翻译： 1,8桥桥4-喹诺酮-3-羧酸抗菌剂
公开(公告)号：US4725595A
公开(公告)日：1988-02-16
申请号：US1318
申请日：1987-01-08
申请人： Michael Schriewer , Klaus Grohe , Hans-Joachim Zeiler , Karl G. Metzger
发明人： Michael Schriewer , Klaus Grohe , Hans-Joachim Zeiler , Karl G. Metzger
IPC分类号： A23K20/116 , A61K31/495 , A61K31/535 , A61K31/55 , A61P31/04 , C07C67/00 , C07C213/00 , C07C225/16 , C07C227/00 , C07C227/08 , C07C229/34 , C07C231/00 , C07C231/12 , C07C237/16 , C07C237/20 , C07C237/30 , C07C253/00 , C07C255/42 , C07C313/00 , C07C315/04 , C07C317/48 , C07C323/25 , C07C323/32 , C07C323/36 , C07C323/37 , C07C323/62 , C07C323/67 , C07D213/73 , C07D471/06 , C07D498/06 , C07D498/16 , A61K31/54 , C07D513/06
CPC分类号： C07D213/73 , A23K20/116 , C07D471/06
摘要： Antibacterially active new 1,8-bridged 4-quinolone-3-carboxylic acid derivatives of the formula ##STR1## in which Y is carboxyl or a derivative thereofR.sup.1, R.sup.2, R.sup.3, R.sup.4, X.sup.1, X.sup.2 and X.sup.5 are H or various radicals,Z is O, NH, substituted NH, --CON
摘要翻译：其中Y为羧基或其衍生物R1，R2，R3，R4，X1，X2和X5的式为“IMAGE”的抗菌活性新的1,8-桥桥4-喹诺酮-3-羧酸衍生物为H或各种基团，Z为O，NH，取代NH，-CON或-SO 2 N，m和n为0或1，A，B，D和E为CH或取代C，或最多三个为N，其可接受的盐。描述了新的中间体以及制备中间体和终产物的方法。

38. 发明授权

US4666920A Antibacterial 1,7-diamino-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids 失效
标题翻译：抗细菌的1,7-二氨基-1,4-二氢-4-氧代-3-喹啉羧酸
公开(公告)号：US4666920A
公开(公告)日：1987-05-19
申请号：US712490
申请日：1985-03-15
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： A61K31/435 , A61K31/47 , A61K31/495 , A61K31/535 , A61P31/04 , C07D215/58 , C07D471/04
CPC分类号： C07D471/04 , C07D215/58
摘要： Antibacterially effective 1,7-diamino-1,4-dihydro-4-oxo-3-(aza)quinolinecarboxylic acids of the formula ##STR1## in which A is nitrogen or C--R.sup.1,R.sup.1 is nitro or halogen,R.sup.2 and R.sup.3 each independently is C.sub.1 -C.sub.3 -alkyl, or together with the nitrogen atom to which they are bonded, form a 5-membered or 6-membered heterocyclic ring, which can additionally contain the atoms or groups --O--, --S--, --SO--, --SO.sub.2 -- or .dbd.N--R.sup.4 as a ring member and can optionally be mono-, di- or tri-substituted on the carbon atoms by C.sub.1 -C.sub.3 -alkyl, hydroxyl, alkoxy with 1-3 carbon atoms, amino, methylamino or ethylamino,R.sup.4 is hydrogen, an alkyl or alkenyl group which has 1 to 4 carbon atoms and is optionally substituted by a hydroxyl, alkoxy, alkylmercapto, alkylamino or dialkylamino group with 1 to 3 carbon atoms per alkyl radical, the cyano group or an alkoxycarbonyl group with 1 to 4 carbon atoms in the alcohol part, or a benzyloxycarbonyl group, a phenylalkyl group which has up to 4 carbon atoms in the aliphatic part and is optionally substituted in the phenyl radical, a phenyl radical which is optionally monosubstituted or disubstituted by hydroxyl, methoxy, chlorine ad fluorine, a phenylacyl radical which is optionally monosubstituted or disubstituted by hydroxyl, methoxy, chlorine or fluorine, an oxoalkyl radical with up to 6 carbon atoms or a cycloalkyl-alkyl radical which has up to 6 carbon atoms in the cyclic part and up to 3 carbon atoms in the acyclic part,R.sup.5 and R.sup.6 each independently is hydrogen or an alkyl group with 1 to 4 carbon atoms, andX is hydrogen, a nitro group or halogen, or pharmaceutically acceptable salts thereof.
摘要翻译：其中A为氮或C-R 1，R1为硝基或卤素的式为“IMAGE”的抗菌有效的1,7-二氨基-1,4-二氢-4-氧代-3-（氮杂）喹啉羧酸，R2和R3 各自独立地为C 1 -C 3 - 烷基，或与它们所键合的氮原子一起形成5元或6元杂环，其可另外含有原子或基团-O - ， - S - ， - SO - ， - SO 2 - 或= N-R 4作为环成员，并且可以任选地在C 1 -C 3烷基，羟基，具有1-3个碳原子的烷氧基，碳原子上被单，二或三取代，氨基，甲基氨基或乙基氨基，R4是氢，具有1至4个碳原子并且任选被每个烷基具有1至3个碳原子的羟基，烷氧基，烷基巯基，烷基氨基或二烷基氨基取代的烷基或链烯基，氰基或在醇部分中具有1至4个碳原子的烷氧基羰基，或苄氧基羰基，在脂族部分具有至多4个碳原子的苯基烷基，i 任选地被苯基取代的苯基，其任选被羟基，甲氧基，氯和氟任意单取代或二取代的苯基，任选被羟基，甲氧基，氯或氟单取代或二取代的苯基酰基，具有至多 6个碳原子或环状部分中具有多达6个碳原子的环烷基 - 烷基或无环部分中具有至多3个碳原子的环烷基 - 烷基，R 5和R 6各自独立地为氢或具有1至4个碳原子的烷基，以及 X是氢，硝基或卤素，或其药学上可接受的盐。

39. 发明授权

US4659603A Immunostimulating agents 失效
标题翻译：免疫刺激剂
公开(公告)号：US4659603A
公开(公告)日：1987-04-21
申请号：US735494
申请日：1985-05-17
申请人： Klaus Grohe , Volker Klimetzek , Karl G. Metzger , Klaus G. Stunkel , Hans-Joachim Zeiler
发明人： Klaus Grohe , Volker Klimetzek , Karl G. Metzger , Klaus G. Stunkel , Hans-Joachim Zeiler
IPC分类号： A61K31/47 , A61K31/495 , A61P37/04 , C07D215/56 , A61K39/00
CPC分类号： C07D215/56 , A61K31/495 , Y10S514/885
摘要： 1-Cyclopropylquinolone-3-carboxylic acids of the formula ##STR1## in which R.sup.1 is hydrogen, methyl, ethyl or .beta.-hydroxyethyl, andR.sup.2 is hydrogen, chlorine or fluorineor salts thereof stimulate the immune system, especially in conjunction with an antigen.
摘要翻译：其中R 1是氢，甲基，乙基或β-羟基乙基，R 2是氢，氯或氟或其盐的1-环丙基喹诺酮-3-羧酸，其中R 1是氢，甲基，乙基或β-羟乙基，其刺激免疫系统，特别是与抗原。

40. 发明授权

US4556658A 7-Amino-1-cyclopropyl-6,8-difluoro-1,4-di hydro-4-oxo-quinoline-3-carboxylic acids and antibacterial agents containing these compounds 失效
标题翻译： 7-氨基-1-环丙基-6,8-二氟-1,4-二氢-4-氧代喹啉-3-羧酸和含有这些化合物的抗菌剂
公开(公告)号：US4556658A
公开(公告)日：1985-12-03
申请号：US603480
申请日：1984-04-24
申请人： Klaus Grohe , Uwe Petersen , Hans-Joachim Zeiler , Karl G. Metzger
发明人： Klaus Grohe , Uwe Petersen , Hans-Joachim Zeiler , Karl G. Metzger
IPC分类号： A01N43/42 , A23K1/16 , A61K31/47 , A61K31/495 , A61K31/535 , A61K31/54 , A61P31/04 , C07D211/00 , C07D215/00 , C07D215/56 , C07D241/00 , C07D401/02 , C07D401/04 , C07D403/04 , C07D413/04
CPC分类号： C07D215/56 , C07D401/04 , C07D413/04
摘要： The invention relates to 7-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-quinoline-3-carboxylic acids, processes for their preparation and compositions containing them as antibacterial agents. Also included in the invention are methods for treating bacterial infection using the compounds and compositions of the invention.
摘要翻译：本发明涉及7-氨基-1-环丙基-6,8-二氟-1,4-二氢-4-氧代 - 喹啉-3-甲酸甲酯，其制备方法和含有它们作为抗菌剂的组合物。本发明还包括使用本发明的化合物和组合物治疗细菌感染的方法。

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