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1. 发明授权

US4686208A Phosphorylated glycosyl-amides, -ureas, -carbamates and -thiocarbamates and method of use 失效
标题翻译：磷酸化糖基酰胺， - 脲， - 氨基甲酸酯和 - 硫代氨基甲酸酯及其使用方法
公开(公告)号：US4686208A
公开(公告)日：1987-08-11
申请号：US673811
申请日：1984-11-21
申请人： Oswald Lockhoff , Bernd-Wieland Kruger , Peter Stadler , Arnold Paessens , Gert Streissle , Peter Taylor , Hans-Joachim Zeiler , Karl-Georg Metzger
发明人： Oswald Lockhoff , Bernd-Wieland Kruger , Peter Stadler , Arnold Paessens , Gert Streissle , Peter Taylor , Hans-Joachim Zeiler , Karl-Georg Metzger
IPC分类号： A61K31/70 , C07H13/06 , C07H13/12 , C07H5/06
CPC分类号： C07H13/06 , C07H13/12
摘要： Compounds of the formula ##STR1## in which R.sup.1 represents an optionally substituted, straight-chain or branched, saturated, monounsaturated or polyunsaturated alkyl radical, an optionally substituted, saturated or one- or polyunsaturated cycloalkyl radical or an optionally substituted aryl radical or aralkyl radical,X represents CH.sub.2, O, S, NH or N-alkyl with up to 20 C atoms,R.sup.2 has the meaning of R.sup.1, and can represent hydrogen if X denotes CH.sub.2, the radicals R.sup.3 independently of one another represent hydrogen, an acyl radical or alkyl radical with in each case up to 20 C atoms, a silyl radical and/or a phosphoric acid or phosphoric acid ester radical andR.sup.4 denotes hydrogen, methyl or --CH.sub.2 --OR.sup.3, with the proviso that one of the radicals R.sup.3 always represents a phosphoric acid or phosphoric acid ester radical, which stimulate a patient's immune system and are thereby effective in combating viral disease and bacterial infection.
摘要翻译：式“IMAGE”的化合物，其中R 1表示任选取代的直链或支链饱和的单不饱和或多不饱和烷基，任选取代的饱和或一或多不饱和环烷基或任选取代的芳基或芳烷基 X表示CH 2，O，S，NH或具有多达20个C原子的N-烷基，R 2具有R 1的含义，如果X表示CH 2，则可表示氢，基团R 3彼此独立地表示氢，酰基或烷基，在每种情况下最多达20个C原子，甲硅烷基和/或磷酸或磷酸酯基，R4表示氢，甲基或-CH2-OR3，条件是基团R3之一总是表示磷酸或磷酸酯基，其刺激患者的免疫系统，从而有效地对抗病毒性疾病和细菌感染。

2. 发明授权

US4235888A Pseudotrissaccharides, a process for their production and their use as medicaments 失效
标题翻译：伪三糖，其生产过程及其作为药物的用途
公开(公告)号：US4235888A
公开(公告)日：1980-11-25
申请号：US52871
申请日：1979-06-28
申请人： Peter Stadler , Karl-Georg Metzger , Eckart Voss , Uwe Petersen , Hans-Joachim Zeiler , Hans-Joachim Kabbe
发明人： Peter Stadler , Karl-Georg Metzger , Eckart Voss , Uwe Petersen , Hans-Joachim Zeiler , Hans-Joachim Kabbe
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , C07D317/72 , C07H15/236 , C07H17/08
CPC分类号： C07D317/72 , C07H15/236
摘要： Pseudotrisaccharides of the sisomycin type are provided which are effective an antibacterial agents, particularly against gram-negative microorganisms. The invention also includes methods for the manufacture of the pseudotrisaccharides, compositions containing said pseudotrisaccharides and methods for the treatment of warm-blooded animals using said compounds and compositions.
摘要翻译：提供了具有抗菌剂，特别是抗革兰氏阴性微生物的抗生素，具有抗生素的类型。本发明还包括制备假三糖的方法，含有所述假三糖的组合物和使用所述化合物和组合物治疗温血动物的方法。

3. 发明授权

US5371090A Naphthyridonecarboxylic acid derivatives 失效
标题翻译：萘啶酮酸衍生物
公开(公告)号：US5371090A
公开(公告)日：1994-12-06
申请号：US199371
申请日：1994-02-18
申请人： Uwe Petersen , Andreas Krebs , Thomas Schenke , Klaus Grohe , Klaus-Dieter Bremm , Rainer Endermann , Karl-Georg Metzger , Hans-Joachim Zeiler
发明人： Uwe Petersen , Andreas Krebs , Thomas Schenke , Klaus Grohe , Klaus-Dieter Bremm , Rainer Endermann , Karl-Georg Metzger , Hans-Joachim Zeiler
IPC分类号： A61K31/435 , A61K31/44 , A61K31/47 , A61K31/535 , A61P31/04 , C07D239/26 , C07D241/12 , C07D471/04 , C07D487/04 , C07D519/00 , C07D471/02
CPC分类号： C07D239/26 , C07D241/12 , C07D471/04 , C07D487/04
摘要： The invention relates to naphthyridonecarboxylic acid derivatives which are substituted in the 7-position by an optionally partially hydrogenated azaisoindolinyl ring, to processes for their preparation, and to antibacterial agents and feed additives containing them.
摘要翻译：本发明涉及通过任选的部分氢化的氮杂吲哚啉基环在7-位上被取代的萘啶酮羧酸衍生物，其制备方法以及含有它们的抗菌剂和饲料添加剂。

4. 发明授权

US5312823A 7-azaisoindolinyl-quinolone-carboxylic acid derivatives 失效
标题翻译： 7-氮杂吲哚啉基 - 喹诺酮 - 羧酸衍生物
公开(公告)号：US5312823A
公开(公告)日：1994-05-17
申请号：US901056
申请日：1992-06-19
申请人： Uwe Petersen , Andreas Krebs , Thomas Schenke , Klaus Grohe , Klaus-Dieter Bremm , Rainer Endermann , Karl-Georg Metzger , Hans-Joachim Zeiler
发明人： Uwe Petersen , Andreas Krebs , Thomas Schenke , Klaus Grohe , Klaus-Dieter Bremm , Rainer Endermann , Karl-Georg Metzger , Hans-Joachim Zeiler
IPC分类号： A61K31/435 , A61K31/44 , A61K31/47 , A61K31/535 , A61P31/04 , C07D239/26 , C07D241/12 , C07D471/04 , C07D487/04 , C07D519/00 , A61K31/55
CPC分类号： C07D239/26 , C07D241/12 , C07D471/04 , C07D487/04
摘要： The invention relates to new quinolonecarboxylic acid derivatives which are substituted in the 7-position by an optionally partially hydrogenated azaisoindolinyl ring, to processes for their preparation, and to antibacterial agents and feed additives containing them.
摘要翻译：本发明涉及通过任选的部分氢化的氮杂吲哚啉基环在7-位上被取代的新的喹诺酮羧酸衍生物，其制备方法以及含有它们的抗菌剂和饲料添加剂。

5. 发明授权

US5464796A 7-isoindolinyl-quinolone-carboxylic acid derivatives 失效
标题翻译： 7-异吲哚啉基 - 喹诺酮 - 羧酸衍生物
公开(公告)号：US5464796A
公开(公告)日：1995-11-07
申请号：US896955
申请日：1992-06-11
申请人： Uwe Petersen , Andreas Krebs , Thomas Schenke , Franz Kunisch , Thomas Philipps , Klaus Grohe , Klaus-Dieter Bremm , Rainer Endermann , Karl-Georg Metzger , Ingo Haller , Hans-Joachim Zeiler
发明人： Uwe Petersen , Andreas Krebs , Thomas Schenke , Franz Kunisch , Thomas Philipps , Klaus Grohe , Klaus-Dieter Bremm , Rainer Endermann , Karl-Georg Metzger , Ingo Haller , Hans-Joachim Zeiler
IPC分类号： A61K31/435 , A61K31/4375 , A61K31/44 , A61K31/47 , A61K31/4709 , A61K31/535 , A61P31/00 , A61P31/04 , C07D209/44 , C07D215/56 , C07D401/04 , C07D405/14 , C07D471/04 , C07D471/06 , C07D498/04 , C07D498/06 , C07D513/06 , C07D215/38
CPC分类号： C07D215/56 , C07D209/44 , C07D401/04 , C07D471/04
摘要： The invention relates to new quinolone- and naphthyridonecarboxylic acid derivatives which are substituted in the 7-position by a partly hydrogenated isoindolinyl ring, processes for their preparation and antibacterial agents and feed additives containing these compounds.
摘要翻译：本发明涉及通过部分氢化的异吲哚啉环在7位上被取代的新的喹诺酮和萘啶酮羧酸衍生物，其制备方法以及含有这些化合物的抗菌剂和饲料添加剂。

6. 发明授权

US5480879A Quinolonecarboxylic acids 失效
标题翻译：喹诺酮羧酸
公开(公告)号：US5480879A
公开(公告)日：1996-01-02
申请号：US131253
申请日：1993-10-01
申请人： Uwe Petersen , Wilfried Schrock , Dieter Habich , Andreas Krebs , Thomas Schenke , Thomas Philipps , Klaus Grohe , Rainer Endermann , Klaus-Dieter Bremm , Karl-Georg Metzger
发明人： Uwe Petersen , Wilfried Schrock , Dieter Habich , Andreas Krebs , Thomas Schenke , Thomas Philipps , Klaus Grohe , Rainer Endermann , Klaus-Dieter Bremm , Karl-Georg Metzger
IPC分类号： A61K31/43 , A61K31/435 , A61K31/47 , A61K31/535 , A61K31/545 , A61P31/04 , C07D417/12 , C07D463/00 , C07D477/00 , C07D477/14 , C07D498/04 , C07D499/88 , C07D501/00 , C07D501/16 , C07D513/06 , C07D519/00 , C07D519/06 , C07D487/04
CPC分类号： C07D477/14 , C07D499/88 , C07D501/00
摘要： The invention relates to novel derivatives of quinolonecarboxylic acid and naphthyridonecarboxylic acid which are linked to a .beta.-lactam antibiotic, to their salts, to processes for their preparation and to antibacterial agents containing these derivatives.
摘要翻译：本发明涉及与β-内酰胺抗生素连接的喹诺酮羧酸和萘啶酮羧酸的新型衍生物，其盐，其制备方法和含有这些衍生物的抗菌剂。

7. 发明授权

US3993770A Penicillins 失效
标题翻译：青霉素
公开(公告)号：US3993770A
公开(公告)日：1976-11-23
申请号：US629526
申请日：1975-11-06
申请人： Wilfried Schrock , Karl-Georg Metzger , Hans-Bodo Konig
发明人： Wilfried Schrock , Karl-Georg Metzger , Hans-Bodo Konig
IPC分类号： C07D231/08 , C07D231/20 , C07D499/00 , C07D499/64 , C07D499/68 , C07D499/70
CPC分类号： C07D231/08 , C07D231/20 , C07D499/00
摘要： A compound of the formula: ##SPC1##Or a pharmaceutically acceptable nontoxic salt thereof whereinR.sub.1 is hydrogen, straight or branched chain alkyl of 1 to 5 carbon atoms, monoaralkyl of up to 8 carbon atoms, monoaryl, substituted monoaryl, or thienyl;A is a moiety of the formula: ##EQU1## wherein R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are the same or different and each is hydrogen, straight or branched chain alkyl of 1 to 5 carbon atoms, monoaralkyl of up to 8 carbon atoms, monoaryl, substituted monoaryl, or thienyl;B is a moiety of the formula: ##SPC2##WhereinR.sub.8, r.sub.9 and R.sub.10 are the same or different and each is hydrogen, fluorine, chlorine, bromine, iodine, lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulphonyl, sulphamyl, nitro, cyano, di(lower alkyl)amino, lower alkanoylamino, lower alkanoyloxy, lower alkylsulphonylamino, trifluoromethyl or hydroxy;E is oxygen or sulphur; andC* is a carbon atom constituting a center of chirality, are useful for their antibacterial activity.
摘要翻译：化学式为：+ q，10或其药学上可接受的非对映盐，其中R1为氢，1至5个碳原子的直链或支链烷基，至多8个碳原子的单烷基，单芳基，取代的单芳基或噻吩基; A是下式的部分：R4R2O || PARALLEL -CCC-，|| R5R3 R3R2O || PARALLEL -CC = NC-，| R4 R6R4R2O R3R2O R2O ||| PARALLEL || PARALLEL | PARALLEL -CCCC-，-C = CC-，-C = NC-，||| R7R5R3 R5R3R2O R4R3R2O OR2O ||| PARALLEL ||| PARALLEL PARALLEL | PARALLEL -CCNC-，-C = CNC-，-CNC-，|| R6R4 OR2R3O平行角度平行+ TR 或-C-C-C-，其中R 2，R 3，R 4，R 5，R 6和R 7相同或不同，各自为氢，1至5个碳原子的直链或支链烷基，至多8个碳原子的直链烷基原子，单芳基，取代的单芳基或噻吩基; B是下式的部分：

8. 发明授权

US3993642A Penicillins 失效
标题翻译：青霉素
公开(公告)号：US3993642A
公开(公告)日：1976-11-23
申请号：US538753
申请日：1975-01-06
申请人： Wilfried Schrock , Karl-Georg Metzger , Hans-Bodo Konig
发明人： Wilfried Schrock , Karl-Georg Metzger , Hans-Bodo Konig
IPC分类号： C07D499/66 , A23K20/195 , A61K31/50 , A61P31/04 , C07D231/08 , C07D231/20 , C07D499/00 , C07D499/12 , C07D499/16 , C07D499/64 , C07D499/68 , C07D499/70
CPC分类号： C07D231/08 , C07D231/20 , C07D499/00
摘要： A compound of the formula: ##SPC1##Or a pharmaceutically acceptable nontoxic salt thereof whereinR.sub.1 is hydrogen, straight or branched chain alkyl of 1 to 5 carbon atoms, monoaralkyl of up to 8 carbon atoms, monoaryl, substituted monoaryl, or thienyl;A is a moiety of the formula: ##EQU1## wherein R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are the same or different and each is hydrogen, straight or branched chain alkyl of 1 to 5 carbon atoms, monoaralkyl of up to 8 carbon atoms, monoaryl, substituted monoaryl, or thienyl;B is a moiety of the formula: ##SPC2##WhereinR.sub.8, r.sub.9 and R.sub.10 are the same or different and each is hydrogen, fluorine, chlorine, bromine, iodine, lower alkyl, lower alkoxy, lower alkythio, lower alkylsulphonyl, sulphamyl, nitro, cyano, di(lower alkyl)amino, lower alkanoylamino, lower alkanoyloxy, lower alkylsulphonylamino, trifluoromethyl or hydroxy;E is oxygen or sulphur; andC is a carbon atom constituting a center of chirality, are useful for their antibacterial activity.
摘要翻译：下式的化合物：

9. 发明授权

US3972869A Penicillins 失效
公开(公告)号：US3972869A
公开(公告)日：1976-08-03
申请号：US502765
申请日：1974-09-03
申请人： Hans-Bodo Konig , Wilfried Schrock , Karl-Georg Metzger
发明人： Hans-Bodo Konig , Wilfried Schrock , Karl-Georg Metzger
IPC分类号： C07D499/00 , C07D499/64 , C07D499/46
CPC分类号： C07D499/00
摘要： Penicillins of the formula ##EQU1## or pharmaceutically acceptable non-toxic salts thereof, wherein C is a carbon atom constituting a center of chirality;A is a moiety of the formula ##EQU2## or ##EQU3## wherein X is ##EQU4## Y is ##EQU5## or wherein Aryl is an aryl moiety; Z is ##EQU6## Q.sub.1 is ##EQU7## or ##SPC1##Q.sub.2 is ##EQU8## ##SPC2##or ##SPC3##R is straight-chain or branched alkyl of 1 to 5 carbon atoms;R.sub.1 is alkyl of 1 to 10 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, alkenyl of 2 to 10 carbon atoms, cycloalkenyl of 3 to 10 carbon atoms, vinyl, arylvinyl, mono-, di-, or tri-halo-lower alkyl, H.sub.2 N--, R--NH--, (R).sub.2 N--, aryl--NH--, aryl-lower alkylamino, alkoxy of 1 to 8 carbon atoms, aralkoxy of 1 to 8 carbon atoms in the alkoxy portion, cycloalkoxy of 3 to 7 carbon atoms, aryloxy, R--O--V--, R--S-- V--, N=C--V--, R--O--CO--V--, H.sub.2 N--CO--V--, R--NH--CO--V--, R--O--CO--NH--, R--SO.sub.2 --NH--, (R).sub.2 N--CO--V--,wherein R is as above defined, ##SPC4## ##SPC5##provided that when X is --SO.sub.2 --, R.sub.1 is not alkoxy, aralkoxy, cycloalkoxy or aryloxy, and further provided that R.sub.1 can also be hydrogen when X is --CO--;V is a divalent organic radical of 1 to 3 carbon atoms;n is 0, 1 or 2;R.sub.2 and R.sub.3 are the same or different and are each hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl of 2 to 8 carbon atoms, vinyl, allyl, propenyl, cycloalkyl of 3 to 6 carbon atoms, cycloalkenyl of 3 to 6 carbon atoms, mono-, di- or tri-halo lower alkyl or aryl;R.sub.4, r.sub.5 and R.sub.6 are the same or different and are each hydrogen, nitro, cyano, (R).sub.2 N--, (R).sub.2 N--CO--, R--CO--NH--, R--O--CO--, R--CO--O--, R--, R--O--, wherein R is as above defined, H.sub.2 N--SO.sub.2 --, chlorine, bromine, iodine, fluorine or trifluoromethyl;G is hydrogen or straight or branched chain alkyl of 1 to 5 carbon atoms; andB is a moiety of the formula ##SPC6##whereinR.sub.7, r.sub.8 ad R.sub.9 are the same or different and are each hydrogen, halogen, nitro, hydroxy, R--, R--0--, R--S--, R--SO--, R--SO.sub.2 --, (R).sub.2 N--, R--CO--NH--, or R--CO--O--, wherein R is as above defined; the arrow in the divalent linking group .fwdarw.means that the linkage of two atoms by the free valencies of his group must take place as indicated by the arrow; exhibit activity against both Gram-positive and Gram-negative bacteria.

10. 发明授权

US3975375A Penicillins 失效
公开(公告)号：US3975375A
公开(公告)日：1976-08-17
申请号：US502753
申请日：1974-09-03
申请人： Hans-Bodo Konig , Wilfried Schrock , Karl-Georg Metzger
发明人： Hans-Bodo Konig , Wilfried Schrock , Karl-Georg Metzger
IPC分类号： C07D233/38 , C07D239/10 , C07D275/02 , C07D333/34 , C07D499/00 , C07D499/64 , C07F7/10 , C07D499/46
CPC分类号： C07D239/10 , C07D233/38 , C07D275/02 , C07D333/34 , C07D499/00 , C07F7/10
摘要： Arylmethyl- and cyclohexenylmethyl- penicillins, substituted on the .alpha.-carbon atom of the side chain by a 2,3-disubstituted imidazolidinylcarbamide or a 2,3-disubstituted imidazolidinylthiocarbamido group, or by the corresponding 2,3-disubstituted 1,3-diazacyclohexylcarbamido or thiocarbamido groups are anti-bacterial agents.

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