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91. 发明授权

US5395944A 7-(aminomethyl-oxa-7-aza-bicyclo[3.3.0]oct-7-yl)quinolonecarboxylic and 7-(aminomethyl-oxa-7-aza-bicyclo[3.3.0]oct-7-yl)naphthyridone-carboxylic acid intermediates 失效
标题翻译： 7-（氨基甲基 - 氧杂-7-氮杂 - 双环[3.3.0]辛-7-基）喹啉酮羧酸和7-（氨基甲基 - 氧杂-7-氮杂 - 双环[3.3.0]辛-7-基）萘啶酮 - 羧酸中间体
公开(公告)号：US5395944A
公开(公告)日：1995-03-07
申请号：US124129
申请日：1993-09-20
申请人： Uwe Petersen , Thomas Schenke , Klaus Grohe , Klaus-Dieter Bremm , Rainer Endermann , Karl G. Metzger
发明人： Uwe Petersen , Thomas Schenke , Klaus Grohe , Klaus-Dieter Bremm , Rainer Endermann , Karl G. Metzger
IPC分类号： A61K31/47 , A61K31/435 , A61K31/4375 , A61K31/4709 , A61K31/4741 , A61P31/04 , C07D491/04 , C07D491/048 , C07D519/00 , C07D491/044
CPC分类号： C07D491/04
摘要： 7-(Aminomethyl-oxa-7-aza-bicyclo[3.3.0]oct-7-yl)quinolonecarboxylic acid and 7-(aminomethyl-oxa-7-aza-bicyclo[3.3.0]oct-7-yl)naphthyridonecarboxylic acid derivatives The invention relates to novel derivatives of quinolonecarboxylic acid and naphthyridonecarboxylic acid which are substituted in the 7 position by a 1- (or 5-)aminomethyl-2- (or 3-)oxa-7-aza-bicyclo[3.3.0]oct-7-yl residue, their salts, processes for their preparation and antibacterial agents containing these compounds.
摘要翻译： 7-（氨基甲基 - 氧杂-7-氮杂 - 双环[3.3.0]辛-7-基）喹啉酮羧酸和7-（氨基甲基 - 氧杂-7-氮杂 - 双环[3.3.0]辛-7-基）萘啶酮酸衍生物本发明涉及由1-（或5-）氨基甲基-2-（或3-）氧杂-7-氮杂 - 双环[3.3.0％]取代的喹诺酮羧酸和萘啶酮酸的新衍生物 ]辛-7-基残基，其盐，其制备方法和含有这些化合物的抗菌剂。

92. 发明授权

US4438114A .beta.-Lactam antibiotics 失效
标题翻译： β-内酰胺抗生素
公开(公告)号：US4438114A
公开(公告)日：1984-03-20
申请号：US415632
申请日：1982-09-07
申请人： Michael Boberg , Dieter Habich , Karl G. Metzger , Paul Naab
发明人： Michael Boberg , Dieter Habich , Karl G. Metzger , Paul Naab
IPC分类号： A23L29/00 , A23L2/44 , A61K31/535 , A61P31/04 , C07D505/00 , C07D498/04
CPC分类号： C07D505/00 , Y02P20/55
摘要： A .beta.-lactam of the formula ##STR1## or a hydrate thereof, in whichR represents a hydrogen atom or a methoxy group,n is 1 or 2,Z represents a group of the formula ##STR2## wherein R.sup.1 denotes an optionally substituted aryl group or an optionally substituted heterocyclyl group;or, when n is 1,Z can also represent an optionally substituted cycloalkyl group or an optionally substituted pseudoaromatic heterocyclic 5-membered or 6-membered ring,B represents an optionally substituted phenyl or cyclohexadienyl group, or an unsaturated optionally subtituted heterocyclic ring,T denotes an alkyl--CO--O--, pyridinium, aminopyridinium, carbamoylpyridinium or carbamoyloxy group, an --S--phenyl group which can be substituted, or an --S--Het group in which Het represents an optionally substituted heterocyclic 5-membered or 6-membered ring; andE represents a hydrogen atom, a pharmaceutically acceptable ester grouping a salt-forming cation or a protective group, or represents a negative charge when T contains a quaternary nitrogen,which possesses antibacterial activity rendering it useful as an antibiotic and animal feed supplement.
摘要翻译：其中R表示氢原子或甲氧基，其中n表示1或2，Z表示下式的基团：其中R 1，R 2，R 3，表示任选取代的芳基或任选取代的杂环基; 或者当n为1时，Z还可以表示任选取代的环烷基或任选取代的假芳香杂环5元或6元环，B表示任选取代的苯基或环己二烯基，或不饱和任选取代的杂环，T 表示烷基-CO-O-，吡啶鎓，氨基吡啶鎓，氨基甲酰基吡啶鎓或氨基甲酰氧基，可被取代的-S-苯基或其中Het表示任选取代的杂环5元或6-元烷基的-S-Het基团，元环并且E表示氢原子，成盐阳离子或保护基的药学上可接受的酯基，或当T含有季氮时具有负电荷，其具有抗菌活性，使其可用作抗生素和动物饲料添加剂。

93. 发明授权

US4344939A Penicillin 1,1-dioxides, compositions thereof and methods of use 失效
标题翻译：青霉素1,1-二氧化物，其组合物和使用方法
公开(公告)号：US4344939A
公开(公告)日：1982-08-17
申请号：US154541
申请日：1980-05-29
申请人： Ekkehard Niemers , Hans-Bodo Konig , Wilfried Schrock , Karl G. Metzger
发明人： Ekkehard Niemers , Hans-Bodo Konig , Wilfried Schrock , Karl G. Metzger
IPC分类号： C07D499/32 , A61K31/43 , A61P31/04 , C07D499/00 , C07D499/04 , C07D499/44 , C07D499/46 , C07D499/60 , C07D499/64 , C07D499/70 , C07D499/74 , A61K31/425 , A61K31/44 , A61K31/445 , A61K31/505 , A61K31/535 , A61K31/655 , C07D499/52 , C07D499/54 , C07D499/76
CPC分类号： C07D499/00
摘要： New penicillin 1,1-dioxides of the formula ##STR1## or a salt thereof, in which R.sub.1 denotes a hydrogen atom or an ester-forming radical,R.sub.2 denotes a hydrogen atom,R.sub.3 denotes a hydrogen atom,R.sub.4 denotes a hydrogen atom, an optionally substituted naphthyl radical or a radical of the general formula ##STR2## and the remaining variables can be various organic radicals.
摘要翻译：式（1）所示的新型青霉素1,1-二氧化物或其盐，其中R1表示氢原子或成酯基团，R2表示氢原子，R3表示氢原子，R4表示氢原子，任选取代的萘基或通式为“IMAGE”的基团，其余的变量可以是各种有机基团。

94. 发明授权

US4235774A Penicillin derivatives 失效
标题翻译：青霉素衍生物
公开(公告)号：US4235774A
公开(公告)日：1980-11-25
申请号：US11347
申请日：1979-02-12
申请人： Michael Preiss , Hans-Bodo Konig , Karl G. Metzger , Gunter Schmidt
发明人： Michael Preiss , Hans-Bodo Konig , Karl G. Metzger , Gunter Schmidt
IPC分类号： A61K31/43 , A61P31/04 , C07D499/00 , C07D499/64 , C07D499/70
CPC分类号： C07D499/00
摘要： New penicillin derivatives, or esters or salts thereof, of the formula ##STR1## in which R is H or alkoxy,B is a heterocyclic radical,A is an ethylene, trimethylene or o-phenylene radical,D is --co-- or a direct bond, andZ is a hydrogen atom, an optionally substituted alkyl or alkenyl group, an optionally substituted cycloalkyl, cycloalkenyl or cycloalkadienyl group, an optionally substituted aryl group, an optionally substituted hetercyclyl group or an acyl radical.
摘要翻译：新颖的青霉素衍生物或其酯或其盐，其中R为H或烷氧基，B为杂环基，A为乙烯，三亚甲基或邻亚苯基，D为 - 或直接键，Z是氢原子，任选取代的烷基或烯基，任选取代的环烷基，环烯基或环二烯基，任选取代的芳基，任选取代的杂环基或酰基。

95. 发明授权

US4147693A .beta.Lactam antibiotics and process for their use 失效
标题翻译： {62内酰胺抗生素及其使用过程
公开(公告)号：US4147693A
公开(公告)日：1979-04-03
申请号：US631515
申请日：1975-11-13
申请人： Hans-Bodo Konig , Karl G. Metzger , Michael Preiss , Wilfried Schrock
发明人： Hans-Bodo Konig , Karl G. Metzger , Michael Preiss , Wilfried Schrock
IPC分类号： A61K31/43 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/545 , A61K31/546 , A61P31/04 , C07D233/34 , C07D233/38 , C07D333/00 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D499/00 , C07D499/04 , C07D499/64 , C07D499/66 , C07D499/68 , C07D501/20 , C07D503/00 , C07D505/00 , A61K31/54 , C07D499/46 , C07D501/34
CPC分类号： C07D505/00 , C07D233/38 , C07D499/00 , C07D503/00
摘要： 6-[.alpha.-(Imidazolidin-2-on-1-ylcarbonylamino)-substutited acetamido]penicillanic acids, and the correspondingly 7-substituted ceph-3-em-4-carboxylic acids, characterized by the presence of a methyleneamino or substituted methyleneamino group on the 3-nitrogen atom of the imidazolidine ring are antibacterial agents. The compounds, of which 6-[.alpha.-(3-benzaliminoimidazolidin-2-on-1-ylcarbonylamino)cyclohexa-1,4-dien-1-ylacetamido]penicillanic acid and 7-[.alpha.-(3-furylideneaminoimidazolidin-2-on-1-ylcarbonylamino)phenylacetamido]-3-(3-methylthiadiazol-5-ylthiomethyl)ceph-3-em-4-carboxylic acid are typical examples, are prepared through acylation of an 6-[.alpha.-(amino)substituted acetamido]penicillanic acid or the corresponding 7-[.alpha.-(amino)substituted acetamido]ceph-3-em-4-carboxylic acid with a reactive nucleofugic derivative of a 3-methyleneaminoimidazolidin-2-on-1-carboxylic acid.
摘要翻译： 6- [α-（咪唑烷-2-酮-1-基羰基氨基） - 亚氨基乙酰氨基]青霉烷酸和相应的7-取代的头孢-3-烯-4-羧酸，其特征在于存在亚甲基氨基或取代的亚甲基氨基咪唑烷环的3-氮原子上的基团是抗菌剂。其中6-（α-（3-亚苄基亚氨基咪唑烷-2-酮-1-基羰基氨基）环己-1,4-二烯-1-基乙酰胺基]青霉烷酸和7- [3-（3-亚芳基氨基咪唑烷-2-基） 1-基羰基氨基）苯乙酰氨基] -3-（3-甲基噻二唑-5-基硫甲基）头孢-3-烯-4-羧酸是典型的实例，通过酰化6- [α-（氨基）取代的乙酰氨基 ]青霉烷酸或相应的7- [α-（氨基）取代的乙酰氨基]头孢-3-烯-4-羧酸与3-亚甲基氨基咪唑烷-2-酮-1-羧酸的反应性核苷衍生物。

96. 发明授权

US5508278A Pyrido[1,2,3-D,E] [1,3,4]benzoxadiazine derivatives 失效
标题翻译：吡啶并[1,2,3-D，E] [1,3,4]苯并恶二嗪衍生物
公开(公告)号：US5508278A
公开(公告)日：1996-04-16
申请号：US296944
申请日：1994-08-26
申请人： Thomas Jaetsch , Burkhard Mielke , Uwe Petersen , Thomas Philipps , Thomas Schenke , Klaus D. Bremm , Rainer Endermann , Karl G. Metzger , Martin Scheer , Michael Stegemann , Heinz-Georg Wetzstein
发明人： Thomas Jaetsch , Burkhard Mielke , Uwe Petersen , Thomas Philipps , Thomas Schenke , Klaus D. Bremm , Rainer Endermann , Karl G. Metzger , Martin Scheer , Michael Stegemann , Heinz-Georg Wetzstein
IPC分类号： A61K31/535 , A61K31/435 , A61K31/47 , A61P31/04 , C07D209/48 , C07D215/58 , C07D401/04 , C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04 , C07D498/06 , C07D519/00 , C07D273/04 , A01N43/88
CPC分类号： C07D498/06 , C07D519/00
摘要： Novel bactericidal pyrido[1,2,3-d,e,][1,3,4]benzoxadiazine derivatives of the formula (I) ##STR1## in which R.sup.1 is hydrogen or C.sub.1 -C.sub.4 -alkyl optionally substituted by hydroxyl or halogen,R.sup.2 independently of R.sup.1 is hydrogen or methyl,R.sup.3 is hydrogen or C.sub.1 -C.sub.4 -alkyl,R.sup.4 is hydrogen, C.sub.1 -C.sub.4 -alkyl optionally substituted by hydroxyl, methoxy, amino, methylamino or dimethylamino, or (5-methyl-2-oxo-1,3-dioxol-4-yl)-methyl,X.sup.1 is hydrogen or halogen andZ is a radical of the structure ##STR2##
摘要翻译：式（I）的新型杀菌吡啶并[1,2,3-d，e，] [1,3,4]苯并恶嗪衍生物其中R 1为氢或任选被羟基或卤素，R 2独立地为R 1为氢或甲基，R 3为氢或C 1 -C 4 - 烷基，R 4为氢，任选被羟基，甲氧基，氨基，甲基氨基或二甲基氨基取代的C 1 -C 4烷基，或（5-甲基 -2-氧代-1,3-二氧杂环戊烯-4-基） - 甲基，X 1是氢或卤素，Z是结构的基团

97. 发明授权

US4223037A .beta.-Lactam antibiotics and their use 失效
标题翻译： β-内酰胺抗生素及其用途
公开(公告)号：US4223037A
公开(公告)日：1980-09-16
申请号：US900402
申请日：1978-04-26
申请人： Michael Preiss , Karl G. Metzger
发明人： Michael Preiss , Karl G. Metzger
IPC分类号： C07D499/66 , A61K31/43 , A61K31/44 , A61K31/535 , A61K31/545 , A61K31/546 , A61P31/04 , C07D233/32 , C07D233/38 , C07D463/00 , C07D499/00 , C07D499/64 , C07D499/68 , C07D499/70 , C07D501/20 , C07D505/00
CPC分类号： C07D499/00 , C07D233/32 , C07D233/38
摘要： New .beta.-lactam antibiotics of the formula ##STR1## in which A is hydrogen or methoxy,B is phenyl optionally substituted by hydroxyl, halogen, methoxy, --CN and/or CH.sub.3 --SO.sub.2 --; thienyl; cyclohexenyl; 1,4-cyclohexadien-1-yl; or furyl,E is oxygen or sulphur,n is an integer having a value of 1 or 2,Y is a group of the formula ##STR2## T is hydrogen, alkyl--CO--O--, hydroxyl, pyridinium, aminopyridinium, carbamoyloxy, azido, cyano, optionally N-substituted thiocarbamoylthio, optionally substituted-S-phenyl, or a --S--Het group in which Het represents an optionally substituted heterocyclic 5-membered or 6-membered ring,U is oxygen, sulphur or --CH.sub.2 --,Z is a group of the formula ##STR3## R.sup.1, R.sup.2 and R.sup.3 each is hydrogen or various organic radicals, i.e. compounds wherein Z is an olefinic or hydrated olefinic radical directly connected to the ring nitrogen, or salts thereof, are antibacterially active and useful as antibiotics in pharmacy, as animal feed supplements for promoting growth, and as preservatives.
摘要翻译：式中，A为氢或甲氧基的新型β-内酰胺抗生素，B为任选被羟基，卤素，甲氧基，-CN和/或CH 3 SO 2取代的苯基; 噻吩基环己烯基 1,4-环己二烯-1-基; 或呋喃基，E是氧或硫，n是1或2的整数，Y是下式的基团：T是氢，烷基-CO-O-，羟基，吡啶鎓，氨基吡啶鎓，氨基甲酰氧基，叠氮基，氰基，任选N-取代的硫代氨基甲酰硫基，任选取代的S-苯基或-S-Het基团，其中Het表示任选取代的杂环5元或6元环，U是氧，硫或-CH 2 - Z是下式的基团：R 1，R 2和R 3各自为氢或各种有机基团，即其中Z为与环氮直接连接的烯属或水合烯属基团或其盐是具有抗菌活性的化合物，作为药剂中的抗生素，作为用于促进生长的动物饲料补充剂和作为防腐剂。

98. 发明授权

US5631291A Cyclopentane- and -pentene-.beta.-amino acids 失效
标题翻译：环戊烷和β-戊烯-β-氨基酸
公开(公告)号：US5631291A
公开(公告)日：1997-05-20
申请号：US336584
申请日：1994-11-09
申请人： Joachim Mittendorf , Franz Kunisch , Michael Matzke , Hans-Christian Militzer , Rainer Endermann , Karl G. Metzger , Klaus-Dieter Bremm , Manfred Plempel
发明人： Joachim Mittendorf , Franz Kunisch , Michael Matzke , Hans-Christian Militzer , Rainer Endermann , Karl G. Metzger , Klaus-Dieter Bremm , Manfred Plempel
IPC分类号： C07C61/15 , C07C61/20 , C07C61/35 , C07C61/39 , C07C61/40 , C07C69/74 , C07C69/753 , C07C69/757 , C07C229/48 , C07C237/04 , C07C251/42 , C07C271/22 , C07C271/24 , C07C271/34 , C07C271/36 , C07D265/12 , C07D307/93 , A61K31/195
CPC分类号： C07C251/42 , C07C229/48 , C07C237/04 , C07C271/22 , C07C271/24 , C07C271/34 , C07C271/36 , C07C61/15 , C07C61/20 , C07C61/35 , C07C61/39 , C07C61/40 , C07C69/74 , C07C69/753 , C07C69/757 , C07D265/12 , C07D307/93 , C07C2101/08 , C07C2101/10 , C07C2103/18
摘要： The invention relates to cyclopentane- and -pentene-.beta.-amino acids, processes for their preparation and their use as medicaments.
摘要翻译：本发明涉及环戊烷和戊烯-β-氨基酸，其制备方法及其作为药物的用途。

99. 发明授权

US5605910A Quinolone-and naphthyridonecarboxylic acid derivatives 失效
标题翻译：喹诺酮和萘啶酮羧酸衍生物
公开(公告)号：US5605910A
公开(公告)日：1997-02-25
申请号：US508603
申请日：1995-07-28
申请人： Uwe Petersen , Thomas Schenke , Thomas Jaetsch , Stephan Bartel , Klaus D. Bremm , Rainer Endermann , Karl G. Metzger
发明人： Uwe Petersen , Thomas Schenke , Thomas Jaetsch , Stephan Bartel , Klaus D. Bremm , Rainer Endermann , Karl G. Metzger
IPC分类号： C07D215/56 , A01N43/42 , A01N43/90 , A61K31/40 , A61K31/47 , A61K31/495 , A61K31/535 , A61P31/04 , C07D209/56 , C07D209/90 , C07D215/233 , C07D221/02 , C07D401/04 , C07D471/04 , C07D498/06 , C07D513/04 , C07D513/06 , C07D513/16 , C07D215/227 , A61K31/475 , C07D215/44
CPC分类号： C07D401/04 , C07D471/04 , C07D498/06 , C07D513/04 , C07D513/16
摘要： The invention relates to new quinolone- and naphthyridonecarboxylic acid derivatives which are substituted in the 7-position by a tricyclic amine radical, their salts, processes for their preparation and antibacterial compositions comprising these compounds.
摘要翻译：本发明涉及通过三环胺基，其盐，其制备方法和包含这些化合物的抗菌组合物在7位上被取代的新的喹诺酮和萘啶酮羧酸衍生物。

100. 发明授权

US4416870A Antibiotic compound, its production and its medicinal use 失效
标题翻译：抗生素，其生产及其药用
公开(公告)号：US4416870A
公开(公告)日：1983-11-22
申请号：US340418
申请日：1982-01-18
申请人： Karl G. Metzger , Jorg Pfitzner , Delf Schmidt , Horst Weyland , Gunter Benz , Theo Schroder
发明人： Karl G. Metzger , Jorg Pfitzner , Delf Schmidt , Horst Weyland , Gunter Benz , Theo Schroder
IPC分类号： C12P19/38 , A61K31/70 , A61K38/00 , A61P31/04 , C07K1/22 , C07K7/06 , C07K9/00 , C07K14/195 , C07K14/41 , C12P21/02 , C12R1/465 , C07C103/52 , A61K31/495
CPC分类号： C07K7/06 , C12R1/465 , A61K38/00 , Y10S930/19
摘要： The invention relates to an antibiotic compound which can be in the iron-free or iron-containing form and has the structural formula (A) as described herein. The compound possesses antimicrobial activity. Also included in the invention are fermentation processes for preparation of the above-mentioned antibiotic compound. In addition, the invention includes pharmaceutical compositions containing said antibiotic compound and the use of said antibiotic compound and compositions for combating bacterial infections.
摘要翻译：本发明涉及一种抗生素化合物，其可以是无铁或含铁形式，并具有如本文所述的结构式（A）。该化合物具有抗菌活性。本发明还包括用于制备上述抗生素化合物的发酵方法。此外，本发明包括含有所述抗生素化合物的药物组合物和所述抗生素化合物和用于对抗细菌感染的组合物的用途。

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