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31. 发明授权

US4980353A 1-aryl-4-quinolone-3-carboxylic acids 失效
标题翻译： 1-芳基-4-喹诺酮-3-羧酸
公开(公告)号：US4980353A
公开(公告)日：1990-12-25
申请号：US862863
申请日：1986-05-13
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： A23K1/16 , A61K31/47 , A61K31/495 , A61P3/00 , A61P31/04 , C07C67/00 , C07C201/00 , C07C205/58 , C07C205/61 , C07D215/56 , C07D401/04
CPC分类号： C07D215/56 , C07C205/58 , C07C205/61 , C07D401/04
摘要： Antibacterially active and animal growth promoting novel 1-aryl-4-quinolone-3-carboxylic acids of the formula ##STR1## in which X is halogen or nitro,X.sup.2 is halogen,R is optionally substituted phenyl, andA is halogen or optionally substituted piperazine or pyrrolidine,or pharmaceutically useable hydrates, acid additions salts, alkali metal, alkaline earth metal, silver or guanidinium salts thereof, and/or esters thereof.
摘要翻译：促进新的式（ⅠA-芳基-4-喹诺酮-3-羧酸，其中X是卤素或硝基，X 2是卤素，R是任意取代的苯基，A是卤素或任意取代的）哌嗪或吡咯烷，或其药学上可用的水合物，酸加成盐，碱金属，碱土金属，银或胍盐，和/或其酯。

32. 发明授权

US4973685A Heteroannellated phenylglycine-.beta.-lactam antibiotics 失效
标题翻译：异烟肼苯基甘氨酸-β-内酰胺抗生素
公开(公告)号：US4973685A
公开(公告)日：1990-11-27
申请号：US250597
申请日：1988-09-28
申请人： Gunter Schmidt , Karl G. Metzger , Hans-Joachim Zeiler
发明人： Gunter Schmidt , Karl G. Metzger , Hans-Joachim Zeiler
IPC分类号： A61K31/43 , A61K31/545 , A61K31/546 , A61P31/04 , C07D499/00 , C07D499/64 , C07D499/68 , C07D499/70 , C07D499/90 , C07D501/20 , C07D501/34 , C07D501/36 , C07D501/46 , C07D501/56
CPC分类号： C07D499/00
摘要： Heteroannellated penicillins and cephalosporins of the formula ##STR1## in which R.sup.1 --stands for a radical of the formula ##STR2##
摘要翻译：具有式（Ⅰ）的无意义的青霉素和头孢菌素，其中R1代表下式的基团： + TR

33. 发明授权

US4847375A Antibacterial 1,8-bridged 4-quinoline-3-carboxylic acids 失效
标题翻译：抗菌1,8桥桥4-喹啉-3-羧酸
公开(公告)号：US4847375A
公开(公告)日：1989-07-11
申请号：US874249
申请日：1986-06-13
申请人： Klaus Grohe , Michael Schriewer , Hans-Joachim Zeiler , Karl G. Metzger
发明人： Klaus Grohe , Michael Schriewer , Hans-Joachim Zeiler , Karl G. Metzger
IPC分类号： A61K31/535 , A61K31/55 , A61P31/04 , C07D471/06 , C07D498/06
CPC分类号： C07D471/06
摘要： As antibacterials and animal growth promoters, the compounds of the formula ##STR1## in which Y is --COOH, --COOR.sup.7 or --CONR.sup.8, R.sup.9,X.sup.1 is H, nitro, alkyl or halogen,R.sup.10 and R.sup.11 preferably complete a piperazine ring,Z is oxygen or NR.sup.15,n is 0 or 1, andthe others can have various meanings,and pharmaceutically acceptable hydrate, alkali metal, alkaline earth metal, silver or guanidinium salt or ester thereof.
摘要翻译：作为抗菌剂和动物生长促进剂，其中Y是-COOH，-COOR7或-CONR8，R9，X1的式“IMAGE”的化合物是H，硝基，烷基或卤素，R10和R11优选完成哌嗪环Z 是氧或NR15，n是0或1，其他可以具有各种含义，以及药学上可接受的水合物，碱金属，碱土金属，银或胍盐或其酯。

34. 发明授权

US4840946A Benzazolythio-carbapenem antibiotics 失效
标题翻译：苯扎硫代碳青霉烯类抗生素
公开(公告)号：US4840946A
公开(公告)日：1989-06-20
申请号：US119752
申请日：1987-11-12
申请人： Dieter Habich , Wolfgang Hartwig , Karl G. Metzger , Hans-Joachim Zeiler
发明人： Dieter Habich , Wolfgang Hartwig , Karl G. Metzger , Hans-Joachim Zeiler
IPC分类号： C07D477/00 , A61K31/397 , A61K31/41 , A61P31/04 , C07D477/20
CPC分类号： C07D477/20 , Y02P20/55
摘要： Antibiotically active benzazolylthio-carbapenems of the formula ##STR1## in which R.sup.1 represents hydrogen or a hydroxyl-protecting group,R.sup.2 represents hydrogen or a carboxyl-protecting group or an ester radical which can be cleaved off in vivo,R.sup.3 represents hydrogen or C.sub.1 -C.sub.10 -alkyl, C.sub.6 -C.sub.12 -aryl or C.sub.7 -C.sub.14 -aralkyl,R.sup.4 represents hydrogen or represents C.sub.1 -C.sub.10 -alkyl, C.sub.6 -C.sub.12 -aryl or C.sub.7 -C.sub.14 aralkyl, or represents C.sub.1 -C.sub.10 -alkylsulphonyl, C.sub.6 -C.sub.12 -arylsulphonyl or C.sub.7 -C.sub.14 -aralkylsulphonyl, or represents an amino-protecting group, or represents a group of the formula ##STR2## in which R.sup.5, R.sup.6 and R.sup.8 are indentical or different and denote hydrogen, C.sub.1 -C.sub.10 -alkyl, C.sub.6 -C.sub.12 -aryl or C.sub.7 -C.sub.14 -aralkyl,andX represents O, S, NH or NCH.sub.3,or salts thereof.
摘要翻译：其中R 1表示氢或羟基保护基，R 2表示氢或羧基保护基或可在体内被切割的酯基的式为“IMAGE”的抗生素活性苯并唑基硫代碳青霉烯类，R3表示氢或C1- C 1 -C 12 - 芳基或C 7 -C 14 - 芳烷基，R 4表示氢或C 1 -C 10 - 烷基，C 6 -C 12 - 芳基或C 7 -C 14芳烷基，或表示C 1 -C 10 - 烷基磺酰基，C 6 -C 12 - 或芳基磺酰基或C 7 -C 14 - 芳烷基磺酰基，或表示氨基保护基，或表示其中R 5，R 6和R 8表示氢，C 1 -C 10 - 烷基，C 6 -C 12 芳基或C 7 -C 14 - 芳烷基，X表示O，S，NH或NCH 3或其盐。

35. 发明授权

US4757065A Cephalosporins 失效
公开(公告)号：US4757065A
公开(公告)日：1988-07-12
申请号：US673246
申请日：1984-11-20
申请人： Rolf Angerbauer , Michael Boberg , Karl G. Metzger , Hans-Joachim Zeiler
发明人： Rolf Angerbauer , Michael Boberg , Karl G. Metzger , Hans-Joachim Zeiler
IPC分类号： A61K20060101 , A61K31/545 , A61K31/546 , A61P31/04 , C07D20060101 , C07D501/00 , C07D501/18 , C07D501/34 , C07D501/38 , C07D501/46 , C07D501/56
CPC分类号： C07D501/46
摘要： Antibacterially effective cephalosporins of the formula ##STR1## in which R.sup.1 denotes C.sub.1 -C.sub.6 -alkyl, phenyl or halogen-substituted phenyl andA represents a nitrogen-containing, positively charged heterocyclic 5-membered to 7-membered ring which is bonded via N and can contain a total of up to 4 hetero-atoms from the group comprising N, O and S, and onto which up to two further rings can be fused, and which can optionally be substituted, with the proviso that, if the ring is a 6-membered ring, A does not represent an unsubstituted pyridine ring or a pyridine ring which is mono- or di-substituted by identical or different substituents from the group comprising C.sub.1 -C.sub.4 -alkyl, chlorine, bromine, carbamoyl or N--C.sub.1 -C.sub.4 -alkylcarbamoyl,or pharmaceutically acceptable salts thereof or esters thereof which can be split under physiological conditions.

36. 发明授权

US4703047A 1-Cyclopropyl-1,4-dihydro-4-oxo-7-(4-(2-oxo-1,3-dioxol-4-yl- methyl)-1-piperazinyl)-3-quinolinecarboxylic acid antibacterial agents 失效
标题翻译： 1-环丙基-1,4-二氢-4-氧代-7-（4-（2-氧代-1,3-二氧杂环戊烯-4-基 - 甲基）-1-哌嗪基）-3-喹啉羧酸抗菌剂
公开(公告)号：US4703047A
公开(公告)日：1987-10-27
申请号：US822714
申请日：1986-01-27
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： A61K31/495 , A61P31/04 , A61P33/02 , C07D215/56 , C07D317/00 , C07D333/00 , C07D401/04 , C07D405/12 , C07D405/14 , C07D409/14
CPC分类号： C07D215/56 , C07D401/04 , C07D405/12 , C07D405/14 , C07D409/14
摘要： Novel antibacterially active 1-cyclopropyl-1,4-dihydro-4-oxo-7-[4-(2-oxo-1,3-dioxol-4-yl-methyl)-1-piperazinyl]-3-quinolinecarboxyic acids of the formula in which ##STR1## R is hydrogen or, together with R.sup.1, forms an alkylene radical with 2 or 3 carbon atoms,R.sup.1 is hydrogen, alkyl with 1 to 4 carbon atom or phenyl,R.sup.2 and R.sup.3 each independently is hydrogen, methyl, ethyl, cyclohexyl, methylene-dioxphenyl, furyl, tetrahydrofuryl or thienyl; or phenyl which is optionally mono-, di or tri-substituted by fluorine, chlorine, bromine, methyl, phenyl, cyano, hydroxyl, ethoxy, benzyloxy, amino, methylamino, dimethylamino, piperidino or nitro,X.sup.1 is hydrogen, halogen, or nitro, andX.sup.2 is hydrogen or halogen,or pharmaceutically acceptable hydrates, acid addition salts, alkali metal salts or alkaline earth metal salts thereof.
摘要翻译：新型抗菌活性1-环丙基-1,4-二氢-4-氧代-7- [4-（2-氧代-1,3-二氧杂环戊烯-4-基 - 甲基）-1-哌嗪基] -3-喹啉羧酸其中 R是氢或与R1一起形成具有2或3个碳原子的亚烷基的式，R 1是氢，具有1至4个碳原子的烷基或苯基，R 2和R 3各自独立地是氢，甲基乙基，环己基，亚甲基二氧苯基，呋喃基，四氢呋喃基或噻吩基; 或苯基，其任选被氟，氯，溴，甲基，苯基，氰基，羟基，乙氧基，苄氧基，氨基，甲基氨基，二甲基氨基，哌啶子基或硝基单，二或三取代，X 1为氢，卤素或硝基，X2为氢或卤素，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。

37. 发明授权

US4670444A 7-amino-1-cyclopropyl-4-oxo-1, 4-dihydro-quinoline-and naphthyridine-3-carboxylic acids and antibacterial agents containing these compounds 失效
标题翻译： 7-氨基-1-环丙基-4-氧代-1,4-二氢 - 喹啉和萘啶-3-羧酸和含有这些化合物的抗菌剂
公开(公告)号：US4670444A
公开(公告)日：1987-06-02
申请号：US614923
申请日：1984-05-29
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 , A61K31/495 , C07D521/00
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 specification. 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：本发明涉及说明书中定义的式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。

38. 发明授权

US4632918A Novel .beta.-lactam antibiotics 失效
标题翻译：新型β-内酰胺抗生素
公开(公告)号：US4632918A
公开(公告)日：1986-12-30
申请号：US730979
申请日：1985-05-06
申请人： Rolf Angerbauer , Michael Boberg , Karl G. Metzger , Hans-Joachim Zeiler
发明人： Rolf Angerbauer , Michael Boberg , Karl G. Metzger , Hans-Joachim Zeiler
IPC分类号： A23K20060101 , A23K1/17 , A23K3/02 , A61K20060101 , A61K31/545 , A61K31/546 , A61P31/04 , C07D20060101 , C07D277/40 , C07D417/12 , C07D417/14 , C07D501/16 , C07D501/18 , C07D501/24 , C07D501/38 , C07D501/46 , C07D501/56 , C09K20060101 , C09K15/30
CPC分类号： C07D501/46 , C07D501/18
摘要： Novel .beta.-lactam antibiotics of the formula ##STR1## in which R.sup.1, R.sup.2 and R.sup.3, which may be identical or different, denote a substituted or unsubstituted alkyl radical or a monocyclic or bicyclic, optionally substituted, carbocyclic or heterocyclic ring, orR.sup.1 represents an optionally substituted alkyl radical or a monocyclic or bicyclic, substituted or unsubstituted, carbocyclic or heterocyclic ring, andR.sup.2 and R.sup.3, together with the N.sup..sym. atom, form an optionally substituted monocyclic or polycyclic ring which can be saturated or unsaturated and can contain oxygen, sulphur and nitrogen as other hetero atoms, orR.sup.1, R.sup.2 and R.sup.3, together with the N.sup..sym. atom, form a bridged, optionally substituted polycyclic ring which can be saturated or unsaturated and can contain oxygen, sulphur and nitrogen as other hetero atoms, andR.sup.4 represents hydrogen or optionally substituted alkyl, aryl or heterocyclyl or hydroxycarbonyl, lower alkoxycarbonyl, halogen, pseudohalogen or a group of the formula ##STR2## in which n denotes 0, 1 or 2, andB represents a direct bond, oxygen or a group ##STR3## and A and W, independently of one another, represent hydrogen or optionally substituted alkyl, aryl or heterocyclyl, or together form an optionally substituted carbocyclic or heterocyclic ring.
摘要翻译：新颖的具有式“IMAGE”的β-内酰胺抗生素，其中R1，R2和R3可以相同或不同，表示取代或未取代的烷基或单环或双环，任选取代的碳环或杂环，或R 1表示任选取代的烷基或单环或双环，取代或未取代的碳环或杂环，并且R 2和R 3与N（+）原子一起形成可以是饱和或不饱和的任选取代的单环或多环，含有氧，硫和氮作为其它杂原子，或者R 1，R 2和R 3与N（+）原子一起形成可以是饱和或不饱和的并且可以含有氧，硫和氮的桥连的任选取代的多环，其它杂原子，R 4表示氢或任选取代的烷基，芳基或杂环基或羟基羰基，低级烷氧基羰基，卤素，假卤素或式IMAG E>其中n表示0,1或2，B表示直接键，氧或基团，且A和W彼此独立地表示氢或任选取代的烷基，芳基或杂环基，或一起形成任选取代的碳环或杂环。

39. 发明授权

US4631275A 1-Oxadethiacephalosporin derivatives and antibacterial use thereof 失效
标题翻译： 1-硫代十八烷基醚衍生物及其抗菌用途
公开(公告)号：US4631275A
公开(公告)日：1986-12-23
申请号：US696275
申请日：1985-01-30
申请人： Wolfgang Hartwig , Dieter Habich , Karl G. Metzger , Hans-Joachim Zeiler
发明人： Wolfgang Hartwig , Dieter Habich , Karl G. Metzger , Hans-Joachim Zeiler
IPC分类号： A61K31/535 , A61P31/04 , C07D498/04 , C07D505/00 , A01N43/90
CPC分类号： C07D505/00
摘要： 1-Oxadethiacephalosporin derivatives of the formula ##STR1## in which R.sup.1 denotes hydrogen or halogen,R.sup.2 denotes hydrogen or methoxy,A is a nitrogen-containing positively charged N-containing heterocyclic 5-membered to 7-membered ring which in total can contain up to 4 heteroatoms from the group of N, O and S, to which ring up to two further rings can be fused and which ring may optionally be substituted, the ring being bonded via N,B denotes optionally substituted alkoxy or amino, and the remaining radicals are more or less conventional,which are antibacterially active.
摘要翻译：式中，R1表示氢或卤素，R2表示氢或甲氧基的式“IMAGE”的1-硫代十八烷基醚衍生物，A是含氮带正电荷的含氮杂环的5元至7元环，其总共可含有至4个来自N，O和S的杂原子，其中多达两个另外的环可以被稠合并且哪个环可以被任选取代，该环通过N键合，B表示任选取代的烷氧基或氨基，剩余的自由基或多或少是常规的，其具有抗菌活性。

40. 发明授权

US4535083A Cleavage products of 4',6'-didesoxy-4'-thio-,6'-amino-hepturonic acid nucleosides 失效
标题翻译： 4'，6'-二氧代-4'-硫代 - ，6'-氨基 - 七糖醛酸核苷的切割产物
公开(公告)号：US4535083A
公开(公告)日：1985-08-13
申请号：US530835
申请日：1983-09-09
申请人： Gunter Benz , Karl G. Metzger , Hans-Joachim Zeiler
发明人： Gunter Benz , Karl G. Metzger , Hans-Joachim Zeiler
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61P31/04 , C07H19/06 , C12P19/38 , A61K31/505 , C07D239/47 , C07D239/54
CPC分类号： C07H19/06 , C12P19/38
摘要： The invention relates to compounds of the formula ##STR1## said compounds being obtainable by cleavage of compounds of formula ##STR2## The compounds of the invention as well as compositions and medicaments containing a compound of the invention are useful as antimicrobial agents.
摘要翻译：本发明涉及下式的化合物：（1）所述化合物可通过将下式化合物裂解而获得：（2）本发明化合物以及含有本发明化合物的组合物和药物可用作抗菌剂。

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