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公开(公告)号:US4344955A
公开(公告)日:1982-08-17
申请号:US158975
申请日:1980-06-12
IPC分类号: A61K31/43 , A61P31/04 , C07D499/00 , C07D499/04 , C07D499/44 , C07D499/46 , C07D499/56 , C07D499/60 , C07D499/64 , C07D499/68 , C07D499/70 , C07D499/72 , C07D499/74 , C07D499/76 , C07D499/78
CPC分类号: C07D499/00 , A61K31/43
摘要: Anti-bacterially active 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 or optionally substituted alkoxy group,R.sub.3 denotes a hydrogen atom, COR.sub.4, SO.sub.2 -alkyl, SO.sub.2 -aryl or an optionally substituted alkyl group, but R.sub.2 and R.sub.3 do not simultaneously denote hydrogen atoms, andR.sub.4 denotes a hydrogen atom or any of many possible organic radicals.The compounds are also inhibitors of .beta.-lactamases so they can be used in conjunction with .beta.-lactamase-susceptible antibiotics. They are useful in fighting bacterial infection, in promoting animal growth and in preserving various materials.
摘要翻译: 其中R1表示氢原子或成酯基团的式为“IMAGE”或其盐的抗细菌活性青霉素1,1-二氧化物,R 2表示氢原子或任选取代的烷氧基,R 3表示氢 原子,COR 4,SO 2 - 烷基,SO 2 - 芳基或任选取代的烷基,但R 2和R 3不同时表示氢原子,R 4表示氢原子或许多可能的有机基团中的任何一种。 这些化合物也是β-内酰胺酶的抑制剂,因此它们可以与β-内酰胺酶敏感的抗生素联合使用。 它们有助于消灭细菌感染,促进动物生长和保存各种材料。
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公开(公告)号:US4344939A
公开(公告)日:1982-08-17
申请号:US154541
申请日:1980-05-29
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。
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公开(公告)号:US4147693A
公开(公告)日:1979-04-03
申请号:US631515
申请日:1975-11-13
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。
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公开(公告)号:US4386089A
公开(公告)日:1983-05-31
申请号:US276762
申请日:1981-06-24
申请人: Hans-Bodo Konig , Karl G. Metzger , Michael Preiss
发明人: Hans-Bodo Konig , Karl G. Metzger , Michael Preiss
IPC分类号: C07D499/70 , A61K31/43 , A61P31/04 , C07D233/38 , C07D277/20 , C07D277/48 , C07D499/00 , C07D499/46 , C07D499/64 , C07D501/20 , C07D501/34 , C07D501/36 , A61K31/545
CPC分类号: C07D277/20 , C07D233/38 , C07D277/48 , C07D499/00
摘要: .beta.-Lactam compounds of the formula ##STR1## in which B denotes an optionally substituted heterocyclic 5-membered or 6-membered ring or an optionally substituted phenyl ring,Z denotes a hydrogen atom or a C.sub.1 to C.sub.4 alkoxy group, ##STR2## Y, E.sub.1 and E.sub.2 independently of one another denote a divalent organic radical andR.sub.1, R.sub.2, R.sub.3 and R.sub.4 independently of one another denote a hydrogen atom or an alkyl, alkenyl, alkinyl, alkadienyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, aryl or heterocyclyl radical, it also being possible for the above-mentioned radicals, with the exception of hydrogen, to be substituted, or an acyl radical,are antibacterial agents with a broad antibacterial spectrum and are useful as agents for promoting growth and for improving feed utilization in animals and as antioxidants.
摘要翻译: 式(I)的β-内酰胺化合物,其中B表示任选取代的杂环5元或6元环或任选取代的苯环,Z表示氢原子或C1至C4烷氧基, Y,E1和E2彼此独立地表示二价有机基团,R 1,R 2,R 3和R 4彼此独立地表示氢原子或烷基,烯基,炔基,链烯基,环烷基,环烯基 ,环链二烯基,芳基或杂环基,除了氢被取代以外,上述基团也可以是酰基,是具有广谱抗菌谱的抗菌剂,并且可用作促进生长的试剂 并提高动物和抗氧化剂的饲料利用率。
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公开(公告)号:US4235774A
公开(公告)日:1980-11-25
申请号:US11347
申请日:1979-02-12
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。
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公开(公告)号:US4338434A
公开(公告)日:1982-07-06
申请号:US45474
申请日:1979-06-04
申请人: Michael Preiss , Hans-Bodo Konig , Karl G. Metzger , Peter Feyen
发明人: Michael Preiss , Hans-Bodo Konig , Karl G. Metzger , Peter Feyen
IPC分类号: A61K31/43 , A61K31/545 , A61K31/546 , A61P31/04 , C07D231/12 , C07D277/20 , C07D277/48 , C07D307/54 , C07D499/00 , C07D499/64 , C07D499/68 , C07D499/70 , C07D501/20 , C07D501/34 , C07D501/46 , C07D501/57
CPC分类号: C07D231/12 , C07D277/48 , C07D277/587 , C07D307/54 , C07D499/00
摘要: 2-Hetero-acetamido-penicillanates and cephalosporinates of the formula ##STR1## in which R is hydrogen or lower alkoxy,Z is ##STR2## R.sup.1 and R .sup.2 independently or together are various radicals, A is --CH.sub.2 --CH.sub.2 --,--CH.sub.2 --CH.sub.2 --CH.sub.2 -- or ##STR3## n is 1 or 2, X is S,O,SO,SO.sub.2 or --CH.sub.2 --,Y is the balance of a penicillin or cephalosporin moiety, andB is a heterocyclic radical, in the form of the acid, a hydrate thereof, a salt thereof or a salt of the hydrate, exhibit marked anti-bacterial properties rendering them suited for use as antibiotics and animal feed supplements.
摘要翻译: 其中R为氢或低级烷氧基的式“IMAGE”的2-异 - 乙酰氨基 - 青霉烷酸和头孢菌素,Z为独立地或一起为不同的基团,A为-CH 2 -CH 2 - , - CH 2 -CH 2 -CH 2 - 或
n为1或2,X为S,O,SO,SO 2或-CH 2 - ,Y为青霉素或头孢菌素部分的余量,B为杂环基, 的酸,其水合物,其盐或水合物的盐表现出显着的抗菌性质,使其适合用作抗生素和动物饲料添加剂。 -
公开(公告)号:US4218451A
公开(公告)日:1980-08-19
申请号:US920505
申请日:1978-06-29
申请人: Peter Feyen , Hans-Bodo Konig , Karl G. Metzger
发明人: Peter Feyen , Hans-Bodo Konig , Karl G. Metzger
IPC分类号: C07D499/66 , A61K31/43 , A61K31/495 , A61P31/04 , C07D499/00 , C07D499/04 , C07D499/21 , C07D499/64 , C07D499/68
CPC分类号: C07D499/00
摘要: New penicillins of the formula ##STR1## in which ##STR2## E is oxygen or sulphur, and R.sub.1 and R.sub.2 are hydrogen or various organic radicals with certain provisos,or salts thereof, are antibacterially ative and useful as antibiotics in pharmacy, as animal feed supplements for promoting growth, and as preservatives.
摘要翻译: 其中
E是氧或硫,R1和R2是氢或具有某些条件的各种有机基团或其盐的新型青霉素具有抗菌活性并且可用作抗生素 在药房,作为促进生长的动物饲料补充剂和防腐剂。 -
公开(公告)号:US4215118A
公开(公告)日:1980-07-29
申请号:US923518
申请日:1978-07-10
申请人: Michael Preiss , Hans-bodo Konig , Karl G. Metzger , Peter Feyen
发明人: Michael Preiss , Hans-bodo Konig , Karl G. Metzger , Peter Feyen
IPC分类号: A61K31/43 , A61K31/545 , A61K31/546 , A61P31/04 , C07D231/12 , C07D277/20 , C07D277/48 , C07D307/54 , C07D499/00 , C07D499/64 , C07D499/68 , C07D499/70 , C07D501/20 , C07D501/34 , C07D501/46 , C07D501/57 , A61K31/535 , C07D499/44
CPC分类号: C07D231/12 , C07D277/48 , C07D277/587 , C07D307/54 , C07D499/00
摘要: 2-Hetero-acetamido-penicillanates and cephalosporinates of the formula ##STR1## in which R is hydrogen or lower alkoxy,Z is ##STR2## R.sup.1 and R.sup.2 independently or together are various radicals, A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 -- or ##STR3## n is 1 or 2, X is S,O,SO,SO.sub.2 or --CH.sub.2 --,Y is the balance of a penicillin or cephalosporin moiety, andB is a heterocyclic radical, in the form of the acid, a hydrate thereof, a salt thereof or a salt of the hydrate, exhibit marked anti-bacterial properties rendering them suited for use as antibiotics and animal feed supplements.
摘要翻译: 其中R是氢或低级烷氧基的式“IMAGE”的2-异 - 乙酰氨基 - 青霉烷酸酯和头孢烯酸酯,Z独立地或一起是各种基团,A是-CH 2 -CH 2 - , - CH2-CH2-或
n为1或2,X为S,O,SO,SO2或-CH2-,Y为青霉素或头孢菌素部分的余量,B为杂环基, 酸,其水合物,其盐或水合物的盐表现出显着的抗菌性能,使其适合用作抗生素和动物饲料添加剂。 -
公开(公告)号:US4626535A
公开(公告)日:1986-12-02
申请号:US566975
申请日:1983-12-30
申请人: Rolf Angerbauer , Michael Boberg , Gunther Kinast , Karl G. Metzger , Wilfried Schrock , Hans-Joachim Zeiler
发明人: Rolf Angerbauer , Michael Boberg , Gunther Kinast , Karl G. Metzger , Wilfried Schrock , Hans-Joachim Zeiler
IPC分类号: A61K31/545 , A61K31/546 , A61P31/04 , C07D285/08 , C07D417/06 , C07D501/20 , C07D501/34 , C07D501/36 , C07D501/46 , C07D501/59 , C07D501/38
CPC分类号: C07D285/08 , C07D417/06
摘要: Novel antibacterially active cephalosporins of the formula ##STR1## in which R.sup.1 denotes hydrogen, optionally substituted alkyl, a substituted or unsubstituted phenyl ring, a polycyclic aromatic ring or an optionally substituted heterocyclic 5- or 6-member ring having 1-4 heteroatoms,R.sup.2 represents hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkenyl, halogen, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, hydroxymethyl, formyloxymethyl, C.sub.1 -C.sub.4 -alkylcarbonyloxymethyl, aminocarbonyloxymethyl, pyridiniummethyl, 4-carbamoylpyridiniummethyl, 4-sulphonylethylpyridiniummethyl, 4-carboxylmethylpyridiniummethyl or heterocyclylthiomethyl, heterocyclyl representing a radical of the formula ##STR2## wherein R.sup.8 denotes hydrogen, methyl, 2-dimethylaminoethyl, carboxymethyl, sulphomethyl, carboxyethyl or sulphoethyl andR.sup.9 denotes hydrogen or methyl,or pharmaceutically tolerated salts or esters thereof.
摘要翻译: 式中,R1表示氢,任选取代的烷基,取代或未取代的苯基环,多环芳环或具有1-4个杂原子的任选取代的杂环的5-或6-元环的新型抗菌活性头孢菌素,R2 表示氢,C 1 -C 4 - 烷基,C 1 -C 4 - 烯基,卤素,C 1 -C 4 - 烷氧基,C 1 -C 4 - 烷硫基,羟甲基,甲酰氧基甲基,C 1 -C 4 - 烷基羰氧基甲基,氨基羰基氧基甲基,吡啶鎓甲基,4-氨基甲酰基吡啶鎓甲基,4-磺基乙基吡啶鎓甲基 ,4-羧基甲基吡啶鎓甲基或杂环硫基甲基,代表下式基团的杂环基,其中R8表示氢,甲基,2-二甲基氨基乙基,羧甲基,磺基甲基,羧乙基或磺基,R9表示氢或甲基, 或其药学上可耐受的盐或酯。
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公开(公告)号:US4515789A
公开(公告)日:1985-05-07
申请号:US483062
申请日:1983-04-07
IPC分类号: C07D499/66 , A61K31/397 , A61K31/43 , A61K31/545 , A61K31/546 , A61P31/04 , C07D205/08 , C07D205/085 , C07D233/32 , C07D233/36 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/12 , C07D417/14 , C07D463/00 , C07D499/00 , C07D499/44 , C07D499/64 , C07D499/68 , C07D499/70 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/38 , C07D501/57 , C07D505/00 , C07F7/18 , C07D501/56
CPC分类号: C07D403/12 , C07D233/32 , C07D233/36 , C07D403/14 , C07D405/14 , C07D409/12 , C07D417/14 , C07D499/00 , C07D505/00 , C07F7/184
摘要: A 3-.beta.-(vic-dihydroxyphenylmethyleneamino-2-oxo-imidazolidine)- or 3-.beta.-(vic-dihydroxyphenyl-methyleneamino-2,3-dioxo-piperazine)-1-carbonylamino-acetamidoazetidin-2-one having an acidic grouping on .sub.1 N, e.g. of the formula ##STR1## The compounds are antibiotically active, especially against Pseudomonas bacteria and can be used in combating bacterial infection, as a preservative and as a growth promoting agent in animal feeds.
摘要翻译: 3β-(咔唑 - 二羟基苯基亚甲基氨基-2-氧代 - 咪唑烷) - 或3β-(咔 - 二羟基苯基 - 亚甲基氨基-2,3-二氧代 - 哌嗪)-1-羰基乙酰氨基吖丁啶-2-酮 在1N上酸性分组,例如 该化合物具有抗菌活性,特别是针对假单胞菌属细菌,可用于防治细菌感染,作为防腐剂和作为动物饲料中的生长促进剂。
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