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1. 发明授权

US4344955A Penicillin 1,1-dioxides 失效
标题翻译：青霉素1,1-二氧化物
公开(公告)号：US4344955A
公开(公告)日：1982-08-17
申请号：US158975
申请日：1980-06-12
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： 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。

2. 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。

3. 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。

4. 发明授权

US3978056A Penicillins 失效
标题翻译：青霉素
公开(公告)号：US3978056A
公开(公告)日：1976-08-31
申请号：US502770
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 , C07D275/02 , C07D333/34 , C07D499/00 , C07D499/64 , C07D499/46
CPC分类号： C07D275/02 , C07D233/38 , C07D333/34 , C07D499/00
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.
摘要翻译：通过2,3-二取代的咪唑烷基酰胺或2,3-二取代的咪唑烷基硫代氨基甲酰基取代在侧链的α-碳原子上的芳基甲基 - 和环己烯基甲基 - 青霉素，或通过相应的2,3-二取代的1,3-二氮杂环己基氨基甲酰基或硫代氨基甲酰基是抗菌剂。

5. 发明授权

US3959258A Ureidoacetamido-penicillins 失效
公开(公告)号：US3959258A
公开(公告)日：1976-05-25
申请号：US425966
申请日：1973-12-19
申请人： Hans-Bodo Konig , Wilfried Schrock , Hans Disselnkotter , Karl Georg Metzger
发明人： Hans-Bodo Konig , Wilfried Schrock , Hans Disselnkotter , Karl Georg Metzger
IPC分类号： A61K31/43 , C07C275/60 , C07D233/38 , C07D261/18 , C07D307/68 , C07D333/24 , C07D333/38 , C07D499/68 , C07F7/08
CPC分类号： C07D499/64 , A61K31/43 , C07C275/60 , C07D233/38 , C07D261/18 , C07D307/68 , C07D333/24 , C07D333/38 , C07D499/68 , C07F7/08
摘要： 6-(.alpha.-3-Acyl-ureidoacetamido)-penicillanic acids and pharmaceutically acceptable non-toxic salts thereof in which the hydrogen atom of the nitrogen atom present in the 3-position is substituted, are effective against Gram-positive and Gram-negative infections, particularly Klebsiella aerobacter infections.

6. 发明授权

US4081539A Penicillins and cephalosporins and their production 失效
标题翻译：青霉素和头孢菌素及其生产
公开(公告)号：US4081539A
公开(公告)日：1978-03-28
申请号：US763728
申请日：1977-01-31
申请人： Hans-Bodo Konig , Karl Georg Metzger , Wilfried Schrock
发明人： Hans-Bodo Konig , Karl Georg Metzger , Wilfried Schrock
IPC分类号： C07D499/00 , A61K31/545
CPC分类号： C07D499/00
摘要： .beta.-Lactams of the formula ##STR1## and pharmaceutically acceptable nontoxic salts thereof wherein A is hydrogen or alkyl of 1 to 4 carbon atoms;B is phenyl, methylphenyl, chlorophenyl, hydroxyphenyl or cyclohexa-1,4-dien-1-yl;R is a moiety of the formula ##STR2## wherein E is hydrogen, --OH or --O--CO--CH.sub.3 ; andC* constitutes a center of chirality; are produced which exhibit antibiotic activity.
摘要翻译：式“IMAGE”的β-内酰胺及其药学上可接受的无毒盐，其中A为氢或1至4个碳原子的烷基; B是苯基，甲基苯基，氯苯基，羟基苯基或环己-1,4-二烯-1-基; R是下式的部分：其中E是氢，-OH或-O-CO-CH 3; 和C *构成手性中心; 产生具有抗生素活性。

7. 发明授权

US4031229A Penicillins and processes for their preparation and use 失效
标题翻译：青霉素及其制备和使用的过程
公开(公告)号：US4031229A
公开(公告)日：1977-06-21
申请号：US692930
申请日：1976-06-04
申请人： Hans-Bodo Konig , Karl Georg Metzger , Wilfried Schrock
发明人： Hans-Bodo Konig , Karl Georg Metzger , Wilfried Schrock
IPC分类号： C07D499/10 , C07D233/32 , C07D233/38 , C07D499/00 , C07D499/04 , C07D499/64 , C07D499/66 , C07D499/68 , C07D499/70 , A61K31/43
CPC分类号： C07D233/32 , C07D233/38 , C07D499/00
摘要： 6-[.alpha.-(Imidazolidin-2-on-1-carbonylamido)acetamido]-penicillanic acids substituted in the 3-position of the imidazolidinone ring with phenyl or a substituted phenyl group and on the .alpha.-carbon atom of the acetamido bridge with a phenyl, thienyl, cyclohexenyl or cyclohexadienyl group, and their salts, are antibacterial agents. The compounds, of which .alpha.-(3-phenylimidazolidin-2-on-1-ylcarbonylamino)benzylpenicillin is a representative example, are prepared by acylation of the corresponding 6-(.alpha.-aminoacetamido)penicillanic acid or a derivative thereof.
摘要翻译：在咪唑啉酮环的3位被苯基或取代的苯基取代的6- [α-（咪唑烷-2-酮-1-羰基酰氨基）乙酰氨基] - 青霉烷酸和乙酰氨基桥的α-碳原子上，苯基，噻吩基，环己烯基或环己二烯基及其盐是抗菌剂。通过酰化相应的6-（α-氨基乙酰氨基）青霉烷酸或其衍生物，制备其中α-（3-苯基咪唑烷-2-酮-1-基羰基氨基）苄青霉素的代表性实例的化合物。

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

US4016282A Ureidoacetamido-penicillins 失效
标题翻译：尿素乙酰氨基青霉素
公开(公告)号：US4016282A
公开(公告)日：1977-04-05
申请号：US568384
申请日：1975-04-16
申请人： Hans-Bodo Konig , Wilfried Schrock , Hans Disselnkotter , Karl Georg Metzer
发明人： Hans-Bodo Konig , Wilfried Schrock , Hans Disselnkotter , Karl Georg Metzer
IPC分类号： A61K31/43 , C07C275/60
CPC分类号： C07D499/64 , A61K31/43 , C07C275/60 , C07D499/68
摘要： 6-(.alpha.-3-Acyl-ureidoacetamido)-penicillanic acids and pharmaceutically acceptable non-toxic salts thereof in which the hydrogen atom of the nitrogen atom present in the 3-position is substituted, are effective against Gram-positive and Gram-negative infections, particularly Klebsiella aerobacter infections.
摘要翻译： 6-（α-3-酰基 - 脲基乙酰胺基） - 青霉烷酸及其药学上可接受的无毒盐，其中存在于3-位的氮原子的氢原子被取代，对革兰氏阳性和革兰氏阴性有效感染，特别是克雷伯杆菌感染。

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