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    .beta.-Lactam antibiotics
    3.
    发明授权
    .beta.-Lactam antibiotics 失效
    β-内酰胺抗生素

    公开(公告)号：US4251524A

    公开(公告)日：1981-02-17

    申请号：US53655

    申请日：1979-06-29

    申请人： Peter Feyen ,  Michael Preiss ,  Karl G. Metzger

    发明人： Peter Feyen ,  Michael Preiss ,  Karl G. Metzger

    IPC分类号： C07D499/66 ,  A61K31/415 ,  A61K31/42 ,  A61K31/43 ,  A61K31/435 ,  A61K31/505 ,  A61K31/535 ,  A61K31/545 ,  A61P31/04 ,  C07D233/38 ,  C07D499/00 ,  C07D499/64 ,  C07D499/68 ,  C07D501/20 ,  C07D501/57 ,  A61K31/655

    CPC分类号： C07D233/38 ,  C07D499/00 ,  Y02P20/55

    摘要： Antibacterially active and animal feedstuff supplement .beta.-lactam antibiotics of the formula ##STR1## in which R is H or --UR',U is O or S,R' is optionally substituted alkyl, alkenyl, alkinyl, aralkyl, aryl or cycloalkyl, ##STR2## R.sup.1 and R.sup.2 individually are hydrogen or, individually or together with the carbon atom to which they are bonded, are any of various radicals,A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 -- or ##STR3## B is optionally substituted phenyl or is cyclohexenyl or cyclohexadienyl; X is S, O, SO, SO.sub.2 or --CH.sub.2 --; andY is a group of the formula ##STR4## T is hydrogen, alkyl-CO-O-, pyridinium, aminopyridinium, carbamoyloxy, azido, cyano, hydroxyl or optionally substituted -S-phenyl, or is -S-Het,in whichHet is an optionally substituted heterocyclic 5-membered or 6-membered ring;and whereinE is hydrogen, a radical forming, with the carboxyl group to which it is attached, a carboxy ester group, a cation of a salt, or a protective group,or a hydrate thereof. A process is also given for converting R directly from H to UR' employing a base, a halogenating agent and R'UH.

    摘要翻译： 抗菌活性和动物饲料补充式为其中R为H或-UR'的式（I）的β-内酰胺抗生素，U为O或S，R'为任选取代的烷基，烯基，炔基，芳烷基，芳基或 环烷基，R 1和R 2分别是氢或者与它们所键合的碳原子单独或一起是各种基团中的任何一个，A是-CH 2 -CH 2 - ， - CH 2 -CH 2 -CH 2 - 或

    Penicillins
    6.
    发明授权
    Penicillins 失效

    公开(公告)号：US3931153A

    公开(公告)日：1976-01-06

    申请号：US419950

    申请日：1973-11-29

    申请人： Gunter Schmidt ,  Karl Georg Metzger

    发明人： Gunter Schmidt ,  Karl Georg Metzger

    IPC分类号： C07D499/66 ,  A23K20/195 ,  A61K31/43 ,  A61P31/04 ,  C07D249/18 ,  C07D317/68 ,  C07D333/38 ,  C07D409/04 ,  C07D499/00 ,  C07D499/64 ,  C07D499/68 ,  C07D499/70 ,  C07D499/44

    CPC分类号： C07D333/38 ,  C07D249/18 ,  C07D317/68 ,  C07D499/00

    摘要： Penicillins of the formula: ##SPC1##And their pharmaceutically acceptable nontoxic salts whereinR.sub.1 is hydrogen, halogen, lower alkyl, hydroxy, nitro or A--NH;A is ##EQU1## wherein R.sub.3 is hydrogen; lower alkyl; halo-(lower alkyl); cycloalkyl of 3 to 11 carbon atoms, unsubstituted or substituted by hydroxy or alkyl of 1 or 2 carbon atoms; cycloalkenyl of 3 to 11 carbon atoms; bicycloalkyl of up to 8 carbon atoms; bicycloalkenyl of up to 8 carbon atoms; aryl of 6 to 10 carbon atoms, unsubstituted or substituted by 1 to 3 substituents selected from the group consisting of alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen, trifluoromethyl, nitro, amino, alkylsulphonyl of 1 to 4 carbon atoms, and methylenedioxy; azidoaryl of 6 to 10 carbon atoms, azido-(lower alkyl); amino; or thienyl;R.sub.4 is lower alkylamino or arylamino of 6 to 10 carbon atoms;B is a direct bond; CH.sub.2 ; S--CH.sub.2 ; CH=CH; or CO--NH--CH.sub.2 ;E is phenyl or phenyl or thenyl, substituted by hydroxy, azido, lower alkyl, lower alkoxy, lower alkylthio or chlorine; andC* is an asymmetric carbon atom,Are useful for their antibacterial activity against both Gram-positive and Gram-negative bacteria.

    Process for producing aminopenicillins
    7.
    发明授权
    Process for producing aminopenicillins 失效
    生产氨基宁霉素的方法

    公开(公告)号：US3595855A

    公开(公告)日：1971-07-27

    申请号：US3595855D

    申请日：1968-12-05

    申请人： AMERICAN HOME PROD

    发明人： ROBINSON CHARLES A

    IPC分类号： C07D499/00 ,  C07D499/12 ,  C07D499/64 ,  C07D499/66 ,  C07D499/68 ,  C07D99/16

    CPC分类号： C07D499/00

    摘要： A PROCESS FOR PREPARING AMINOPENICILLINS IN HIGH YIELD WHEREIN 6-AMINOPENICILLANIC ACID IS SILYLATED WITH THE USE OF HEXAMETHYLDISILAZANE IN METHYLENE CHLORIDE AT REFLUX TEMPERATURE TO GIVE MONOSILYLATED 6-AMINOPENICILLANIC ACID. THE REACTION MIXTURE IS THEN TREATED WITH A WEAK AMINE FOLLOWED BY REACTION WITH A SUITABLE ORGANIC ACID HALIDE HYDROHALIDE. SOLVOLYSIS WITH WATER OR AN ALCOHOL IS THEN EMPLOYED TO REMOVE THE SILYL GROUP THEREBY TO AFFORD A SOLUTION OF THE AMINOPENICILLIN HYDROHALIDE, WHICH IS THEN ISOLATED AS THE AMINOPENICILLIN.

    Cephalosporin derivatives
    8.
    发明授权
    Cephalosporin derivatives 失效
    头孢菌素衍生物

    公开(公告)号：US4415566A

    公开(公告)日：1983-11-15

    申请号：US191423

    申请日：1980-09-26

    申请人： Bernd Wetzel ,  Eberhard Woitun ,  Wolfgang Reuter ,  Roland Maier ,  Uwe Lechner ,  Hanns Goeth

    发明人： Bernd Wetzel ,  Eberhard Woitun ,  Wolfgang Reuter ,  Roland Maier ,  Uwe Lechner ,  Hanns Goeth

    IPC分类号： C07D499/66 ,  A61K31/43 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D239/36 ,  C07D499/00 ,  C07D499/64 ,  C07D499/68 ,  C07D499/70 ,  C07D501/20 ,  C07D501/22 ,  C07D501/34 ,  C07D501/36 ,  C07D501/46

    CPC分类号： C07D239/36 ,  C07D499/00 ,  Y02P20/55

    摘要： Penicillins and cephalosporins of the formula ##STR1## wherein A is phenyl, 4-hydroxyphenyl, cyclohexyl, cyclohene-1-yl, cyclohexa-1,4-diene-1-yl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl or 3,4-disubstituted phenyl, where the substituents, which may be identical to or different from each other, are each chlorine, hydroxyl or methoxy;R.sub.1 is an unsubstituted or substituted 5- or 6-membered heterocycle comprising carbon atoms and 1 to 4, preferably 1 to 2, identical or different heteroatoms such as oxygen, sulfur or nitrogen;n is 0 or 1;X is ##STR2## D is hydrogen, hydroxyl, acetoxy, aminocarbonyloxy, pyridinium, aminocarbonyl-pyridinium or S-Het, where Het is 1-methyl-tetrazol-5-yl, tetrazol-5-yl, 3-methyl-1,2,4-thiadiazol-5-yl, 1,2,4-triadiazol-5-yl, 1,3,4-thiadiazol-5-yl, 2-methyl-1,3,4-thiadiazol-5-yl, 2-methylamino-1,3,4-thiadiazol-5-yl, 2-dimethylamino-1,3,4-thiadiazol-5-yl, 2-formylamino-1,2,4-thiadiazol-5-yl, 2-acetylamino-1,3,4-thiadiazol-5-yl, 2-methyl-1,3,4-oxadiazol-5-yl, 1,2,3-triazol-4-yl or 1,2,4-triazol-3-yl; andE is hydrogen or a protective group which is easily removable in nitro or in vivo, especially an ester-forming group which can be removed under mild conditions by hydrogenation or hydrolysis or other treatments, or an ester-forming group which can easily be split off in the living organism;and, when E is hydrogen, their non-toxic, pharmacologically acceptable salts thereof, such as their alkali metal or alkaline earth metal salts, especially the sodium, potassium, magnesium or calcium salts; their ammonium salts; or their organic amine salts, especially the triethylamine or dicyclohexylamine salts. The compounds are useful as antibiotics.

    摘要翻译： 其中A是苯基，4-羟基苯基，环己基，环烯-1-基，环己-1,4-二烯-1-基，2-噻吩基，3-噻吩基，2-呋喃基， 3-呋喃基或3,4-二取代的苯基，其中可以相同或不同的取代基各自为氯，羟基或甲氧基; R1是包含碳原子和1至4个，优选1至2个相同或不同的杂原子如氧，硫或氮的未取代或取代的5或6元杂环; n为0或1; X是H，羟基，乙酰氧基，氨基羰基氧基，吡啶鎓，氨基羰基 - 吡啶鎓或S-Het，其中Het是1-甲基 - 四唑-5-基，四唑-5-基，3-甲基-1- 2,4-噻二唑-5-基，1,2,4-三唑-5-基，1,3,4-噻二唑-5-基，2-甲基-1,3,4-噻二唑-5-基， 2-甲基氨基-1,3,4-噻二唑-5-基，2-二甲基氨基-1,3,4-噻二唑-5-基，2-甲酰氨基-1,2,4-噻二唑-5-基，2- 乙酰氨基-1,3,4-噻二唑-5-基，2-甲基-1,3,4-恶二唑-5-基，1,2,3-三唑-4-基或1,2,4-三唑-4-基， 吡啶-3-基; E是氢或在硝基或体内容易除去的保护基团，特别是可在温和条件下通过氢化或水解或其它处理方法除去的酯形成基团或易于分解的酯形成基团 在有机体中脱落; 并且当E是氢时，其无毒的药学上可接受的盐，例如它们的碱金属或碱土金属盐，特别是钠，钾，镁或钙盐; 其铵盐; 或它们的有机胺盐，特别是三乙胺或二环己基胺盐。 该化合物可用作抗生素。

    .beta.-Lactam antibiotics and their use
    10.
    发明授权
    .beta.-Lactam antibiotics and their use 失效
    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。