公开(公告)号：US4215124A

公开(公告)日：1980-07-29

申请号：US948712

申请日：1978-10-10

申请人： Burton G. Christensen ,  Frank P. DiNinno

发明人： Burton G. Christensen ,  Frank P. DiNinno

IPC分类号： C07D499/897 ,  A61K31/43 ,  A61P31/04 ,  C07D205/08 ,  C07D205/085 ,  C07D205/09 ,  C07D205/095 ,  C07D499/00 ,  C07D499/06 ,  C07D499/44 ,  C07D499/46 ,  C07D499/86 ,  C07D499/861 ,  C07D499/87 ,  C07D499/88 ,  C07F9/568 ,  C07D277/02

CPC分类号： C07F9/5683 ,  C07D205/08 ,  C07D205/085 ,  C07D205/09 ,  C07D205/095 ,  C07D499/00 ,  C07D499/88

摘要： Disclosed are 6-substituted amino-2-substituted-pen-2-em-3-carboxylic acids of the following structure: ##STR1## wherein R.sup.1 is hydrogen or acyl, R.sup.2 is hydrogen or methoxyl, and R.sup.3 is inter alia, hydrogen, --R, --OR, --SR, --NR.sub.2, R is alkyl, aryl, aralkyl, heterocyclyl or heterocyclylalkyl; n is 0 or 1; when n=1, R.sup.3 is not --SR.Such compounds and their pharmaceutically acceptable salt, and ester derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.

公开(公告)号：US4205180A

公开(公告)日：1980-05-27

申请号：US870932

申请日：1978-01-18

申请人： Michihiko Ochiai ,  Taiiti Okada ,  Osami Aki ,  Akira Morimoto ,  Kenji Kawakita ,  Yoshihiro Matsushita

发明人： Michihiko Ochiai ,  Taiiti Okada ,  Osami Aki ,  Akira Morimoto ,  Kenji Kawakita ,  Yoshihiro Matsushita

IPC分类号： C07D277/20 ,  C07D277/32 ,  C07D277/34 ,  C07D277/38 ,  C07D277/40 ,  C07D277/46 ,  C07D277/48 ,  C07D499/46 ,  C07D499/58 ,  C07D501/20 ,  C07D501/24 ,  C07D501/34 ,  C07D501/36 ,  C07D501/46 ,  C07C119/12

CPC分类号： C07D277/20 ,  C07D277/34 ,  C07D277/40 ,  C07D277/46 ,  C07D277/48 ,  C07D277/587

摘要： Novel cephem compounds of the formula; ##STR1## wherein R.sup.1 represents amino or hydroxyl group which may be protected, R.sup.2 represents amino or hydroxyl group or a group convertible into these groups, R.sup.3 represents hydrogen or methoxy group or a group convertible into methoxy group, R.sup.4 represents hydrogen or a residue of a nucleophilic compound and R.sup.8 represents hydrogen or a halogen, or a pharmaceutically acceptable salt or ester thereof, have strong antibiotic properties against a wide variety of microorganisms including gram-positive bacteria as well as gram-negative ones, especially by oral administration and can be used as therapeutic agent for various bacterial infections of animals including human beings.

公开(公告)号：US4138397A

公开(公告)日：1979-02-06

申请号：US881610

申请日：1978-02-27

申请人： Ekkehard H. Bohme

发明人： Ekkehard H. Bohme

IPC分类号： A61K31/43 ,  A61P31/04 ,  C07D307/79 ,  C07D499/00 ,  C07D499/44 ,  C07D499/46 ,  C07D499/60 ,  C07D499/62 ,  C07D499/68 ,  C07D499/72 ,  C07D499/58

CPC分类号： C07D307/79 ,  C07D499/00

摘要： New 6-(2,3-dihydro-5-benzofuranyl)acetamido penicillin compounds are described which are useful as antibacterial agents.

摘要翻译： 描述了可用作抗菌剂的新的6-（2,3-二氢-5-苯并呋喃基）乙酰氨基青霉素化合物。

公开(公告)号：US4130558A

公开(公告)日：1978-12-19

申请号：US797928

申请日：1977-05-18

申请人： Otto Roos ,  Dieter Essig

发明人： Otto Roos ,  Dieter Essig

IPC分类号： C07D499/44 ,  A61K9/14 ,  A61K31/43 ,  C07D20060101 ,  C07D499/16 ,  C07D499/46 ,  C07D499/68

CPC分类号： C07D499/68

摘要： A process for the preparation of an alkali metal salt of ampicillin, especially the sodium salt, which comprises adding to an aqueous suspension of ampicillin, at a temperature not exceeding about 4.degree. C, an aqueous solution of an equimolar or somewhat lesser amount of an alkali metal base, filtering the resulting solution until sterile, freezing the filtrate, and lyophilizing the frozen filtrate.

摘要翻译： 一种制备氨苄青霉素，特别是钠盐的碱金属盐的方法，其包括在不超过约4℃的温度下向氨苄青霉素的水性悬浮液中加入等摩尔或稍微少量的 碱金属碱，过滤所得溶液直至灭菌，冷冻滤液，冻干冷冻滤液。

公开(公告)号：US4041029A

公开(公告)日：1977-08-09

申请号：US615856

申请日：1975-09-23

申请人： Raymond A. Firestone ,  Lovji D. Cama ,  Burton G. Christensen

发明人： Raymond A. Firestone ,  Lovji D. Cama ,  Burton G. Christensen

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D499/00 ,  C07D499/04 ,  C07D499/10 ,  C07D499/21 ,  C07D499/44 ,  C07D499/46 ,  C07D499/68 ,  C07D499/70 ,  C07D499/72 ,  C07D501/04 ,  C07D501/16 ,  C07D501/57 ,  C07D499/02

CPC分类号： C07D499/00

摘要： A process is provided which yields derivatives of cephalosporins and penicillins. The process starts with 7-acylaminocephalosporin, or 6-acylaminopenicillin, then the latter compounds are treated with an organolithium compound, followed with t-butyl-hypochlorite. Finally, a defined reagent is added yielding a side chain on the carbon adjacent to the amino-nitrogen. Novel intermediate compounds are also described. The end compounds prepared are active against both gram-positive and gram-negative bacteria.

摘要翻译： 提供了产生头孢菌素和青霉素衍生物的方法。 该过程从7-酰基氨基头孢菌素或6-酰基氨基青霉素开始，然后后者化合物用有机锂化合物处理，然后用叔丁基次氯酸盐处理。 最后，加入定义的试剂，在邻近氨基氮的碳上产生侧链。 还描述了新的中间体化合物。 所制备的最终化合物对革兰氏阳性菌和革兰氏阴性细菌均有活性。

公开(公告)号：US4009160A

公开(公告)日：1977-02-22

申请号：US658489

申请日：1976-02-17

申请人： James W. McFarland ,  Colin Thomson

发明人： James W. McFarland ,  Colin Thomson

IPC分类号： C07D499/00 ,  C07D499/46 ,  C07D499/58

CPC分类号： C07D499/00

摘要： 6-(Aminomethyl substituted phenyl- and thienylacetamido)penicillanic acid and esters, and synthetic methods for the preparation thereof.

摘要翻译： 6-（氨基甲基取代的苯基和噻吩基乙酰胺基）青霉烷酸和酯，以及其制备的合成方法。

公开(公告)号：US4009159A

公开(公告)日：1977-02-22

申请号：US427232

申请日：1973-12-21

申请人： Takashi Kamiya ,  Yoshihisa Saito ,  Tsutomu Teraji ,  Osamu Nakaguti ,  Teruo Oku ,  Hitoshi Nakamura ,  Masashi Hashimoto

发明人： Takashi Kamiya ,  Yoshihisa Saito ,  Tsutomu Teraji ,  Osamu Nakaguti ,  Teruo Oku ,  Hitoshi Nakamura ,  Masashi Hashimoto

IPC分类号： C07D205/08 ,  C07D205/095 ,  C07D499/00 ,  C07D499/04 ,  C07D499/21 ,  C07D499/44 ,  C07D501/10 ,  C07D501/14 ,  C07D499/46 ,  C07D499/48 ,  C07D499/64

CPC分类号： C07D499/00 ,  C07D205/08 ,  C07D205/095

摘要： A penam derivative having the formula: ##STR1## wherein X represents a halogen atom, and wherein R.sub.1 represents an amino or acylamino, and R.sub.3 represents a radical selected from the group consisting of carboxy, ester, acid amide, acid anhydride, acid halide, and acid azide.

公开(公告)号：US3997527A

公开(公告)日：1976-12-14

申请号：US658384

申请日：1976-02-17

申请人： James W. McFarland ,  Colin Thomson

发明人： James W. McFarland ,  Colin Thomson

IPC分类号： C07D499/00 ,  C07D499/46 ,  C07D499/58

CPC分类号： C07D499/00

摘要： 6-(Aminomethyl substituted phenyl- and thienylacetamido)-penicillanic acid and esters, and synthetic methods for the preparation thereof.

摘要翻译： 6-（氨基甲基取代的苯基 - 和噻吩基乙酰胺基） - 青霉烷酸和酯，以及其制备方法。

公开(公告)号：US3996208A

公开(公告)日：1976-12-07

申请号：US344020

申请日：1973-03-21

申请人： Bruno Fechtig ,  Karoly Kocsis ,  Hans Bikel

发明人： Bruno Fechtig ,  Karoly Kocsis ,  Hans Bikel

IPC分类号： C07D207/34 ,  C07D213/75 ,  C07D213/78 ,  C07D233/90 ,  C07D241/22 ,  C07D277/36 ,  C07D307/68 ,  C07D499/00 ,  C07D499/64 ,  C07D501/20 ,  C07F7/18 ,  C07D499/46

CPC分类号： C07D213/75 ,  C07D207/34 ,  C07D213/78 ,  C07D233/90 ,  C07D241/22 ,  C07D277/36 ,  C07D307/68 ,  C07D499/00 ,  C07F7/1896

摘要： 6-acylamino-penam-3-carboxylic acids and 7-acylamino-3-cephem-4-carboxylic acids in which the acyl group has the formula ##STR1## in which R.sub.1 is hydrogen, R.sub.2 is optionally substituted phenyl, thienyl or furyl or R.sub.1 and R.sub.2 together are optionally substituted cycloalkyl, and R is a radical which is linked through a carbon, oxygen, sulphur or nitrogen atom.

摘要翻译： 6-酰基氨基 - penam-3-羧酸和7-酰基氨基-3-头孢烯-4-羧酸，其中酰基具有式“IMAGE”，其中R 1是氢，R 2是任选取代的苯基，噻吩基或呋喃基，或 R1和R2一起是任选取代的环烷基，R是通过碳，氧，硫或氮原子连接的基团。

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.