公开(公告)号：US5064824A

公开(公告)日：1991-11-12

申请号：US347567

申请日：1989-05-05

申请人： David G. Acton ,  David H. Davies ,  Jeffrey P. Poyser

发明人： David G. Acton ,  David H. Davies ,  Jeffrey P. Poyser

IPC分类号： C07D501/38 ,  A61K31/545 ,  A61K31/546 ,  C07C281/14 ,  C07D501/18 ,  C07D501/46

CPC分类号： C07D501/46 ,  C07C281/14

摘要： Cephalosporin antibiotics having a 3-position substituent of the formula: ##STR1## are described; wherein R.sup.1 is hydrogen or certain substituted alkyl groups, Z is CH or N, R.sup.2 and R.sup.3 are hydroxy or in vivo hydrolysable esters thereof, (R.sup.12).sub.n represents various optional substituents and X=Y is an olefin, oxime, azo or related group. Processes for their preparation and use are described.

公开(公告)号：US5019570A

公开(公告)日：1991-05-28

申请号：US223988

申请日：1988-07-25

申请人： Jean C. Arnould ,  Dominique Boucherot ,  David H. Davies ,  Frederick H. Jung ,  Colin J. Strawson

发明人： Jean C. Arnould ,  Dominique Boucherot ,  David H. Davies ,  Frederick H. Jung ,  Colin J. Strawson

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D209/04 ,  C07D209/42 ,  C07D215/22 ,  C07D215/48 ,  C07D215/54 ,  C07D215/56 ,  C07D217/22 ,  C07D217/26 ,  C07D237/28 ,  C07D239/28 ,  C07D239/72 ,  C07D239/74 ,  C07D239/80 ,  C07D239/88 ,  C07D239/90 ,  C07D241/00 ,  C07D241/44 ,  C07D251/54 ,  C07D311/04 ,  C07D311/08 ,  C07D311/18 ,  C07D311/22 ,  C07D311/76 ,  C07D471/00 ,  C07D501/00 ,  C07D501/04 ,  C07D501/24 ,  C07D501/38 ,  C07D501/40 ,  C07D501/46 ,  C07D501/48 ,  C07D501/56 ,  C07D501/57

CPC分类号： C07D501/46 ,  C07D501/40

摘要： Cephalosporin derivatives having a 3-position substituent of the formula I are described: ##STR1## wherein R.sup.1 is hydrogen, alkenyl or optionally substituted alkyl, Het us a 5- or 6-membered heterocyclic ring bonded via a carbon atom to the amide linkage, wherein Het is selected from a group of the formulae II-III: ##STR2## wherein A is CH or a nitrogen atom; B is oxygen, sulphur or a group NR.sup.4 ; one or two of D, E, F and G are nitrogen atoms and the remainder are CH groups: or Het is a pyrazinone, pyridinone, pyridazinone or pyrimidinone ring, or is a thione equivalent of such a ring, said rings having a substituent R.sup.4 on one nitrogen atom, or is pyranone, or pyranthione; the ring Het being fused by any adjacent carbon atoms to the benzene ring; and Het being attached to the --CH.sub.2 NR.sup.1 CO-- group via a carbon atom;R.sup.2 is hydroxy or an in vivo hydrolyzable ester thereof;R.sup.3 is ortho to R.sup.2 and is hydroxy or an in vivo hydrolyzable ester thereof; and R.sup.4 has various values. The use of such compounds as antibacterial agents is described as are processes for their preparation and intermediates therefor.

公开(公告)号：US4279894A

公开(公告)日：1981-07-21

申请号：US60682

申请日：1979-07-25

申请人： David H. Davies ,  Geoffrey L. F. Norris

发明人： David H. Davies ,  Geoffrey L. F. Norris

IPC分类号： A23K1/165 ,  A23K1/17 ,  A61K35/66 ,  A61K35/74 ,  C07G11/00 ,  C12N11/00 ,  C12P1/06 ,  C12P17/06 ,  C12R1/465 ,  A61K35/00

CPC分类号： C12P1/06 ,  A23K20/195 ,  Y02P60/56

摘要： The invention relates to a novel metabolite, M.139603, of the empirical formula C.sub.35 H.sub.53 O.sub.8 Na, which is obtained from the aerobic fermentation of a novel Streptomyces species, NCIB 11426, and to the corresponding free acid form thereof, C.sub.35 H.sub.54 O.sub.8. M.139,603 reduces the proportion of methane produced by the "digestion" of food in the rumen of ruminant animals and increases the proportion of propionate to acetate in the rumen contents. The compound is therefore useful for increasing the growth rate of ruminant animals, and/or for increasing their efficiency of food conversion. The compound also possesses activity against Gram positive micro-organisms, and against coccidia, for example Eimeria tenella.

摘要翻译： 本发明涉及经验化学式C35H53O8Na的新型代谢物M.139603，其由新型链霉菌属物种NCIB 11426的需氧发酵得到，并且与相应的游离酸形式C35H54O8有关。 M.139,603减少了反刍动物瘤胃食物“消化”产生的甲烷的比例，并增加了胃酸含量中丙酸酯对醋酸盐的比例。 因此，该化合物可用于增加反刍动物的生长速率和/或用于提高其食物转化效率。 该化合物还具有抗革兰氏阳性微生物和针对球虫的活性，例如艾美球虫（Eimeria tenella）。

公开(公告)号：US4225593A

公开(公告)日：1980-09-30

申请号：US967796

申请日：1978-12-04

申请人： David H. Davies ,  Geoffrey L. F. Norris

发明人： David H. Davies ,  Geoffrey L. F. Norris

IPC分类号： A23K20/195 ,  C12P17/18 ,  A61K31/69

CPC分类号： A23K20/195 ,  Y02P60/56

摘要： This invention relates to the use of aplasmomycin, boromycin and acylated and hydrogenated derivatives thereof for modifying rumen metabolism in domestic ruminant animals, by reducing the proportion of methane formed, and increasing the proportion of propionate at the expense of methane and/or acetate. This modification of rumen metabolism is believed to improve growth in ruminant animals. The disclosure also describes compositions which may be used in the claimed method, an improved process for the production of aplasmomycin, and novel analogs of aplasmomycin and boromycin together with processes for their manufacture.

摘要翻译： 本发明涉及阿曲霉素，硼霉素及其酰化和氢化衍生物在家用反刍动物体内改善瘤胃代谢的用途，通过减少形成的甲烷的比例，以及以甲烷和/或乙酸盐为代价增加丙酸酯的比例。 据信这种瘤胃新陈代谢的改良可以改善反刍动物的生长。 本公开还描述了可以在要求保护的方法中使用的组合物，用于生产阿曲霉素的改进方法以及阿曲霉素和硼霉素的新类似物及其制备方法。