公开(公告)号：US4520101A

公开(公告)日：1985-05-28

申请号：US472444

申请日：1983-03-07

申请人： David A. Lowe ,  Guna Romancik ,  Leonardo M. Cappelletti ,  Richard P. Elander

发明人： David A. Lowe ,  Guna Romancik ,  Leonardo M. Cappelletti ,  Richard P. Elander

IPC分类号： C07D501/28 ,  C12P35/06 ,  C12R1/75 ,  C12N9/18

CPC分类号： C12P35/06

摘要： Production of undesired desacetylcephalosporin C during fermentation of cephalosporin C-producing microorganisms is substantially reduced by addition of certain phosphorous compounds to the culture medium.

摘要翻译： 通过向培养基中加入某些磷化合物，在产生头孢菌素C-产生微生物的发酵期间产生不期望的去乙酰头孢菌素C.

公开(公告)号：US4429115A

公开(公告)日：1984-01-31

申请号：US338117

申请日：1982-01-08

申请人： Leonardo M. Cappelletti ,  Roberto Spagnoli ,  Luciano Toscano

发明人： Leonardo M. Cappelletti ,  Roberto Spagnoli ,  Luciano Toscano

IPC分类号： C12N1/20 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08 ,  C12P19/62 ,  C12R1/465 ,  A61K31/71

CPC分类号： C07H17/08 ,  C12P19/62 ,  C12R1/48 ,  Y10S435/888

摘要： The fermentation of a substrate selected among erythronolide B, erythronolide A and erythronolide A oxime with a novel mutant, Streptomyces antibioticus ATCC 31771, obtained from an industrial stock for the production of oleandomycin, said novel mutant being incapable of producing the same oleandomycin, permits novel macrolide antibiotics to be produced, having not only an activity range like that of erythromycin, but characterized by a greater stability in acidic environment, whereby for the administration of antibiotic it is no longer necessary to have recourse to esters and/or salts highly toxic for the organism.

摘要翻译： 选自赤藓酮ide内酯B，赤藓酮酸苷A和赤藓酮ide ide肟的底物的发酵与获自木兰霉素的工业原料获得的新型突变体Streptomyces抗生素链霉菌ATCC 31771的所述新型突变体不能产生相同的夹竹桃霉素，允许新颖的 大环内酯类抗生素不仅具有类似于红霉素的活性范围，而且在酸性环境中具有较高的稳定性，因此为了施用抗生素，不再需要对于高毒性的酯和/或盐 有机体。

公开(公告)号：US4560662A

公开(公告)日：1985-12-24

申请号：US548323

申请日：1983-11-03

申请人： Leonardo M. Cappelletti ,  Roberto Spagnoli ,  Luciano Toscano

发明人： Leonardo M. Cappelletti ,  Roberto Spagnoli ,  Luciano Toscano

IPC分类号： C12N1/20 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08 ,  C12P19/62 ,  C12R1/465 ,  C12R1

CPC分类号： C07H17/08 ,  C12P19/62 ,  C12R1/48 ,  Y10S435/888

摘要： The fermentation of a substrate selected among erythronolide B, erythronolide A and erythronolide A oxime with a novel mutant, Streptomyces antibioticus ATCC 31771, obtained from an industrial stock for the production of oleandomycin, said novel mutant being incapable of producing the same oleandomycin, permits novel macrolide antibiotics to be produced, having not only an activity range like that of erythromycin, but characterized by a greater stability in acidic environment, whereby for the administration of the antibiotic it is no longer necessary to have recourse to esters and/or salts highly toxic for the organism.

摘要翻译： 选自赤藓酮ide内酯B，赤藓酮酸苷A和赤藓酮ide ide肟的底物的发酵与获自木兰霉素的工业原料获得的新型突变体Streptomyces抗生素链霉菌ATCC 31771的所述新型突变体不能产生相同的夹竹桃霉素，允许新颖的 大环内酯类抗生素不仅具有红霉素的活性范围，而且在酸性环境中具有更大的稳定性，因此对于抗生素的施用，不再需要追求高毒性的酯和/或盐 为生物体。

公开(公告)号：US4439426A

公开(公告)日：1984-03-27

申请号：US338105

申请日：1982-01-08

申请人： Luciano Toscano ,  Leonardo M. Cappelletti

发明人： Luciano Toscano ,  Leonardo M. Cappelletti

IPC分类号： C07D313/00 ,  C07D493/08 ,  C07D493/18 ,  C07H17/08 ,  C12P19/62 ,  A61K31/71

CPC分类号： C07D493/08 ,  C07D313/00 ,  C07H17/08 ,  C12P19/62 ,  C12R1/465 ,  C12R1/48 ,  Y10S435/886 ,  Y10S435/888

摘要： From the fermentation carried, out with mutants blocked in the synthesis respectively of erythromycin and of oleandomycin, namely Streptomyces erythreus ATCC 31772 and Streptomyces antibioticus ATCC 31771, using as the substrate a derivative of erythronolide A, namely (8S)-8-fluoroerythronolide A, a derivative of erythronolide B, namely (8S)-8-fluoroerythronolide B, or a derivative of 3-O-mycarosyl-erythronolide B, namely 3-O-mycarosyl-(8S)-fluoroerythronolide B, the corresponding (8S)-8-fluoro derivatives of the erythromycins A, B, C and D, as well as 3-O-oleandrosyl-5-desosaminyl-(8S)-8-fluoroerythronolide A and 3-O-oleandrosyl-5-O-desosaminyl-(8S)-8-fluoroerythronolide B, all belonging to the class of the macrolide antibiotics are obtained.The preparation of the aforesaid substrate comprises the convention of erythronolide A, erythronolide B or 3-O-mycarosyl-erythronolide B into the corresponding hermiacetal, the reaction of the latter with a compound capable of generating electrophlic fluorine and the opening of the resulting acetal with aqueous acid.

摘要翻译： 使用红霉素和木兰霉素（即，链霉菌ATCC 31772和抗链霉菌ATCC 31771）的合成中的突变体，从赤霉素A的衍生物即（8S）-8-氟代红霉内酯A， （8S）-8-氟丙烯腈B的衍生物，或3-O-霉酚酰 - 赤藓酮苷B的衍生物，即3-O-霉酚酰 - （8S） - 氟蒿腈B，相应的（8S）-8 红霉素A，B，C和D的三氟代衍生物，以及3-O-肉豆蔻酰基-5-脱氨基甲酰基 - （8S）-8-氟代红葡萄烯内酰胺A和3-O-肉豆蔻酰基-5-O-脱葡糖胺基 - （8S ）-8-氟代红霉素B，均属于大环内酯类抗生素类。 上述底物的制备包括将红细胞生成素A，红细胞生成素B或3-O-霉酚酰 - 赤藓酮苷B转化成相应的米缩醛，后者与能够产生电性氟的化合物的反应以及所得缩醛的打开与 酸水溶液。