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    Streptomyces antibioticus ATCC 31771 and process for obtaining same
    5.
    发明授权
    Streptomyces antibioticus ATCC 31771 and process for obtaining same 失效
    链霉菌抗生素ATCC 31771及其获得的方法

    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。

    Semisynthetic macrolidic antibiotics, intermediate compounds for their preparation and related pharmaceutical compositions containing them
    6.
    发明授权
    Semisynthetic macrolidic antibiotics, intermediate compounds for their preparation and related pharmaceutical compositions containing them 失效
    半合成大环内酯抗生素，其制备的中间体化合物和含有它们的相关药物组合物

    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。

    Process for the preparation of (8S)-8-fluoroerythromycins
    7.
    发明授权
    Process for the preparation of (8S)-8-fluoroerythromycins 失效
    制备（8S）-8-氟尿嘧啶的方法

    公开(公告)号：US4673736A

    公开(公告)日：1987-06-16

    申请号：US629768

    申请日：1984-07-11

    申请人： Luciano Toscano

    发明人： Luciano Toscano

    IPC分类号： C07H17/08 ,  C07H1/00

    CPC分类号： C07H17/08

    摘要： For the synthesis of (8S)-8-fluoroerythromycins the corresponding 8,9-anhydroerythromycins 6,9-hemiketal are directly fluorinated with perchloryl fluoride.

    摘要翻译： 对于（8S）-8-氟尿嘧啶的合成，相应的8,9-去水红霉素6,9-半缩酮直接用高氯氟化物氟化。

    3-O-Oleandrosyl-5-O-desosaminyl erythronolide compounds
    8.
    发明授权
    3-O-Oleandrosyl-5-O-desosaminyl erythronolide compounds 失效
    3-O-奥兰德酰基-5-O-脱氨基甲酰基红新丝菌素化合物

    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。

    Fluorinated erythromycin compounds and a process for preparation
    9.
    发明授权
    Fluorinated erythromycin compounds and a process for preparation 失效
    氟化红霉素化合物及其制备方法

    公开(公告)号：US4514562A

    公开(公告)日：1985-04-30

    申请号：US443580

    申请日：1982-11-22

    申请人： Luciano Toscano

    发明人： Luciano Toscano

    IPC分类号： C07H17/00 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08 ,  C07H17/04

    CPC分类号： C07H17/08

    摘要： Fluorinated derivatives of erythromycins A, B, C and D, having antibiotic activity, are prepared, starting from 8,9-anhydroerythromycin 6,9-hemiacetals or their N-oxides, through the reaction with a compound capable of generating electrophilic reactive fluorine, the resulting reaction product undergoing thereafter a reduction, possibly together with a methylation, to the corresponding (8S)-8-fluoroerythomycins.

    摘要翻译： 通过与能够产生亲电子活性氟的化合物的反应，从8,9-脱水红霉素6,9-半缩醛或其N-氧化物开始制备具有抗生素活性的红霉素A，B，C和D的氟化衍生物， 所得的反应产物随后进行还原（可能与甲基化）一起还原成相应的（8S）-8-氟孕酮。

    (8S)-8-fluoroerythromycin derivatives, the process for the preparation thereof and the pharmaceutical compositions containing them
    10.
    发明授权
    (8S)-8-fluoroerythromycin derivatives, the process for the preparation thereof and the pharmaceutical compositions containing them 失效
    （8S）-8-氟红霉素衍生物，其制备方法和含有它们的药物组合物

    公开(公告)号：US4588712A

    公开(公告)日：1986-05-13

    申请号：US706496

    申请日：1985-02-28

    申请人： Luciano Toscano

    发明人： Luciano Toscano

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08 ,  A61K31/71

    CPC分类号： C07H17/08

    摘要： (8S)-8-fluoroerythromycin derivatives of formula ##STR1## wherein R is an optionally substituted alkyl, alkenyl or phenyl groupR' is hydrogen or methyl andR" is hydrogen or hydroxy,may be prepared by fluorination of the corresponding 8,9-anhydroerythromycin 6,9-hemiketals with perchloryl fluoride in the presence of a compound ROH in strictly anhydrous conditions.The new compounds as well as their pharmaceutically acceptable esters, salts and salt-esters may be employed as the active ingredients of pharmaceutical compositions for antibacterial use suitable for oral administration.

    摘要翻译： （8S）-8-氟红霉素衍生物其中R是任选取代的烷基，烯基或苯基R'是氢或甲基，R“是氢或羟基，可以通过氟化 在严格无水条件下，在化合物ROH存在下，将高分子量的8,9-脱水红霉素6,9-半缩酮与高氯氟化物反应。 可以使用新的化合物及其药学上可接受的酯，盐和盐 - 酯作为适于口服给药的用于抗菌用途的药物组合物的活性成分。