公开(公告)号：US09605015B2

公开(公告)日：2017-03-28

申请号：US14369869

申请日：2012-08-31

申请人： Eung-Soo Kim ,  Kyu Boem Han ,  Shuangjun Lin ,  Dekun Kong ,  Linquan Bai ,  Zixin Deng ,  David H. Sherman ,  Mi-Jin Lee

发明人： Eung-Soo Kim ,  Kyu Boem Han ,  Shuangjun Lin ,  Dekun Kong ,  Linquan Bai ,  Zixin Deng ,  David H. Sherman ,  Mi-Jin Lee

IPC分类号： C07H15/26 ,  C12P19/62 ,  C07H17/08 ,  C07D493/08

CPC分类号： C07H17/08 ,  C07D493/08 ,  C07H15/26 ,  C12P19/62

摘要： The present invention relates to a novel polyene compound similar to nystatin, a method for preparing the same, and an antifungal drug comprising the novel polyene compound as an active ingredient. Compared to nystatin comprising one sugar, NNP, which is the polyene compound similar to nystatin, displays 300 times higher solubility and ten times lower cytotoxicity while maintaining antifungal activity, and thus can be useful in developing a novel polyene antifungal agent having improved solubility and less toxicity in terms of pharmacokinetics.

公开(公告)号：US20140371436A1

公开(公告)日：2014-12-18

申请号：US14369869

申请日：2012-08-31

申请人： Eung-Soo Kim ,  Kyu Boem Han ,  Shuangjun Lin ,  Dekun Kong ,  Linquan Bai ,  Zixin Deng ,  David H. Sherman ,  Mi-Jin Lee

发明人： Eung-Soo Kim ,  Kyu Boem Han ,  Shuangjun Lin ,  Dekun Kong ,  Linquan Bai ,  Zixin Deng ,  David H. Sherman ,  Mi-Jin Lee

IPC分类号： C07H17/08 ,  C12P19/62

CPC分类号： C07H17/08 ,  C07D493/08 ,  C07H15/26 ,  C12P19/62

摘要： The present invention relates to a novel polyene compound similar to nystatin, a method for preparing the same, and an antifungal drug comprising the novel polyene compound as an active ingredient. Compared to nystatin comprising one sugar, NNP, which is the polyene compound similar to nystatin, displays 300 times higher solubility and ten times lower cytotoxicity while maintaining antifungal activity, and thus can be useful in developing a novel polyene antifungal agent having improved solubility and less toxicity in terms of pharmacokinetics.

摘要翻译： 本发明涉及类似于制霉菌素的新型多烯化合物，其制备方法，以及包含新型多烯化合物作为活性成分的抗真菌药物。 与包含一种糖的制霉菌素相比，与制霉菌素类似的多烯化合物，NNP显示出300倍的溶解度和10倍的细胞毒性，同时保持抗真菌活性，因此可用于开发具有改善的溶解度和更少的新型多烯抗真菌剂 在药代动力学方面的毒性。

公开(公告)号：US08101732B2

公开(公告)日：2012-01-24

申请号：US12560283

申请日：2009-09-15

申请人： Taifo Mahmud ,  Zixin Deng ,  Linquan Bai ,  Hui Xu ,  Jongtae Yang

发明人： Taifo Mahmud ,  Zixin Deng ,  Linquan Bai ,  Hui Xu ,  Jongtae Yang

IPC分类号： C07H15/00

CPC分类号： C12N9/0004 ,  C07H15/22 ,  C12P19/46

摘要： This disclosure relates to validamycin A biosynthesis and in particular, to methods of producing validamycin A analogs and uses thereof. In a particular example, a method for making a validamycin A analog includes transforming a host cell with one or more recombinant DNA vectors to produce a valN-inactivated mutant; and culturing the valN-inactivated mutant in a culture medium to produce a validamycin A analog, such as 1,1′-bis-valienamine and validienamycin, and their conversion to valienamine. The present disclosure further relates to compositions including such compounds as well as methods of using the compositions, such as for antifungal agents.

摘要翻译： 本公开涉及有效霉素A生物合成，特别涉及产生有效霉素A类似物的方法及其用途。 在具体实例中，制备有效霉素A类似物的方法包括用一种或多种重组DNA载体转化宿主细胞以产生ValN失活的突变体; 并在培养基中培养valN灭活的突变体以产生有效霉素A类似物，例如1,1'-双 - 缬胺和有效霉素，以及它们转化为valienamine。 本公开还涉及包含这些化合物的组合物以及使用组合物如抗真菌剂的方法。

公开(公告)号：US20100151528A1

公开(公告)日：2010-06-17

申请号：US12560283

申请日：2009-09-15

申请人： Taifo Mahmud ,  Zixin Deng ,  Linquan Bai ,  Hui Xu ,  Jongtae Yang

发明人： Taifo Mahmud ,  Zixin Deng ,  Linquan Bai ,  Hui Xu ,  Jongtae Yang

IPC分类号： C12P19/46 ,  C12P13/00 ,  C12N1/21 ,  C12N15/63 ,  C07H15/00

CPC分类号： C12N9/0004 ,  C07H15/22 ,  C12P19/46

摘要： This disclosure relates to validamycin A biosynthesis and in particular, to methods of producing validamycin A analogs and uses thereof. In a particular example, a method for making a validamycin A analog includes transforming a host cell with one or more recombinant DNA vectors to produce a valN-inactivated mutant; and culturing the valN-inactivated mutant in a culture medium to produce a validamycin A analog, such as 1,1′-bis-valienamine and validienamycin, and their conversion to valienamine. The present disclosure further relates to compositions including such compounds as well as methods of using the compositions, such as for antifungal agents.

摘要翻译： 本公开涉及有效霉素A生物合成，特别涉及产生有效霉素A类似物的方法及其用途。 在具体实例中，制备有效霉素A类似物的方法包括用一种或多种重组DNA载体转化宿主细胞以产生ValN失活的突变体; 并在培养基中培养valN灭活的突变体以产生有效霉素A类似物，例如1,1'-双 - 缬胺和有效霉素，以及它们转化为valienamine。 本公开还涉及包含这些化合物的组合物以及使用组合物如抗真菌剂的方法。