公开(公告)号：EP1548121B1

公开(公告)日：2015-04-29

申请号：EP03771459.9

申请日：2003-07-31

申请人： Eisai R&D Management Co., Ltd.

发明人： KOTAKE, Yoshihiko ,  NIIJIMA, Jun ,  FUKUDA, Yoshio ,  NAGAI, Mitsuo ,  KANADA, Regina Mikie ,  TAKEDA, Susumu ,  NAKASHIMA, Takashi ,  YOSHIDA, Masashi ,  TSUCHIDA, Toshio ,  SAMESHIMA, Tomohiro

IPC分类号： C07D407/06 ,  C07D313/00 ,  C12P17/16 ,  C12P17/08

CPC分类号： C07D407/06 ,  C07D313/00 ,  C12P17/08 ,  C12P17/16 ,  C12P17/162

公开(公告)号：EP2168961A1

公开(公告)日：2010-03-31

申请号：EP08778055.7

申请日：2008-07-04

申请人： Eisai R&D Management Co., Ltd. ,  MERCIAN CORPORATION

发明人： TSUCHIDA, Toshio ,  YOSHIDA, Masashi ,  OHTA, Kazuo ,  KANEKO, Katsura ,  KOMINATO, Kaichiro

IPC分类号： C07D407/06 ,  C07D295/18 ,  C07F7/22

CPC分类号： C07D295/18 ,  C07D407/06 ,  C07F7/2232

摘要： The present invention provides a method for producing a 12-membered ring macrolide compound expected as a prophylactic or therapeutic agent for solid tumors and the like, and a production intermediate thereof. In detail, by acetalizing hydroxyl groups at 6- and 7-positions of a 12-membered ring macrolide compound being a raw material with dialkyl tin (IV) oxide and, after that, reacting the product with a carbamoyl halide derivative, the 7-position urethane derivative of the 12-membered ring macrolide compound being the target is effectively produced, without protecting hydroxyl groups at other positions.

摘要翻译： 本发明提供了预期作为实体瘤等的预防或治疗剂等的12元环大环内酯类化合物的制造方法及其制造中间体。 具体地说，通过使作为原料的12元环大环内酯化合物的6位和7位羟基被二烷基锡（Ⅳ）缩醛化，然后使该产物与氨基甲酰卤衍生物反应， 有效地制备作为目标的12元环大环内酯化合物的位置氨基甲酸酯衍生物，而不保护其它位置的羟基。

公开(公告)号：EP1770165B1

公开(公告)日：2011-12-21

申请号：EP05766205.8

申请日：2005-07-19

申请人： Eisai R&D Management Co., Ltd. ,  MERCIAN CORPORATION

发明人： MACHIDA, Kazuhiro ,  ARISAWA, Akira ,  TAKEDA, Susumu ,  YOSHIDA, Masashi ,  TSUCHIDA, Toshio

IPC分类号： C12N15/52 ,  C07K14/36 ,  C12N9/00 ,  C12N9/02 ,  C12P17/16 ,  C12P17/08

CPC分类号： C12P17/08 ,  C07K14/36 ,  C12N9/0071 ,  C12N9/0073 ,  C12N15/52 ,  C12P17/162

摘要： A polypeptide participating in the biosynthesis of pladienolide as a macrolide compound; a DNA coding for such a polypeptide; a variant thereof; a transformant in which part or the whole of such a DNA or variant thereof has been incorporated; and a process for producing pladienolide as a macrolide compound with the use of such a transformant. In particular, there is provided an isolated pure DNA comprising at least one region coding for a polypeptide participating in the biosynthesis of pladienolide. Further, there are provided a polypeptide coded for by this DNA and a recombinant plasmid capable of self-replication or integration replication carrying this DNA. Still further, there are provided a transformant carrying this DNA and a process for producing pladienolide, characterized in that this transformant is cultured in a culture medium and pladienolide is collected from the culture solution.

公开(公告)号：EP1770165A1

公开(公告)日：2007-04-04

申请号：EP05766205.8

申请日：2005-07-19

申请人： Eisai R&D Management Co., Ltd. ,  MERCIAN CORPORATION

发明人： MACHIDA, Kazuhiro ,  ARISAWA, Akira ,  TAKEDA, Susumu ,  YOSHIDA, Masashi ,  TSUCHIDA, Toshio

IPC分类号： C12N15/52 ,  C07K14/36 ,  C12N1/15 ,  C12N1/19 ,  C12N1/21 ,  C12N5/10 ,  C12N9/00 ,  C12N9/02 ,  C12P17/16

CPC分类号： C12P17/08 ,  C07K14/36 ,  C12N9/0071 ,  C12N9/0073 ,  C12N15/52 ,  C12P17/162

摘要： The present invention provides polypeptides that participate in the biosynthesis of the pladienolide macrolide compounds, DNA that encodes these polypeptides and variants of this DNA, transformants that maintain all or a portion of this DNA or variant thereof, and a method of producing the pladienolide macrolide compounds using these transformants. More particularly, it provides an isolated pure DNA that contains at least one region encoding a polypeptide that participates in pladienolide biosynthesis; polypeptide encoded by this DNA; a self-replicating or integrated-replicating recombinant plasmid carrying this DNA; a transformant maintaining this DNA; and a method of producing a pladienolide, characterized by culturing this transformant on culture medium and collecting pladienolide from this culture medium.

摘要翻译： 本发明提供了参与扁桃苷内酰胺大环内酯化合物的生物合成的多肽，编码这些多肽的DNA和该DNA的变体，保持该DNA或其变体的全部或一部分的转化体，以及生产该扁桃苷内酰胺大环内酯化合物的方法 使用这些转化体。 更具体地，其提供了分离的纯DNA，其含有至少一个编码参与泛二烯内酯生物合成的多肽的区域; 由该DNA编码的多肽; 携带该DNA的自复制或整合复制重组质粒; 维持该DNA的转化体; 以及生产普拉二烯内酯的方法，其特征在于在培养基上培养该转化体并从该培养基中收集普拉地奈内酯。