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    PROCESS FOR PRODUCING MACROLIDE COMPOUND AND INTERMEDIATE THEREFOR
    1.
    发明公开
    PROCESS FOR PRODUCING MACROLIDE COMPOUND AND INTERMEDIATE THEREFOR 审中-公开
    VERFAHREN ZUR HERSTELLUNG EINER MAKROLIDVERBINDUNG UND ZWISCHENPRODUKT DARAUS

    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。

    DNA CODING FOR POLYPEPTIDE PARTICIPATING IN BIOSYNTHESIS OF PLADIENOLIDE
    3.
    发明公开
    DNA CODING FOR POLYPEPTIDE PARTICIPATING IN BIOSYNTHESIS OF PLADIENOLIDE 有权
    FÜRAN DER BIOSYNTHESE VON PLADIENOLID BETEILIGTES POLYPEPTID CODIERENDE DNA

    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。

    PROCESS FOR PRODUCTION OF 1-HYDROXY-19-NORCYCLOVITAMIN D DERIVATIVE AND INTERMEDIATE FOR THE PRODUCTION
    5.
    发明公开
    PROCESS FOR PRODUCTION OF 1-HYDROXY-19-NORCYCLOVITAMIN D DERIVATIVE AND INTERMEDIATE FOR THE PRODUCTION 审中-公开
    用于生产用于生产1-羟基19-D NORCYCLOVITAMIN衍生物和中间体

    公开(公告)号：EP2085380A1

    公开(公告)日：2009-08-05

    申请号：EP07831047.1

    申请日：2007-11-01

    申请人： MERCIAN CORPORATION

    发明人： TOYODA, Asako ,  NAGAI, Hazuki ,  KONUKI, Kaname ,  TSUCHIDA, Toshio

    IPC分类号： C07C401/00 ,  A61K31/59

    CPC分类号： C07C401/00

    摘要： A cyclovitamin D derivative produced from 25-hydroxyvitamin D is reacted with osmium tetraoxide or a permanganic acid salt to produce a 10,19-diolcyclovitamin D derivative. The 10,19-diolcyclovitamin D derivative is reacted with a perhalogenic acid salt or lead tetraacetate to produce a 10-oxocyclovitamin D derivative. A 1-hydroxycyclovitamin D derivative is produced from the 10-oxocyclovitamin D derivative via a cyclovitamin D derivative and a 1,10-olefincyclovitamin D derivative. The 1-hydrocyclovitamin D derivative is subjected to solvolysis, thereby producing a 1-hydroxy-19-norviatmin D derivative. Thus provided are a novel process for production of 1-hydroxy-19-norcyclovitamin D derivative that is utilizable as an intermediate in the synthesis of 1-hydroxy-19-norvitamin D derivative which is useful as a pharmaceutical agent; and an intermediate for the production.

    摘要翻译： 从25-羟基维生素D产生的环维生素D衍生物进行反应与四氧化锇或高锰酸盐，以产生10.19-diolcyclovitamin D衍生物。 的10.19-diolcyclovitamin D衍生物进行反应与高卤酸盐或四乙酸铅，以产生10-氧代环维生素D衍生物。 A 1-hydroxycyclovitamin D衍生物是从经由环维生素D衍生物和1.10烯烃环维生素D衍生物的10-氧代环维生素D衍生物制备。 1-水力环维生素D衍生物进行溶剂分解，由此产生1-羟基-19- norviatmin D衍生物。 因此，提供用于制备1-羟基-19- norcyclovitamin D衍生物的新方法所做的是可利用的，以在1-羟基-19-去甲维生素D衍生物的合成中间体的所有其是作为医药品有用的; 并在中间生产。

    DNA PARTICIPATING IN HYDROXYLATION OF MACROLIDE COMPOUND
    9.
    发明公开
    DNA PARTICIPATING IN HYDROXYLATION OF MACROLIDE COMPOUND 审中-公开
    ER ER UNG UNG E E E E E E E E E E E DNA E

    公开(公告)号：EP1705247A1

    公开(公告)日：2006-09-27

    申请号：EP04799902.4

    申请日：2004-11-25

    申请人： MERCIAN CORPORATION ,  Eisai Co., Ltd.

    发明人： MACHIDA, Kazuhiro ,  NAKASHIMA, Takashi ,  ARITOKU, Yasuhide ,  TSUCHIDA, Toshio

    IPC分类号： C12N15/09 ,  C12N1/15 ,  C12N1/19 ,  C12N1/21 ,  C12N5/10 ,  C12N9/02 ,  C12P17/08 ,  C07K14/00

    CPC分类号： C12P17/08 ,  C12N9/10

    摘要： The present invention provides a DNA participating in biological transformation of a macrolide compound 11107B. The present invention provides, paticularly, a DNA participating in biological transformation of a macrolide compound 11107B represented by the formula (I) into a 16-position hydroxy macrolide compound 11107D represented by the formula (II), the DNA encoding a protein having 16-position hydroxylating enzymatic activity or ferredoxin, to a method of isolating the DNA, to a protein encoded by the DNA, a plasmid carrying the DNA, a transformant obtained by transforming using the plasmid and a method of producing a 16-position hydroxy compound by using the transformant.

    摘要翻译： 本发明提供参与大环内酯化合物11107B的生物转化的DNA。 本发明特别提供参与由式（I）表示的大环内酯化合物11107B的生物转化成由式（II）表示的16位羟基大环内酯化合物11107D的DNA，编码具有16位的式 位置羟化酶活性或铁氧还蛋白，分离DNA的方法，由DNA编码的蛋白质，携带DNA的质粒，通过使用质粒转化获得的转化体和通过使用制备16位羟基化合物的方法 转化体。

    PROCESS FOR PRODUCING PIPECOLAMIDE DERIVATIVE
    10.
    发明公开
    PROCESS FOR PRODUCING PIPECOLAMIDE DERIVATIVE 审中-公开
    生产脂肪族酰胺衍生物的方法

    公开(公告)号：EP1433782A1

    公开(公告)日：2004-06-30

    申请号：EP02772841.9

    申请日：2002-09-10

    申请人： MERCIAN CORPORATION

    发明人： TSUCHIDA, Toshio ,  KANEKO, Katsura ,  MATSUMOTO, Naoki

    IPC分类号： C07D211/00

    CPC分类号： C07D211/60

    摘要： A method of manufacturing a pipecolamide derivative, characterized in that pipecolic acid or an acid salt thereof is reacted with an amine in an inert solvent in the presence of a condensing agent such as dicyclohexylcarbodiimide, 1-ethyl- 2-(2-dimethylaminopropyl) carbodiimide, methanesulfonyl chloride or phosphoryl chloride. Pipecolamide derivatives, particularly in optically active forms thereof can be efficiently and economically manufactured without harmful gas by-products.

    摘要翻译： 1.一种制造哌啶酰胺衍生物的方法，其特征在于使2-哌啶酸或其酸盐与胺在惰性溶剂中在缩合剂如二环己基碳化二亚胺，1-乙基-2-（2-二甲基氨基丙基）碳化二亚胺 ，甲磺酰氯或磷酰氯。 哌醋酰胺衍生物，特别是其光学活性形式可以有效且经济地制造而没有有害的气体副产物。