公开(公告)号：US07745198B2

公开(公告)日：2010-06-29

申请号：US10532412

申请日：2003-11-27

申请人： Akifumi Okuda ,  Satoshi Yamamoto ,  Takashi Sakai ,  Susumu Takeda ,  Takashi Nakashima ,  Katsura Kaneko ,  Tomohiro Sameshima ,  Taira Kato ,  Naoto Kawamura

发明人： Akifumi Okuda ,  Satoshi Yamamoto ,  Takashi Sakai ,  Susumu Takeda ,  Takashi Nakashima ,  Katsura Kaneko ,  Tomohiro Sameshima ,  Taira Kato ,  Naoto Kawamura

IPC分类号： C12N1/20 ,  A01N43/02

CPC分类号： C07D407/06 ,  A61K31/336 ,  C12P17/162

摘要： The present invention provides a novel method of producing the 12-membered ring macrolide compound 11107D having an antitumor activity by biological transformation. Starting material which is the 12-membered ring macrolide compound 11107B represented by the formula (I) is incubated in the presence of a strain belonging to the genus Mortierella, the genus Streptomyces or the family Micromonosporaceae (for example, Streptomyces sp. AB-1704 strain (FERM BP-8551)), each of which has the ability of transforming the 12-membered ring macrolide compound 11107B into a 11107D substance represented by the formula (II), or a preparation of its cultured myceha and oxygen, and then 11107D substance which is a target material is collected from the treating solution.

摘要翻译： 本发明提供了通过生物转化制备具有抗肿瘤活性的12元环大环内酯化合物11107D的新方法。 作为式（I）所示的12元环大环内酯化合物11107B的起始原料在属于被孢霉属（Mortierella），链霉菌属（Streptomyces）属或小单孢菌属（Micromonosporaceae）的菌株（例如，链霉菌属AB-1704 菌株（FERM BP-8551）），其各自具有将12元环大环内酯化合物11107B转化为由式（II）表示的11107D物质或其培养的肌肉和氧的制剂的能力，然后将11107D 从处理液中收集作为目标物质的物质。

公开(公告)号：US20060141589A1

公开(公告)日：2006-06-29

申请号：US10532412

申请日：2003-11-27

申请人： Akifumi Okuda ,  Satoshi Yamamoto ,  Takashi Sakai ,  Susumu Takeda ,  Takashi Nakashima ,  Katsura Kaneko ,  Tomohiro Sameshima ,  Taira Kato ,  Naoto Kawamura

发明人： Akifumi Okuda ,  Satoshi Yamamoto ,  Takashi Sakai ,  Susumu Takeda ,  Takashi Nakashima ,  Katsura Kaneko ,  Tomohiro Sameshima ,  Taira Kato ,  Naoto Kawamura

IPC分类号： C12P17/02 ,  C12N1/21

CPC分类号： C07D407/06 ,  A61K31/336 ,  C12P17/162

摘要： The present invention provides a novel method of producing the 12-membered ring macrolide compound 11107D having an antitumor activity by biological transformation. Starting material which is the 12-membered ring macrolide compound 11107B represented by the formula (I) is incubated in the presence of a strain belonging to the genus Mortierella, the genus Streptomyces or the family Micromonosporaceae (for example, Streptomyces sp. AB-1704 strain (FERM BP-8551)), each of which has the ability of transforming the 12-membered ring macrolide compound 11107B into a 11107D substance represented by the formula (II), or a preparation of its cultured mycelia and oxygen, and then 11107D substance which is a target material is collected from the treating solution.

摘要翻译： 本发明提供了通过生物转化制备具有抗肿瘤活性的12元环大环内酯化合物11107D的新方法。 作为式（I）所示的12元环大环内酯化合物11107B的起始原料在属于被孢霉属（Mortierella），链霉菌属（Streptomyces）属或小单孢菌属（Micromonosporaceae）的菌株（例如，链霉菌属AB-1704 菌株（FERM BP-8551）），其各自具有将12元环大环内酯化合物11107B转化为由式（II）表示的11107D物质或其培养的菌丝体和氧气的制剂的能力，然后将11107D 从处理液中收集作为目标物质的物质。

公开(公告)号：US07247729B2

公开(公告)日：2007-07-24

申请号：US10488470

申请日：2002-09-10

申请人： Toshio Tsuchida ,  Katsura Kaneko ,  Naoki Matsumoto

发明人： Toshio Tsuchida ,  Katsura Kaneko ,  Naoki Matsumoto

IPC分类号： C07D211/32

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： 一种制备哌可酰胺衍生物的方法，其特征在于，在缩合剂如二环己基碳二亚胺，1-乙基-2-（2-二甲基氨基丙基）碳二亚胺，1-乙基-2-（2-二甲基氨基丙基）碳化二亚胺等存在下，使哌啶酸或其酸式盐与惰性溶剂中的胺反应 ，甲磺酰氯或磷酰氯。 特别是其光学活性形式的哌癸酰胺衍生物可以有效地和经济地制造而没有有害气体副产物。

公开(公告)号：US20100197919A1

公开(公告)日：2010-08-05

申请号：US12667843

申请日：2008-07-04

申请人： Toshio Tsuchida ,  Masashi Yoshida ,  Kazuo Ohta ,  Katsura Kaneko ,  Kaichiro Kominato

发明人： Toshio Tsuchida ,  Masashi Yoshida ,  Kazuo Ohta ,  Katsura Kaneko ,  Kaichiro Kominato

IPC分类号： C07D405/14 ,  C07D241/04 ,  C07F7/22

CPC分类号： C07D295/18 ,  C07D407/06 ,  C07F7/2224

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的12元环大环内酯类化合物的制造方法及其制造中间体。 详细地，通过使作为原料的12元环大环内酯化合物的6-和7-位的羟基被二烷基锡（IV）氧化物缩醛化，然后使产物与氨基甲酰卤衍生物反应， 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被有效地制备，而不保护其它位置的羟基。