公开(公告)号：EP1235065A1

公开(公告)日：2002-08-28

申请号：EP00979061.9

申请日：2000-12-04

申请人： Japan Science and Technology Corporation

发明人： INOUE, Yoshihisa ,  BOROVKOV, Victor ,  LINTULUOTO, Juha, The 29-703

IPC分类号： G01N21/19 ,  G01N21/77 ,  C07D487/22 ,  C09B47/00

CPC分类号： C07D487/22 ,  C09B47/00 ,  Y10T436/145555 ,  Y10T436/173845 ,  Y10T436/174614

摘要： The object of the present invention is to provide a novel general-purpose method of precisely and easily determining the absolute configuration of chiral compounds having a wide variety of basic groups.
The present invention provides a method for determining the absolute configuration of a chiral compound which comprises:

coordinating the chiral compound to a metalloporphyrin, the metalloporphyrin having a carbon chain-crosslinked porphyrin dimer structure in which one of the two porphyrin rings has at least one ethyl or substituent bulkier than ethyl at at least one of the second peripheral carbon atoms from the carbon atom at the carbon chain crosslink site,
the chiral compound having an asymmetric carbon bonded to a basic group capable of coordinating to the metal of the other porphyrin ring of the metalloporphyrin dimer or an asymmetric carbon atom adjacent to the carbon atom bonded to the basic group; and
analyzing the resultant coordination compound by circular dichroism spectrophotometry to determine the absolute configuration of the asymmetric carbon of the chiral compound based on the sign of the Cotton effect.

摘要翻译： 本发明的目的是提供一种新颖的通用方法，其精确且容易地确定具有多种基团的手性化合物的绝对构型。 本发明提供了一种用于确定手性化合物的绝对构型的方法，其包括：将手性化合物与金属卟啉配位，金属卟啉具有碳链交联的卟啉二聚体结构，其中两个卟啉环中的一个具有至少一个乙基 或在碳链交联部位的碳原子的至少一个第二外周碳原子上比乙基更大的取代基，所述手性化合物具有与能够与其他卟啉环的金属配位的碱性基团键合的不对称碳 金属卟啉二聚体或与结合到碱性基团上的碳原子相邻的不对称碳原子; 并通过圆二色性分光光度法分析得到的配位化合物，以确定手性化合物的不对称碳的绝对构型，基于棉花效应的符号。

公开(公告)号：EP1063237B1

公开(公告)日：2007-05-16

申请号：EP99939144.4

申请日：1999-03-08

申请人： Japan Science and Technology Corporation

发明人： INOUE, Yoshihisa ,  VICTOR, Borovkov ,  JUHA, Lintuluoto

IPC分类号： C07D487/22

CPC分类号： C07D487/22 ,  C07D519/00

摘要： A method for preparing a metal complex of a porphyrin which has a structure obtained by inserting a transition metal into a porphyrin ring, wherein a porphyrin and a transition metal salt are dissolved separately in a solvent, and then the resulting solutions each containing a porphyrin or a transition metal salt are mixed and reacted in the presence of a basic compound, and wherein a metal complex of a porphyrin having a structure obtained by inserting a transition metal into a porphyrin ring can be synthesized in high selectivity, not only with a simple and easy means but also under a mild condition.

公开(公告)号：EP1235065B1

公开(公告)日：2004-08-04

申请号：EP00979061.9

申请日：2000-12-04

申请人： JAPAN SCIENCE AND TECHNOLOGY CORPORATION

发明人： INOUE, Yoshihisa ,  BOROVKOV, Victor ,  LINTULUOTO, Juha, The 29-703

IPC分类号： G01N21/19 ,  G01N21/77 ,  C07D487/22 ,  C09B47/00 ,  C07D519/00

CPC分类号： C07D487/22 ,  C09B47/00 ,  Y10T436/145555 ,  Y10T436/173845 ,  Y10T436/174614

摘要： A novel general-purpose method of precisely and easily determining the absolute configuration of a chiral compound which can have various kinds of basic groups bonded. The method uses a metal porphyrin having a structure which comprises a porphyrin dimer crosslinked with a carbon chain and in which one of the two porphyrin rings has a substituent bulkier than an ethyl group and bonded to at least one of the second peripheral carbon atoms from the carbon atom at the crosslink with the carbon chain. In this method, either a chiral compound having an asymmetric carbon atom having, bonded thereto, a basic group capable of coordinating to the metal of the other porphyrin ring of the dimer structure of the metal porphyrin or a chiral compound having an asymmetric carbon atom adjacent to a carbon atom having the basic group bonded thereto is coordinated to the metal porphyrin. The resultant coordination compound is analyzed by spectrophotometry based on circular dichroism to determine the absolute configuration of the chiral compound based on the symbol of a Cotton effect.

公开(公告)号：EP1063237A1

公开(公告)日：2000-12-27

申请号：EP99939144.4

申请日：1999-03-08

申请人： Japan Science and Technology Corporation

发明人： INOUE, Yoshihisa ,  VICTOR, Borovkov ,  JUHA, Lintuluoto

IPC分类号： C07D487/22

CPC分类号： C07D487/22 ,  C07D519/00

摘要： A process for producing a metalloporphyrin containing a transition metal inserted into the porphyrin ring which comprises dissolving a porphyrin compound and a transition metal salt each in an independent solvent, combining the solutions, and carrying out the reaction in the presence of a basic substance. By this process, a metalloporphyrin containing a transition metal inserted into the porphyrin ring can be synthesized easily under mild conditions and with high selectivity.

摘要翻译： 一种制备含有插入卟啉环中的过渡金属的金属卟啉的方法，其包括将卟啉化合物和过渡金属盐各自溶解在独立的溶剂中，将该溶液混合，并在碱性物质的存在下进行反应。 通过该方法，可以在温和条件下以高选择性容易地合成含有插入卟啉环中的过渡金属的金属卟啉。

公开(公告)号：EP1295892A1

公开(公告)日：2003-03-26

申请号：EP01938632.5

申请日：2001-06-13

申请人： JAPAN SCIENCE AND TECHNOLOGY CORPORATION

发明人： WADA, Takehiko ,  INOUE, Yoshihisa

IPC分类号： C07H19/06 ,  C07H19/16 ,  A61K31/7064 ,  A61K31/7076 ,  A61K45/00 ,  A61K47/02 ,  A61K47/04 ,  A61K47/26 ,  A61P43/00

CPC分类号： C12N15/113 ,  C07H19/06 ,  C07H23/00 ,  C12N2310/318 ,  C12N2310/33 ,  C12N2310/351

摘要： An antisense molecule which acts on both directions of the inhibition and expression of a gene function and is capable of on-off switching of a gene function appropriately depending on the external factors (orientation controlling factors); and a method for reversibly controlling the expression of a gene function by using the antisense molecule. Such an antisense molecule, which has at least one sugar-base moiety consisting of sugar and a purine or pyrimidine base bonded thereto via a glucoside bond, can bind to a mRNA/gene and/or dissociate therefrom under the orientation control of the base moiety in the molecule by the orientation controlling factors.

摘要翻译： 作用于抑制和表达基因功能的两个方向的反义分子，并且能够根据外部因素（取向控制因子）适当地开关基因功能的切换。 以及通过使用反义分子可逆地控制基因功能的表达的方法。 这种具有至少一个由糖组成的糖基部分和通过葡糖苷键键合到其上的嘌呤或嘧啶碱基的反义分子可以在碱基部分的取向控制下与mRNA /基因结合和/或从其解离 在分子中由方向控制因素。

公开(公告)号：EP1295891A1

公开(公告)日：2003-03-26

申请号：EP01938631.7

申请日：2001-06-13

申请人： JAPAN SCIENCE AND TECHNOLOGY CORPORATION

发明人： INOUE, Yoshihisa ,  WADA, Takehiko

IPC分类号： C07H19/06 ,  C07H19/16

CPC分类号： C07H19/06 ,  C07H19/04 ,  C07H21/00

摘要： Novel nucleoside derivatives represented by the following general formula (1):
wherein X is(are) the same or different and each represents a pyrimidine or purine base or a derivative thereof, Y and Y' are the same or different and each represents at least one amino acid or amino acid derivative selected from the group consisting of serine, threonine, ornithine, aspartic acid, glutamic acid, lysine, arginine, cysteine, methionine, δ-hydroxylysine, N-aminoethylglycine, N-aminoethylserine, N-aminoethyllysine, N-aminoethylornithine, N-aminoethylaspartic acid, N-aminoethylglutamic acid, homoglutamic acid, β-thiocarbonylaspartic acid, γ-thiocarbonylglutamic acid, and δ-thiocarbonylhomoglutamic acid, R 1 represents a hydrogen atom or a hydroxyl group, A represents a single bond or a carbonyl or thiocarbonyl group, 1 is an integer of 0 to 5, and n is an integer of 1 to 100.

摘要翻译： 由以下通式（1）表示的新型核苷衍生物：其中X为（均）相同或不同，各自表示嘧啶或嘌呤碱或其衍生物，Y和Y'相同或不同， 代表选自丝氨酸，苏氨酸，鸟氨酸，天冬氨酸，谷氨酸，赖氨酸，精氨酸，半胱氨酸，甲硫氨酸，δ-羟基赖氨酸，N-氨基乙基甘氨酸，N-氨基乙基丝氨酸，N-氨基乙基丝氨酸， 氨基乙基赖氨酸，N-氨基乙基鸟氨酸，N-氨基乙基天冬氨酸，N-氨基乙基谷氨酸，高谷氨酸，β-硫羰基天冬氨酸，γ-硫代羰基谷氨酸和δ-硫代羰基氨基谷氨酸，R 1表示氢原子或羟基，A表示 单键或羰基或硫代羰基，1表示0〜5的整数，n表示1〜100的整数。