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。