G cap-stabilized oligonucleotides
    43.
    发明授权
    G cap-stabilized oligonucleotides 有权
    G帽稳定的寡核苷酸

    公开(公告)号:US6121434A

    公开(公告)日:2000-09-19

    申请号:US258408

    申请日:1999-02-26

    摘要: Oligonucleotides of the formula:5'-(CAP)-(Oligo)-(CAP)-3'are disclosed where (oligo) is a nucleotide sequence of from 10 to 40 nucleotides in length, and CAP is G.sub.m, where m is an integer of from zero to ten, the two CAP's which are present in the molecule can be defined independently of each other and must be different in the case where m is zero at the 5' or 3' end and the end of the oligo sequence is other than guanine. The oligonucleotides can be synthesized chemically. The oligonucleotides are used to diagnose or treat cancer, restenosis, a disease caused by a virus, a disease affected by integrins or cell-cell adhesion receptor or a disease triggered by diffusible factors.

    摘要翻译: 公开了式(5' - (CAP) - (Oligo) - (CAP)-3'的寡核苷酸,其中(oligo)是长度为10至40个核苷酸的核苷酸序列,CAP为Gm,其中m为 存在于分子中的两个CAP可以彼此独立地定义,并且在5'或3'端的m为零并且寡核苷酸序列的末端为 鸟嘌呤除外。 寡核苷酸可以化学合成。 寡核苷酸用于诊断或治疗癌症,再狭窄,由病毒引起的疾病,受整联蛋白或细胞粘附受体影响的疾病或由可扩散因子引发的疾病。

    Oligonucleotide analogs, their preparation and use
    44.
    发明授权
    Oligonucleotide analogs, their preparation and use 失效
    寡核苷酸类似物,其制备和用途

    公开(公告)号:US6033909A

    公开(公告)日:2000-03-07

    申请号:US281203

    申请日:1994-07-27

    IPC分类号: C07H21/00 C12Q1/68 C07H21/04

    CPC分类号: C07H21/00 C07B2200/11

    摘要: The invention relates to compounds of the formula I ##STR1## where R.sup.1 is H, alkyl, acyl, aryl, or a phosphate residue; R.sup.2 is H, OH, alkoxy, NH.sub.2, or halogen; B is a base customary in nucleotide chemistry; a is O or CH.sub.2 ; n is an integer from 1 to 100; W=O, S or Se; V=O, S, or NH; Y=O, S, NH, or CH.sub.2 ; Y'=O, S, NH, or alkylene; X=OH or SH; U=OH, SH, SeH, alkyl, alkoxy, aryl, aryloxy, or amine, and Z=OH, SH, SeH, an optionally substituted radical from the group comprising alkyl, aryl, heteroaryl, alkoxy, or amino, or a group which favors intracellular uptake or serves as the label of a DNA probe or attacks the target nucleic acid during hybridization, where if Z=OH, SH, CH.sub.3, or OC.sub.2 H.sub.5, at least one of the groups X, Y, Y', V, or W is not OH or O or R.sup.1 is not H; a process for their preparation and their use as inhibitors of gene expression, as probes for detecting nucleic acids and as aids in molecular biology.

    摘要翻译: 本发明涉及式Ⅰ化合物,其中R1是H,烷基,酰基,芳基或磷酸酯残基; R2是H,OH,烷氧基,NH2或卤素; B是核苷酸化学中常规的基础; a是O或CH2; n为1〜100的整数, W = O,S或Se; V = O,S或NH; Y = O,S,NH或CH 2; Y'= O,S,NH或亚烷基; X = OH或SH; U = OH,SH,SeH,烷基,烷氧基,芳基,芳氧基或胺,Z = OH,SH,SeH,任选取代的基团,其包含烷基,芳基,杂芳基,烷氧基或氨基, 其有利于细胞内吸收或用作DNA探针的标记或在杂交期间攻击靶核酸,其中如果Z = OH,SH,CH 3或OC 2 H 5,X,Y,Y',V, 或W不是OH或O或R 1不是H; 其制备方法及其作为基因表达抑制剂的用途,作为检测核酸的探针和分子生物学的辅助工具。

    Process for the preparation of derivatives of bis(amino-methyl)
phosphinic acid
    47.
    发明授权
    Process for the preparation of derivatives of bis(amino-methyl) phosphinic acid 失效
    制备双(氨基 - 甲基)次膦酸的衍生物的方法

    公开(公告)号:US5510504A

    公开(公告)日:1996-04-23

    申请号:US313044

    申请日:1995-01-04

    CPC分类号: C07F9/301 C07F9/3211

    摘要: A process for the preparation of .alpha.- or .alpha.,.alpha.'-substituted derivatives of the bis(aminomethyl)phosphinic acid of the formula I and their acid or basic salts, ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 are defined as in the description, wherein a bis(aminomethyl)phosphinate is converted into the corresponding bisimine, which is alkylated by R.sup.2 and R.sup.3 in the .alpha.- and/or .alpha.,.alpha.'-position after reaction with a base, and is converted into a compound of the formula I by subsequent treatment with an acid.

    摘要翻译: PCT No.PCT / EP93 / 00838 Sec。 371日期1995年1月4日 102(e)日期1995年1月4日PCT提交1993年4月5日PCT公布。 WO93 / 20086 PCT出版物 日期:1993年10月14日。一种制备式I的双(氨基甲基)次膦酸的α-或α,α'-取代衍生物及其酸或碱式盐的方法,其中 R1,R2和R3如描述中所定义,其中双(氨基甲基)次膦酸盐转化为相应的双亚胺,其在与a反应后的α和/或α,α'-位中被R2和R3烷基化 并通过随后用酸处理转化成式I的化合物。