Oligonucleotide analogs, their preparation and use
    1.
    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。

    Use of benzylphosphonic acid derivatives for the treatment of diseases
caused by viruses
    3.
    发明授权
    Use of benzylphosphonic acid derivatives for the treatment of diseases caused by viruses 失效
    用于治疗病毒引起的疾病的苯并恶唑酸衍生物的应用

    公开(公告)号:US5242908A

    公开(公告)日:1993-09-07

    申请号:US648622

    申请日:1991-02-01

    摘要: The use of a compound of the formula I ##STR1## in which V is an alkyl group, fluorine, chlorine, bromine, or iodine, n is an integer from 1 to 5, W is an alkyl, alkenyl, alkynyl or alkoxy group, cyanide, nitro, carboxyl, hydrogen or a cycloalkyl, aryl, aralkyl or carboalkoxy group, R.sup.1 and R.sup.2 are an alkyl, alkenyl, alkynyl, cycloalkyl or halogenoalkyl group, sodium, potassium, calcium, magnesium, aluminum, lithium, ammonium, triethylammonium or hydrogen, R.sup.1 and R.sup.2 together form a cyclic diester, R.sup.3 and R.sup.4 are an alkyl, alkenyl, alkynyl, carboalkoxy, cycloalkyl or alkoxy group, hydrogen, fluorine, chlorine, bromine or iodine and X, Y and Z are oxygen or sulfur, for the treatment of diseases caused by DNA viruses or RNA viruses is described.

    摘要翻译: 使用其中V为烷基,氟,氯,溴或碘的式I化合物I,其为1至5的整数,W为烷基,烯基,炔基或烷氧基 ,氰基,硝基,羧基,氢或环烷基,芳基,芳烷基或烷氧基,R1和R2是烷基,烯基,炔基,环烷基或卤代烷基,钠,钾,钙,镁,铝,锂,铵, 或氢,R1和R2一起形成环状二酯,R3和R4是烷基,烯基,炔基,烷氧羰基,环烷基或烷氧基,氢,氟,氯,溴或碘,X,Y和Z是氧或硫, 描述了用于治疗由DNA病毒或RNA病毒引起的疾病。

    2-formylbenzylphosphonic acid derivatives useful for the treatment of
diseases caused by viruses
    6.
    发明授权
    2-formylbenzylphosphonic acid derivatives useful for the treatment of diseases caused by viruses 失效
    用于治疗由病毒引起的疾病的2-甲酰基苄基膦酸衍生物

    公开(公告)号:US5278152A

    公开(公告)日:1994-01-11

    申请号:US19822

    申请日:1993-02-18

    CPC分类号: C07F9/4056

    摘要: The compound of the formula I ##STR1## in which R is an aldehyde group or a group which can be converted into an aldehyde, R.sup.1 and R.sup.2 are alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, hydrogen, sodium, potassium, calcium, magnesium, aluminum, lithium, ammonium or triethylamnonium, orR.sup.1 and R.sup.2 together form a cyclic diester,R.sup.3 and R.sup.4 are alkyl, alkenyl, alkynyl, cycloalkyl, hydrogen, alkoxy or halogen, R.sup.5 and R.sup.8 are alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, alkoxy, phenyl, cyanide, hydroxyl or hydrogen, and X, Y or Z are oxygen or sulfur, or prodrug forms of the compound of the formula I can be used for the treatment of diseases caused by viruses.The preparation of these compounds and pharmaceutical preparations containing them and their use is described.

    摘要翻译: 其中R是醛基的式I化合物或可以转化为醛的基团,R 1和R 2是烷基,烯基,炔基,芳烷基,环烷基,氢,钠,钾,钙, 镁,铝,锂,铵或三乙基铵,或R 1和R 2一起形成环状二酯,R 3和R 4是烷基,烯基,炔基,环烷基,氢,烷氧基或卤素,R 5和R 8是烷基,烯基,炔基,芳烷基, 环烷基,烷氧基,苯基,氰基,羟基或氢,X,Y或Z是氧或硫,或式I化合物的前药形式可用于治疗由病毒引起的疾病。 描述了这些化合物和含有它们的药物制剂及其应用的制备。

    G cap-stabilized oligonucleotides
    7.
    发明授权
    G cap-stabilized oligonucleotides 失效
    G帽稳定的寡核苷酸

    公开(公告)号:US6013639A

    公开(公告)日:2000-01-11

    申请号:US594452

    申请日:1996-01-31

    摘要: Oligonucleotides of the formula5'-(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为整数 分子中存在的两个C​​AP可以彼此独立地定义,并且在5'或3'端的m为零并且Oligo序列的末端是其它的情况下必须是不同的 比鸟嘌呤。 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。