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。
摘要:
The present invention relates to novel oligonucleotide analogs with valuable physical, biological and pharmacological properties, and a process for their preparation.
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:
The invention relates to novel stabilized oligonucleotides in which at least one non-terminal pyrimidine nucleoside is modified, and to their use as a diagnostic or pharamaceutical for the treatment of viral infections, cancer or diseases in which integrins or cell-cell adhesion receptors are active.
摘要:
The invention relates to novel antisense oligonucleotides having the sequences ##STR1## and their mixtures, homologs or modified forms, against HSV 1.
摘要翻译:本发明涉及具有序列AO1(Herp099):+ TR 5'-GCGGGGCTCCATGGGGGTCG-3'(SEQ ID NO:1)AO2(Herp018):+ TR 5'-GCAGGAGGATGCTGAGGAGG-3'(SEQ ID NO: 2)AO3(Herp002):+ TR 5'-GGGGCGGGGCTCCATGGGGG-3'(SEQ ID NO:3)AO4(Herp112):+ TR 5'-GGCGGGGCTCCATGGGGGTC-3'(SEQ ID NO:4)AO5(Herp034) TR 5'-GGGGCTCCATGGGGGTCGTA-3'(SEQ ID NO:5)AO6(Herp024):+ TR 5'-AAGAGGTCCATTGGGTGGGG-3'(SEQ ID NO:6)AO7(Herp028):+ TR 5'-GGCCCTGCTGTTCCGTGGCG-3' (SEQ ID NO:7)。 及其混合物,同系物或修饰形式,针对HSV 1。
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:
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:
Novel oligonucleotide analogs of the formula (I) are described, ##STR1## in which A, B, D, G, L, P, Q, Q', R.sup.5, R.sup.6, X, Y, Z and n are as defined in the description, which have useful physical, biological and pharmacological properties, as well as a process for their preparation. Their application relates to use as inhibitors of gene expression (antisense oligonucleotides, ribozymes, sense oligonucleotides and triplex-forming oligonucleotides), as probes for the detection of nucleic acids and as auxiliaries in molecular biology.
摘要:
Antisense oligonucleotides against tenascin for the treatment of vitiligo The invention relates to specific, optionally modified oligonucleotides having a length of up to 18 nucleotides, which correspond to sections of tenascin-coding sequences or can bind to these sequences, to their preparation and to the use thereof, for example for the specific inhibition of the expression of tenascin and for the production of pharmaceuticals which can be used for the treatment of vitiligo.
摘要:
The invention relates to specific, optionally modified oligonucleotides with a length of up to 17 nucleotides. Said oligonucleotides correspond to segments of tenascin-coding sequences or can bind to these sequences. The invention also relates to the production and use of the oligonucleotides, for example for the specific inhibition of the expression of tenascin and for producing medicaments used to treat vitiligo.